AR031528A1 - Compuestos de pirazolopirimidina y su uso para preparar una composicion farmaceutica - Google Patents

Compuestos de pirazolopirimidina y su uso para preparar una composicion farmaceutica

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AR031528A1
AR031528A1 ARP000104888A ARP000104888A AR031528A1 AR 031528 A1 AR031528 A1 AR 031528A1 AR P000104888 A ARP000104888 A AR P000104888A AR P000104888 A ARP000104888 A AR P000104888A AR 031528 A1 AR031528 A1 AR 031528A1
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substituted
unsubstituted
alkyl
group
independently
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Abbott Gmbh & Co Kg
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Abstract

Un compuesto de pirazolopirimidina que posee una formula (1): la mezclas diastereomérico racémicas, isomeros opticos, sales farmacéuticamente aceptables, prodrogas o metabolitos biologicamente activos del mismo en los cuales: G es formula (2) donde Z100 es formula (3) o un grupo opcionalmente sustituido con R1 seleccionado del grupo que consiste de cicloalquilo, naftilo, tetrahidronaftilo, benzotenilo, furanilo, tienilo, benzoxazolilo, benzotiazolilo de formulas (4) y (5), tiazolilo, benzofuranilo, 2,3-dihidrobenzofuranilo, indolilo, isoxazolilo, tetrahidropiranilo, tetrahidrofuranilo, piperidinilo, pirazolilo, pirrolilo, oxazolilo, isotiazolilo, oxadiazolilo, tiadiazolilo, indolinilo, indazolilo , benzoisotiazolilo, pirido-oxazolilo, pirido-tiazolilo, pirimido-oxazolilo, pirimidotiazolilo y bencimidazolilo; Z110 es un enlace covalente, o un (C1-6) opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste de alquilo, CN, OH, halogeno, NO2, COOH, amino sustituido o sin sustituir y fenilo sustituido o sin sustituir; Z111 es un enlace covalente,(C1-6) opcionalmente sustituido o un û(CH2)n-cicloalquil-(CH2)n- opcionalmente sustituido; donde los grupos opcionalmente sustituidos con uno o más sustituyentes seleccionados del grupo que consiste de alquilo, CN, OH, halogeno, NO2, COOH, amino sustituido o sin sustituir y fenilo sustituido o sin sustituir; Ra y R1 cada uno representa uno o más sustituyentes para cada circunstancia seleccionada independientemente del grupo que consiste de hidrogeno, halogeno, -CN, -NO2, -C(O)OH, -C(O)H, -OH, -C(O)O-alquilo, carboxamido sustituido o sin sustituir, tetrazolilo, trifluorometilcarbonilamino, trifluorometilsulfonamido, alquilo sustituido o sin sustituir, alcoxilo sustituido o sin sustituir, arilo sustituido o sin sustituir, alquenilo sustituido o sin sustituir, ariloxilo sustituido o sin sustituir, heteroariloxilo sustituido o sin sustituir, arilalquilo sustituido o sin sustituir, alquinilo sustituido o sin sustituir, amino, sustituido o sin sustituir, aminoalquilo sustituido o sin sustituir, grupo amido sustituido o sin sustituir, heteroariltio sustituido o sin sustituir, ariltio sustituido o sin sustituir, -Z105-C(O)NR2, -Z105-N(R)-CO2-Z100, -Z105-N(R)-SO2-Z200, -Z105-N(R)-C(O)-N(R)-Z200, Rc y CH2ORc; donde Rc para cada circunstancia es independientemente hidrogeno, alquilo sustituido o sin sustituir, arilo sustituido o sin sustituir, -CH2-NRdRe, -W-(CH2)t-NRdRe, -W- -(CH2)t-O alquilo, -W-(CH2)t-S-alquilo, o ûW-(CH2)t-OH; Z105 para cada circunstancia es independientemente un enlace covalente o (C1-6); Z200 para cada circunstancia es independientemente (C1-6) sustituido o sin sustituir, fenilo sustituido o sin sustituir o û(C1-6)-fenilo sustituido o sin sustituir; Rd y Re para cada circunstancia es independientemente H, alquilo, alcanoilo o SO2-alquilo; o Rd, Re y el átomo de nitrogeno al cual estos están unidos forman un anillo heterocíclico de cinco o seis miembros; t para cada circunstancia es independientemente un entero de valor 2 a 6 ; W para cada circunstancia es independientemente un enlace directo u O, S, S(O), SO2, o NRf en donde Rf para cada circunstancia es independientemente H o alquilo; o Rf es un anillo carbocíclico o heterocíclico sustituido sin sustituir fusionado con el anillo 2; R3 es hidrogeno, hidroxilo, alquilo sustituido o sin sustituir o alcoxilo sustituido o sin sustituir; A es ûO-; -S-; SOp-; -N(R)-; -N(C(O)OR)-; -N(C(O)R)-; -N(SO2R)-; -CH2O-; -CH2S-; -CH2N(R)-; -CH(NR)-; CH2N(C(O)R)-; -CH2N(C(O)OR)-; -CH2N(SO2R)-; -CH(NHR)-; -CH(NHC(O)R)-; -CH(NHSO2R)-; -CH(NHC(O)OR)-; -CH(OC(O)R)-; -CH(OC(O)NHR)-; -CH=CH-; -C(=NOR)-; -C(O)-;-CH(OR)-; -C(O)N(R)-; -N(R)C(O)-; -N(R)S(O)p-; -OC(O)N(R)-; -N(R)-C(O)-(CH2)n-N(R)-, -N(R)C(O)O-; -N(R)(CH2)n+1 -C(O)-, -S(O)pN(R)-; -O-(CR2)n+1-C(O). ûO-(CR2)n+1-O-, ûN(C(O)R)S(O)p-; -N(R)S(O)pN(R)-; N(R)-C(O)-(CH2)n-O-, -C(O)N(R)C(O)-; -S(O)pN(R)C(O)-;-OS(O)pN(R)C(O)-; -OS(O)pN(R)-; -N(R)S(O)pO-; -N(R)S(O)pC(O)-; -SOpN(C(O)R)-; -N(R)SOpN(R)-; -C(O)O-; -N(R)P(ORb)O-; -N(R)P(ORb)-; N(R)P(O)(ORb)O-; -N(R)P(O)(ORb)-; -N(C(O)R)P(ORb)O-; -N(C(O)R)P(ORb)-; -N(C(O)R)P(O)(ORb)O-; o ûN(C(O)R)P(ORb)-; donde R para cada circunstancia es independientemente H, alquilo sustituido o sin sustituir, arilalquilo sustituido o sin sustituir o arilo sustituido o sin sustituir; Rb para cada circunstancia es independientemente H, alquilo sustituido o sin sustituir, arilalquilo sustituido o sin sustituir, cicloalquilo sustituido o sin sustituir o arilo sustituido o sin sustituir; p es 1 o 2; o en el grupo conteniendo fosforo, el átomo de nitrogeno, el átomo de fosforo, R y Rb juntos forman un anillo heterocíclico de cinco o seis miembros; o A es NRSO2 y R y Ra y el átomo de nitrogeno forman juntos un anillo heterocíclico de cinco o seis miembros sustituidos o sin sustituir fusionado al anillo1; A es NRSO2 y R, Ra y el átomo de nitrogeno forman juntos un anillo 1; R2 es ûZ101, Z102 es un enlace covalente, -(alquiloC1-6)-, -(alquiloC1-6)-O-, -(C1-6)-C(O)-, -(alquiloC1-6)-C(O)-NH-, -(C1-6)-C(O)-N((alquiloC1-6))- o un grupo de fenilo sustituido o sin sustituir; Z102 es hidrogeno, un grupo alquilo sustituido o sin sustituir, un grupo cicloalquilo sustituido o sin sustituir, un grupo heterocíclico saturado o no saturado, sustituido o sin sustituir , los grupos heterobicíclico saturados o no saturados, sustituido o sin sustituir; dicho grupo heterocíclico sustituido o heterobicíclico sustituido que posee uno o mas sustituyentes cada uno seleccionado independientemente del grupo que consiste de hidroxilo, ciano, alcoxilo sustituido o sin sustituir, sulfonamido sustituido o sin sustituir, ureido sustituido o sin sustituir, carboxamido sustituido o sin sustituir; amino sustituido o sin sustituir, oxo, un grupo heterocíclico saturado, no saturado o aromático sustituido o sin sustituir que comprende uno o más átomos de nitrogeno, uno más átomos de oxígeno o una combinacion de los mismos; en donde dichos átomos de nitrogeno se sustituyen independientemente opcionalmente por un alquilo sustituido o sin sustituir, arilo sustituido o sin sustituir o grupo arilalquilo sustituido o sin sustituir, o R2 es de la formula B-E, en donde B es un cicloalquilo sustituido o sin sustituir, azacicloalquilo sustituido o sin sustituir, amino sustituido o sin sustituir, aminoalquilsulfonilo sustituido o sin sustituir, alcoxialquilo sustituido o sin sustituir, alcoxilo sustituido o sin sustituir, aminoalquilcarbonilo sustituido o sin sustituir, hidroxilo, alquileno sustituido o sin sustituir, aminoalquilo, sustituido o sin sustituir, alquilencarbonilo sustituido o sin sustituir o grupo aminoalquilcarbonilo sustituido o sin sustituir, y E es azacicloalquilo sustituido o sin sustituir azacicloalquilcarbonilo sustituido o sin sustituir, azacicloalquilsulfonilo sustituido o sin sustituir azacicloalquilalquilo sustituido o sin sustituir, heteroarilo sustituido o sin sustituir, heteroarilcarbonilo sustituido o sin sustituir, heteroarilsulfonilo sustituido o sin sustituir, heteroaril alquilo sustituido o sin sustituir, azacicloalquilcarbonilamino sustituido o sin sustituir, heteroaril carbonilamino sustituido o sin sustituir o arilo sustituido o sin sustituir; a es 1 y D1, G1, J1, L1 y M1 son independientemente cada uno seleccionado del grupo que consiste de CRa y N, con la condicion que por lo menos dos de D1, G1, J1, L1, y M1, sea CRa; o a es 0, y cada uno de D1, G1, L1, y M1 es NRa, uno de D1, G1, L1, y M1 es CRa y el resto es independientemente seleccionado del grupo que consiste de CRa y N, en donde Ra es igual al definido precedentemente; b es uno y D2, G2, J2, L2 y M2 son independientemente cada uno seleccionado del grupo que consiste de CRa y N, con la condicion que por lo menos dos de D2, G2, J2, L2, y M2 son CRa; o b es 0, y uno de D2, G2, L2, y M2 es MRa, uno de D2, G2, L2, y M2 es CRa; y el resto se selecciona independientemente del grupo que consiste de CRa y N, en donde Ra es igual al definido precedentemente; y n para cada circunstancia es independientemente un entero de valor de 0 a 6. Uso del compuesto de pirazolopirimidina de la formula (1) para preparar una composicion farmacéutica para inhibir la actividad de la quinasaproteínica. La composicion farmacéutica es util para afectar desordenes hiperproliferativos, angiogénesis, una o más ulceras, para tratar una condicion patologica o para disminuir la fertilidad de un paciente.
ARP000104888A 1999-09-17 2000-09-18 Compuestos de pirazolopirimidina y su uso para preparar una composicion farmaceutica AR031528A1 (es)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0233222A4 (en) * 1985-07-19 1987-10-19 Armtech Ltd FIREARMS WITH DISC SHAPE CHARGER.
US7863444B2 (en) * 1997-03-19 2011-01-04 Abbott Laboratories 4-aminopyrrolopyrimidines as kinase inhibitors
US7223724B1 (en) 1999-02-08 2007-05-29 Human Genome Sciences, Inc. Use of vascular endothelial growth factor to treat photoreceptor cells
US6921763B2 (en) * 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
JP2004505619A (ja) * 2000-08-04 2004-02-26 ヒューマン　ジノーム　サイエンシーズ，　インコーポレイテッド 血管内皮増殖因子２
MXPA03008560A (es) * 2001-03-22 2004-06-30 Abbot Gmbh & Co Kg Pirazolopirimidinas como agentes terapeuticos.
US20050232921A1 (en) * 2001-04-13 2005-10-20 Rosen Craig A Vascular endothelial growth factor 2
DE60236646D1 (de) * 2001-04-13 2010-07-22 Human Genome Sciences Inc Anti-VEGF-2 Antikörper
US20030176674A1 (en) * 2001-04-13 2003-09-18 Rosen Craig A. Vascular endothelial growth factor 2
BR0209267A (pt) 2001-04-30 2004-06-15 Glaxo Group Ltd Pirimidinas fundidas como antagonistas do fator de liberação de corticotropina (crf)
WO2003029209A2 (en) * 2001-10-02 2003-04-10 Smithkline Beecham Corporation Chemical compounds
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
US20030199525A1 (en) * 2002-03-21 2003-10-23 Hirst Gavin C. Kinase inhibitors
US20030225273A1 (en) * 2002-03-21 2003-12-04 Michaelides Michael R. Thiopyrimidine and isothiazolopyrimidine kinase inhibitors
US6695881B2 (en) 2002-04-29 2004-02-24 Alcon, Inc. Accommodative intraocular lens
US7456222B2 (en) * 2002-05-17 2008-11-25 Sequella, Inc. Anti tubercular drug: compositions and methods
CN101404986B (zh) * 2002-05-17 2011-09-28 赛奎拉公司 用于诊断和治疗感染性疾病的组合物和制药方法
US20040033986A1 (en) * 2002-05-17 2004-02-19 Protopopova Marina Nikolaevna Anti tubercular drug: compositions and methods
US20050267133A1 (en) * 2002-07-23 2005-12-01 Brown Matthew L Pyrazolopyrimidines as kinase inhibitors
AU2003261204A1 (en) * 2002-07-23 2004-02-09 Smithkline Beecham Corporation Pyrazolopyrimidines as kinase inhibitors
WO2004009597A2 (en) * 2002-07-23 2004-01-29 Smithkline Beecham Corporation Pyrazolopyrimidines as protein kinase inhibitors
AU2003246972A1 (en) 2002-08-06 2004-02-23 Astrazeneca Ab Condensed pyridines and pyrimidines with tie2 (tek) activity
GB0226370D0 (en) * 2002-11-12 2002-12-18 Novartis Ag Organic compounds
GB0230089D0 (en) * 2002-12-24 2003-01-29 Astrazeneca Ab Therapeutic agents
PL377847A1 (pl) 2003-01-14 2006-02-20 Arena Pharmaceuticals Inc. 1,2,3-Tripodstawione pochodne arylowe i heteroarylowe jako modulatory metabolizmu oraz profilaktyka i leczenie związanych z nim zaburzeń takich jak cukrzyca i hiperglikemia
US20050008640A1 (en) * 2003-04-23 2005-01-13 Wendy Waegell Method of treating transplant rejection
US7429596B2 (en) 2003-06-20 2008-09-30 The Regents Of The University Of California 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof
MXPA06000554A (es) * 2003-07-14 2006-07-03 Arena Pharm Inc Derivados arilo y heteroarilo fusionados como moduladores del metabolismo y la profilaxis y tratamiento de trastornos relacionados con los mismos.
US7884097B2 (en) * 2003-09-05 2011-02-08 Sequella, Inc. Methods and compositions comprising diamines as new anti-tubercular therapeutics
SG148161A1 (en) 2003-11-05 2008-12-31 Palingen Inc Enhanced b cell cytotoxicity of cdim binding antibody
GB0401334D0 (en) * 2004-01-21 2004-02-25 Novartis Ag Organic compounds
US20060025383A1 (en) * 2004-02-03 2006-02-02 Neil Wishart Aminobenzoxazoles as therapeutic agents
AU2005219525B2 (en) * 2004-02-27 2011-08-18 F. Hoffmann-La Roche Ag Fused derivatives of pyrazole
CN101389345A (zh) * 2004-03-19 2009-03-18 宾州研究基金会 治疗黑素瘤的组合方法和组合物
WO2005112936A1 (en) * 2004-05-14 2005-12-01 The Regents Of The University Of Michigan Compositions and methods relating to protein kinase inhibitors
WO2005117932A1 (en) * 2004-06-04 2005-12-15 The Board Of Governors For Higher Education, State Of Rhode Island And Providence Plantations Bisubstrate inhibitors of protein tyrosine kinases as therapeutic agents
EP2583678A3 (en) 2004-06-24 2013-11-13 Novartis Vaccines and Diagnostics, Inc. Small molecule immunopotentiators and assays for their detection
KR20080007425A (ko) 2004-11-05 2008-01-21 팔링겐, 인코포레이티드 항체 유도된 세포막 손상
WO2006068760A2 (en) * 2004-11-19 2006-06-29 The Regents Of The University Of California Anti-inflammatory pyrazolopyrimidines
DOP2006000009A (es) * 2005-01-13 2006-08-15 Arena Pharm Inc Procedimiento para preparar eteres de pirazolo [3,4-d] pirimidina
US8143285B2 (en) 2005-09-06 2012-03-27 Shionogi & Co., Ltd. Indolecarboxylic acid derivative having PGD2 receptor antagonistic activity
US20070072933A1 (en) * 2005-09-26 2007-03-29 Peyman Gholam A Delivery of an ocular agent
WO2007061737A2 (en) 2005-11-17 2007-05-31 Osi Pharmaceuticals, Inc. FUSED BICYCLIC mTOR INHIBITORS
KR101461680B1 (ko) * 2005-12-02 2014-11-19 바이엘 헬스케어 엘엘씨 과다-증식성 장애 및 맥관형성과 관련된 질환의 치료에유용한 치환된 4-아미노-피롤로트리아진 유도체
PE20070855A1 (es) * 2005-12-02 2007-10-14 Bayer Pharmaceuticals Corp Derivados de 4-amino-pirrolotriazina sustituida como inhibidores de quinasas
JP5193876B2 (ja) * 2005-12-02 2013-05-08 バイエル・ヘルスケア・エルエルシー オーロラキナーゼの阻害により癌を処置するために有用なピロロトリアジン誘導体
CN101389630A (zh) * 2005-12-29 2009-03-18 艾博特公司 蛋白激酶抑制剂
US7625880B2 (en) * 2006-01-13 2009-12-01 Pharmacyclics, Inc. Inhibitors of tyrosine kinases and uses thereof
US7897634B2 (en) * 2006-02-09 2011-03-01 Athersys, Inc. Pyrazoles for the treatment of obesity and other CNS disorders
CA2645137A1 (en) * 2006-03-07 2007-09-13 James F. Blake Heterobicyclic pyrazole compounds and methods of use
EP2004654B1 (en) 2006-04-04 2013-05-22 The Regents of the University of California Pyrazolopyrimidine derivatives for use as kinase antagonists
NL2000613C2 (nl) * 2006-05-11 2007-11-20 Pfizer Prod Inc Triazoolpyrazinederivaten.
GB0610242D0 (en) 2006-05-23 2006-07-05 Novartis Ag Organic compounds
PL2526934T4 (pl) 2006-09-22 2016-09-30 Inhibitory kinazy tyrozynowej Brutona
EP2089391B1 (en) 2006-11-03 2013-01-16 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
ES2371723T3 (es) 2006-12-20 2012-01-09 Bayer Healthcare, Llc 4-{4-[({3-terc-butil-1-[3-(hidroximetil)fenil]-1h-pirazol-5-il}carbamoil)amino]-3-clorofenoxi}-n-metilpiridina-2-carboxamida como un inhibidor de vegfr cinasa para el tratamiento contra el cáncer.
KR20090101362A (ko) * 2006-12-26 2009-09-25 파마시클릭스, 인코포레이티드 병용 치료에 있어서 히스톤 디아세틸라제 억제제 이용 및 생체표지 감시 방법
WO2008089310A2 (en) * 2007-01-18 2008-07-24 Lexicon Pharmaceuticals, Inc. Delta 5 desaturase inhibitors for the treatment of obesity
WO2008089307A2 (en) * 2007-01-18 2008-07-24 Lexicon Pharmaceuticals, Inc. Delta 5 desaturase inhibitors for the treatment of pain, inflammation and cancer
ES2562215T3 (es) 2007-03-28 2016-03-03 Pharmacyclics Llc Inhibidores de la tirosina quinasa de Bruton
US8809273B2 (en) 2007-03-28 2014-08-19 Pharmacyclics, Inc. Inhibitors of Bruton's tyrosine kinase
CA2695004C (en) 2007-07-17 2016-01-19 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
RU2477282C2 (ru) * 2007-08-17 2013-03-10 Эл Джи Лайф Сайенсиз Лтд. Соединения индола в качестве ингибиторов клеточного некроза
WO2009046448A1 (en) 2007-10-04 2009-04-09 Intellikine, Inc. Chemical entities and therapeutic uses thereof
EP3613743B1 (en) 2008-01-04 2022-03-16 Intellikine, LLC Processes for the preparation of 1h-pyrazolo[3,4-d]pyrimidin-4-amine derivatives
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
WO2009111529A2 (en) * 2008-03-04 2009-09-11 Children's Medical Center Corporation Method of treating polycystic kidney disease
WO2009114874A2 (en) 2008-03-14 2009-09-17 Intellikine, Inc. Benzothiazole kinase inhibitors and methods of use
WO2009114870A2 (en) 2008-03-14 2009-09-17 Intellikine, Inc. Kinase inhibitors and methods of use
WO2009136965A1 (en) * 2008-05-06 2009-11-12 Sequella, Inc. Compositions and methods comprising capuramycin analogues
US20100101977A1 (en) * 2008-06-05 2010-04-29 United Comb & Novelty Corporation Stackable Packaging For Lipped Containers
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
US9096611B2 (en) 2008-07-08 2015-08-04 Intellikine Llc Kinase inhibitors and methods of use
US8946239B2 (en) 2008-07-10 2015-02-03 Duquesne University Of The Holy Spirit Substituted pyrrolo, -furano, and cyclopentylpyrimidines having antimitotic and/or antitumor activity and methods of use thereof
CA2730930C (en) 2008-07-16 2015-01-13 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors
CA2738429C (en) 2008-09-26 2016-10-25 Intellikine, Inc. Heterocyclic kinase inhibitors
AU2009305669A1 (en) * 2008-10-16 2010-04-22 The Regents Of The University Of California Fused ring heteroaryl kinase inhibitors
WO2010051561A1 (en) * 2008-11-03 2010-05-06 Chemocentryx, Inc. Compounds for the treatment of osteoporosis and cancers
US8476282B2 (en) 2008-11-03 2013-07-02 Intellikine Llc Benzoxazole kinase inhibitors and methods of use
CA2758136A1 (en) * 2009-04-15 2010-10-21 Fondazione Irccs Istituto Nazionale Dei Tumori Use of multi-kinase inhibitors in the treatment of vascular hyperpermeability
JP5789252B2 (ja) 2009-05-07 2015-10-07 インテリカイン， エルエルシー 複素環式化合物およびその使用
JP5819831B2 (ja) 2009-08-17 2015-11-24 インテリカイン， エルエルシー 複素環式化合物およびそれらの使用
CA2771895A1 (en) * 2009-08-28 2011-03-03 Array Biopharma Inc. Raf inhibitor compounds and methods of use thereof
US7741330B1 (en) 2009-10-12 2010-06-22 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase
WO2011047384A2 (en) 2009-10-16 2011-04-21 The Regents Of The University Of California Methods of inhibiting ire1
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
EP3378854B1 (en) 2010-01-27 2022-12-21 Arena Pharmaceuticals, Inc. Processes for the preparation of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid and salts thereof
EP2534151B1 (en) 2010-02-08 2018-11-14 Merck Sharp & Dohme B.V. 8-methyl-1-phenyl-imidazol[1,5-a]pyrazine compounds
JP5951600B2 (ja) 2010-05-21 2016-07-13 インフィニティー ファーマシューティカルズ， インコーポレイテッド キナーゼ調節のための、化合物、組成物および方法
US9096531B2 (en) 2010-05-24 2015-08-04 Toa Eiyo Ltd. Fused imidazole derivative
EA031737B1 (ru) 2010-06-03 2019-02-28 Фармасайкликс, Инк. Применение ингибиторов тирозинкиназы брутона (btk) для лечения лейкоза и лимфомы
BR112013008100A2 (pt) 2010-09-22 2016-08-09 Arena Pharm Inc "moduladores do receptor de gpr19 e o tratamento de distúrbios relacionados a eles."
CN103298474B (zh) 2010-11-10 2016-06-29 无限药品股份有限公司 杂环化合物及其用途
BR112013017670B1 (pt) 2011-01-10 2022-07-19 Infinity Pharmaceuticals, Inc Processos de preparação de isoquinolinonas e formas sólidas de isoquinolinonas
US8889684B2 (en) * 2011-02-02 2014-11-18 Boehringer Ingelheim International Gmbh Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors
US9295673B2 (en) 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
HUE033019T2 (en) 2011-05-17 2017-11-28 Principia Biopharma Inc Tyrosine kinase inhibitors
WO2012158795A1 (en) 2011-05-17 2012-11-22 Principia Biopharma Inc. Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors
EP2726634B1 (en) 2011-07-01 2017-02-22 Dana-Farber Cancer Institute, Inc. Discovery of a somatic mutation in myd88 gene in lymphoplasmacytic lymphoma
US9138436B2 (en) 2011-07-13 2015-09-22 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase
WO2013012915A1 (en) 2011-07-19 2013-01-24 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
EP2548877A1 (en) * 2011-07-19 2013-01-23 MSD Oss B.V. 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
EP2734530A1 (en) 2011-07-19 2014-05-28 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
AR091790A1 (es) 2011-08-29 2015-03-04 Infinity Pharmaceuticals Inc Derivados de isoquinolin-1-ona y sus usos
JP6342805B2 (ja) * 2011-09-02 2018-06-13 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 置換ピラゾロ［３，４−ｄ］ピリミジンおよびその用途
CA2845806C (en) 2011-09-13 2019-06-11 Pharmacyclics, Inc. Formulations of histone deacetylase inhibitor in combination with bendamustine and uses thereof
CA2856291C (en) 2011-11-17 2020-08-11 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
BR112014019459B1 (pt) 2012-02-08 2023-04-18 Mcure Biosciences Inc Proteínas de ligação à cdim e usos das mesmas
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
WO2013177668A1 (en) * 2012-05-31 2013-12-05 Pharmascience, Inc. Protein kinase inhibitors
NZ702548A (en) 2012-06-04 2015-11-27 Pharmacyclics Llc Crystalline forms of a bruton’s tyrosine kinase inhibitor
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
GB201211309D0 (en) * 2012-06-26 2012-08-08 Fujifilm Mfg Europe Bv Process for preparing membranes
JP6575950B2 (ja) 2012-07-24 2019-09-18 ファーマサイクリックス エルエルシー Ｂｒｕｔｏｎ型チロシンキナーゼ（Ｂｔｋ）阻害剤に対する耐性を伴う変異
EP2878601B1 (en) 2012-07-27 2018-03-28 Riken Agent for treating or controlling recurrence of acute myelogenous leukemia
US9266895B2 (en) 2012-09-10 2016-02-23 Principia Biopharma Inc. Substituted pyrazolo[3,4-d]pyrimidines as kinase inhibitors
CA2886240A1 (en) 2012-09-26 2014-04-03 The Regents Of The University Of California Modulation of ire1
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
US9758522B2 (en) * 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
EP2920180A4 (en) 2012-11-15 2016-04-13 Pharmacyclics Inc PYRROLOPYRIMIDINE COMPOUNDS AS KINASE INHIBITORS
AU2013355110B2 (en) 2012-12-07 2017-11-09 VenatoRx Pharmaceuticals, Inc. Beta-lactamase inhibitors
US9040504B2 (en) 2013-01-10 2015-05-26 VenatoRx Pharmaceuticals, Inc. Beta-lactamase inhibitors
EP2953940B1 (en) 2013-02-07 2018-08-22 Heptares Therapeutics Limited Piperidin-1-yl and azepin-1-yl carboxylates as muscarinic m4 receptor agonists
LT2970291T (lt) * 2013-03-15 2022-06-10 Janssen Pharmaceutica, N.V. Vaisto paruošimo technologiniai procesai ir tarpiniai junginiai
US9481667B2 (en) 2013-03-15 2016-11-01 Infinity Pharmaceuticals, Inc. Salts and solid forms of isoquinolinones and composition comprising and methods of using the same
CA2907726A1 (en) 2013-03-22 2014-09-25 Millennium Pharmaceuticals, Inc. Combination of catalytic mtorc1/2 inhibitors and selective inhibitors of aurora a kinase
US8957080B2 (en) 2013-04-09 2015-02-17 Principia Biopharma Inc. Tyrosine kinase inhibitors
KR101793807B1 (ko) 2013-04-25 2017-11-03 베이진 엘티디 단백질 키나제 억제제로서의 융합된 헤테로시클릭 화합물
CA2919996A1 (en) 2013-08-02 2015-02-05 Pharmacyclics Llc Methods for the treatment of solid tumors
EP3033079B1 (en) 2013-08-12 2018-10-31 Pharmacyclics LLC Methods for the treatment of her2 amplified cancer
KR102100419B1 (ko) 2013-09-13 2020-04-14 베이진 스위찰랜드 게엠베하 항-pd1 항체 및 이의 치료 및 진단 용도
BR112016006978A2 (pt) 2013-09-30 2017-08-01 Pharmacyclics Llc inibidores de tirosina quinase de bruton
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CN105793255B (zh) 2013-10-04 2018-11-16 无限药品股份有限公司 杂环化合物及其用途
EP3057955B1 (en) 2013-10-18 2018-04-11 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
JP6491202B2 (ja) 2013-10-18 2019-03-27 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド サイクリン依存性キナーゼ７（ｃｄｋ７）の多環阻害剤
EP3060218A4 (en) 2013-10-25 2017-07-19 Pharmacyclics LLC Methods of treating and preventing graft versus host disease
CA2932351A1 (en) 2013-12-13 2015-06-18 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
WO2015132799A2 (en) * 2014-02-03 2015-09-11 Cadila Healthcare Limited Novel heterocyclic compounds
AU2015217221A1 (en) * 2014-02-13 2016-08-11 Ligand Pharmaceuticals, Inc. Prodrug compounds and their uses
US10092569B2 (en) 2014-02-21 2018-10-09 Principia Biopharma Inc. Salts and solid form of a BTK inhibitor
EP4066834A1 (en) 2014-03-19 2022-10-05 Infinity Pharmaceuticals, Inc. Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders
JP2017509336A (ja) 2014-03-20 2017-04-06 ファーマサイクリックス エルエルシー ホスホリパーゼｃガンマ２及び耐性に関連した変異
US20150320755A1 (en) 2014-04-16 2015-11-12 Infinity Pharmaceuticals, Inc. Combination therapies
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
GB201410430D0 (en) 2014-06-11 2014-07-23 Redx Pharma Ltd Compounds
TWI687438B (zh) 2014-07-03 2020-03-11 英屬開曼群島商百濟神州生物科技有限公司 抗ｐｄ-ｌ１抗體及其作為治療及診斷之用途
AU2015296215A1 (en) 2014-08-01 2017-03-23 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
BR112017002231A2 (pt) 2014-08-07 2018-07-17 Pharmacyclics Llc novas formulações de um inibidor de tirosina cinase de bruton
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
ITRM20140620A1 (it) 2014-10-30 2016-04-30 Lead Discovery Siena S R L Compounds and uses thereof
CN107205970A (zh) 2014-11-05 2017-09-26 弗莱塞斯生物科学公司 免疫调节剂
UY36390A (es) 2014-11-05 2016-06-01 Flexus Biosciences Inc Compuestos moduladores de la enzima indolamina 2,3-dioxigenasa (ido), sus métodos de síntesis y composiciones farmacéuticas que los contienen
CN104478884A (zh) * 2014-12-05 2015-04-01 广东东阳光药业有限公司 一种中间体的制备方法
CN107257686B (zh) 2014-12-18 2021-01-29 普林斯匹亚生物制药公司 天疱疮的治疗
JP6736253B2 (ja) * 2014-12-22 2020-08-05 ザ チャイニーズ ユニバーシティ オブ ホンコン 体細胞から多能性幹細胞を作製するための機械的操作とプログラミンの併用
US10167451B2 (en) 2014-12-22 2019-01-01 The Chinese University Of Hong Kong Combinational use of mechanical manipulation and programin derivatives to increase Oct4, Sox2, or Nanog expression in fibroblasts
US10870651B2 (en) 2014-12-23 2020-12-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
KR102595163B1 (ko) 2015-01-06 2023-10-30 아레나 파마슈티칼스, 인크. S1p1 수용체와 관련된 상태의 치료 방법
CN105777755A (zh) * 2015-01-07 2016-07-20 常州百敖威生物科技有限公司 一种伊鲁替尼中间体3-碘-1h-吡唑并[3,4-d]嘧啶-4-胺的制备方法
IL315294A (en) 2015-03-03 2024-10-01 Pharmacyclics Llc Pharmaceutical formulations of proton tyrosine kinase inhibitor
CA2978518C (en) 2015-03-27 2023-11-21 Nathanael S. Gray Inhibitors of cyclin-dependent kinases
US10702527B2 (en) 2015-06-12 2020-07-07 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
KR20230160955A (ko) 2015-06-22 2023-11-24 아레나 파마슈티칼스, 인크. Ｓ1ｐ1 수용체-관련 장애에서의 사용을 위한 (ｒ)-2-(7-(4-시클로펜틸-3-(트리플루오로메틸)벤질옥시)-1,2,3,4-테트라히드로시클로-펜타[ｂ]인돌-3-일)아세트산 (화합물 1)의 결정성 ｌ-아르기닌 염
MA42242A (fr) 2015-06-24 2018-05-02 Principia Biopharma Inc Inhibiteurs de la tyrosine kinase
AU2016319125B2 (en) 2015-09-09 2021-04-08 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
CA2998469A1 (en) 2015-09-14 2017-03-23 Infinity Pharmaceuticals, Inc. Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same
EP3350184B1 (en) 2015-09-16 2022-10-19 Loxo Oncology, Inc. Pyrazolopyrimidine derivatives as btk inhibitors for the treatment of cancer
TN2018000213A1 (en) 2015-12-16 2019-10-04 Loxo Oncology Inc Compounds useful as kinase inhibitors
WO2017161116A1 (en) 2016-03-17 2017-09-21 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors
WO2017214269A1 (en) 2016-06-08 2017-12-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
UA125216C2 (uk) 2016-06-24 2022-02-02 Інфініті Фармасьютікалз, Інк. Комбінована терапія
CN115054586B (zh) 2016-06-29 2024-08-02 普林斯匹亚生物制药公司 改性的释放制剂
WO2018007885A1 (en) 2016-07-05 2018-01-11 Beigene, Ltd. COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER
MX2019001900A (es) 2016-08-16 2019-07-01 Beigene Ltd Forma cristalina de (s)-7-(1-acriloilpiperidin-4-il)-2-(4-fenoxife nil)-4,5,6,7-tetra-hidropirazolo[1,5-a]pirimidin-3-carboxamida, preparacion y usos de la misma.
FI3500299T3 (fi) 2016-08-19 2024-02-14 Beigene Switzerland Gmbh Tsanubrutinibin yhdistelmä cd20-tai pd-1-vasta-aineen kanssa käytettäväksi syövän hoidossa
CN110461847B (zh) 2017-01-25 2022-06-07 百济神州有限公司 (S)-7-(1-(丁-2-炔酰基)哌啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氢吡唑并[1,5-a]嘧啶-3-甲酰胺的结晶形式、其制备及用途
KR20190116416A (ko) 2017-02-16 2019-10-14 아레나 파마슈티칼스, 인크. 원발 담즙성 담관염을 치료하기 위한 화합물 및 방법
WO2019001417A1 (en) 2017-06-26 2019-01-03 Beigene, Ltd. IMMUNOTHERAPY FOR HEPATOCELLULAR CARCINOMA
US11377449B2 (en) 2017-08-12 2022-07-05 Beigene, Ltd. BTK inhibitors with improved dual selectivity
WO2019108795A1 (en) 2017-11-29 2019-06-06 Beigene Switzerland Gmbh Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors
AU2019207625A1 (en) 2018-01-09 2020-07-30 Ligand Pharmaceuticals, Inc. Acetal compounds and therapeutic uses thereof
CN108299311A (zh) * 2018-02-28 2018-07-20 杭州福斯特药业有限公司 一种5-溴-2-氯-n-环戊基嘧啶-4-胺的制备方法
CN111171035B (zh) * 2018-11-13 2021-03-30 山东大学 4-苯氧基苯基吡唑并嘧啶酰胺衍生物的制备方法和应用
CN111454268B (zh) * 2019-01-18 2023-09-08 明慧医药（上海）有限公司 作为布鲁顿酪氨酸激酶抑制剂的环状分子
WO2020263935A1 (en) * 2019-06-24 2020-12-30 Dana-Farber Cancer Institute, Inc. Hck degraders and uses thereof
CN110511225B (zh) * 2019-08-19 2023-07-18 杭州中美华东制药有限公司 一种伊布替尼中间体的合成方法
WO2021038540A1 (en) 2019-08-31 2021-03-04 Sun Pharma Advanced Research Company Limited Cycloalkylidene carboxylic acids and derivatives as btk inhibitors
PT4031547T (pt) 2019-09-18 2024-08-27 Takeda Pharmaceuticals Co Inibidores de calicreína plasmática e utilizações dos mesmos
US11370803B2 (en) 2019-09-18 2022-06-28 Takeda Pharmaceutical Company Limited Heteroaryl plasma kallikrein inhibitors
EP4041239A1 (en) * 2019-10-08 2022-08-17 Dana-Farber Cancer Institute, Inc. A pyrazolopyrimidine derivative as a hck inhibitor for use in therapy, in particular myd88 mutated diseases
CN112961158B (zh) * 2020-03-05 2022-07-01 四川大学华西医院 氨基嘧啶并吡唑/吡咯类衍生物及其制备方法和用途
AU2020436612A1 (en) 2020-03-16 2022-09-01 Flash Therapeutics, Llc Compounds for treating or inhibiting recurrence of acute myeloid leukemia
TWI797711B (zh) 2020-08-13 2023-04-01 大陸商上海和譽生物醫藥科技有限公司 一種fgfr及其突變抑制劑，其製備方法和應用
JP2023549540A (ja) 2020-11-18 2023-11-27 デシフェラ・ファーマシューティカルズ，エルエルシー Ｇｃｎ２およびｐｅｒｋキナーゼ阻害剤およびその使用方法
US20240226106A1 (en) * 2021-03-17 2024-07-11 Shire Human Genetic Therapies, Inc. Inhibitors of plasma kallikrein
US11786531B1 (en) 2022-06-08 2023-10-17 Beigene Switzerland Gmbh Methods of treating B-cell proliferative disorder
CN115650986B (zh) * 2022-10-22 2024-07-30 浙江工业大学 肉桂酰氨基吡唑并[3,4-d]嘧啶类化合物及其制备和应用

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4140851A (en) 1977-11-21 1979-02-20 The United States Of America As Represented By The Department Of Health, Education And Welfare Synthesis and antitumor activity of 2,4,5-trisubstituted-pyrrolo2,3-d]-pyrimidine nucleosides
DE2818676A1 (de) 1978-04-27 1979-11-08 Troponwerke Gmbh & Co Kg Substituierte 5,6-dimethylpyrrolo 2,3-d pyrimidine, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
DE3036390A1 (de) 1980-09-26 1982-05-13 Troponwerke GmbH & Co KG, 5000 Köln Neue pyrrolo-pyrimidine, verfahren zu ihrer herstellung und ihre verwendung bei der herstellung von biologischen wirkstoffen
US4892865A (en) 1987-12-01 1990-01-09 The Regents Of The University Of Michigan Pyrrolo[2,3-d]pyrimidine nucleosides as antiviral agents
US4968686A (en) 1988-04-08 1990-11-06 The Regents Of The University Of Michigan Acyclic pyrrolo [2,3-d]pyrimidine analogs as antiviral agents
US4927830A (en) 1988-04-08 1990-05-22 The Regents Of The University Of Michigan Acyclic pyrrolo[2,3-D]pyrimidine analogs as antiviral agents
JP2983254B2 (ja) 1989-06-14 1999-11-29 武田薬品工業株式会社 ピロロ〔２，３―ｄ〕ピリミジン誘導体の製造法およびその中間体
US5674998A (en) 1989-09-15 1997-10-07 Gensia Inc. C-4' modified adenosine kinase inhibitors
US5721356A (en) 1989-09-15 1998-02-24 Gensia, Inc. Orally active adenosine kinase inhibitors
US5726302A (en) 1989-09-15 1998-03-10 Gensia Inc. Water soluble adenosine kinase inhibitors
KR0162654B1 (ko) 1989-12-11 1998-11-16 알렌 제이. 시니스갤리 N-(피롤로[2,3-d]피리미딘-3-일아크릴)-글루타민산 유도체
US4996206A (en) 1989-12-11 1991-02-26 The Trustees Of Princeton University N-(pyrrolo[2,3-d]pyrimidin-3-ylacyl)-glutamic acid derivatives
US5248775A (en) 1989-12-11 1993-09-28 The Trustees Of Princeton University Pyrrolo(2,3-d)pyrimidines
CA2100863A1 (en) 1991-01-23 1992-07-24 David A. Bullough Adenosine kinase inhibitors
US5254687A (en) 1991-12-04 1993-10-19 The Trustees Of Princeton University Process for the preparation of pyrrolo[2,3-d]pyrimidines
IL108523A0 (en) 1993-02-03 1994-05-30 Gensia Inc Pharmaceutical compositions containing adenosine kinase inhibitors for preventing or treating conditions involving inflammatory responses and pain
NZ293249A (en) 1994-09-29 1999-04-29 Novartis Ag 4-amino-5,7-diaryl-pyrrolo[2,3-d]pyrimidines and their use
DE69609602T2 (de) * 1995-04-03 2001-04-12 Novartis Ag, Basel Pyrazolderivate und verfahren zu deren herstellung
US5593997A (en) * 1995-05-23 1997-01-14 Pfizer Inc. 4-aminopyrazolo(3-,4-D)pyrimidine and 4-aminopyrazolo-(3,4-D)pyridine tyrosine kinase inhibitors
GB9514265D0 (en) 1995-07-13 1995-09-13 Wellcome Found Hetrocyclic compounds
AR004010A1 (es) 1995-10-11 1998-09-30 Glaxo Group Ltd Compuestos heterociclicos
CH690773A5 (de) 1996-02-01 2001-01-15 Novartis Ag Pyrrolo(2,3-d)pyrimide und ihre Verwendung.
ES2202827T3 (es) 1997-03-19 2004-04-01 ABBOTT GMBH & CO. KG Pirrolo(2,3-d)pirimidinas y su uso como inhibidores de la tirosina kinasa.

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