PE20141281A1 - Compuestos de tetrahidropirido-piridina y tetrahidropirido-pirimidina y su uso como moduladores de receptores de c5a - Google Patents

Compuestos de tetrahidropirido-piridina y tetrahidropirido-pirimidina y su uso como moduladores de receptores de c5a

Info

Publication number
PE20141281A1
PE20141281A1 PE2014000114A PE2014000114A PE20141281A1 PE 20141281 A1 PE20141281 A1 PE 20141281A1 PE 2014000114 A PE2014000114 A PE 2014000114A PE 2014000114 A PE2014000114 A PE 2014000114A PE 20141281 A1 PE20141281 A1 PE 20141281A1
Authority
PE
Peru
Prior art keywords
alkyl
tetrahydropyride
pyrimidine
pyridine
dimethylphenyl
Prior art date
Application number
PE2014000114A
Other languages
English (en)
Inventor
Christine Gelin
Alec Flyer
Christopher Michael Adams
Veronique Darsigny
Timothy Brian Hurley
Rajeshri Ganesh Karki
Nan Jiang
Toshio Kawanami
Erik Meredith
Michael H Serrano-Wu
Chang Rao
Catherine Solovay
George Tien-San Lee
Christopher Towler
Denis Har
Lichun Shen
Bin Hu
Xinglong Jiang
Christina Cappaci-Daniel
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46604083&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20141281(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20141281A1 publication Critical patent/PE20141281A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Transplantation (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE TETRAHIDROPIRIDO-PIRIDINA Y TETRAHIDROPIRIDO-PIRIMIDINA DE FORMULA (I) DONDE X ES N O CH; Z1 ES N O CR1c, EN DONDE R1c ES H, HALOGENO O ALQUILO(C1-C6); Z2 ES N O CR1d, EN DONDE R1d ES H, ALQUILO(C1-C6), ALCOXILO(C1-C6), ENTRE OTROS; R1a ES H, ALQUILO(C1-C6), ALCOXILO(C1-C6), CN, ENTRE OTROS; R1b ES H, AMINO, ALQUILAMINO(C1-C4), ENTRE OTROS; R1e ES H, HALOGENO, CN, ALQUILO(C1-C6), ENTRE OTROS; R2 ES H, ALQUILO(C1-C6); CICLOALQUILO(C3-C7), ENTRE OTROS; R3 ES FENILO, HETEROARILO O FENILALQUILO(C1-C3); R4 ES H O ALQUILO(C1-C4); R5 ES H, O R4 Y R5 EN COMBINACION SON OXO; R6 ES H O AMBOS R6 FORMAN UN CARBONILO. SON COMPUESTOS PREFERIDOS: 1-(2-(2,6-DIMETILFENIL)-6-(3-ISOPROPIL-1-METIL-1H-PIRAZOL-5-IL)-5,6,7,8-TETRAHIDROPIRIDO[4,3-d]PIRIMIDIN-4-IL)-2-METILPIPERIDIN-4-OL RACEMICO; 2-(2,6-DIMETILFENIL)-4-(3,3-DIMETILPIPERIDIN-1-IL)-6-(3-ISOPROPIL-1-METIL-1H-PIRAZOL-5-IL)-5,6,7,8-TETRAHIDROPIRIDO[4,3-d]PIRIMIDINA; (S)-2-(2,6-DIMETILFENIL)-6-(3-ISOPROPIL-1-METIL-1H-PIRAZOL-5-IL)-4-(2-METILPIPERIDIN-1-IL)-5,6,7,8-TETRAHIDROPIRIDO[4,3-d]PIRIMIDINA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DE RECEPTORES DE C5A DEL COMPLEMENTO MAMIFERO SIENDO UTILES EN EL TRATAMIENTO DE RETINOPATIA DIABETICA, RETINITIS PIGMENTOSA, PENFIGO OCULAR
PE2014000114A 2011-07-22 2012-07-20 Compuestos de tetrahidropirido-piridina y tetrahidropirido-pirimidina y su uso como moduladores de receptores de c5a PE20141281A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161510643P 2011-07-22 2011-07-22
US201161539732P 2011-09-27 2011-09-27

Publications (1)

Publication Number Publication Date
PE20141281A1 true PE20141281A1 (es) 2014-09-24

Family

ID=46604083

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2014000114A PE20141281A1 (es) 2011-07-22 2012-07-20 Compuestos de tetrahidropirido-piridina y tetrahidropirido-pirimidina y su uso como moduladores de receptores de c5a

Country Status (25)

Country Link
US (2) US8846656B2 (es)
EP (1) EP2734521B1 (es)
JP (1) JP6040237B2 (es)
KR (1) KR20140096020A (es)
CN (1) CN103814027B (es)
AP (1) AP2014007398A0 (es)
AR (1) AR087288A1 (es)
AU (1) AU2012287183B2 (es)
BR (1) BR112014001468A2 (es)
CA (1) CA2842528A1 (es)
CL (1) CL2014000171A1 (es)
CO (1) CO6862157A2 (es)
CR (1) CR20140032A (es)
EA (1) EA201490320A1 (es)
ES (1) ES2637167T3 (es)
IL (1) IL230501A0 (es)
MA (1) MA35275B1 (es)
MX (1) MX336497B (es)
PE (1) PE20141281A1 (es)
PL (1) PL2734521T3 (es)
PT (1) PT2734521T (es)
TN (1) TN2014000030A1 (es)
TW (1) TW201311688A (es)
UY (1) UY34209A (es)
WO (1) WO2013016197A1 (es)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012035078A1 (en) * 2010-09-16 2012-03-22 Novartis Ag 17α-HYDROXYLASE/C17,20-LYASE INHIBITORS
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
US8846656B2 (en) 2011-07-22 2014-09-30 Novartis Ag Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators
ES2630079T3 (es) * 2012-05-04 2017-08-17 Novartis Ag Moduladores de la ruta del complemento y usos de los mismos
US9056874B2 (en) 2012-05-04 2015-06-16 Novartis Ag Complement pathway modulators and uses thereof
NZ702747A (en) 2012-06-13 2017-03-31 Incyte Holdings Corp Substituted tricyclic compounds as fgfr inhibitors
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
JP6387391B2 (ja) * 2013-03-14 2018-09-05 ノバルティス アーゲー 眼科疾患の処置に有用な補体因子Ｂ阻害剤としての２−（１Ｈ−インドール−４−イルメチル）−３Ｈ−イミダゾ［４，５−ｂ］ピリジン−６−カルボニトリル誘導体
EP2986610B9 (en) 2013-04-19 2018-10-17 Incyte Holdings Corporation Bicyclic heterocycles as fgfr inhibitors
WO2015061693A1 (en) 2013-10-24 2015-04-30 Trustees Of Boston University Infusion system employing an infusion set for preventing mischanneling of multiple medicaments
CN105849090A (zh) 2013-10-30 2016-08-10 诺华股份有限公司 2-苄基-苯并咪唑补体因子b抑制剂及其用途
TWI656121B (zh) * 2014-08-04 2019-04-11 德商拜耳製藥公司 ２－（嗎啉－４－基）－１，７－萘啶
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
JP6506845B2 (ja) 2014-12-30 2019-04-24 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｂ型肝炎ウイルス感染症の治療及び予防のための新規テトラヒドロピリドピリミジン類及びテトラヒドロピリドピリジン類
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US9708318B2 (en) 2015-02-20 2017-07-18 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
US10898487B2 (en) 2016-12-22 2021-01-26 Boehringer Ingelheim International Gmbh Benzylamino substituted quinazolines and derivatives as SOS1 inhibitors
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
US10683294B2 (en) * 2017-05-31 2020-06-16 Chemocentryx, Inc. 5-5 fused rings as C5a inhibitors
CN110997674B (zh) * 2017-05-31 2022-12-20 凯莫森特里克斯股份有限公司 作为C5a抑制剂的6-5稠合环类
TWI810230B (zh) 2017-12-21 2023-08-01 德商百靈佳殷格翰國際股份有限公司 作為sos1抑制劑之新穎芐胺基取代吡啶并嘧啶酮及衍生物
CN111788184B (zh) 2017-12-22 2023-12-22 凯莫森特里克斯股份有限公司 用作C5aR抑制剂的二芳基取代的5,5-稠合环化合物
EP3728203B1 (en) * 2017-12-22 2024-03-13 ChemoCentryx, Inc. DIARYL SUBSTITUTED 6,5-FUSED RING COMPOUNDS AS C5aR INHIBITORS
MA51558B1 (fr) * 2018-01-10 2022-12-30 Idorsia Pharmaceuticals Ltd Dérivés de 2,4,6,7-tetrahydro-pyrazolo[4,3-d]pyrimidin-5-one et composés similaires en tant que modulateurs du récepteur c5a pour le traitement de la vascularité et de maladies inflammatoires
AR114464A1 (es) * 2018-04-02 2020-09-09 Chemocentryx Inc PROFÁRMACOS DE ANTAGONISTAS DE C5aR BICÍCLICOS FUSIONADOS
IL312465A (en) 2018-05-04 2024-06-01 Incyte Corp FGFR inhibitor solid forms and processes for their preparation
CR20200591A (es) 2018-05-04 2021-03-31 Incyte Corp Sales de un inhibidor de fgfr
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
TW202128685A (zh) 2019-10-14 2021-08-01 美商英塞特公司 作為ｆｇｆｒ抑制劑之雙環雜環
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US11407750B2 (en) 2019-12-04 2022-08-09 Incyte Corporation Derivatives of an FGFR inhibitor
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR20220143717A (ko) * 2020-02-17 2022-10-25 알레스타 테라퓨틱스 비브이 Gcn2 조정제 화합물
PE20231073A1 (es) * 2020-04-29 2023-07-17 Relay Therapeutics Inc Inhibidores de pi3k y metodos de uso de los mismos
CA3195519A1 (en) 2020-09-18 2022-03-24 Bayer Aktiengesellschaft Pyrido[2,3-d]pyrimidin-4-amines as sos1 inhibitors
EP4238961A4 (en) * 2020-10-30 2024-05-29 Daiichi Sankyo Company, Limited PROCESS FOR PREPARING A 3-METHYL-4-HALO-INDOLE DERIVATIVE
JP2024513575A (ja) 2021-04-12 2024-03-26 インサイト・コーポレイション Ｆｇｆｒ阻害剤及びネクチン－４標的化剤を含む併用療法
EP4074317A1 (en) 2021-04-14 2022-10-19 Bayer AG Phosphorus derivatives as novel sos1 inhibitors
JP2024522189A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式ヘテロ環

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
US4727149A (en) 1982-03-11 1988-02-23 John Wyeth & Brother Limited Preparation of nitriles of fused ring pyridine derivatives
US5853740A (en) 1996-08-07 1998-12-29 Abbott Laboratories Delivery system for pharmaceutical agents encapsulated with oils
WO2002022606A1 (en) 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
AU2003253130A1 (en) 2002-08-19 2004-03-03 Glenmark Pharmaceuticals Limited Condensed heterocyclic compounds as pde-iv inhibitors for the treatment of inflammatory and allergic disorders
JP2007524596A (ja) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド 共結晶医薬組成物
CA2520465A1 (en) 2003-03-28 2004-10-14 Scios Inc. Bi-cyclic pyrimidine inhibitors of tgf.beta.
BRPI0409211A (pt) 2003-04-18 2006-03-28 Lilly Co Eli composto, composição farmacêutica, métodos para ativar receptores 5-ht1f, para inibir extravasão de proteìna neuronial, e para o tratamento ou prevenção de enxaqueca em um mamìfero, e, uso de um composto
AU2004263515A1 (en) * 2003-08-05 2005-02-17 Vertex Pharmaceuticals Incorporated Condensed pyrimidine compounds as inhibitors of voltage-gated ion channels
GB0403038D0 (en) 2004-02-11 2004-03-17 Novartis Ag Organic compounds
US7482350B2 (en) 2004-05-08 2009-01-27 Neurogen Corporation 4,5-disubstituted-2-aryl pyrimidines
US7429666B2 (en) 2004-06-10 2008-09-30 Merck Frosst Canada Ltd. Pyridine analogs as C5a antagonists
JP5046942B2 (ja) 2004-09-30 2012-10-10 テイボテク・フアーマシユーチカルズ Ｈｃｖ阻害性の二環式ピリミジン類
CN102627640A (zh) 2005-08-12 2012-08-08 默沙东公司 可用作p38激酶抑制剂的杂二环化合物
JP5016666B2 (ja) 2006-04-20 2012-09-05 エフ．ホフマン−ラ ロシュ アーゲー ケモカイン受容体のジアゼパン誘導体モジュレーター
WO2007125320A1 (en) 2006-04-25 2007-11-08 Astex Therapeutics Limited Pharmaceutical compounds
US8563566B2 (en) 2007-08-01 2013-10-22 Valeant Pharmaceuticals International Naphthyridine derivatives as potassium channel modulators
WO2009023669A1 (en) 2007-08-13 2009-02-19 Janssen Pharmaceutica N.V. Substituted 5,6,7,8-tetrahydroquinoline derivatives, compositions, and methods of use thereof
CA2729045A1 (en) 2008-07-31 2010-02-04 Philippe Bergeron Pyrimidine compounds, compositions and methods of use
WO2010028174A1 (en) 2008-09-03 2010-03-11 Dr. Reddy's Laboratories Ltd. Novel biccyclic compounds as gata modulators
AR073304A1 (es) 2008-09-22 2010-10-28 Jerini Ag Moduladores del receptor de bradiquinina b2 de molecula pequena
WO2010120994A2 (en) 2009-04-17 2010-10-21 Wyeth Llc Ureidoaryl-and carbamoylaryl-morpholino- pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their synthesis
WO2010126833A1 (en) 2009-04-27 2010-11-04 Jerini Ophthalmic Inc. Sustained release formulations of peptidomimetic drugs and uses thereof
EP2434885B1 (en) 2009-05-27 2014-03-26 Merck Sharp & Dohme Corp. Alkoxy tetrahydro-pyridopyrimidine pde10 inhibitors
EP2467382B1 (en) 2009-08-17 2014-06-25 Merck Sharp & Dohme Corp. Amino tetrahydro-pyridopyrimidine pde10 inhibitors
JP2013032290A (ja) 2009-11-20 2013-02-14 Dainippon Sumitomo Pharma Co Ltd 新規縮合ピリミジン誘導体
US8846656B2 (en) 2011-07-22 2014-09-30 Novartis Ag Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators
US20140227321A1 (en) 2011-09-30 2014-08-14 Kineta, Inc. Anti-viral compounds
US10220002B2 (en) 2011-12-02 2019-03-05 Board Of Regents Of The University Of Nebraska Controlled-release peptide compositions and uses thereof

Also Published As

Publication number Publication date
CA2842528A1 (en) 2013-01-31
CN103814027B (zh) 2016-07-06
EP2734521A1 (en) 2014-05-28
CN103814027A (zh) 2014-05-21
IL230501A0 (en) 2014-03-31
KR20140096020A (ko) 2014-08-04
AP2014007398A0 (en) 2014-01-31
MX2014000898A (es) 2014-02-19
UY34209A (es) 2013-02-28
CR20140032A (es) 2014-05-16
BR112014001468A2 (pt) 2017-01-10
PT2734521T (pt) 2017-08-11
CL2014000171A1 (es) 2014-10-03
MX336497B (es) 2016-01-21
AU2012287183A1 (en) 2014-01-30
TN2014000030A1 (en) 2015-07-01
JP6040237B2 (ja) 2016-12-07
CO6862157A2 (es) 2014-02-10
EP2734521B1 (en) 2017-05-10
AU2012287183B2 (en) 2014-11-20
JP2014521607A (ja) 2014-08-28
US20130184253A1 (en) 2013-07-18
WO2013016197A1 (en) 2013-01-31
PL2734521T3 (pl) 2017-10-31
US9505755B2 (en) 2016-11-29
ES2637167T3 (es) 2017-10-11
TW201311688A (zh) 2013-03-16
US8846656B2 (en) 2014-09-30
MA35275B1 (fr) 2014-07-03
EA201490320A1 (ru) 2014-06-30
AR087288A1 (es) 2014-03-12
US20140349995A1 (en) 2014-11-27

Similar Documents

Publication Publication Date Title
PE20141281A1 (es) Compuestos de tetrahidropirido-piridina y tetrahidropirido-pirimidina y su uso como moduladores de receptores de c5a
PE20110835A1 (es) Piridiloxi-indoles inhibidores del vegf-r2 y uso de los mismos para el tratamiento de enfermedades
PE20141205A1 (es) Spiro-[1,3]-oxacinas y spiro-[1,4]-oxacepinas como inhibidores de bace1 y/o bace2
PE20130306A1 (es) Morfolinopirimidinas y su uso en terapia
PE20081755A1 (es) Nuevas 2-aminooxazolinas como ligandos taar1
PE20161443A1 (es) Compuestos
MX348920B (es) Derivados de 2-(fenil o pirid-3-il)aminopirimidina como moduladores de proteina cinasa 2 de repeticion rica en leucina (lrrk2) para el tratamiento de la enfermedad de parkinson.
MX349556B (es) Derivados de aminopirimidina como moduladores de proteina cinasa 2 rica en unidades repetitivas de leucina (lrrk2).
PE20141827A1 (es) Inhibidores de proteinas quinasas
MX2013007295A (es) Quinoxalinas y aza-quinoxalinas como moduladores del receptor de crth2.
PE20160664A1 (es) Compuestos heteroaromaticos y su uso como ligandos d1 de dopamina
PE20141974A1 (es) Compuestos de heterociclilo
PE20191142A1 (es) 2,4 diamino-quinolina sustituida como nuevos agentes anti-cancerigenos
PE20060691A1 (es) Serinamidas sustituidas por benzoilo
PE20110405A1 (es) Derivados de piridino-piridinonas como inhibidores de la actividad de la tirosina quinasa de pdgf-r y/o flt-3 y su preparacion
CR20120591A (es) Derivados de aminopirimidina como moduladores de la lrrk2
PE20110852A1 (es) Antagonistas del receptor de orexina de isonicotinamida
PE20141685A1 (es) Novedosas dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de transtornos inflamatorios
PE20131377A1 (es) Triazina-oxadiazoles
PE20091818A1 (es) DERIVADOS POLISUSTITUIDOS DE 2-ARIL-6-FENIL-IMIDAZO[1,2-a] PIRIDINAS, SU PREPARACION Y SU APLICACION EN TERAPEUTICA
DOP2013000243A (es) Inhibidores sustituidos de acetil-coa carboxilasa
PE20141307A1 (es) Aril dihidropiridinona y piperidinona como inhibidores de monoacilglicerol aciltransferasa (mgat2)
PE20091811A1 (es) DERIVADOS DE IMIDAZOLIDINONA COMO INHIBIDORES DE 11b-HSD1
MX358172B (es) Derivados de pirazol aminopirimidina como moduladores de la proteina cinasa 2 de repeticion rica en leucina (lrrk2) para usarse en el tratamiento de la enfermedad de parkinson.
TW200519112A (en) Tropane derivatives

Legal Events

Date Code Title Description
FD Application declared void or lapsed