AR089939A1 - COMPUESTOS BICICLICOS COMO INHIBIDORES DE mPGES-1 - Google Patents

COMPUESTOS BICICLICOS COMO INHIBIDORES DE mPGES-1

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Publication number
AR089939A1
AR089939A1 ARP130100396A AR089939A1 AR 089939 A1 AR089939 A1 AR 089939A1 AR P130100396 A ARP130100396 A AR P130100396A AR 089939 A1 AR089939 A1 AR 089939A1
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AR
Argentina
Prior art keywords
substituted
unsubstituted
cycloalkyl
alkyl
independently selected
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English (en)
Inventor
Atmaram Gharat Laxmikant
Banerjee Abhisek
Khairatkar-Joshi Neelima
Ganapati Kattige Vidya
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Glenmark Pharmaceuticals Sa
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
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Application filed by Glenmark Pharmaceuticals Sa filed Critical Glenmark Pharmaceuticals Sa
Publication of AR089939A1 publication Critical patent/AR089939A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88Oxygen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20Oxygen atoms
    • C07D215/22Oxygen atoms attached in position 2 or 4
    • C07D215/233Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/24Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La presente se refiere a compuestos de fórmula (1) y sales farmacéuticamente aceptables de estos, como inhibidores de mPGES-1. Estos compuestos son inhibidores de la enzima prostaglandina E1 sintasa microsomal (mPGES-1) y por lo tanto son útiles en el tratamiento de dolor y/o inflamación de una variedad de enfermedades o afecciones, tales como asma, osteoartritis, artritis reumatoide, dolor agudo o crónico y enfermedades neurodegenerativas. Reivindicación 1: Un compuesto de fórmula (1) o una sal farmacéuticamente aceptable de este, donde Y es O, NH o NRᶜ; Z¹ y Z³, que pueden ser iguales o diferentes, se seleccionan independientemente de N y CR²; G¹ se selecciona de N y CR³; con una condición de que al menos uno de Z¹, Z³ y G¹ sea N; Q¹, Q², Q³ y Q⁴, que pueden ser iguales o diferentes, se seleccionan independientemente de N, CH y CR⁴; con una condición de que Q², Q³ y Q⁴ no sean N simultáneamente; W se selecciona de alquilo C₁₋₈ sustituido o no sustituido, alcoxi C₁₋₈alquilo C₁₋₈ sustituido o no sustituido, haloalquilo C₁₋₈ sustituido o no sustituido, hidroxialquilo C₁₋₈ sustituido o no sustituido, cicloalquilo C₃₋₁₂ sustituido o no sustituido y tetrahidrofurilo o tetrahidrofuranilo sustituido o no sustituido; R¹ se selecciona de alquilo C₁₋₈ sustituido o no sustituido, alcoxi C₁₋₈alquilo C₁₋₈ sustituido o no sustituido, haloalquilo C₁₋₈ sustituido o no sustituido, hidroxialquilo C₁₋₈ sustituido o no sustituido, cicloalquilo C₃₋₁₂ sustituido o no sustituido, arilo C₆₋₁₄ sustituido o no sustituido, heterociclilo de 3 - 15 miembros sustituido o no sustituido y heteroarilo de 5 - 14 miembros sustituido o no sustituido; cada aparición de R² y R³, que pueden ser iguales o diferentes, se selecciona independientemente de hidrógeno, halógeno, nitro, ciano, hidroxilo, alquilo C₁₋₈ sustituido o no sustituido, alcoxi C₁₋₈ sustituido o no sustituido, haloalquilo C₁₋₈ sustituido o no sustituido, hidroxialquilo C₁₋₈ sustituido o no sustituido, cicloalquilo C₃₋₁₂ sustituido o no sustituido y cicloalquil C₃₋₈alquilo C₁₋₈ sustituido o no sustituido; en cada aparición, R⁴ se selecciona independientemente de halógeno, nitro, ciano, hidroxilo, alquilo C₁₋₈ sustituido o no sustituido, alcoxi C₁₋₈ sustituido o no sustituido, alcoxi C₁₋₈alquilo C₁₋₈ sustituido o no sustituido, haloalquilo C₁₋₈ sustituido o no sustituido, hidroxialquilo C₁₋₈ sustituido o no sustituido y cicloalquilo C₃₋₁₂ sustituido o no sustituido y cicloalquilo C₃₋₈alquilo C₁₋₈ sustituido o no sustituido; en cada aparición, Rᶜ se selecciona independientemente de alquilo C₁₋₈ sustituido o no sustituido y aril C₆₋₁₄alquil C₁₋₈ sustituido o no sustituido; o RC y R¹, junto con el N al que están unidos, forman un anillo de morfolina; cada aparición de RX y Rʸ, que pueden ser iguales o diferentes, se seleccionan independientemente de hidrógeno, alquilo C₁₋₈ sustituido o no sustituido y aril C₆₋₁₄alquilo C₁₋₈ sustituido o no sustituido; y n es un entero que se encuentra en el intervalo de 1 a 4, ambos inclusive.
ARP130100396 2012-02-09 2013-02-07 COMPUESTOS BICICLICOS COMO INHIBIDORES DE mPGES-1 AR089939A1 (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
IN372MU2012 2012-02-09
US201261602227P 2012-02-23 2012-02-23
IN1302MU2012 2012-04-24
US201261645193P 2012-05-10 2012-05-10
IN2576MU2012 2012-09-05
US201261707838P 2012-09-28 2012-09-28

Publications (1)

Publication Number Publication Date
AR089939A1 true AR089939A1 (es) 2014-10-01

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ID=48946104

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130100396 AR089939A1 (es) 2012-02-09 2013-02-07 COMPUESTOS BICICLICOS COMO INHIBIDORES DE mPGES-1

Country Status (3)

Country Link
US (1) US9006257B2 (es)
AR (1) AR089939A1 (es)
WO (1) WO2013118071A1 (es)

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2900652C (en) 2013-02-15 2021-05-04 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
WO2014130612A1 (en) 2013-02-20 2014-08-28 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
US9688688B2 (en) 2013-02-20 2017-06-27 Kala Pharmaceuticals, Inc. Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof
MX355330B (es) 2013-11-01 2018-04-16 Kala Pharmaceuticals Inc Formas cristalinas de compuestos terapeuticos y sus usos.
US9890173B2 (en) 2013-11-01 2018-02-13 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
BR112016023679A2 (pt) * 2014-04-14 2017-08-15 Jiangsu Hengrui Medicine Co derivados de amida e sais farmaceuticamente aceitáveis dos mesmos, método de preparação dos mesmos e aplicação medicinal dos mesmos
US20200347038A1 (en) 2014-08-29 2020-11-05 Russell Dahl Quinolines that modulate serca and their use for treating disease
WO2016032569A1 (en) * 2014-08-29 2016-03-03 Celladon Corporation Quinolines and their use for treating endoplasmic reticulum stress-caused diseases
CN105237476A (zh) * 2015-10-31 2016-01-13 高大元 一种4-氯-8-氨基喹啉的合成方法
CN109688818A (zh) 2016-09-08 2019-04-26 卡拉制药公司 治疗化合物的晶型及其用途
EP3509422A4 (en) 2016-09-08 2020-05-20 Kala Pharmaceuticals, Inc. CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
EP3509423A4 (en) 2016-09-08 2020-05-13 Kala Pharmaceuticals, Inc. CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
BR112019009529A2 (pt) 2016-11-11 2019-07-30 Bayer Animal Health Gmbh novos derivados de quinolina
US11254661B2 (en) 2017-08-04 2022-02-22 Bayer Animal Health Gmbh Quinoline derivatives for treating infections with helminths
KR20200090818A (ko) 2017-11-22 2020-07-29 콘드리온 아이피 비.브이. Mpges-1 억제제로서의 신규 화합물
MX2020006185A (es) 2017-12-15 2020-09-03 Bayer Animal Health Gmbh Proceso para la preparacion de derivados de quinolina.
CN112074514B (zh) 2018-05-09 2024-10-29 礼蓝动物保健有限公司 新的喹啉衍生物
PT3814347T (pt) 2018-06-27 2023-07-18 Bristol Myers Squibb Co Compostos de naftiridinona úteis como ativadores de células t
HRP20231253T1 (hr) 2018-06-27 2024-02-02 Bristol-Myers Squibb Company Supstituirani spojevi naftiridina korisni kao aktivatori t stanica
JP2021529830A (ja) * 2018-07-02 2021-11-04 エコール・ポリテクニーク・フェデラル・ドゥ・ローザンヌ(ウペエフエル)Ecole Polytechnique Federale de Lausanne (EPFL) ラクテート増強化合物及びその使用
BR112021026376A2 (pt) 2019-06-25 2022-05-10 Gilead Sciences Inc Proteínas de fusão flt3l-fc e métodos de uso
AR119821A1 (es) 2019-08-28 2022-01-12 Bristol Myers Squibb Co Compuestos de piridopirimidinonilo sustituidos útiles como activadores de células t
PL4045083T3 (pl) 2019-10-18 2024-05-13 Forty Seven, Inc. Terapie skojarzone do leczenia zespołów mielodysplastycznych i ostrej białaczki szpikowej
MX2022005123A (es) 2019-10-31 2022-05-30 Forty Seven Inc Tratamiento basado en anti-cd47 y anti-cd20 para cancer hematologico.
TWI778443B (zh) 2019-11-12 2022-09-21 美商基利科學股份有限公司 Mcl1抑制劑
CN111018777B (zh) * 2019-11-25 2021-02-12 武汉智顿科技发展有限公司 一种地喹氯铵的制备方法
CN110963967B (zh) * 2019-11-25 2021-02-12 武汉智顿科技发展有限公司 一种2-甲基-4-氨基喹啉的制备方法
AR120823A1 (es) 2019-12-23 2022-03-23 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos útiles como activadores de células t
CR20220303A (es) 2019-12-24 2022-09-02 Gilead Sciences Inc Compuestos moduladores de la diacilglicerol quinasa
PE20231067A1 (es) 2020-02-14 2023-07-17 Jounce Therapeutics Inc Anticuerpos y proteinas de fusion que se unen a ccr8 y usos de estos
US12110294B2 (en) 2020-05-01 2024-10-08 Gilead Sciences, Inc. CD73 compounds
US11730729B2 (en) 2020-07-20 2023-08-22 Neurodon Corporation Quinolines that modulate SERCA and their use for treating disease
TW202302145A (zh) 2021-04-14 2023-01-16 美商基利科學股份有限公司 CD47/SIRPα結合及NEDD8活化酶E1調節次單元之共抑制以用於治療癌症
TW202313094A (zh) 2021-05-18 2023-04-01 美商基利科學股份有限公司 使用FLT3L—Fc融合蛋白之方法
AU2022295990A1 (en) 2021-06-18 2024-01-04 Aligos Therapeutics, Inc. Methods and compositions for targeting pd-l1
US11976072B2 (en) 2021-06-23 2024-05-07 Gilead Sciences, Inc. Diacylglycerol kinase modulating compounds
US11926628B2 (en) 2021-06-23 2024-03-12 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
US11999733B2 (en) 2021-06-23 2024-06-04 Gilead Sciences, Inc. Diacylglycerol kinase modulating compounds
AU2022297373A1 (en) 2021-06-23 2024-01-04 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
CN118139858A (zh) 2021-10-28 2024-06-04 吉利德科学公司 吡地嗪-3(2h)-酮衍生物
KR20240125012A (ko) 2021-12-22 2024-08-19 길리애드 사이언시즈, 인코포레이티드 이카로스 아연 핑거 패밀리 분해제 및 이의 용도
AU2022419982A1 (en) 2021-12-22 2024-06-06 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
JPWO2023127883A1 (es) 2021-12-28 2023-07-06
TW202340168A (zh) 2022-01-28 2023-10-16 美商基利科學股份有限公司 Parp7抑制劑
DK4245756T3 (da) 2022-03-17 2024-10-21 Gilead Sciences Inc Ikaros zinkfinger-familiens nedbrydere og anvendelse heraf
US20230355796A1 (en) 2022-03-24 2023-11-09 Gilead Sciences, Inc. Combination therapy for treating trop-2 expressing cancers
TW202345901A (zh) 2022-04-05 2023-12-01 美商基利科學股份有限公司 用於治療結腸直腸癌之組合療法
IL316058A (en) 2022-04-21 2024-11-01 Gilead Sciences Inc Compounds modulate KRAS G12D
WO2024006929A1 (en) 2022-07-01 2024-01-04 Gilead Sciences, Inc. Cd73 compounds
CN115124463B (zh) * 2022-07-01 2023-11-28 浙江工业大学 取代喹啉类化合物及其制备方法和应用
WO2024064668A1 (en) 2022-09-21 2024-03-28 Gilead Sciences, Inc. FOCAL IONIZING RADIATION AND CD47/SIRPα DISRUPTION ANTICANCER COMBINATION THERAPY
US20240254118A1 (en) 2022-12-22 2024-08-01 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
WO2024215754A1 (en) 2023-04-11 2024-10-17 Gilead Sciences, Inc. Kras modulating compounds
WO2024220917A1 (en) 2023-04-21 2024-10-24 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2410905T3 (es) 2004-12-17 2013-07-03 Merck Canada Inc. 2-(Fenil o heterociclo)-1H-fenantro[9,10-d]imidazoles como inhibidores de la MPGES-1
US7442716B2 (en) 2004-12-17 2008-10-28 Merck Frosst Canada Ltd. 2-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors
UY32138A (es) 2008-09-25 2010-04-30 Boehringer Ingelheim Int Amidas sustituidas del ácido 2-(2,6-dicloro-fenilamino)-6-fluoro-1-metil-1h-bencimidazol-5-carboxílico y sus sales farmacéuticamente aceptables
UY32470A (es) 2009-03-05 2010-10-29 Boehringer Ingelheim Int Derivados de 2-{2-cloro-5-[(sustituido) metil]fenilamino} -1-metil]fenilamino}-1-metilbencimidazol-5-carboxamidas-n-(sustituidas) y sus sales fisiológicamente aceptables, composiciones conteniéndolos y aplicaciones
WO2011023812A1 (en) * 2009-08-27 2011-03-03 Novasaid Ab Microsomal prostaglandin e synthase-1 (mpges1) inhibitors
TW201305178A (zh) 2010-10-29 2013-02-01 Glenmark Pharmaceuticals Sa 作為mPGES-1抑制物的三環化合物
WO2012110860A1 (en) 2011-02-17 2012-08-23 Glenmark Pharmaceuticals S.A. TRICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
EP2495244A1 (en) * 2011-03-02 2012-09-05 NovaSaid AB Piperidinyl benzoimidazole derivatives as mPGEs-1 inhibitors

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US20130210844A1 (en) 2013-08-15
US9006257B2 (en) 2015-04-14
WO2013118071A1 (en) 2013-08-15

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