ES2895626T3 - Derivados de imidazol condensados como inhibidores de TGF-beta - Google Patents

Derivados de imidazol condensados como inhibidores de TGF-beta Download PDF

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Publication number
ES2895626T3
ES2895626T3 ES15801080T ES15801080T ES2895626T3 ES 2895626 T3 ES2895626 T3 ES 2895626T3 ES 15801080 T ES15801080 T ES 15801080T ES 15801080 T ES15801080 T ES 15801080T ES 2895626 T3 ES2895626 T3 ES 2895626T3
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Spain
Prior art keywords
imidazol
pyrrolo
dihydro
alkyl
methylphenyl
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ES15801080T
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English (en)
Spanish (es)
Inventor
Rajinder Singh
Todd Kinsella
Jiaxin Yu
Marina Gelman
Ihab Darwish
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Rigel Pharmaceuticals Inc
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Rigel Pharmaceuticals Inc
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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ES15801080T 2014-11-21 2015-11-16 Derivados de imidazol condensados como inhibidores de TGF-beta Active ES2895626T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462082959P 2014-11-21 2014-11-21
US201562141509P 2015-04-01 2015-04-01
PCT/US2015/060872 WO2016081364A1 (en) 2014-11-21 2015-11-16 Fused imidazole derivatives as tgf-beta inhibitors

Publications (1)

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ES2895626T3 true ES2895626T3 (es) 2022-02-22

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ES15801080T Active ES2895626T3 (es) 2014-11-21 2015-11-16 Derivados de imidazol condensados como inhibidores de TGF-beta

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US (1) US10696693B2 (enExample)
EP (1) EP3221318B1 (enExample)
JP (1) JP6789941B2 (enExample)
CN (1) CN107207531B (enExample)
ES (1) ES2895626T3 (enExample)
WO (1) WO2016081364A1 (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11040027B2 (en) 2017-01-17 2021-06-22 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
ES3053505T3 (en) 2017-03-23 2026-01-22 Clavius Pharmaceuticals Llc Tri-substituted imidazoles for the inhibition of tgf beta and methods of treatment
WO2020041562A1 (en) 2018-08-22 2020-02-27 Clavius Pharmaceuticals, Llc Substituted imidazoles for the inhibition of tgf-beta and methods of treatment
CA3117710A1 (en) 2018-12-11 2020-06-18 Theravance Biopharma R&D Ip, Llc Alk5 inhibitors
KR20220104208A (ko) 2019-11-22 2022-07-26 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 Alk5 억제제로서 치환된 1,5-나프티리딘 또는 퀴놀린
WO2021110142A1 (en) * 2019-12-04 2021-06-10 Henan Normal University Substituted imidazolecarboxamide as bruton's tyrosine kinase inhibitors
WO2021138391A1 (en) 2019-12-30 2021-07-08 Tyra Biosciences, Inc. Indazole compounds
US20250270215A1 (en) 2022-04-27 2025-08-28 Chiesi Farmaceutici S.P.A. Imidazole derivatives as alk5 inhibitors
MA71237A (fr) 2022-06-22 2025-04-30 Chiesi Farmaceutici S.P.A. Dérivés de 5-(4-fluorophényl)-2,3-dihydro-1h-imidazo[1,2-a]imidazole utilisés en tant qu'inhibiteurs d'alk pour traiter la fibrose
KR20250051687A (ko) * 2022-08-08 2025-04-17 메디노 파마슈티컬 테크놀로지 (주하이) 컴퍼니 리미티드 TGF-β 억제제 화합물 및 그 사용
PL248267B1 (pl) * 2023-04-13 2025-11-17 Univ Medyczny W Lublinie 1-arylo-6-hydroksyimino-5(1H)okso-2,3-dihydroimidazo[1,2-a] imidazole oraz sposób ich wytwarzania oraz ich zastosowanie

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003517580A (ja) 1999-01-21 2003-05-27 メタモーフイクス・インコーポレーテツド 増殖分化因子インヒビター及びそれらの用途
US6610697B1 (en) * 1999-11-10 2003-08-26 Ortho-Mcneil Pharmaceutical, Inc. Substituted 2-aryl-3-(heteroaryl)-imidazo[1,2-a]pyrimidines, and related pharmaceutical compositions and methods
US7320789B2 (en) 2001-09-26 2008-01-22 Wyeth Antibody inhibitors of GDF-8 and uses thereof
AU2003256297A1 (en) * 2002-08-09 2004-02-25 Eli Lilly And Company Benzimidazoles and benzothiazoles as inhibitors of map kinase
US7405299B2 (en) * 2002-11-27 2008-07-29 Eli Lilly And Company Compounds as pharmaceutical agents
PA8595001A1 (es) * 2003-03-04 2004-09-28 Pfizer Prod Inc Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf)
EP1973914A2 (en) * 2005-12-22 2008-10-01 Biogen Idec MA Inc. Transforming growth factor modulators
CN101553224A (zh) * 2006-10-06 2009-10-07 艾博特公司 新型咪唑并噻唑和咪唑并唑
WO2009005675A1 (en) * 2007-06-28 2009-01-08 Abbott Laboratories Novel triazolopyridazines
RU2612958C2 (ru) * 2011-07-13 2017-03-14 Ск Кемикалз Ко., Лтд. 2-пиридилзамещенные имидазолы в качестве ингибиторов alk5 и/или alk4
JP6267231B2 (ja) * 2012-12-21 2018-01-24 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company カゼインキナーゼ1δ/ε阻害剤としての新規な置換イミダゾール
AU2014363032A1 (en) 2013-12-11 2016-06-09 Pfizer Limited Method for producing retinal pigment epithelial cells

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US20180346487A1 (en) 2018-12-06
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