AU2012300833B2 - Novel soft ROCK inhibitors - Google Patents

Novel soft ROCK inhibitors Download PDF

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Publication number
AU2012300833B2
AU2012300833B2 AU2012300833A AU2012300833A AU2012300833B2 AU 2012300833 B2 AU2012300833 B2 AU 2012300833B2 AU 2012300833 A AU2012300833 A AU 2012300833A AU 2012300833 A AU2012300833 A AU 2012300833A AU 2012300833 B2 AU2012300833 B2 AU 2012300833B2
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group
20alkyl
halo
aryl
diseases
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AU2012300833A1 (en
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Jo ALEN
Sandro Boland
Arnaud Pierre Jean BOURIN
Olivier Defert
Dirk Leysen
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Amakem NV
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Amakem NV
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/72—Nitrogen atoms
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
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    • C07D401/12—Heterocyclic 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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  • Reproductive Health (AREA)
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  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
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  • Psychiatry (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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AU2012300833A 2011-08-31 2012-08-31 Novel soft ROCK inhibitors Expired - Fee Related AU2012300833B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11179491.3 2011-08-31
EP11179491 2011-08-31
PCT/EP2012/067017 WO2013030366A1 (en) 2011-08-31 2012-08-31 Novel soft rock inhibitors

Publications (2)

Publication Number Publication Date
AU2012300833A1 AU2012300833A1 (en) 2014-04-17
AU2012300833B2 true AU2012300833B2 (en) 2016-06-30

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Application Number Title Priority Date Filing Date
AU2012300833A Expired - Fee Related AU2012300833B2 (en) 2011-08-31 2012-08-31 Novel soft ROCK inhibitors
AU2012300832A Abandoned AU2012300832A1 (en) 2011-08-31 2012-08-31 Novel ROCK kinase inhibitors
AU2012300834A Abandoned AU2012300834A1 (en) 2011-08-31 2012-08-31 Biphenylcarboxamides as ROCK kinase inhibitors

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Application Number Title Priority Date Filing Date
AU2012300832A Abandoned AU2012300832A1 (en) 2011-08-31 2012-08-31 Novel ROCK kinase inhibitors
AU2012300834A Abandoned AU2012300834A1 (en) 2011-08-31 2012-08-31 Biphenylcarboxamides as ROCK kinase inhibitors

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Country Link
US (3) US9067889B2 (enExample)
EP (3) EP2751080B1 (enExample)
JP (3) JP2014525427A (enExample)
KR (2) KR20140072879A (enExample)
CN (3) CN103874684A (enExample)
AU (3) AU2012300833B2 (enExample)
BR (3) BR112014004435A2 (enExample)
CA (3) CA2846695A1 (enExample)
EA (3) EA201490516A1 (enExample)
ES (1) ES2560830T3 (enExample)
IL (2) IL231122A0 (enExample)
MX (3) MX2014002393A (enExample)
PT (1) PT2751080E (enExample)
SG (2) SG11201400117QA (enExample)
WO (3) WO2013030365A1 (enExample)
ZA (3) ZA201401418B (enExample)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10842669B2 (en) * 2008-11-13 2020-11-24 Gholam A. Peyman Ophthalmic drug delivery method
WO2013030365A1 (en) * 2011-08-31 2013-03-07 Amakem Nv Novel rock kinase inhibitors
LT2903618T (lt) 2012-10-05 2022-08-25 Kadmon Corporation, Llc Rho kinazės inhibitoriai
DK2951172T3 (en) 2013-01-29 2017-07-17 Redx Pharma Plc PYRIDINE DERIVATIVES LIKE SOFT ROCK INHIBITORS
JP5840324B2 (ja) 2013-04-15 2016-01-06 株式会社レナサイエンス Ｐａｉ−１阻害剤の新規用途
CN105793236B (zh) * 2013-12-17 2017-10-10 伊莱利利公司 二甲基苯甲酸化合物
WO2015196072A2 (en) 2014-06-19 2015-12-23 Whitehead Institute For Biomedical Research Uses of kinase inhibitors for inducing and maintaining pluripotency
US12281308B2 (en) 2018-08-29 2025-04-22 University Of Massachusetts Inhibition of protein kinases to treat Friedreich ataxia
CN113801111B (zh) * 2020-06-12 2025-10-17 上海翰森生物医药科技有限公司 联苯类衍生物抑制剂及其制备方法和应用
US12371667B2 (en) 2021-05-13 2025-07-29 Washington University Enhanced methods for inducing and maintaining naive human pluripotent stem cells
EP4431596A1 (en) 2021-11-11 2024-09-18 The Doshisha Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation
EP4387730B1 (en) * 2022-09-08 2025-05-28 Redx Pharma Limited Solid forms of a rock inhibitor
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ｒａｓ相關疾病或病症之組合療法
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007006547A1 (en) * 2005-07-11 2007-01-18 Devgen N.V. Amide derivatives as kinase inhibitors
WO2007042321A2 (en) * 2005-10-13 2007-04-19 Devgen N.V. Kinase inhibitors

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990005723A1 (fr) 1988-11-24 1990-05-31 Yoshitomi Pharmaceutical Industries, Ltd. Composes de trans-4-amino(alkyl)-1-pyridylcarbamoylcyclohexane et leur utilisation en medecine
IS2334B (is) 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
CN1110300C (zh) 1993-10-01 2003-06-04 阿斯特拉公司 工艺技术ⅰ
US6043358A (en) 1995-11-01 2000-03-28 Merck & Co., Inc. Hexahydro-5-imino-1,4-heteroazepine derivatives as inhibitors of nitric oxide synthases
GB9718913D0 (en) 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
US6369087B1 (en) 1999-08-26 2002-04-09 Robert R. Whittle Alkoxy substituted benzimidazole compounds, pharmaceutical preparations containing the same, and methods of using the same
GB0124928D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
WO2005014599A1 (en) * 2003-06-04 2005-02-17 Cellular Genomics, Inc. Imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton’s tyrosine kinase by such compounds
US7683097B2 (en) * 2004-05-27 2010-03-23 Propharmacon Inc. Topoisomerase inhibitors
CN101248046A (zh) * 2005-07-11 2008-08-20 德福根有限公司 作为激酶抑制剂的酰胺衍生物
BRPI0615524A2 (pt) 2005-07-11 2010-04-06 Devgen Nv derivados da amida como inibidores da quinase
US20070042321A1 (en) * 2005-08-22 2007-02-22 Florman Michael J Grinder guard
KR20080050490A (ko) * 2005-09-16 2008-06-05 애로우 쎄라퓨틱스 리미티드 바이페닐 유도체, 및 ｃ형 간염 치료에 있어서의 그의 용도
WO2009025239A1 (ja) * 2007-08-17 2009-02-26 Eisai R & D Management Co., Ltd. 新規外用剤
GB201018996D0 (en) * 2010-11-10 2010-12-22 Amakem Nv Novel ROCK inhibitors
DK2542528T3 (da) 2010-03-02 2013-09-23 Amakem Nv Heterocykliske amider som rock-inhibitorer
KR20140020972A (ko) * 2011-03-28 2014-02-19 에프. 호프만-라 로슈 아게 티아졸로피리미딘 화합물
GB201114854D0 (en) * 2011-08-29 2011-10-12 Amakem Nv Novel rock inhibitors
WO2013030365A1 (en) * 2011-08-31 2013-03-07 Amakem Nv Novel rock kinase inhibitors
JP2014526484A (ja) * 2011-09-13 2014-10-06 ノバルティス アーゲー Ｓ１ｐ受容体修飾物質を含む組み合わせ

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007006547A1 (en) * 2005-07-11 2007-01-18 Devgen N.V. Amide derivatives as kinase inhibitors
WO2007042321A2 (en) * 2005-10-13 2007-04-19 Devgen N.V. Kinase inhibitors

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