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PE20080972A1 - RHO KINASE INHIBITORS - Google Patents

RHO KINASE INHIBITORS

Info

Publication number
PE20080972A1
PE20080972A1 PE2007001317A PE2007001317A PE20080972A1 PE 20080972 A1 PE20080972 A1 PE 20080972A1 PE 2007001317 A PE2007001317 A PE 2007001317A PE 2007001317 A PE2007001317 A PE 2007001317A PE 20080972 A1 PE20080972 A1 PE 20080972A1
Authority
PE
Peru
Prior art keywords
quinazolin
phenyl
alkyl
kinase inhibitors
rho kinase
Prior art date
Application number
PE2007001317A
Other languages
Spanish (es)
Inventor
Siya Ram
Paul Sweetnam
Martin Hauer-Jensen
Junru Wang
Alessandra Bartolozzi
Stewart Campbell
Bridget COLE
James Ellis
Hope Foudoulakis
Brian Kirk
Original Assignee
Surface Logix Inc
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
Application filed by Surface Logix Inc filed Critical Surface Logix Inc
Publication of PE20080972A1 publication Critical patent/PE20080972A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE A ES UN ANILLO AROMATICO DE 5-6 MIEMBROS QUE PUEDE ABARCAR 0-3 HETEROATOMOS SELECCIONADOS DE N, O Y S; R1 ES ARILO, NH-(ALQUILOC1-C6); -CONH2; ENTRE OTROS; R2 ES CN, HALO, HIDROXI; ENTRE OTROS; R3 ES CN, HIDROXI, AMINO, ENTRE TROS; R4 ES -O-CO2-(ALQUILO C1-C6), O-HETEROARIL, -O-CICLOALQUILO, ENTRE OTROS; R5 ES H, ALQUILO C1-C6, -COOH, O-ARILO, ENTRE OTROS; R6 ES H, ALQUILO C1-C6, CONH2, ENTRE OTROS; n ES 0-4; m ES 0-3; p ES 0-1. SON COMPUESTOS PREFERIDOS: 2-(3-(4-(1H-INDAZOL-5-ILAMINO)QUINAZOLIN-2IL)FENOXI)-N-ISOPROPILACETAMIDA; N-((3-(4-(1H-IDAZOL-5-ILAMINO)QUINAZOLIN-2-IL)FENIL)-2-MORFOLINOACETAMIDA; 6-(2-(DIMETILAMINO)ETOXI)-N-(1H-INDAZOL-5-IL)-7-METOXI-2-(3-(FENIL)FENIL)QUINAZOLIN-4-AMINA; ENTRE OTROS. DICHOS COMPUESTOS SON UTILES EN EL TRATAMIENTO DE FIBROSIS O ENFERMEDADES CARDIOVASCULARESIT REFERS TO A COMPOUND OF FORMULA I, WHERE A IS AN AROMATIC RING OF 5-6 MEMBERS THAT CAN COVER 0-3 HETEROATOMS SELECTED FROM N, O AND S; R1 IS ARYL, NH- (C6-ALKYLOC); -CONH2; AMONG OTHERS; R2 IS CN, HALO, HYDROXY; AMONG OTHERS; R3 IS CN, HYDROXY, AMINO, BETWEEN THREE; R4 IS -O-CO2- (C1-C6 ALKYL), O-HETEROARYL, -O-CYCLOALKYL, AMONG OTHERS; R5 IS H, C1-C6 ALKYL, -COOH, O-ARYL, AMONG OTHERS; R6 IS H, C1-C6 ALKYL, CONH2, AMONG OTHERS; n IS 0-4; m IS 0-3; p IS 0-1. THE PREFERRED COMPOUNDS ARE: 2- (3- (4- (1H-INDAZOL-5-ILAMINE) QUINAZOLIN-2YL) PHENOXY) -N-ISOPROPYLACETAMIDE; N - ((3- (4- (1H-IDAZOL-5-ILAMINO) QUINAZOLIN-2-IL) PHENYL) -2-MORPHOLINOACETAMIDE; 6- (2- (DIMETHYLAMINO) ETHOXY) -N- (1H-INDAZOL-5 -IL) -7-METOXY-2- (3- (PHENYL) PHENYL) QUINAZOLIN-4-AMINE; AMONG OTHERS, SAID COMPOUNDS ARE USEFUL IN THE TREATMENT OF FIBROSIS OR CARDIOVASCULAR DISEASES

PE2007001317A 2006-09-27 2007-10-16 RHO KINASE INHIBITORS PE20080972A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US84769406P 2006-09-27 2006-09-27
US85012506P 2006-10-05 2006-10-05
US85012706P 2006-10-05 2006-10-05

Publications (1)

Publication Number Publication Date
PE20080972A1 true PE20080972A1 (en) 2008-10-04

Family

ID=39344830

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2007001317A PE20080972A1 (en) 2006-09-27 2007-10-16 RHO KINASE INHIBITORS

Country Status (3)

Country Link
CA (1) CA2700988A1 (en)
PE (1) PE20080972A1 (en)
WO (1) WO2008054599A2 (en)

Families Citing this family (43)

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EP1910297B1 (en) 2005-07-11 2016-05-25 Aerie Pharmaceuticals, Inc. Isoquinoline compounds
JP5235887B2 (en) 2006-09-20 2013-07-10 アエリー ファーマシューティカルズ インコーポレイテッド Rho kinase inhibitor
US8455513B2 (en) 2007-01-10 2013-06-04 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US8455514B2 (en) 2008-01-17 2013-06-04 Aerie Pharmaceuticals, Inc. 6-and 7-amino isoquinoline compounds and methods for making and using the same
US8450344B2 (en) 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
US20120202793A1 (en) * 2009-03-09 2012-08-09 Paul Sweetnam Rho kinase inhibitors
ES2553827T3 (en) 2009-05-01 2015-12-14 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
WO2011092695A1 (en) * 2010-01-28 2011-08-04 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd Quinazoline-based t cell proliferation inhibitors
LT2903618T (en) 2012-10-05 2022-08-25 Kadmon Corporation, Llc Rho kinase inhibitors
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
CN105073744B (en) 2012-12-21 2019-11-08 齐尼思表观遗传学有限公司 Novel heterocyclic compounds as bromodomain inhibitors
HK1222793A1 (en) 2013-03-14 2017-07-14 康威基内有限公司 Methods and compositions for inhibition of bromodomain-containing proteins
FI3811943T3 (en) 2013-03-15 2023-04-14 Aerie Pharmaceuticals Inc A compound for use in the treatment of eye diseases
US9636328B2 (en) 2013-06-21 2017-05-02 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
CA2915838C (en) 2013-06-21 2023-04-18 Zenith Epigenetics Corp. Bicyclic bromodomain inhibitors
CN105593224B (en) 2013-07-31 2021-05-25 恒元生物医药科技(苏州)有限公司 Novel quinazolinones as bromodomain inhibitors
ES2779152T3 (en) * 2013-10-07 2020-08-13 Kadmon Corporation Llc Derivatives of (2- (5-isoindolin-2-yl) pyrimidin-4-yl) -amine as Rho-kinase inhibitors to treat autoimmune diseases
EP3227281A4 (en) 2014-12-01 2018-05-30 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
EP3227280B1 (en) 2014-12-01 2019-04-24 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
US10292968B2 (en) 2014-12-11 2019-05-21 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
HK1245247A1 (en) 2014-12-17 2018-08-24 恒翼生物医药科技(上海)有限公司 Inhibitors of bromodomains
WO2016160833A1 (en) * 2015-04-01 2016-10-06 Rigel Pharmaceuticals, Inc. TGF-β INHIBITORS
CN108601355B (en) 2015-11-17 2021-03-30 爱瑞制药公司 Process for preparing kinase inhibitors and intermediates thereof
US9643927B1 (en) 2015-11-17 2017-05-09 Aerie Pharmaceuticals, Inc. Process for the preparation of kinase inhibitors and intermediates thereof
ES2918589T3 (en) * 2015-11-25 2022-07-19 Convergene Llc Bicyclic BET bromodome inhibitors and uses thereof
US11390609B2 (en) 2017-06-30 2022-07-19 Beijing Tide Pharmaceutical Co., Ltd. Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof
EP3421465B1 (en) 2017-06-30 2022-10-26 Beijing Tide Pharmaceutical Co., Ltd. Rho-associated protein kinase inhibitor, pharmaceutical composition comprising the same, as well as preparation method and use thereof
WO2019000683A1 (en) 2017-06-30 2019-01-03 北京泰德制药股份有限公司 Rho-associated protein kinase inhibitor, pharmaceutical composition containing rho-associated protein kinase inhibitor, preparation method and use of the pharmaceutical composition
WO2019018562A1 (en) 2017-07-19 2019-01-24 Ideaya Biosciences, Inc. AMIDO COMPOUNDS AS AhR MODULATORS
JP2020532551A (en) 2017-09-03 2020-11-12 アンジオン バイオメディカ コーポレーション Vinyl heterocycle as a Rho-related coiled coil kinase (ROCK) inhibitor
JP7382348B2 (en) 2018-02-06 2023-11-16 アイディアヤ バイオサイエンシーズ，インコーポレイティド AhR modulator
WO2019201297A1 (en) 2018-04-18 2019-10-24 南京明德新药研发有限公司 Benzopyrazole compound used as rho kinase inhibitor
CN114786675A (en) 2019-04-24 2022-07-22 康威基内有限公司 Small molecule bromodomain inhibitors and uses thereof
JP7252417B2 (en) 2019-10-18 2023-04-04 メッドシャイン ディスカバリー インコーポレイテッド Benzopyrazole Compounds as RHO Kinase Inhibitors, Salt Forms, Crystal Forms and Methods of Making Same
CN114746412A (en) * 2019-12-27 2022-07-12 广东东阳光药业有限公司 Novel crystal form of KD-025 and preparation method thereof
US12014835B2 (en) 2020-02-19 2024-06-18 Vanderbilt University Methods for evaluating therapeutic benefit of combination therapies
JP2023535447A (en) 2020-07-22 2023-08-17 テバ・ファーマシューティカルズ・インターナショナル・ゲーエムベーハー Solid Forms of Vermosdil and Vermosdil Salts
CN115124514A (en) * 2021-03-26 2022-09-30 广东东阳光药业有限公司 Eutectic crystal of KD-025 and preparation method thereof
WO2022229351A1 (en) * 2021-04-28 2022-11-03 Graviton Bioscience Bv Selective inhibitors of rock2 for the treatment of muscular dystrophy
EP4370205A1 (en) 2021-07-16 2024-05-22 Sandoz Ag Solid-state forms of 2-(3-(4-(1h-indazol-5-ylamino)quinazolin-2-yl )phenoxy)-n- isopropylacetamide methane sulfonic acid salt
CN120035442A (en) * 2022-10-13 2025-05-23 北京泰德制药股份有限公司 Treatment for pneumoconiosis
WO2025257846A1 (en) * 2024-06-14 2025-12-18 Natco Pharma Limited An improved process for the preparation of belumosudil mesylate and its intermediates thereof

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Publication number Priority date Publication date Assignee Title
CA2441501C (en) * 2001-03-23 2010-09-14 Bayer Corporation Rho-kinase inhibitors
US7645878B2 (en) * 2002-03-22 2010-01-12 Bayer Healthcare Llc Process for preparing quinazoline Rho-kinase inhibitors and intermediates thereof

Also Published As

Publication number Publication date
WO2008054599A3 (en) 2008-11-20
CA2700988A1 (en) 2008-05-08
WO2008054599A2 (en) 2008-05-08

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