JP2009521494A5 - - Google Patents
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- Publication number
- JP2009521494A5 JP2009521494A5 JP2008547727A JP2008547727A JP2009521494A5 JP 2009521494 A5 JP2009521494 A5 JP 2009521494A5 JP 2008547727 A JP2008547727 A JP 2008547727A JP 2008547727 A JP2008547727 A JP 2008547727A JP 2009521494 A5 JP2009521494 A5 JP 2009521494A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- alkyl
- independently
- membered ring
- compound
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
- 239000000203 mixture Substances 0.000 claims 21
- 125000000217 alkyl group Chemical group 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 10
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 8
- 208000010412 Glaucoma Diseases 0.000 claims 7
- 239000003814 drug Substances 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 229940124597 therapeutic agent Drugs 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000003277 amino group Chemical group 0.000 claims 4
- -1 amino, hydroxyl Chemical group 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 239000000556 agonist Substances 0.000 claims 3
- 229940006133 antiglaucoma drug and miotics carbonic anhydrase inhibitors Drugs 0.000 claims 3
- 239000002876 beta blocker Substances 0.000 claims 3
- 229940097320 beta blocking agent Drugs 0.000 claims 3
- 239000003489 carbonate dehydratase inhibitor Substances 0.000 claims 3
- 230000003547 miosis Effects 0.000 claims 3
- 239000003604 miotic agent Substances 0.000 claims 3
- 239000004090 neuroprotective agent Substances 0.000 claims 3
- 150000003180 prostaglandins Chemical class 0.000 claims 3
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 2
- 230000004410 intraocular pressure Effects 0.000 claims 2
- 239000002585 base Substances 0.000 claims 1
- 239000000872 buffer Substances 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003623 enhancer Substances 0.000 claims 1
- 239000003349 gelling agent Substances 0.000 claims 1
- 230000002209 hydrophobic effect Effects 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 230000035515 penetration Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000003755 preservative agent Substances 0.000 claims 1
- 102000000568 rho-Associated Kinases Human genes 0.000 claims 1
- 108010041788 rho-Associated Kinases Proteins 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 239000004094 surface-active agent Substances 0.000 claims 1
- 239000002562 thickening agent Substances 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US75313605P | 2005-12-22 | 2005-12-22 | |
| PCT/US2006/062307 WO2007076360A1 (en) | 2005-12-22 | 2006-12-19 | (indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)- pyrazines for treating rho kinase-mediated diseases and conditions |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009521494A JP2009521494A (ja) | 2009-06-04 |
| JP2009521494A5 true JP2009521494A5 (https=) | 2011-02-03 |
Family
ID=37963712
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008547727A Pending JP2009521494A (ja) | 2005-12-22 | 2006-12-19 | ｒｈｏキナーゼ媒介性疾患および状態を治療するための（インダゾール−５−イル）−ピラジンおよび（１，３−ジヒドロインドール−２−オン）−ピラジン |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US7655662B2 (https=) |
| EP (1) | EP1962853A1 (https=) |
| JP (1) | JP2009521494A (https=) |
| KR (1) | KR20080077652A (https=) |
| CN (1) | CN101340912A (https=) |
| AR (1) | AR058618A1 (https=) |
| BR (1) | BRPI0620463A2 (https=) |
| CA (1) | CA2629342A1 (https=) |
| MX (1) | MX2008008328A (https=) |
| RU (1) | RU2008130111A (https=) |
| TW (1) | TW200733964A (https=) |
| UY (1) | UY30058A1 (https=) |
| WO (1) | WO2007076360A1 (https=) |
| ZA (1) | ZA200804497B (https=) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7470787B2 (en) * | 2005-07-11 | 2008-12-30 | Aerie Pharmaceuticals, Inc. | Isoquinoline compounds |
| WO2007008942A2 (en) * | 2005-07-11 | 2007-01-18 | Aerie Pharmaceuticals, Inc. | Phenylamino-acetic acid [1-(pyridin-4-yl)-methylidene]-hydrazide derivatives and related compounds as modulators of g protein-coupled receptor kinases for the treatment of eye diseases |
| ES2729424T3 (es) | 2006-09-20 | 2019-11-04 | Aerie Pharmaceuticals Inc | Inhibidores de Rho cinasa |
| EP2079739A2 (en) * | 2006-10-04 | 2009-07-22 | Pfizer Products Inc. | Pyrido[4,3-d]pyrimidin-4(3h)-one derivatives as calcium receptor antagonists |
| US20100022517A1 (en) * | 2006-12-18 | 2010-01-28 | Richards Lori A | Ophthalmic formulation of rho kinase inhibitor compound |
| 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 |
| JP2011524912A (ja) * | 2008-06-18 | 2011-09-08 | インスパイアー ファーマシューティカルズ，インコーポレイティド | Ｒｈｏキナーゼ阻害化合物の眼科用製剤 |
| US8450344B2 (en) | 2008-07-25 | 2013-05-28 | Aerie Pharmaceuticals, Inc. | Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds |
| CA2743134A1 (en) | 2008-11-10 | 2010-05-14 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| ES2921576T3 (es) | 2008-12-19 | 2022-08-29 | Vertex Pharma | Compuestos útiles como inhibidores de la quinasa ATR |
| EP3828172A1 (en) | 2009-05-01 | 2021-06-02 | Aerie Pharmaceuticals, Inc. | Dual mechanism inhibitors for the treatment of disease |
| PL2516433T3 (pl) | 2009-12-21 | 2014-10-31 | Array Biopharma Inc | Podstawione związki N-(1H-indazol-4-ilo)imidazo[1,2-a]pirydyno-3-karboksyamidowe jako inhibitory cFMS |
| CA2798760A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | 2-aminopyridine derivatives useful as inhibitors of atr kinase |
| US8962631B2 (en) | 2010-05-12 | 2015-02-24 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| EP2568984A1 (en) | 2010-05-12 | 2013-03-20 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| NZ603477A (en) | 2010-05-12 | 2014-09-26 | Vertex Pharma | Compounds useful as inhibitors of atr kinase |
| US9062008B2 (en) | 2010-05-12 | 2015-06-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| US9334244B2 (en) | 2010-05-12 | 2016-05-10 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| MX2013000103A (es) | 2010-06-23 | 2013-06-13 | Vertex Pharma | Derivados de pirrolo-pirazina utiles como inhibidores de cinasa art. |
| MX2013011450A (es) | 2011-04-05 | 2014-02-03 | Vertex Pharma | Compuestos de aminopirazina utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr). |
| US8822469B2 (en) | 2011-06-22 | 2014-09-02 | Vertex Pharmaceuticals Incorporated | Pyrrolo[2,3-B]pyrazines useful as inhibitors of ATR kinase |
| EP2723747A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| US9309250B2 (en) | 2011-06-22 | 2016-04-12 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors |
| WO2013049720A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| CN106496173A (zh) | 2011-09-30 | 2017-03-15 | 沃泰克斯药物股份有限公司 | 用于制备可用作atr激酶抑制剂的化合物的方法 |
| WO2013049722A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| CN108685922A (zh) | 2011-09-30 | 2018-10-23 | 沃泰克斯药物股份有限公司 | 用atr抑制剂治疗胰腺癌和非小细胞肺癌 |
| US8765751B2 (en) | 2011-09-30 | 2014-07-01 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| US8841450B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| JP2015502925A (ja) | 2011-11-09 | 2015-01-29 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | Ａｔｒキナーゼの阻害剤として有用なピラジン化合物 |
| US8841337B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| US8846917B2 (en) | 2011-11-09 | 2014-09-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| US8846918B2 (en) | 2011-11-09 | 2014-09-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| CN108478577A (zh) | 2012-04-05 | 2018-09-04 | 沃泰克斯药物股份有限公司 | 可用作atr激酶抑制剂的化合物及其组合疗法 |
| DK2904406T3 (en) | 2012-10-04 | 2018-06-18 | Vertex Pharma | METHOD OF DETERMINING THE ATR INHIBITION, INCREASED DNA DAMAGE |
| EP2909202A1 (en) | 2012-10-16 | 2015-08-26 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| SI2941432T1 (en) | 2012-12-07 | 2018-07-31 | Vertex Pharmaceuticals Incorporated | 2-AMINO-6-FLUORO-N- (5-FLUORO-4- (4- (4- (OXETHAN-3-YL) PIPERAZIN-1-CARBONYL) PIPERIDIN-1-YLIPRIDIN-3-YL) 1,5 ALFA) PYRIMIDINE-3-CARBOXAMIDE AS ATR KINAZE INHIBITOR |
| WO2014143240A1 (en) | 2013-03-15 | 2014-09-18 | Vertex Pharmaceuticals Incorporated | Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase |
| ES2852377T3 (es) | 2013-03-15 | 2021-09-13 | Aerie Pharmaceuticals Inc | Sales dimesilato de 4-(3-amino-1-(isoquinolin-6-ilamino)-1-oxopropan-2-il)bencilo, sus combinaciones con prostaglandinas y el uso de las mismas en el tratamiento de trastornos oculares |
| US9328200B2 (en) * | 2013-07-17 | 2016-05-03 | Ultrasci Discovery Llp | Branched polymeric quaternary ammonium compounds and their uses |
| PT3077397T (pt) | 2013-12-06 | 2020-01-22 | Vertex Pharma | Composto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-carboxamida útil como inibidor da atr quinase, a sua preparação, diferentes formas sólidas e derivados radiomarcados do mesmo |
| MX373102B (es) | 2014-06-05 | 2020-04-17 | Vertex Pharma | Derivados radiomarcados de un compuesto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida útil como inhibidor de ataxia telangiectasia mutada y rad3 relacionado (atr) cinasa, preparación de tal compuesto y diferentes formas sólidas del mismo. |
| SG11201610500WA (en) | 2014-06-17 | 2017-01-27 | Vertex Pharma | Method for treating cancer using a combination of chk1 and atr inhibitors |
| AU2016331955B2 (en) | 2015-09-30 | 2022-07-21 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors |
| US9643927B1 (en) | 2015-11-17 | 2017-05-09 | Aerie Pharmaceuticals, Inc. | Process for the preparation of kinase inhibitors and intermediates thereof |
| KR102579582B1 (ko) | 2015-11-17 | 2023-09-15 | 에어리 파마슈티컬즈, 인코포레이티드 | 키나아제 억제제 및 이의 중간체의 제조 방법 |
| KR102568079B1 (ko) | 2016-08-31 | 2023-08-17 | 에어리 파마슈티컬즈, 인코포레이티드 | 안과용 조성물 |
| AU2018243687C1 (en) | 2017-03-31 | 2020-12-24 | Alcon Inc. | Aryl cyclopropyl-amino-isoquinolinyl amide compounds |
| WO2020010197A1 (en) | 2018-07-05 | 2020-01-09 | Incyte Corporation | Fused pyrazine derivatives as a2a / a2b inhibitors |
| CA3112391A1 (en) | 2018-09-14 | 2020-03-19 | Aerie Pharmaceuticals, Inc. | Aryl cyclopropyl-amino-isoquinolinyl amide compounds |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
| AU2021285850A1 (en) * | 2020-06-03 | 2023-02-09 | Glaukos Corporation | Rho kinase inhibitor releasing implants and related methods of use |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0492903A1 (en) * | 1990-12-21 | 1992-07-01 | MERCK SHARP & DOHME LTD. | Substituted pyrazines, pyrimidines and pyridazines for use in the treatment of glaucoma |
| ATE289815T1 (de) | 1995-12-21 | 2005-03-15 | Alcon Lab Inc | Verwendung von substituierten isochinolinsulfonyl-verbindungen zur herstellung eines medikaments für die behandlung von glaukom und okularer ischämie |
| US6586425B2 (en) | 1996-02-21 | 2003-07-01 | Wisconsin Alumni Research Foundation | Cytoskeletal active agents for glaucoma therapy |
| US5798380A (en) | 1996-02-21 | 1998-08-25 | Wisconsin Alumni Research Foundation | Cytoskeletal active agents for glaucoma therapy |
| BR9711154A (pt) | 1996-08-12 | 1999-08-17 | Yoshitomi Pharmaceutical | Agente farmac-utico contendo inibidor cinase rho |
| CA2214841A1 (en) | 1997-10-31 | 1999-04-30 | Lisa Mckerracher | Rho antagonists and their use to block inhibition of neurite outgrowth |
| CA2307285C (en) | 1998-08-17 | 2009-03-31 | Senju Pharmaceutical Co., Ltd. | Agent for prophylaxis and treatment of glaucoma |
| EP1177796B1 (en) | 1999-04-27 | 2011-04-27 | Mitsubishi Tanabe Pharma Corporation | Medicament for prevention or therapeutic treatment of liver disease |
| JP3430254B2 (ja) | 2000-03-13 | 2003-07-28 | 独立行政法人産業技術総合研究所 | β−ジケトナートを有する金属錯体及びその製法、光電変換素子並びに、光化学電池 |
| WO2001068607A1 (en) | 2000-03-16 | 2001-09-20 | Mitsubishi Pharma Corporation | Amide compounds and use thereof |
| AU2001236006A1 (en) | 2000-03-31 | 2001-10-15 | Mitsubishi Pharma Corporation | Preventives/remedies for kidney diseases |
| WO2002100833A1 (en) | 2001-06-12 | 2002-12-19 | Sumitomo Pharmaceuticals Company, Limited | Rho KINASE INHIBITORS |
| US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
| JP4505228B2 (ja) | 2002-01-10 | 2010-07-21 | バイエル・シェーリング・ファルマ・アクチェンゲゼルシャフト | Ｒｈｏ−キナーゼ阻害剤 |
| MXPA04007196A (es) | 2002-01-23 | 2005-06-08 | Bayer Pharmaceuticals Corp | Inhibidores de rho-quinasa. |
| GB0206860D0 (en) * | 2002-03-22 | 2002-05-01 | Glaxo Group Ltd | Compounds |
| AU2003249369A1 (en) | 2002-06-21 | 2004-01-06 | Cellular Genomics, Inc. | Certain amino-substituted monocycles as kinase modulators |
| EP1541559A4 (en) | 2002-07-22 | 2007-08-22 | Asahi Kasei Pharma Corp | 5-SUBSTITUTED ISOQUINOLINE DERIVATIVE |
| AU2003264427A1 (en) | 2002-09-12 | 2004-04-30 | Kirin Beer Kabushiki Kaisha | Isoquinoline derivatives having kinasae inhibitory activity and drugs containing the same |
| JP2006521357A (ja) | 2003-03-24 | 2006-09-21 | メルク エンド カムパニー インコーポレーテッド | ナトリウムチャンネル遮断薬としてのビアリール置換６員複素環化合物 |
| GB2400101A (en) | 2003-03-28 | 2004-10-06 | Biofocus Discovery Ltd | Compounds capable of binding to the active site of protein kinases |
| WO2005003101A2 (en) * | 2003-07-02 | 2005-01-13 | Biofocus Discovery Limited | Pyrazine and pyridine derivatives as rho kinase inhibitors |
| EP1670794A2 (en) | 2003-09-30 | 2006-06-21 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments |
| MX2007007797A (es) * | 2004-12-27 | 2007-08-23 | Alcon Inc | Analogo de aminopirazina para tratar glaucoma y otras enfermedades mediadas por rho cinasa. |
-
2006
- 2006-12-19 MX MX2008008328A patent/MX2008008328A/es active IP Right Grant
- 2006-12-19 CA CA002629342A patent/CA2629342A1/en not_active Abandoned
- 2006-12-19 EP EP06846689A patent/EP1962853A1/en not_active Withdrawn
- 2006-12-19 KR KR1020087015628A patent/KR20080077652A/ko not_active Ceased
- 2006-12-19 JP JP2008547727A patent/JP2009521494A/ja active Pending
- 2006-12-19 CN CNA2006800482845A patent/CN101340912A/zh active Pending
- 2006-12-19 RU RU2008130111/04A patent/RU2008130111A/ru unknown
- 2006-12-19 ZA ZA200804497A patent/ZA200804497B/xx unknown
- 2006-12-19 WO PCT/US2006/062307 patent/WO2007076360A1/en not_active Ceased
- 2006-12-19 US US11/612,894 patent/US7655662B2/en not_active Expired - Fee Related
- 2006-12-19 BR BRPI0620463-5A patent/BRPI0620463A2/pt not_active IP Right Cessation
- 2006-12-21 UY UY30058A patent/UY30058A1/es not_active Application Discontinuation
- 2006-12-21 TW TW095148175A patent/TW200733964A/zh unknown
- 2006-12-21 AR ARP060105725A patent/AR058618A1/es not_active Application Discontinuation
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