JP2012506381A - c−METタンパク質キナーゼ阻害剤 - Google Patents
c−METタンパク質キナーゼ阻害剤 Download PDFInfo
- Publication number
- JP2012506381A JP2012506381A JP2011532324A JP2011532324A JP2012506381A JP 2012506381 A JP2012506381 A JP 2012506381A JP 2011532324 A JP2011532324 A JP 2011532324A JP 2011532324 A JP2011532324 A JP 2011532324A JP 2012506381 A JP2012506381 A JP 2012506381A
- Authority
- JP
- Japan
- Prior art keywords
- compound
- ring
- pharmaceutically acceptable
- mmol
- cancer
- 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
- 0 *C(C1*)C(*)=C(*)C(*)=C1[n]1nnnc1-c1cc(*)cnc1N Chemical compound *C(C1*)C(*)=C(*)C(*)=C1[n]1nnnc1-c1cc(*)cnc1N 0.000 description 6
- QUZKPKCSLGOVRS-UHFFFAOYSA-N CN(C(CC1)C2)C1CC2Oc(c(F)c1F)ccc1-[n]1nnnc1-c1c(N)ncc(C2=CSCC2)c1 Chemical compound CN(C(CC1)C2)C1CC2Oc(c(F)c1F)ccc1-[n]1nnnc1-c1c(N)ncc(C2=CSCC2)c1 QUZKPKCSLGOVRS-UHFFFAOYSA-N 0.000 description 1
- BFFJPBBEYROJIK-UHFFFAOYSA-N CNC(CC1)CCC1Oc(c(F)c1F)ccc1-[n]1nnnc1-c1cc(-c2c[n](C3CCOCC3)nc2)cnc1N Chemical compound CNC(CC1)CCC1Oc(c(F)c1F)ccc1-[n]1nnnc1-c1cc(-c2c[n](C3CCOCC3)nc2)cnc1N BFFJPBBEYROJIK-UHFFFAOYSA-N 0.000 description 1
- IOQPOPIZRAHORG-UHFFFAOYSA-N C[n]1ncc(-c(cc2-c3nnn[n]3-c(c(F)c3F)ccc3OC3CNCCC3)cnc2N)c1 Chemical compound C[n]1ncc(-c(cc2-c3nnn[n]3-c(c(F)c3F)ccc3OC3CNCCC3)cnc2N)c1 IOQPOPIZRAHORG-UHFFFAOYSA-N 0.000 description 1
- ZAWOFMYXLUZSRV-UHFFFAOYSA-N Nc(c(-c1nnn[n]1-c(c(F)c1F)ccc1OC1CCNCC1)c1)ncc1-c1ccncc1 Chemical compound Nc(c(-c1nnn[n]1-c(c(F)c1F)ccc1OC1CCNCC1)c1)ncc1-c1ccncc1 ZAWOFMYXLUZSRV-UHFFFAOYSA-N 0.000 description 1
- FLUWWLZKHUFXJF-UHFFFAOYSA-N Nc(c(/C(/Nc(ccc(OC1C(CC2)CCN2C1)c1F)c1F)=N/N=N)c1)ncc1-c1ccc2OCOc2c1 Chemical compound Nc(c(/C(/Nc(ccc(OC1C(CC2)CCN2C1)c1F)c1F)=N/N=N)c1)ncc1-c1ccc2OCOc2c1 FLUWWLZKHUFXJF-UHFFFAOYSA-N 0.000 description 1
- KWIJNSJNUDRVHO-UHFFFAOYSA-N Nc(ncc(-c1c[s]cc1)c1)c1-c1nnn[n]1-c(c(F)c1F)ccc1OC1CNCCC1 Chemical compound Nc(ncc(-c1c[s]cc1)c1)c1-c1nnn[n]1-c(c(F)c1F)ccc1OC1CNCCC1 KWIJNSJNUDRVHO-UHFFFAOYSA-N 0.000 description 1
- SRNPXJVILPBBOB-UHFFFAOYSA-N Nc(ncc(Br)c1)c1-c1nnn[n]1-c(c(F)c1F)ccc1OCCCl Chemical compound Nc(ncc(Br)c1)c1-c1nnn[n]1-c(c(F)c1F)ccc1OCCCl SRNPXJVILPBBOB-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- C07D401/02—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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
- C07D451/06—Oxygen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10701308P | 2008-10-21 | 2008-10-21 | |
| US61/107,013 | 2008-10-21 | ||
| PCT/US2009/061253 WO2010048131A1 (en) | 2008-10-21 | 2009-10-20 | C-met protein kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012506381A true JP2012506381A (ja) | 2012-03-15 |
| JP2012506381A5 JP2012506381A5 (enExample) | 2012-11-29 |
Family
ID=41381943
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011532324A Pending JP2012506381A (ja) | 2008-10-21 | 2009-10-20 | c−METタンパク質キナーゼ阻害剤 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US8518938B2 (enExample) |
| EP (1) | EP2350045A1 (enExample) |
| JP (1) | JP2012506381A (enExample) |
| CN (1) | CN102317277A (enExample) |
| AU (1) | AU2009307770A1 (enExample) |
| CA (1) | CA2740583A1 (enExample) |
| MX (1) | MX2011004188A (enExample) |
| NZ (1) | NZ592569A (enExample) |
| WO (1) | WO2010048131A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8991876B2 (en) | 2009-04-23 | 2015-03-31 | Fresenius Medical Care Deutschland Gmbh | Connection means and method for connecting at least two fluid-conducting medical-technical systems, as well as medical-technical apparatus |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2370424A1 (en) | 2008-11-10 | 2011-10-05 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP2376485B1 (en) | 2008-12-19 | 2017-12-06 | Vertex Pharmaceuticals Incorporated | Pyrazine derivatives useful as inhibitors of atr kinase |
| WO2011143399A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| JP2013526540A (ja) | 2010-05-12 | 2013-06-24 | 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 | Atrキナーゼ阻害剤として有用な化合物 |
| EP2569284B1 (en) | 2010-05-12 | 2015-07-08 | Vertex Pharmaceuticals Incorporated | 2-aminopyridine derivatives useful as inhibitors of atr kinase |
| KR20130066633A (ko) | 2010-05-12 | 2013-06-20 | 버텍스 파마슈티칼스 인코포레이티드 | Atr 키나제의 억제제로서 유용한 화합물 |
| EP2569286B1 (en) | 2010-05-12 | 2014-08-20 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| US8962631B2 (en) | 2010-05-12 | 2015-02-24 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| WO2011163527A1 (en) | 2010-06-23 | 2011-12-29 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase |
| WO2012138938A1 (en) | 2011-04-05 | 2012-10-11 | Vertex Pharmaceuticals Incorporated | Aminopyrazine compounds useful as inhibitors of tra kinase |
| US9309250B2 (en) | 2011-06-22 | 2016-04-12 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors |
| US8822469B2 (en) | 2011-06-22 | 2014-09-02 | Vertex Pharmaceuticals Incorporated | Pyrrolo[2,3-B]pyrazines useful as inhibitors of ATR kinase |
| US9096602B2 (en) | 2011-06-22 | 2015-08-04 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-B]pyrazines as ATR kinase inhibitors |
| CN103987709B (zh) | 2011-09-30 | 2016-09-28 | 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 |
| BR112014007690B1 (pt) | 2011-09-30 | 2022-10-04 | Vertex Pharmaceuticals Incorporated | Usos de inibidores de atr no tratamento de câncer pancreático e câncer de pulmão de células não pequenas |
| EP2751088B1 (en) | 2011-09-30 | 2016-04-13 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| US8853217B2 (en) | 2011-09-30 | 2014-10-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| IN2014KN00943A (enExample) | 2011-09-30 | 2015-08-21 | Vertex Pharma | |
| WO2013071093A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
| WO2013071090A1 (en) | 2011-11-09 | 2013-05-16 | 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 |
| US8841449B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| WO2013071094A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP3311816A1 (en) | 2012-04-05 | 2018-04-25 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase for the treatment of cancer |
| WO2014020467A2 (en) * | 2012-07-30 | 2014-02-06 | Fresenius Kabi Oncology Ltd | Process for the preparation of pyrazole substituted aminoheteroaryl compounds |
| US8999632B2 (en) | 2012-10-04 | 2015-04-07 | Vertex Pharmaceuticals Incorporated | Method for measuring ATR inhibition mediated increases in DNA damage |
| EP2909202A1 (en) | 2012-10-16 | 2015-08-26 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| PL3808749T3 (pl) | 2012-12-07 | 2023-07-10 | Vertex Pharmaceuticals Incorporated | Pirazolo[1,5-a]pirymidyny użyteczne jako inhibitory kinazy atr do leczenia chorób nowotworowych |
| JP2016512815A (ja) | 2013-03-15 | 2016-05-09 | 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縮合ピラゾロピリミジン誘導体 |
| PL3077397T3 (pl) | 2013-12-06 | 2020-04-30 | Vertex Pharmaceuticals Inc. | Związek 2-amino-6-fluoro-n-[5-fluoro-pirydyn-3-ylo]pyrazolo [1,5-a]pirymidino-3-karboksamidu przydatny jako inhibitor kinazy atr, jego wytwarzanie, różne postacie stałe i ich radioznakowane pochodne |
| SG10201902206QA (en) | 2014-06-05 | 2019-04-29 | Vertex Pharma | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof |
| PT3157566T (pt) | 2014-06-17 | 2019-07-11 | Vertex Pharma | Método para tratamento de cancro utilizando uma combinação de inibidores chk1 e atr |
| RU2768621C1 (ru) | 2015-09-30 | 2022-03-24 | Вертекс Фармасьютикалз Инкорпорейтед | Способ лечения рака с использованием комбинации повреждающих днк средств и ингибиторов atr |
| IL277071B2 (en) | 2018-03-08 | 2024-07-01 | Incyte Corp | AMINOPYRAZINE DIOL COMPOUNDS AS PI3K-y INHIBITORS |
| US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007111904A2 (en) * | 2006-03-22 | 2007-10-04 | Vertex Pharmaceuticals Incorporated | C-met protein kinase inhibitors for the treatment of proliferative disorders |
| JP2010540649A (ja) * | 2007-10-03 | 2010-12-24 | 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 | c−METタンパク質の阻害剤 |
-
2009
- 2009-10-20 CN CN2009801471841A patent/CN102317277A/zh active Pending
- 2009-10-20 MX MX2011004188A patent/MX2011004188A/es not_active Application Discontinuation
- 2009-10-20 JP JP2011532324A patent/JP2012506381A/ja active Pending
- 2009-10-20 CA CA2740583A patent/CA2740583A1/en not_active Abandoned
- 2009-10-20 EP EP09744003A patent/EP2350045A1/en not_active Withdrawn
- 2009-10-20 NZ NZ592569A patent/NZ592569A/en not_active IP Right Cessation
- 2009-10-20 WO PCT/US2009/061253 patent/WO2010048131A1/en not_active Ceased
- 2009-10-20 AU AU2009307770A patent/AU2009307770A1/en not_active Abandoned
-
2011
- 2011-04-20 US US13/090,563 patent/US8518938B2/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007111904A2 (en) * | 2006-03-22 | 2007-10-04 | Vertex Pharmaceuticals Incorporated | C-met protein kinase inhibitors for the treatment of proliferative disorders |
| JP2010540649A (ja) * | 2007-10-03 | 2010-12-24 | 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 | c−METタンパク質の阻害剤 |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8991876B2 (en) | 2009-04-23 | 2015-03-31 | Fresenius Medical Care Deutschland Gmbh | Connection means and method for connecting at least two fluid-conducting medical-technical systems, as well as medical-technical apparatus |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2010048131A1 (en) | 2010-04-29 |
| AU2009307770A1 (en) | 2010-04-29 |
| US8518938B2 (en) | 2013-08-27 |
| MX2011004188A (es) | 2011-06-09 |
| US20120165333A1 (en) | 2012-06-28 |
| NZ592569A (en) | 2012-05-25 |
| EP2350045A1 (en) | 2011-08-03 |
| CA2740583A1 (en) | 2010-04-29 |
| CN102317277A (zh) | 2012-01-11 |
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| A521 | Request for written amendment filed |
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| A621 | Written request for application examination |
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