CN107074768B - 作为转染重排(ret)激酶抑制剂的吡啶酮衍生物 - Google Patents
作为转染重排(ret)激酶抑制剂的吡啶酮衍生物 Download PDFInfo
- Publication number
- CN107074768B CN107074768B CN201580058320.5A CN201580058320A CN107074768B CN 107074768 B CN107074768 B CN 107074768B CN 201580058320 A CN201580058320 A CN 201580058320A CN 107074768 B CN107074768 B CN 107074768B
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—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
- C07D213/02—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
- 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
- C07D213/62—Oxygen or sulfur atoms
- C07D213/69—Two or more oxygen atoms
-
- 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
- C07D401/12—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
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2014086197 | 2014-09-10 | ||
| CNPCT/CN2014/086197 | 2014-09-10 | ||
| CNPCT/CN2015/086995 | 2015-08-14 | ||
| CN2015086995 | 2015-08-14 | ||
| PCT/IB2015/056905 WO2016038552A1 (en) | 2014-09-10 | 2015-09-09 | Pyridone derivatives as rearranged during transfection (ret) kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN107074768A CN107074768A (zh) | 2017-08-18 |
| CN107074768B true CN107074768B (zh) | 2019-12-10 |
Family
ID=54186249
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201580058320.5A Expired - Fee Related CN107074768B (zh) | 2014-09-10 | 2015-09-09 | 作为转染重排(ret)激酶抑制剂的吡啶酮衍生物 |
Country Status (36)
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2918588T3 (pl) | 2010-05-20 | 2017-10-31 | Array Biopharma Inc | Związki makrocykliczne jako inhibitory kinazy TRK |
| CA2960768A1 (en) | 2014-09-10 | 2016-03-17 | Glaxosmithkline Intellectual Property Development Limited | Pyridone derivatives as rearranged during transfection (ret) kinase inhibitors |
| WO2016037578A1 (en) * | 2014-09-10 | 2016-03-17 | Glaxosmithkline Intellectual Property Development Limited | Novel compounds as rearranged during transfection (ret) inhibitors |
| US10202365B2 (en) | 2015-02-06 | 2019-02-12 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors |
| WO2017011776A1 (en) | 2015-07-16 | 2017-01-19 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
| MX384884B (es) | 2015-11-02 | 2025-03-14 | Blueprint Medicines Corp | Inhibidores de ret. |
| WO2017161269A1 (en) | 2016-03-17 | 2017-09-21 | Blueprint Medicines Corporation | Inhibitors of ret receptor tyrosine kinases |
| WO2018017983A1 (en) | 2016-07-22 | 2018-01-25 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to ret |
| JP2018052878A (ja) * | 2016-09-29 | 2018-04-05 | 第一三共株式会社 | ピリジン化合物 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JP6888101B2 (ja) | 2017-01-18 | 2021-06-16 | アレイ バイオファーマ インコーポレイテッド | ＲＥＴキナーゼ阻害剤としての置換ピラゾロ［１，５−ａ］ピラジン化合物 |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| CN110891573A (zh) | 2017-05-15 | 2020-03-17 | 缆图药品公司 | Ret抑制剂和mtorc1抑制剂的组合及其用于治疗由异常ret活性介导的癌症的用途 |
| TWI876442B (zh) | 2017-10-10 | 2025-03-11 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| US11472802B2 (en) | 2018-01-18 | 2022-10-18 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors |
| US11524963B2 (en) | 2018-01-18 | 2022-12-13 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidines as RET kinase inhibitors |
| EP3773589B1 (en) | 2018-04-03 | 2023-11-01 | Blueprint Medicines Corporation | Ret inhibitor for use in treating cancer having a ret alteration |
| EP3849986B1 (en) | 2018-09-10 | 2022-06-08 | Array Biopharma, Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
| KR20230017234A (ko) | 2020-05-29 | 2023-02-03 | 블루프린트 메디신즈 코포레이션 | 프랄세티닙의 고체 형태 |
| WO2022017524A1 (zh) * | 2020-07-23 | 2022-01-27 | 深圳晶泰科技有限公司 | 吡啶酮类化合物及其制备方法和应用 |
| WO2024043257A1 (ja) | 2022-08-24 | 2024-02-29 | 東レ株式会社 | 癌の治療及び／又は予防のための医薬品 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1544420A (zh) * | 1997-12-22 | 2004-11-10 | 用取代杂环脲抑制raf激酶 | |
| WO2007048070A2 (en) * | 2005-10-21 | 2007-04-26 | Amgen Inc. | Pyrrolo-pyridine derivatives for the treatment of cancer diseases |
| WO2008046802A1 (en) * | 2006-10-16 | 2008-04-24 | Novartis Ag | Phenylacetamides useful as protein kinase inhibitors |
| WO2008058341A1 (en) * | 2006-11-15 | 2008-05-22 | Cytopia Research Pty Ltd | Inhibitors of kinase activity |
| CN101553482A (zh) * | 2006-09-15 | 2009-10-07 | 艾科睿制药公司 | 激酶抑制剂化合物 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070244120A1 (en) | 2000-08-18 | 2007-10-18 | Jacques Dumas | Inhibition of raf kinase using substituted heterocyclic ureas |
| ATE529109T1 (de) | 1997-12-22 | 2011-11-15 | Bayer Healthcare Llc | Hemmung der p38 kinase aktivität durch substituierte heterocyclische harnstoffe |
| US20120046290A1 (en) | 1997-12-22 | 2012-02-23 | Jacques Dumas | Inhibition of p38 kinase activity using substituted heterocyclic ureas |
| PL353455A1 (en) | 1999-08-12 | 2003-11-17 | Pharmacia Italia S.P.A. | 3(5)-amino-pyrazole derivatives, process for their preparation and their use as antitumor agents |
| CA2430151A1 (en) | 2000-11-27 | 2002-06-20 | Pharmacia Italia S.P.A. | Phenylacetamido- pyrazole derivatives and their use as antitumor agents |
| DE10201764A1 (de) | 2002-01-18 | 2003-07-31 | Bayer Cropscience Ag | Substituierte 4-Aminopyridin-Derivate |
| PE20040522A1 (es) | 2002-05-29 | 2004-09-28 | Novartis Ag | Derivados de diarilurea dependientes de la cinasa de proteina |
| AU2003264386A1 (en) | 2002-09-10 | 2004-04-30 | Kyorin Pharmaceutical Co., Ltd. | 4-(substituted aryl)-5-hydroxyisoquinolinone derivative |
| BRPI0413757A (pt) | 2003-08-22 | 2006-10-31 | Boehringer Ingelheim Pharma | métodos para o tratamento de copd e da hipertensão pulmonar |
| TW200530236A (en) * | 2004-02-23 | 2005-09-16 | Chugai Pharmaceutical Co Ltd | Heteroaryl phenylurea |
| JP5124285B2 (ja) * | 2004-12-28 | 2013-01-23 | キネックス ファーマシューティカルズ， エルエルシー | 細胞増殖性障害を処置する組成物および方法 |
| US7968574B2 (en) | 2004-12-28 | 2011-06-28 | Kinex Pharmaceuticals, Llc | Biaryl compositions and methods for modulating a kinase cascade |
| GB0507575D0 (en) * | 2005-04-14 | 2005-05-18 | Novartis Ag | Organic compounds |
| TW200804349A (en) * | 2005-12-23 | 2008-01-16 | Kalypsys Inc | Novel substituted pyrimidinyloxy ureas as inhibitors of protein kinases |
| DK2041071T3 (da) | 2006-06-29 | 2014-09-01 | Kinex Pharmaceuticals Llc | Biarylsammensætninger og fremgangsmåder til modulering af en kinasekaskade |
| JP2013502429A (ja) | 2009-08-19 | 2013-01-24 | アムビト ビオスシエンセス コルポラチオン | ビアリール化合物及びその使用方法 |
| WO2012082817A1 (en) | 2010-12-16 | 2012-06-21 | Boehringer Ingelheim International Gmbh | Biarylamide inhibitors of leukotriene production |
| EP2970191B1 (en) * | 2013-03-15 | 2016-12-21 | GlaxoSmithKline Intellectual Property Development Limited | Pyridine derivatives as rearranged during transfection (ret) kinase inhibitors |
| US8937071B2 (en) | 2013-03-15 | 2015-01-20 | Glaxosmithkline Intellectual Property Development Limited | Compounds as rearranged during transfection (RET) inhibitors |
| CA2960768A1 (en) * | 2014-09-10 | 2016-03-17 | Glaxosmithkline Intellectual Property Development Limited | Pyridone derivatives as rearranged during transfection (ret) kinase inhibitors |
| WO2016037578A1 (en) | 2014-09-10 | 2016-03-17 | Glaxosmithkline Intellectual Property Development Limited | Novel compounds as rearranged during transfection (ret) inhibitors |
-
2015
- 2015-09-09 CA CA2960768A patent/CA2960768A1/en not_active Abandoned
- 2015-09-09 AU AU2015313841A patent/AU2015313841B2/en not_active Ceased
- 2015-09-09 BR BR112017004900A patent/BR112017004900A2/pt not_active IP Right Cessation
- 2015-09-09 MA MA040581A patent/MA40581A/fr unknown
- 2015-09-09 EA EA201790546A patent/EA033544B1/ru not_active IP Right Cessation
- 2015-09-09 MY MYPI2017700782A patent/MY181913A/en unknown
- 2015-09-09 PT PT15767599T patent/PT3191450T/pt unknown
- 2015-09-09 US US15/509,613 patent/US9918974B2/en not_active Expired - Fee Related
- 2015-09-09 EP EP19160650.8A patent/EP3517526B1/en active Active
- 2015-09-09 LT LTEP15767599.2T patent/LT3191450T/lt unknown
- 2015-09-09 DK DK15767599.2T patent/DK3191450T3/da active
- 2015-09-09 WO PCT/IB2015/056905 patent/WO2016038552A1/en not_active Ceased
- 2015-09-09 MX MX2017003114A patent/MX373863B/es active IP Right Grant
- 2015-09-09 PE PE2017000417A patent/PE20170705A1/es unknown
- 2015-09-09 UA UAA201703478A patent/UA122213C2/uk unknown
- 2015-09-09 ME MEP-2019-136A patent/ME03432B/me unknown
- 2015-09-09 SM SM20190304T patent/SMT201900304T1/it unknown
- 2015-09-09 HR HRP20190815TT patent/HRP20190815T1/hr unknown
- 2015-09-09 HU HUE15767599 patent/HUE044604T2/hu unknown
- 2015-09-09 SG SG11201701694QA patent/SG11201701694QA/en unknown
- 2015-09-09 CN CN201580058320.5A patent/CN107074768B/zh not_active Expired - Fee Related
- 2015-09-09 KR KR1020177009237A patent/KR20170045350A/ko not_active Ceased
- 2015-09-09 ES ES19160650T patent/ES2816453T3/es active Active
- 2015-09-09 EP EP15767599.2A patent/EP3191450B1/en active Active
- 2015-09-09 CR CR20170093A patent/CR20170093A/es unknown
- 2015-09-09 SI SI201530720T patent/SI3191450T1/sl unknown
- 2015-09-09 RS RS20190559A patent/RS58813B1/sr unknown
- 2015-09-09 PL PL15767599T patent/PL3191450T3/pl unknown
- 2015-09-09 ES ES15767599T patent/ES2725704T3/es active Active
- 2015-09-09 JP JP2017513450A patent/JP6538154B2/ja not_active Expired - Fee Related
- 2015-09-10 TW TW104129876A patent/TWI683807B/zh not_active IP Right Cessation
- 2015-09-10 UY UY0001036293A patent/UY36293A/es unknown
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2017
- 2017-03-02 IL IL250908A patent/IL250908B/en active IP Right Grant
- 2017-03-07 CO CONC2017/0002273A patent/CO2017002273A2/es unknown
- 2017-03-07 DO DO2017000059A patent/DOP2017000059A/es unknown
- 2017-03-07 PH PH12017500425A patent/PH12017500425B1/en unknown
- 2017-03-09 CL CL2017000588A patent/CL2017000588A1/es unknown
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2018
- 2018-01-23 US US15/877,524 patent/US10111866B2/en not_active Expired - Fee Related
- 2018-09-28 US US16/145,271 patent/US10292975B2/en not_active Expired - Fee Related
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2019
- 2019-04-05 US US16/376,858 patent/US10709695B2/en not_active Expired - Fee Related
- 2019-05-09 CY CY20191100502T patent/CY1121661T1/el unknown
- 2019-05-31 JP JP2019102776A patent/JP6728447B2/ja not_active Expired - Fee Related
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1544420A (zh) * | 1997-12-22 | 2004-11-10 | 用取代杂环脲抑制raf激酶 | |
| WO2007048070A2 (en) * | 2005-10-21 | 2007-04-26 | Amgen Inc. | Pyrrolo-pyridine derivatives for the treatment of cancer diseases |
| CN101553482A (zh) * | 2006-09-15 | 2009-10-07 | 艾科睿制药公司 | 激酶抑制剂化合物 |
| WO2008046802A1 (en) * | 2006-10-16 | 2008-04-24 | Novartis Ag | Phenylacetamides useful as protein kinase inhibitors |
| WO2008058341A1 (en) * | 2006-11-15 | 2008-05-22 | Cytopia Research Pty Ltd | Inhibitors of kinase activity |
Also Published As
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