CN101068805B - 作为bcr-abl激酶抑制剂的新的苯基氨基嘧啶衍生物 - Google Patents
作为bcr-abl激酶抑制剂的新的苯基氨基嘧啶衍生物 Download PDFInfo
- Publication number
- CN101068805B CN101068805B CN2005800300912A CN200580030091A CN101068805B CN 101068805 B CN101068805 B CN 101068805B CN 2005800300912 A CN2005800300912 A CN 2005800300912A CN 200580030091 A CN200580030091 A CN 200580030091A CN 101068805 B CN101068805 B CN 101068805B
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- CN
- China
- Prior art keywords
- formula
- methyl
- compound
- phenyl
- trifluoromethyl
- 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.)
- Expired - Fee Related
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
- C07C323/62—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
-
- 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
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
- C07C233/66—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
- C07C279/18—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to carbon atoms of six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
-
- 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
- C07D213/82—Amides; Imides in position 3
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN908/CHE/2004 | 2004-09-09 | ||
| IN908CH2004 | 2004-09-09 | ||
| PCT/IN2005/000243 WO2006027795A1 (en) | 2004-09-09 | 2005-07-19 | Novel phenylaminopyrimidine derivatives as inhibitors of bcr-abl kinase |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101068805A CN101068805A (zh) | 2007-11-07 |
| CN101068805B true CN101068805B (zh) | 2013-04-03 |
Family
ID=35395645
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2005800300912A Expired - Fee Related CN101068805B (zh) | 2004-09-09 | 2005-07-19 | 作为bcr-abl激酶抑制剂的新的苯基氨基嘧啶衍生物 |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US7910598B2 (https=) |
| EP (2) | EP1786799B1 (https=) |
| JP (1) | JP5184887B2 (https=) |
| KR (1) | KR100948453B1 (https=) |
| CN (1) | CN101068805B (https=) |
| AP (1) | AP2470A (https=) |
| AU (1) | AU2005281299B2 (https=) |
| BR (1) | BRPI0515081B8 (https=) |
| CA (1) | CA2591321C (https=) |
| CY (1) | CY1113617T1 (https=) |
| DK (1) | DK1786799T3 (https=) |
| EA (1) | EA013328B1 (https=) |
| ES (1) | ES2390227T3 (https=) |
| HR (1) | HRP20070146B1 (https=) |
| IL (1) | IL181811A (https=) |
| MA (1) | MA28922B1 (https=) |
| MX (1) | MX2007002819A (https=) |
| NO (1) | NO337598B1 (https=) |
| NZ (1) | NZ554361A (https=) |
| PL (1) | PL1786799T3 (https=) |
| PT (1) | PT1786799E (https=) |
| SI (1) | SI1786799T1 (https=) |
| UA (1) | UA94570C2 (https=) |
| WO (1) | WO2006027795A1 (https=) |
| ZA (2) | ZA200701942B (https=) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6667300B2 (en) * | 2000-04-25 | 2003-12-23 | Icos Corporation | Inhibitors of human phosphatidylinositol 3-kinase delta |
| SI2612862T1 (sl) | 2004-05-13 | 2017-04-26 | Icos Corporation | Kinazolini kot inhibitorji humane fosfatidilinozitol 3-kinaze delta |
| US20110190328A1 (en) * | 2004-09-09 | 2011-08-04 | Natco Pharma Limited | Acid addition salts of (3,5-bis trifluoromethyl)-n-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide |
| US8735415B2 (en) | 2004-09-09 | 2014-05-27 | Natco Pharma Limited | Acid addition salts of (3,5-Bis trifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide |
| UA94570C2 (en) | 2004-09-09 | 2011-05-25 | Натко Фарма Лимитед | Phenylaminopyrimidine derivatives as inhibitors of bcr-abl kinase |
| US7939541B2 (en) * | 2004-09-09 | 2011-05-10 | Natco Pharma Limited | Intermediates and a process employing the intermediates for the preparation of (3-trifluoromethylsulfonyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide |
| WO2008031534A1 (en) * | 2006-09-11 | 2008-03-20 | Syngenta Participations Ag | Insecticidal compounds |
| WO2008058037A1 (en) * | 2006-11-03 | 2008-05-15 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| ES2396160T3 (es) * | 2006-12-14 | 2013-02-19 | Bayer Intellectual Property Gmbh | Derivados de DIHIDROPIRIDINA que utiliza como inhibidores de la proteina quinasa |
| EP2152688A1 (en) * | 2007-05-04 | 2010-02-17 | Irm Llc | Compounds and compositions as c-kit and pdgfr kinase inhibitors |
| EP2148874B1 (en) * | 2007-05-04 | 2012-02-08 | Irm Llc | Pyrimidine derivatives and compositions as c-kit and pdgfr kinase inhibitors |
| CA2697077C (en) | 2007-08-22 | 2012-10-16 | Irm Llc | 2-heteroarylamino-pyrimidine derivatives as kinase inhibitors |
| CA2697081C (en) | 2007-08-22 | 2013-04-23 | Irm Llc | 5-(4-(haloalkoxy)phenyl)pyrimidine-2-amine compounds and compositions as kinase inhibitors |
| US8067422B2 (en) | 2008-03-04 | 2011-11-29 | Natco Pharma Limited | Crystal form of phenylamino pyrimidine derivatives |
| MY183331A (en) * | 2008-03-04 | 2021-02-18 | Natco Pharma Ltd | Crystal form of phenylamino pyrimidine derivatives |
| WO2012004801A1 (en) * | 2010-07-07 | 2012-01-12 | Hetero Research Foundation | Process for imatinib mesylate |
| GB2488788B (en) | 2011-03-07 | 2013-07-10 | Natco Pharma Ltd | Oral formulation of phenylaminopyrymidine compound with enhanced bioavailability and pharmacological response |
| CN103797011B (zh) | 2011-09-01 | 2016-03-30 | 诺华股份有限公司 | 作为c-Kit激酶抑制剂的化合物和组合物 |
| US9061028B2 (en) | 2012-02-15 | 2015-06-23 | Natco Pharma Limited | Process for the preparation of Nilotinib |
| CN104379582A (zh) * | 2012-06-15 | 2015-02-25 | 巴斯夫欧洲公司 | 包含达沙替尼和所选择的共晶体形成剂的多组分晶体 |
| PT3389633T (pt) | 2015-12-18 | 2021-08-05 | Natco Pharma Ltd | Composições farmacêuticas compreendendo derivados de fenilaminopirimidina |
| US10722484B2 (en) | 2016-03-09 | 2020-07-28 | K-Gen, Inc. | Methods of cancer treatment |
| JP2023534963A (ja) | 2020-07-15 | 2023-08-15 | サード ハーモニック バイオ, インコーポレイテッド | 選択的c-kitキナーゼ阻害剤の結晶質形態 |
| US11744823B2 (en) | 2020-11-19 | 2023-09-05 | Third Harmonic Bio, Inc. | Pharmaceutical compositions of a selective c-kit kinase inhibitor and methods for making and using same |
| CN113125689B (zh) * | 2021-03-29 | 2022-02-22 | 创芯国际生物科技(广州)有限公司 | 一种新型mtt细胞活力检测试剂盒及其应用 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW225528B (https=) | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| US5516775A (en) | 1992-08-31 | 1996-05-14 | Ciba-Geigy Corporation | Further use of pyrimidine derivatives |
| KR100330553B1 (ko) | 1993-10-01 | 2002-11-27 | 노파르티스 아게 | 약물학적활성피리딘유도체및그의제조방법 |
| JPH08503971A (ja) | 1993-10-01 | 1996-04-30 | チバ−ガイギー アクチェンゲゼルシャフト | ピリミジンアミン誘導体及びその調製のための方法 |
| WO1995009851A1 (en) | 1993-10-01 | 1995-04-13 | Ciba-Geigy Ag | Pharmacologically active pyrimidineamine derivatives and processes for the preparation thereof |
| CO4940418A1 (es) | 1997-07-18 | 2000-07-24 | Novartis Ag | Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso |
| AU739066B2 (en) * | 1997-09-23 | 2001-10-04 | Astrazeneca Ab | Amide derivatives for the treatment of diseases mediated by cytokines |
| CA2338121A1 (en) * | 1998-08-04 | 2000-02-17 | Astrazeneca Ab | Amide derivatives useful as inhibitors of the production of cytokines |
| GB0022438D0 (en) | 2000-09-13 | 2000-11-01 | Novartis Ag | Organic Compounds |
| WO2004002963A1 (ja) * | 2002-06-28 | 2004-01-08 | Nippon Shinyaku Co., Ltd. | アミド誘導体及び医薬 |
| GB0222514D0 (en) | 2002-09-27 | 2002-11-06 | Novartis Ag | Organic compounds |
| AU2003242988A1 (en) * | 2003-06-06 | 2005-01-04 | Adibhatla Kali Sathya Bhujanga Rao | Process for the preparation of the anti-cancer drug imatinib and its analogues |
| AU2004246800B2 (en) * | 2003-06-13 | 2008-12-04 | Novartis Ag | 2-aminopyrimidine derivatives as Raf kinase inhibitors |
| UA94570C2 (en) | 2004-09-09 | 2011-05-25 | Натко Фарма Лимитед | Phenylaminopyrimidine derivatives as inhibitors of bcr-abl kinase |
| WO2008058037A1 (en) * | 2006-11-03 | 2008-05-15 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
-
2005
- 2005-07-19 UA UAA200703971A patent/UA94570C2/ru unknown
- 2005-07-19 SI SI200531589T patent/SI1786799T1/sl unknown
- 2005-07-19 EP EP05779775A patent/EP1786799B1/en not_active Expired - Lifetime
- 2005-07-19 HR HRP20070146AA patent/HRP20070146B1/hr not_active IP Right Cessation
- 2005-07-19 DK DK05779775.5T patent/DK1786799T3/da active
- 2005-07-19 PT PT05779775T patent/PT1786799E/pt unknown
- 2005-07-19 ES ES05779775T patent/ES2390227T3/es not_active Expired - Lifetime
- 2005-07-19 PL PL05779775T patent/PL1786799T3/pl unknown
- 2005-07-19 NZ NZ554361A patent/NZ554361A/en not_active IP Right Cessation
- 2005-07-19 AU AU2005281299A patent/AU2005281299B2/en not_active Ceased
- 2005-07-19 AP AP2007003944A patent/AP2470A/xx active
- 2005-07-19 JP JP2007530854A patent/JP5184887B2/ja not_active Expired - Fee Related
- 2005-07-19 KR KR1020077008040A patent/KR100948453B1/ko not_active Expired - Fee Related
- 2005-07-19 EA EA200700601A patent/EA013328B1/ru unknown
- 2005-07-19 BR BRPI0515081A patent/BRPI0515081B8/pt not_active IP Right Cessation
- 2005-07-19 WO PCT/IN2005/000243 patent/WO2006027795A1/en not_active Ceased
- 2005-07-19 MX MX2007002819A patent/MX2007002819A/es active IP Right Grant
- 2005-07-19 EP EP10184904.0A patent/EP2295424B1/en not_active Expired - Lifetime
- 2005-07-19 CN CN2005800300912A patent/CN101068805B/zh not_active Expired - Fee Related
- 2005-07-19 CA CA2591321A patent/CA2591321C/en not_active Expired - Fee Related
-
2007
- 2007-03-05 US US11/714,565 patent/US7910598B2/en not_active Expired - Fee Related
- 2007-03-06 ZA ZA200701942A patent/ZA200701942B/xx unknown
- 2007-03-08 IL IL181811A patent/IL181811A/en active IP Right Grant
- 2007-03-22 NO NO20071521A patent/NO337598B1/no not_active IP Right Cessation
- 2007-04-06 MA MA29808A patent/MA28922B1/fr unknown
- 2007-04-12 ZA ZA200703123A patent/ZA200703123B/en unknown
-
2008
- 2008-03-04 US US12/042,235 patent/US8183253B2/en not_active Expired - Fee Related
-
2012
- 2012-09-28 CY CY20121100895T patent/CY1113617T1/el unknown
Non-Patent Citations (2)
| Title |
|---|
| masaru ogata.synthesis and antiviral activity.journal of medicinal chemistry29 3.1986,29(3),417-423. |
| masaru ogata.synthesis and antiviral activity.journal of medicinal chemistry29 3.1986,29(3),417-423. * |
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