IN2012DN03180A - - Google Patents
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- Publication number
- IN2012DN03180A IN2012DN03180A IN3180DEN2012A IN2012DN03180A IN 2012DN03180 A IN2012DN03180 A IN 2012DN03180A IN 3180DEN2012 A IN3180DEN2012 A IN 3180DEN2012A IN 2012DN03180 A IN2012DN03180 A IN 2012DN03180A
- Authority
- IN
- India
- Prior art keywords
- phenyl
- compound
- compositions
- piperazin
- pyrimidin
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 abstract 3
- 239000000203 mixture Substances 0.000 abstract 3
- QADPYRIHXKWUSV-UHFFFAOYSA-N BGJ-398 Chemical compound C1CN(CC)CCN1C(C=C1)=CC=C1NC1=CC(N(C)C(=O)NC=2C(=C(OC)C=C(OC)C=2Cl)Cl)=NC=N1 QADPYRIHXKWUSV-UHFFFAOYSA-N 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- ZEOWTGPWHLSLOG-UHFFFAOYSA-N Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F Chemical compound Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F ZEOWTGPWHLSLOG-UHFFFAOYSA-N 0.000 abstract 1
- 102100023593 Fibroblast growth factor receptor 1 Human genes 0.000 abstract 1
- 101710182386 Fibroblast growth factor receptor 1 Proteins 0.000 abstract 1
- 102100023600 Fibroblast growth factor receptor 2 Human genes 0.000 abstract 1
- 101710182389 Fibroblast growth factor receptor 2 Proteins 0.000 abstract 1
- 102100027842 Fibroblast growth factor receptor 3 Human genes 0.000 abstract 1
- 101710182396 Fibroblast growth factor receptor 3 Proteins 0.000 abstract 1
- 102100027844 Fibroblast growth factor receptor 4 Human genes 0.000 abstract 1
- 101000917134 Homo sapiens Fibroblast growth factor receptor 4 Proteins 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 230000001668 ameliorated effect Effects 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 239000007800 oxidant agent Substances 0.000 abstract 1
- 230000001590 oxidative effect Effects 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D403/10—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 carbon chain containing aromatic 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
- C07D403/02—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
An N-oxide of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1 -{6-[4-(4-ethyl-piperazin-1 -yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea, pharmaceutically acceptable salts thereof, compositions including the compound and its pharmaceutically acceptable salts, and methods of preparing the compound and the compositions (such as, for example, by oxidizing 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1 -{6-[4-(4-ethyl-piperazin-1 -yl)-phenyl-amino]-pyrimidin-4-yl}-1-methyl-urea with an oxidizing agent) are described. Further described herein are methods of using the compound and compositions of the present technology, alone and in combination with other suitable agents, to treat various diseases, including but not limited to, those that can be prevented, inhibited or ameliorated by inhibition of kinase activity selected from FGFR1, FGFR2, FGFR3 or FGFR4.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09174619 | 2009-10-30 | ||
| PCT/EP2010/066435 WO2011051425A1 (en) | 2009-10-30 | 2010-10-29 | N-oxide of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IN2012DN03180A true IN2012DN03180A (en) | 2015-09-25 |
Family
ID=41396002
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IN3180DEN2012 IN2012DN03180A (en) | 2009-10-30 | 2010-10-29 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US20120220600A1 (en) |
| EP (1) | EP2493864B1 (en) |
| KR (1) | KR20120101367A (en) |
| CN (1) | CN102596916B (en) |
| ES (1) | ES2524548T3 (en) |
| IN (1) | IN2012DN03180A (en) |
| WO (1) | WO2011051425A1 (en) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0512324D0 (en) * | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| AU2013241664B2 (en) | 2012-03-30 | 2016-05-19 | Novartis Ag | FGFR inhibitor for use in the treatment of hypophosphatemic disorders |
| ES2984771T3 (en) | 2012-06-13 | 2024-10-31 | Incyte Holdings Corp | Substituted tricyclic compounds as FGFR inhibitors |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| AR094812A1 (en) | 2013-02-20 | 2015-08-26 | Eisai R&D Man Co Ltd | DERIVED FROM MONOCYCLIC PYRIDINE AS AN FGFR INHIBITOR |
| ES2657451T3 (en) | 2013-04-19 | 2018-03-05 | Incyte Holdings Corporation | Bicyclic heterocyclics as FGFR inhibitors |
| MX387702B (en) | 2013-10-25 | 2025-03-18 | Novartis Ag | PYRIDYL-DERIVED BICYCLIC FUSED RING COMPOUNDS AS FGFR4 INHIBITORS. |
| KR102344105B1 (en) | 2014-08-18 | 2021-12-29 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | Salt of monocyclic pyridine derivative and crystal thereof |
| WO2016054483A1 (en) | 2014-10-03 | 2016-04-07 | Novartis Ag | Use of ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (en) | 2015-02-20 | 2017-12-26 | Incyte Corp | BICYCLIC HETEROCYCLES USED AS FGFR4 INHIBITORS |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| CN107438607B (en) | 2015-02-20 | 2021-02-05 | 因赛特公司 | Bicyclic heterocycles as FGFR inhibitors |
| US9802917B2 (en) | 2015-03-25 | 2017-10-31 | Novartis Ag | Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide |
| KR20170129757A (en) * | 2015-03-25 | 2017-11-27 | 노파르티스 아게 | Formylated N-heterocyclic derivatives as FGFR4 inhibitors |
| RU2712222C2 (en) | 2015-03-25 | 2020-01-27 | Нэшнл Кэнсер Сентер | Therapeutic agent for bile duct cancer |
| KR102486722B1 (en) | 2015-12-17 | 2023-01-11 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | breast cancer treatment |
| AR111960A1 (en) | 2017-05-26 | 2019-09-04 | Incyte Corp | CRYSTALLINE FORMS OF A FGFR INHIBITOR AND PROCESSES FOR ITS PREPARATION |
| AU2019241625A1 (en) | 2018-03-28 | 2020-09-03 | Eisai R&D Management Co., Ltd. | Therapeutic agent for hepatocellular carcinoma |
| FI3788047T3 (en) | 2018-05-04 | 2024-11-02 | Incyte Corp | SOLID FORM OF FGFT INHIBITOR AND METHODS FOR THEIR PREPARATION |
| JP7568512B2 (en) | 2018-05-04 | 2024-10-16 | インサイト・コーポレイション | Salt of FGFR inhibitor |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021076602A1 (en) | 2019-10-14 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| AU2020395185A1 (en) | 2019-12-04 | 2022-06-02 | Incyte Corporation | Derivatives of an FGFR inhibitor |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CN114539258A (en) * | 2020-11-27 | 2022-05-27 | 首药控股(北京)股份有限公司 | Polymorphic substance of FGFR4 protein kinase inhibitor and preparation method thereof |
| CN113185510B (en) * | 2021-04-12 | 2022-05-13 | 南京海纳医药科技股份有限公司 | Preparation method of alpha-vatripopa impurity |
| TW202304459A (en) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| TW202313611A (en) | 2021-06-09 | 2023-04-01 | 美商英塞特公司 | Tricyclic heterocycles as fgfr inhibitors |
| EP4352060A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA02003436A (en) * | 1999-10-07 | 2002-08-20 | Amgen Inc | Triazine kinase inhibitors. |
| GB0512324D0 (en) * | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| AU2006326989B2 (en) * | 2005-12-21 | 2011-11-24 | Novartis Ag | Pyrimidinyl aryl urea derivatives being FGF inhibitors |
-
2010
- 2010-10-29 US US13/504,258 patent/US20120220600A1/en not_active Abandoned
- 2010-10-29 KR KR1020127010832A patent/KR20120101367A/en not_active Ceased
- 2010-10-29 EP EP10771744.9A patent/EP2493864B1/en not_active Not-in-force
- 2010-10-29 IN IN3180DEN2012 patent/IN2012DN03180A/en unknown
- 2010-10-29 WO PCT/EP2010/066435 patent/WO2011051425A1/en active Application Filing
- 2010-10-29 CN CN201080048756.3A patent/CN102596916B/en not_active Expired - Fee Related
- 2010-10-29 ES ES10771744.9T patent/ES2524548T3/en active Active
-
2014
- 2014-09-05 US US14/477,949 patent/US20140378468A1/en not_active Abandoned
-
2015
- 2015-12-16 US US14/971,412 patent/US20160102062A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CN102596916B (en) | 2015-06-17 |
| EP2493864B1 (en) | 2014-10-01 |
| KR20120101367A (en) | 2012-09-13 |
| US20120220600A1 (en) | 2012-08-30 |
| WO2011051425A1 (en) | 2011-05-05 |
| US20140378468A1 (en) | 2014-12-25 |
| CN102596916A (en) | 2012-07-18 |
| ES2524548T3 (en) | 2014-12-10 |
| EP2493864A1 (en) | 2012-09-05 |
| US20160102062A1 (en) | 2016-04-14 |
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