NI201200016A - Derivados de piridina y pirazina como moduladores de cinasa de proteína - Google Patents
Derivados de piridina y pirazina como moduladores de cinasa de proteínaInfo
- Publication number
- NI201200016A NI201200016A NI201200016A NI201200016A NI201200016A NI 201200016 A NI201200016 A NI 201200016A NI 201200016 A NI201200016 A NI 201200016A NI 201200016 A NI201200016 A NI 201200016A NI 201200016 A NI201200016 A NI 201200016A
- Authority
- NI
- Nicaragua
- Prior art keywords
- pyridine
- protein kinase
- kinase modulators
- pirazine
- derivatives
- Prior art date
Links
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 title 2
- 102000001253 Protein Kinase Human genes 0.000 title 1
- 108060006633 protein kinase Proteins 0.000 title 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 title 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 102100024457 Cyclin-dependent kinase 9 Human genes 0.000 abstract 1
- 101000980930 Homo sapiens Cyclin-dependent kinase 9 Proteins 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- 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
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- A—HUMAN NECESSITIES
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- 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
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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- 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
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- 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
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- 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
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
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- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/20—Nitrogen atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Tropical Medicine & Parasitology (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Emergency Medicine (AREA)
- Pulmonology (AREA)
- Obesity (AREA)
- AIDS & HIV (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
Abstract
La presente invención proporciona un compuesto de la fórmula (I): y las sales farmacéuticamente aceptables, enantiómeros, estereoisómero, rotámeros, tautómeros, diaestereómeros, o racematos del mismo. También se proporciona un método para el tratamiento de una enfermedad o condición mediada por CDK9.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US27315409P | 2009-07-30 | 2009-07-30 | |
| US35772010P | 2010-06-23 | 2010-06-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NI201200016A true NI201200016A (es) | 2012-08-15 |
Family
ID=42727614
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NI201200016A NI201200016A (es) | 2009-07-30 | 2012-01-27 | Derivados de piridina y pirazina como moduladores de cinasa de proteína |
Country Status (31)
| Country | Link |
|---|---|
| US (3) | US8415381B2 (es) |
| EP (1) | EP2459535B1 (es) |
| JP (2) | JP5650735B2 (es) |
| KR (1) | KR101464052B1 (es) |
| CN (1) | CN102482218B (es) |
| AR (1) | AR077505A1 (es) |
| AU (1) | AU2010277588B2 (es) |
| BR (1) | BR112012008074A2 (es) |
| CA (1) | CA2767066A1 (es) |
| CL (1) | CL2012000092A1 (es) |
| CO (1) | CO6612188A2 (es) |
| CR (1) | CR20120051A (es) |
| CU (1) | CU24091B1 (es) |
| DO (1) | DOP2012000025A (es) |
| EA (1) | EA023561B1 (es) |
| EC (1) | ECSP12011638A (es) |
| ES (1) | ES2536479T3 (es) |
| GE (1) | GEP20146101B (es) |
| GT (1) | GT201200022A (es) |
| IL (2) | IL217524A0 (es) |
| MA (1) | MA33540B1 (es) |
| MX (1) | MX2012001281A (es) |
| MY (1) | MY183373A (es) |
| NI (1) | NI201200016A (es) |
| NZ (1) | NZ597551A (es) |
| PE (1) | PE20121127A1 (es) |
| SG (1) | SG177660A1 (es) |
| TW (1) | TW201107307A (es) |
| UY (1) | UY32810A (es) |
| WO (1) | WO2011012661A1 (es) |
| ZA (1) | ZA201109166B (es) |
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG173175A1 (en) | 2009-02-05 | 2011-09-29 | Takeda Pharmaceutical | Pyridazinone compounds |
| US8415381B2 (en) * | 2009-07-30 | 2013-04-09 | Novartis Ag | Heteroaryl compounds and their uses |
| US8247436B2 (en) | 2010-03-19 | 2012-08-21 | Novartis Ag | Pyridine and pyrazine derivative for the treatment of CF |
| US20130303507A1 (en) * | 2011-01-28 | 2013-11-14 | Novartis Ag | Substituted hetero-biaryl compounds and their uses |
| WO2012117048A1 (en) | 2011-03-02 | 2012-09-07 | Lead Discovery Center Gmbh | Pharmaceutically active disubstituted triazine derivatives |
| JP5947818B2 (ja) | 2011-03-02 | 2016-07-06 | リード ディスカバリー センター ゲーエムベーハー | 薬学的活性化二置換ピリジン誘導体 |
| EP2699554B1 (en) * | 2011-04-19 | 2016-11-02 | Bayer Intellectual Property GmbH | Substituted 4-aryl-n-phenyl-1,3,5-triazin-2-amines |
| TW201636330A (zh) | 2011-05-24 | 2016-10-16 | 拜耳知識產權公司 | 含有硫醯亞胺基團之4-芳基-n-苯基-1,3,5-三氮雜苯-2-胺 |
| EP2527332A1 (en) | 2011-05-24 | 2012-11-28 | Bayer Intellectual Property GmbH | 4-Aryl-N-phenyl-1,3,5-triazin-2-amines containing a sulfoximine group as CDK9 inhibitors |
| EP2561867A1 (en) | 2011-08-22 | 2013-02-27 | Lead Discovery Center GmbH | CDK9 inhibitors in the treatment of midline carcinoma |
| EP2562265A1 (en) | 2011-08-22 | 2013-02-27 | Lead Discovery Center GmbH | Susceptibility to selective CDK9 inhibitors |
| WO2013037896A1 (en) | 2011-09-16 | 2013-03-21 | Bayer Intellectual Property Gmbh | Disubstituted 5-fluoro-pyrimidines |
| CA2848615C (en) | 2011-09-16 | 2020-02-25 | Bayer Intellectual Property Gmbh | Disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group |
| US9498471B2 (en) | 2011-10-20 | 2016-11-22 | The Regents Of The University Of California | Use of CDK9 inhibitors to reduce cartilage degradation |
| CA2888383A1 (en) | 2012-10-18 | 2014-04-24 | Bayer Pharma Aktiengesellschaft | N-(pyridin-2-yl)pyrimidin-4-amine derivatives containing a sulfone group |
| EP2909176B1 (en) | 2012-10-18 | 2016-07-20 | Bayer Pharma Aktiengesellschaft | 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group |
| US20150259300A1 (en) | 2012-10-18 | 2015-09-17 | Bayer Pharma Aktiengesellschaft | 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amines containing a sulfone group |
| TW201418243A (zh) | 2012-11-15 | 2014-05-16 | Bayer Pharma AG | 含有磺醯亞胺基團之n-(吡啶-2-基)嘧啶-4-胺衍生物 |
| CA2891358C (en) | 2012-11-15 | 2021-05-18 | Bayer Pharma Aktiengesellschaft | 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group |
| CA2917096C (en) | 2013-07-04 | 2021-05-18 | Bayer Pharma Aktiengesellschaft | Sulfoximine substituted 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives and their use as cdk9 kinase inhibitors |
| CA2942119A1 (en) | 2014-03-13 | 2015-09-17 | Bayer Pharma Aktiengesellschaft | 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group |
| CA2944251C (en) | 2014-04-01 | 2022-10-18 | Bayer Pharma Aktiengesellschaft | Disubstituted 5-fluoro pyrimidine derivatives containing a sulfondiimine group |
| JP6605493B2 (ja) | 2014-04-11 | 2019-11-13 | バイエル ファーマ アクチエンゲゼルシャフト | 新規大環状化合物 |
| JO3589B1 (ar) | 2014-08-06 | 2020-07-05 | Novartis Ag | مثبطات كيناز البروتين c وطرق استخداماتها |
| JP6930913B2 (ja) | 2014-10-14 | 2021-09-01 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニアThe Regents Of The University Of California | 炎症を阻害するためのcdk9及びbrd4阻害剤の使用法 |
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| CA2771563A1 (en) * | 2009-09-04 | 2011-03-10 | Novartis Ag | Bipyridines useful for the treatment of proliferative diseases |
| BR112012004836A2 (pt) * | 2009-09-04 | 2019-09-24 | Novartis Ag | pirazinilpiridinas úteis para o tratamento de doenças proliferativas |
| US20130303507A1 (en) * | 2011-01-28 | 2013-11-14 | Novartis Ag | Substituted hetero-biaryl compounds and their uses |
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