AR078321A1 - Derivados de 2,4'-bipiridina como inhibidores de cinasa (cdk9) - Google Patents
Derivados de 2,4'-bipiridina como inhibidores de cinasa (cdk9)Info
- Publication number
- AR078321A1 AR078321A1 ARP100103239A ARP100103239A AR078321A1 AR 078321 A1 AR078321 A1 AR 078321A1 AR P100103239 A ARP100103239 A AR P100103239A AR P100103239 A ARP100103239 A AR P100103239A AR 078321 A1 AR078321 A1 AR 078321A1
- Authority
- AR
- Argentina
- Prior art keywords
- carbon atoms
- alkyl
- haloalkyl
- hydrogen
- cycloalkyl
- Prior art date
Links
- 102100024457 Cyclin-dependent kinase 9 Human genes 0.000 title 1
- 101000980930 Homo sapiens Cyclin-dependent kinase 9 Proteins 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 37
- 125000000217 alkyl group Chemical group 0.000 abstract 12
- 229910052739 hydrogen Inorganic materials 0.000 abstract 8
- 239000001257 hydrogen Substances 0.000 abstract 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 8
- 125000001188 haloalkyl group Chemical group 0.000 abstract 6
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 150000002367 halogens Chemical class 0.000 abstract 6
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 125000005347 halocycloalkyl group Chemical group 0.000 abstract 3
- 229940126074 CDK kinase inhibitor Drugs 0.000 abstract 2
- 102100034770 Cyclin-dependent kinase inhibitor 3 Human genes 0.000 abstract 2
- 101000945639 Homo sapiens Cyclin-dependent kinase inhibitor 3 Proteins 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000002875 cyclin dependent kinase inhibitor Substances 0.000 abstract 2
- 229940043378 cyclin-dependent kinase inhibitor Drugs 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 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
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 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
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- 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
- 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Neurosurgery (AREA)
- Virology (AREA)
- Psychiatry (AREA)
- Obesity (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Transplantation (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Communicable Diseases (AREA)
- Vascular Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
También se proporciona un compuesto de la formula 1 para el tratamiento de una enfermedad o condicion mediada por un inhibidor de la cinasa dependiente de ciclina (CDK). Reivindicacion 1: Un compuesto de la formula 1 o una sal farmacéuticamente aceptable del mismo, en donde: R1 se selecciona a partir de -(CH2)0-2-heteroarilo, -(CH2)0-2-arilo, alquilo de 1 a 8 átomos de carbono, alquilo de 1 a 8 átomos de carbono ramificado, cicloalquilo de 1 a 8 átomos de carbono, y un grupo hetero-cicloalquilo de 4 a 8 miembros, en donde los grupos están cada uno opcionalmente sustituidos independientemente; R2 se selecciona a partir de hidrogeno, alcoxilo de 1 a 4 átomos de carbono, haloalquilo de 1 a 4 átomos de carbono, alquilo de 1 a 4 átomos de carbono, y halogeno; A1 es N; A4 es CR6; R4 se selecciona a partir de hidrogeno, halogeno, heterociclilo-R14 de 5 a 7 miembros, y A6-L-R9; R5 se selecciona a partir de hidrogeno, alquilo de 1 a 4 átomos de carbono, haloalquilo de 1 a 4 átomos de carbono, hidroxilo, CN, -O-alquilo de 1 a 4 átomos de carbono, -O-haloalquilo de 1 a 4 átomos de carbono, cicloalquilo de 3 a 4 átomos de carbono, halo-cicloalquilo de 3 a 4 átomos de carbono, y halogeno; R6 se selecciona a partir de hidrogeno, alquilo de 1 a 4 átomos de carbono, haloalquilo de 1 a 4 átomos de carbono, CN, -O- alquilo de 1 a 4 átomos de carbono, cicloalquilo de 3 a 4 átomos de carbono, halo-cicloalquilo de 3 a 4 átomos de carbono, -O-haloalquilo de 1 a 4 átomos de carbono, y halogeno; R7 se selecciona a partir de hidrogeno, alquilo de 1 a 4 átomos de carbono, haloalquilo de 1 a 4 átomos de carbono, O-alquilo de 1 a 3 átomos de carbono, y halogeno; A6 se selecciona a partir de O, SO2, y NR8; L se selecciona a partir de alquileno de 0 a 3 átomos de carbono, -CHD-, -CD2-, cicloalquilo de 3 a 6 átomos de carbono, halo-cicloalquilo de 3 a 6 átomos de carbono, hetero-cicloalquilo de 4 a 7 átomos de carbono, alquileno de 3 a 8 átomos de carbono ramificado, halo-alquileno de 3 a 8 átomos de carbono ramificado; R8 se selecciona a partir de hidrogeno, alquilo de 1 a 4 átomos de carbono, y alquilo de 3 a 8 átomos de carbono ramificado, y haloalquilo de 3 a 8 átomos de carbono ramificado; R9 se selecciona a partir de hidrogeno, alquilo de 1 a 6 átomos de carbono, cicloalquilo de 1 a 8 átomos de carbono, alquilo de 1 a 8 átomos de carbono ramificado, -(CH2)0-2-heteroarilo, (CH2)0-2-heterociclo-alquilo de 4 a 8 miembros, y (CH2)0-2-arilo, en donde los grupos están opcionalmente sustituidos; y R14 se selecciona a partir de hidrogeno, fenilo, halogeno, hidroxilo, alquilo de 1 a 4 átomos de carbono, alquilo de 3 a 6 átomos de carbono ramificado, haloalquilo de 1 a 4 átomos de carbono, CF3, =O, y O-alquilo de 1 a 4 átomos de carbono.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US27593809P | 2009-09-04 | 2009-09-04 | |
| US28496109P | 2009-12-28 | 2009-12-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR078321A1 true AR078321A1 (es) | 2011-11-02 |
Family
ID=43478200
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100103239A AR078321A1 (es) | 2009-09-04 | 2010-09-03 | Derivados de 2,4'-bipiridina como inhibidores de cinasa (cdk9) |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20110130380A1 (es) |
| EP (1) | EP2473499A1 (es) |
| KR (1) | KR20120092586A (es) |
| CN (1) | CN102471310A (es) |
| AR (1) | AR078321A1 (es) |
| AU (1) | AU2010291206A1 (es) |
| CA (1) | CA2771563A1 (es) |
| MX (1) | MX2012002761A (es) |
| TW (1) | TW201113273A (es) |
| UY (1) | UY32877A (es) |
| WO (1) | WO2011026911A1 (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8415381B2 (en) * | 2009-07-30 | 2013-04-09 | Novartis Ag | Heteroaryl compounds and their uses |
| EP2668162A1 (en) * | 2011-01-28 | 2013-12-04 | Novartis AG | Substituted bi-heteroaryl compounds as cdk9 inhibitors and their uses |
| WO2012101064A1 (en) * | 2011-01-28 | 2012-08-02 | Novartis Ag | N-acyl pyrimidine biaryl compounds as protein kinase inhibitors |
| US9242969B2 (en) | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
| EP3094326A4 (en) | 2014-01-14 | 2017-07-26 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| MX2016009135A (es) | 2014-01-14 | 2016-10-05 | Millennium Pharm Inc | Heteroarilos y usos de estos. |
| UY36294A (es) | 2014-09-12 | 2016-04-29 | Novartis Ag | Compuestos y composiciones como inhibidores de quinasa |
| ES2974991T3 (es) | 2016-09-19 | 2024-07-02 | Novartis Ag | Combinaciones terapéuticas que comprenden un inhibidor de RAF y un inhibidor de ERK |
| WO2018073687A1 (en) | 2016-10-20 | 2018-04-26 | Pfizer Inc. | Anti-proliferative agents for treating pah |
| FI3618875T3 (fi) | 2017-05-02 | 2023-07-04 | Novartis Ag | Raf-inhibiittoria ja trametinibia käsittävä yhdistelmähoito |
| MX2021013817A (es) | 2019-05-13 | 2021-12-14 | Novartis Ag | Nuevas formas cristalinas de n-(3-(2-(2-hidroxietoxi)-6-morfolinop iridin-4-il)-4-metilfenil)-2-(trifluorometil)isonicotinamida como inhibidores de raf para el tratamiento del cancer. |
| KR20220113773A (ko) * | 2019-12-09 | 2022-08-16 | 씨에스피씨 종콰이 팔마씨우티컬 테크놀로지 (스자좡) 컴퍼니 리미티드 | 사이클린 의존성 키나아제 9 억제제로서의 화합물 및 그의 용도 |
| WO2022247785A1 (zh) * | 2021-05-24 | 2022-12-01 | 石药集团中奇制药技术（石家庄）有限公司 | 一种周期蛋白依赖性激酶9抑制剂的用途 |
| CN115381824B (zh) * | 2021-05-24 | 2024-11-05 | 石药集团中奇制药技术（石家庄）有限公司 | 周期蛋白依赖性激酶9抑制剂的用途 |
| CN115448874B (zh) * | 2021-06-09 | 2024-11-01 | 石药集团中奇制药技术（石家庄）有限公司 | 固体形式的周期蛋白依赖性激酶9抑制剂及其用途 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT72878B (en) | 1980-04-24 | 1983-03-29 | Merck & Co Inc | Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents |
| EP1631260A2 (en) | 2003-02-28 | 2006-03-08 | Transform Pharmaceuticals, Inc. | Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen |
| WO2005040152A1 (en) * | 2003-10-20 | 2005-05-06 | E.I. Dupont De Nemours And Company | Heteroyclylphenyl-and heterocyclylpyridyl-substituted azolecarboxamides as herbicides |
| AU2007336933A1 (en) * | 2006-12-22 | 2008-07-03 | Novartis Ag | Heteroaryl-heteroaryl compounds as CDK inhibitors for the treatment of cancer, inflammation and viral infections |
-
2010
- 2010-09-02 WO PCT/EP2010/062893 patent/WO2011026911A1/en not_active Ceased
- 2010-09-02 US US12/874,389 patent/US20110130380A1/en not_active Abandoned
- 2010-09-02 EP EP10750114A patent/EP2473499A1/en not_active Withdrawn
- 2010-09-02 KR KR1020127008620A patent/KR20120092586A/ko not_active Withdrawn
- 2010-09-02 CN CN2010800367237A patent/CN102471310A/zh active Pending
- 2010-09-02 AU AU2010291206A patent/AU2010291206A1/en not_active Abandoned
- 2010-09-02 CA CA2771563A patent/CA2771563A1/en not_active Abandoned
- 2010-09-02 MX MX2012002761A patent/MX2012002761A/es not_active Application Discontinuation
- 2010-09-03 UY UY0001032877A patent/UY32877A/es not_active Application Discontinuation
- 2010-09-03 AR ARP100103239A patent/AR078321A1/es unknown
- 2010-09-03 TW TW099129948A patent/TW201113273A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2011026911A8 (en) | 2011-04-21 |
| AU2010291206A1 (en) | 2012-02-23 |
| EP2473499A1 (en) | 2012-07-11 |
| WO2011026911A1 (en) | 2011-03-10 |
| TW201113273A (en) | 2011-04-16 |
| CN102471310A (zh) | 2012-05-23 |
| US20110130380A1 (en) | 2011-06-02 |
| KR20120092586A (ko) | 2012-08-21 |
| MX2012002761A (es) | 2012-04-19 |
| UY32877A (es) | 2011-04-29 |
| CA2771563A1 (en) | 2011-03-10 |
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