NZ598907A - Heterocyclyl pyrazolopyrimidine analogues as jak inhibitors - Google Patents
Heterocyclyl pyrazolopyrimidine analogues as jak inhibitorsInfo
- Publication number
- NZ598907A NZ598907A NZ598907A NZ59890710A NZ598907A NZ 598907 A NZ598907 A NZ 598907A NZ 598907 A NZ598907 A NZ 598907A NZ 59890710 A NZ59890710 A NZ 59890710A NZ 598907 A NZ598907 A NZ 598907A
- Authority
- NZ
- New Zealand
- Prior art keywords
- pyrazolo
- pyrimidin
- methyl
- pyrazol
- ylamino
- Prior art date
Links
- -1 Heterocyclyl pyrazolopyrimidine analogues Chemical class 0.000 title abstract 3
- 229940122245 Janus kinase inhibitor Drugs 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 238000011282 treatment Methods 0.000 abstract 2
- XBKRKCDHJDJSGK-UHFFFAOYSA-N (4-methylpiperazin-1-yl)-[4-[6-[(1-methylpyrazol-4-yl)amino]pyrazolo[3,4-d]pyrimidin-1-yl]phenyl]methanone Chemical compound C1CN(C)CCN1C(=O)C1=CC=C(N2C3=NC(NC4=CN(C)N=C4)=NC=C3C=N2)C=C1 XBKRKCDHJDJSGK-UHFFFAOYSA-N 0.000 abstract 1
- CEKLDWOYICSDNK-UHFFFAOYSA-N 2-[4-[[1-[(2-cyanophenyl)methyl]pyrazolo[3,4-d]pyrimidin-6-yl]amino]pyrazol-1-yl]-n-methylacetamide Chemical compound C1=NN(CC(=O)NC)C=C1NC1=NC=C(C=NN2CC=3C(=CC=CC=3)C#N)C2=N1 CEKLDWOYICSDNK-UHFFFAOYSA-N 0.000 abstract 1
- RKUXEKHGGXNIIR-UHFFFAOYSA-N 2-[[6-[[1-(2-morpholin-4-yl-2-oxoethyl)pyrazol-4-yl]amino]pyrazolo[3,4-d]pyrimidin-1-yl]methyl]benzonitrile Chemical compound C1COCCN1C(=O)CN(N=C1)C=C1NC(N=C12)=NC=C1C=NN2CC1=CC=CC=C1C#N RKUXEKHGGXNIIR-UHFFFAOYSA-N 0.000 abstract 1
- YJHMAOMVUNNQLQ-UHFFFAOYSA-N 4-[[1-[(2-fluorophenyl)methyl]pyrazolo[3,4-d]pyrimidin-6-yl]amino]pyrazole-1-carboxamide Chemical compound C1=NN(C(=O)N)C=C1NC1=NC=C(C=NN2CC=3C(=CC=CC=3)F)C2=N1 YJHMAOMVUNNQLQ-UHFFFAOYSA-N 0.000 abstract 1
- SMXRCJBCWRHDJE-UHFFFAOYSA-N 7-deaza-8-aza-2-aminopurine Chemical class NC1=NC=C2C=NNC2=N1 SMXRCJBCWRHDJE-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- XXTTWEXGGJVIIQ-UHFFFAOYSA-N [2-[[6-[(1-methylpyrazol-4-yl)amino]pyrazolo[3,4-d]pyrimidin-1-yl]methyl]phenyl]methanol Chemical compound C1=NN(C)C=C1NC1=NC=C(C=NN2CC=3C(=CC=CC=3)CO)C2=N1 XXTTWEXGGJVIIQ-UHFFFAOYSA-N 0.000 abstract 1
- 230000000172 allergic effect Effects 0.000 abstract 1
- 208000010668 atopic eczema Diseases 0.000 abstract 1
- 230000001363 autoimmune Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000001900 immune effect Effects 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- GQDGDVHYEFKTGI-UHFFFAOYSA-N n-[2-[[6-[[1-(2,2-difluoroethyl)pyrazol-4-yl]amino]pyrazolo[3,4-d]pyrimidin-1-yl]methyl]phenyl]methanesulfonamide;hydrochloride Chemical compound Cl.CS(=O)(=O)NC1=CC=CC=C1CN1C2=NC(NC3=CN(CC(F)F)N=C3)=NC=C2C=N1 GQDGDVHYEFKTGI-UHFFFAOYSA-N 0.000 abstract 1
- XCUMJBFRPJWHRK-UHFFFAOYSA-N n-[4-[6-[(1-methylpyrazol-4-yl)amino]pyrazolo[3,4-d]pyrimidin-1-yl]phenyl]methanesulfonamide Chemical compound C1=NN(C)C=C1NC1=NC=C(C=NN2C=3C=CC(NS(C)(=O)=O)=CC=3)C2=N1 XCUMJBFRPJWHRK-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- 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
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- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
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- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P7/06—Antianaemics
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Reproductive Health (AREA)
- Neurology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Biomedical Technology (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Transplantation (AREA)
- Gastroenterology & Hepatology (AREA)
- Nutrition Science (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09173535 | 2009-10-20 | ||
| US37535810P | 2010-08-20 | 2010-08-20 | |
| PCT/EP2010/065700 WO2011048082A1 (en) | 2009-10-20 | 2010-10-19 | Heterocyclyl pyrazolopyrimidine analogues as jak inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NZ598907A true NZ598907A (en) | 2014-03-28 |
Family
ID=41531257
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ598907A NZ598907A (en) | 2009-10-20 | 2010-10-19 | Heterocyclyl pyrazolopyrimidine analogues as jak inhibitors |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US9242987B2 (enExample) |
| EP (1) | EP2491039A1 (enExample) |
| JP (1) | JP5744887B2 (enExample) |
| KR (1) | KR20120102601A (enExample) |
| CN (1) | CN102666545B (enExample) |
| AR (1) | AR078675A1 (enExample) |
| AU (1) | AU2010309882B2 (enExample) |
| BR (1) | BR112012009327A2 (enExample) |
| CA (1) | CA2775009A1 (enExample) |
| EA (1) | EA022120B1 (enExample) |
| IL (1) | IL218751A0 (enExample) |
| MX (1) | MX2012004020A (enExample) |
| NZ (1) | NZ598907A (enExample) |
| TW (1) | TW201125867A (enExample) |
| WO (1) | WO2011048082A1 (enExample) |
Families Citing this family (70)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK3184526T3 (en) | 2005-12-13 | 2019-01-14 | Incyte Holdings Corp | PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR |
| EP2740731B1 (en) | 2007-06-13 | 2016-03-23 | Incyte Holdings Corporation | Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| JP5769199B2 (ja) | 2008-10-31 | 2015-08-26 | ジェネンテック， インコーポレイテッド | ピラゾロピリミジンｊａｋ阻害剤化合物と方法 |
| WO2010135621A1 (en) | 2009-05-22 | 2010-11-25 | Incyte Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| PE20120493A1 (es) | 2009-06-29 | 2012-05-20 | Incyte Corp | Pirimidinonas como inhibidores de pi3k |
| UA110324C2 (en) | 2009-07-02 | 2015-12-25 | Genentech Inc | Jak inhibitory compounds based on pyrazolo pyrimidine |
| US8759359B2 (en) | 2009-12-18 | 2014-06-24 | Incyte Corporation | Substituted heteroaryl fused derivatives as PI3K inhibitors |
| SMT201800137T1 (it) | 2010-03-10 | 2018-07-17 | Incyte Holdings Corp | Derivati di piperidin-4-il azetidina come inibitori di jak1 |
| AR081823A1 (es) | 2010-04-14 | 2012-10-24 | Incyte Corp | DERIVADOS FUSIONADOS COMO INHIBIDORES DE PI3Kd |
| PH12012502296B1 (en) | 2010-05-21 | 2017-10-06 | Incyte Holdings Corp | Topical formulation for a jak inhibitor |
| WO2011163195A1 (en) | 2010-06-21 | 2011-12-29 | Incyte Corporation | Fused pyrrole derivatives as pi3k inhibitors |
| JP2013534233A (ja) * | 2010-08-20 | 2013-09-02 | セルゾーム リミティッド | 選択的ｊａｋ阻害剤としてのヘテロシクリルピラゾロピリミジン類似体 |
| BR112013006016A2 (pt) | 2010-09-15 | 2016-06-07 | Hoffmann La Roche | compostos de azabenzotiazol, composições e métodos de uso |
| SG190839A1 (en) | 2010-11-19 | 2013-07-31 | Incyte Corp | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| KR20140009259A (ko) | 2010-11-19 | 2014-01-22 | 에프. 호프만-라 로슈 아게 | 피라졸로피리딘 및 tyk2 억제제로서 이의 용도 |
| ES2764848T3 (es) | 2010-12-20 | 2020-06-04 | Incyte Holdings Corp | N-(1-(fenilo sustituido)etilo)-9H-purina-6-aminas como inhibidores de PI3K |
| WO2012125629A1 (en) | 2011-03-14 | 2012-09-20 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors |
| WO2012135009A1 (en) | 2011-03-25 | 2012-10-04 | Incyte Corporation | Pyrimidine-4,6-diamine derivatives as pi3k inhibitors |
| WO2012143320A1 (en) | 2011-04-18 | 2012-10-26 | Cellzome Limited | (7h-pyrrolo[2,3-d]pyrimidin-2-yl)amine compounds as jak3 inhibitors |
| WO2012177606A1 (en) | 2011-06-20 | 2012-12-27 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| US20140179664A1 (en) | 2011-07-28 | 2014-06-26 | Cellzome Limited | Heterocyclyl Pyrimidine Analogues As JAK Inhibitors |
| WO2013017480A1 (en) | 2011-07-29 | 2013-02-07 | Cellzome Limited | Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors |
| WO2013017479A1 (en) | 2011-07-29 | 2013-02-07 | Cellzome Limited | Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors |
| KR20230038593A (ko) | 2011-09-02 | 2023-03-20 | 인사이트 홀딩스 코포레이션 | Ｐｉ３ｋ 억제제로서 헤테로시클릴아민 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| JP2014531449A (ja) * | 2011-09-20 | 2014-11-27 | セルゾーム リミティッド | キナーゼ阻害剤としてのピラゾロ［４，３―ｃ］ピリジン誘導体 |
| US20150005281A1 (en) | 2011-12-23 | 2015-01-01 | Cellzome Limited | Pyrimidine-2,4-diamine derivatives as kinase inhibitors |
| CN103193600B (zh) * | 2012-01-07 | 2016-04-06 | 浙江九洲药物科技有限公司 | 卡巴拉汀中间体的制备方法 |
| CN104066734B (zh) * | 2012-01-28 | 2017-03-29 | 默克专利股份公司 | 三唑并[4,5‑d]嘧啶衍生物 |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| US9296725B2 (en) | 2012-05-24 | 2016-03-29 | Cellzome Limited | Heterocyclyl pyrimidine analogues as TYK2 inhibitors |
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- 2010-10-19 CA CA2775009A patent/CA2775009A1/en not_active Abandoned
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- 2010-10-19 MX MX2012004020A patent/MX2012004020A/es not_active Application Discontinuation
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| BR112012009327A2 (pt) | 2017-06-06 |
| EA022120B1 (ru) | 2015-11-30 |
| IL218751A0 (en) | 2012-06-28 |
| KR20120102601A (ko) | 2012-09-18 |
| CN102666545A (zh) | 2012-09-12 |
| AR078675A1 (es) | 2011-11-23 |
| US20120252779A1 (en) | 2012-10-04 |
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| AU2010309882A1 (en) | 2012-04-12 |
| CN102666545B (zh) | 2016-04-06 |
| CA2775009A1 (en) | 2011-04-28 |
| MX2012004020A (es) | 2012-05-08 |
| JP2013508332A (ja) | 2013-03-07 |
| WO2011048082A1 (en) | 2011-04-28 |
| EP2491039A1 (en) | 2012-08-29 |
| TW201125867A (en) | 2011-08-01 |
| US9242987B2 (en) | 2016-01-26 |
| EA201270572A1 (ru) | 2012-12-28 |
| AU2010309882B2 (en) | 2016-01-28 |
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