CR20110620A - Derivados de n-(hetero)aril-pirrolidina de pirazo-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como ihnibidores de la quinasa janus - Google Patents
Derivados de n-(hetero)aril-pirrolidina de pirazo-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como ihnibidores de la quinasa janusInfo
- Publication number
- CR20110620A CR20110620A CR20110620A CR20110620A CR20110620A CR 20110620 A CR20110620 A CR 20110620A CR 20110620 A CR20110620 A CR 20110620A CR 20110620 A CR20110620 A CR 20110620A CR 20110620 A CR20110620 A CR 20110620A
- Authority
- CR
- Costa Rica
- Prior art keywords
- pirrolo
- hetero
- derivatives
- pirimidines
- ihnibitors
- Prior art date
Links
- 102000015617 Janus Kinases Human genes 0.000 title 1
- 108010024121 Janus Kinases Proteins 0.000 title 1
- 150000003230 pyrimidines Chemical class 0.000 title 1
- 102000042838 JAK family Human genes 0.000 abstract 1
- 108091082332 JAK family Proteins 0.000 abstract 1
- 229940116839 Janus kinase 1 inhibitor Drugs 0.000 abstract 1
- 229940122245 Janus kinase inhibitor Drugs 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000005842 heteroatom Chemical group 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
- A61K31/495—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
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- A—HUMAN NECESSITIES
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- 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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Pulmonology (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La presente invención se relaciona con derivados de N-(hetero)aril-pirrolidina de fórmula (I); que son inhibidores de JAK, tal como inhibidores selectivos de JAK1, útiles en el tratamiento de enfermedades asociadas con JAK.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US18062209P | 2009-05-22 | 2009-05-22 | |
| US22509209P | 2009-07-13 | 2009-07-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CR20110620A true CR20110620A (es) | 2012-02-02 |
Family
ID=42543342
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20110620A CR20110620A (es) | 2009-05-22 | 2011-11-24 | Derivados de n-(hetero)aril-pirrolidina de pirazo-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como ihnibidores de la quinasa janus |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US8716303B2 (es) |
| EP (1) | EP2432555B1 (es) |
| JP (1) | JP5775070B2 (es) |
| KR (1) | KR101771401B1 (es) |
| CN (1) | CN102458581B (es) |
| AR (1) | AR076794A1 (es) |
| AU (1) | AU2010249380B2 (es) |
| BR (1) | BRPI1012159B1 (es) |
| CA (1) | CA2762174C (es) |
| CL (1) | CL2011002956A1 (es) |
| CO (1) | CO6440524A2 (es) |
| CR (1) | CR20110620A (es) |
| EA (1) | EA025520B1 (es) |
| ES (1) | ES2487542T3 (es) |
| IL (1) | IL216463A (es) |
| MX (1) | MX2011012353A (es) |
| MY (1) | MY156727A (es) |
| NZ (1) | NZ596479A (es) |
| SG (1) | SG176130A1 (es) |
| TW (1) | TW201100429A (es) |
| WO (1) | WO2010135650A1 (es) |
| ZA (1) | ZA201108544B (es) |
Families Citing this family (112)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE025173T2 (hu) | 2005-12-13 | 2016-01-28 | Incyte Corp | Heteroaril-szubsztituált pirrollo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok |
| EP3070090B1 (en) | 2007-06-13 | 2018-12-12 | Incyte Holdings Corporation | Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile |
| CL2008001709A1 (es) | 2007-06-13 | 2008-11-03 | Incyte Corp | Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras. |
| KR101580482B1 (ko) * | 2007-11-16 | 2015-12-28 | 인사이트 홀딩스 코포레이션 | 야누스 키나제 억제제로서의 4-피라졸릴-n-아릴피리미딘-2-아민 및 4-피라졸릴-n-헤테로아릴피리미딘-2-아민 |
| CL2009001884A1 (es) * | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco. |
| JOP20190230A1 (ar) | 2009-01-15 | 2017-06-16 | Incyte Corp | طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به |
| LT2432472T (lt) | 2009-05-22 | 2020-02-10 | Incyte Holdings Corporation | 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- arba heptan-nitrilas, kaip jak inhibitoriai |
| TW201100429A (en) | 2009-05-22 | 2011-01-01 | Incyte Corp | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| DK2448938T5 (en) | 2009-06-29 | 2015-10-05 | Incyte Corp | Pyrimidinones AS PI3K inhibitors |
| TWI466885B (zh) | 2009-07-31 | 2015-01-01 | Japan Tobacco Inc | 含氮螺環化合物及其醫藥用途 |
| AR078012A1 (es) * | 2009-09-01 | 2011-10-05 | Incyte Corp | Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus |
| US8486902B2 (en) | 2009-10-09 | 2013-07-16 | Incyte Corporation | Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d] pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| WO2011103423A1 (en) * | 2010-02-18 | 2011-08-25 | Incyte Corporation | Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors |
| CA2792508C (en) | 2010-03-10 | 2018-01-16 | Incyte Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| TWI499421B (zh) | 2010-05-21 | 2015-09-11 | Incyte Corp | Jak抑制劑的局部製劑 |
| AU2011329734B2 (en) | 2010-11-19 | 2015-05-28 | Incyte Holdings Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
| JP5917544B2 (ja) | 2010-11-19 | 2016-05-18 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Jak阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン |
| SG190957A1 (en) * | 2010-12-01 | 2013-07-31 | Nissan Chemical Ind Ltd | Pyrazole compounds having therapeutic effect on multiple myeloma |
| AR084366A1 (es) | 2010-12-20 | 2013-05-08 | Incyte Corp | N-(1-(fenil sustituido)etil)-9h-purin-6-aminas como inhibidores de pi3k |
| KR102024948B1 (ko) | 2011-02-18 | 2019-11-04 | 노파르티스 파르마 아게 | mTOR/JAK 저해제 병용 요법 |
| ES2560611T3 (es) | 2011-06-20 | 2016-02-22 | Incyte Holdings Corporation | Derivados de fenil de azetidinilo, carboxamida de piridilo o pirazinilo como inhibidores de JAK |
| CA2844507A1 (en) | 2011-08-10 | 2013-02-14 | Novartis Pharma Ag | Jak pi3k/mtor combination therapy |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為jak抑制劑之環己基氮雜環丁烷衍生物 |
| HRP20170285T1 (hr) | 2011-09-02 | 2017-04-21 | Incyte Holdings Corporation | Heterociklilamini kao inhibitori pi3k |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| JP6014148B2 (ja) * | 2011-09-22 | 2016-10-25 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | ヤヌスキナーゼ阻害剤としてのシクロアルキルニトリルピラゾールカルボキサミド |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| TW201406761A (zh) | 2012-05-18 | 2014-02-16 | Incyte Corp | 做爲jak抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物 |
| UA117572C2 (uk) | 2012-11-01 | 2018-08-27 | Інсайт Холдинґс Корпорейшн | Трициклічні конденсовані похідні тіофену як інгібітори jak |
| SG10202111768XA (en) | 2012-11-15 | 2021-11-29 | Incyte Holdings Corp | Sustained-release dosage forms of ruxolitinib |
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| PE20200298A1 (es) | 2013-03-06 | 2020-02-06 | Incyte Holdings Corp | Procesos e intermedios para hacer un inhibidor de jak |
| PL2986594T3 (pl) | 2013-04-15 | 2017-10-31 | Fmc Corp | Amidy grzybobójcze |
| HUE043573T2 (hu) | 2013-05-17 | 2019-08-28 | Incyte Corp | Bipirazol só, amely JAK-gátlóként alkalmazható |
| CN114010611B (zh) | 2013-08-07 | 2023-11-28 | 因赛特控股公司 | Jak1抑制剂的持续释放剂型 |
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-
2010
- 2010-05-21 TW TW099116419A patent/TW201100429A/zh unknown
- 2010-05-21 SG SG2011084860A patent/SG176130A1/en unknown
- 2010-05-21 CA CA2762174A patent/CA2762174C/en active Active
- 2010-05-21 CN CN201080033308.6A patent/CN102458581B/zh active Active
- 2010-05-21 MY MYPI2011005626A patent/MY156727A/en unknown
- 2010-05-21 JP JP2012512060A patent/JP5775070B2/ja active Active
- 2010-05-21 KR KR1020117030795A patent/KR101771401B1/ko active Active
- 2010-05-21 AU AU2010249380A patent/AU2010249380B2/en not_active Ceased
- 2010-05-21 ES ES10720113.9T patent/ES2487542T3/es active Active
- 2010-05-21 EA EA201171454A patent/EA025520B1/ru unknown
- 2010-05-21 AR ARP100101791A patent/AR076794A1/es not_active Application Discontinuation
- 2010-05-21 NZ NZ596479A patent/NZ596479A/en not_active IP Right Cessation
- 2010-05-21 BR BRPI1012159-5A patent/BRPI1012159B1/pt active IP Right Grant
- 2010-05-21 EP EP10720113.9A patent/EP2432555B1/en active Active
- 2010-05-21 US US12/784,916 patent/US8716303B2/en active Active
- 2010-05-21 WO PCT/US2010/035783 patent/WO2010135650A1/en not_active Ceased
- 2010-05-21 MX MX2011012353A patent/MX2011012353A/es active IP Right Grant
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- 2011-11-21 ZA ZA2011/08544A patent/ZA201108544B/en unknown
- 2011-11-22 CL CL2011002956A patent/CL2011002956A1/es unknown
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- 2011-12-09 CO CO11169876A patent/CO6440524A2/es active IP Right Grant
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2014
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| ZA201108544B (en) | 2013-04-24 |
| CN102458581A (zh) | 2012-05-16 |
| TW201100429A (en) | 2011-01-01 |
| EP2432555A1 (en) | 2012-03-28 |
| US9334274B2 (en) | 2016-05-10 |
| MX2011012353A (es) | 2011-12-14 |
| EP2432555B1 (en) | 2014-04-30 |
| US20140221379A1 (en) | 2014-08-07 |
| CA2762174C (en) | 2018-02-20 |
| ES2487542T3 (es) | 2014-08-21 |
| WO2010135650A1 (en) | 2010-11-25 |
| BRPI1012159B1 (pt) | 2022-01-25 |
| KR101771401B1 (ko) | 2017-08-25 |
| CA2762174A1 (en) | 2010-11-25 |
| AR076794A1 (es) | 2011-07-06 |
| CN102458581B (zh) | 2016-03-30 |
| SG176130A1 (en) | 2011-12-29 |
| JP2012527483A (ja) | 2012-11-08 |
| KR20120034665A (ko) | 2012-04-12 |
| AU2010249380B2 (en) | 2015-08-20 |
| JP5775070B2 (ja) | 2015-09-09 |
| NZ596479A (en) | 2014-01-31 |
| US8716303B2 (en) | 2014-05-06 |
| CL2011002956A1 (es) | 2012-05-25 |
| IL216463A0 (en) | 2012-02-29 |
| US20100298334A1 (en) | 2010-11-25 |
| EA201171454A1 (ru) | 2012-06-29 |
| EA025520B1 (ru) | 2017-01-30 |
| MY156727A (en) | 2016-03-15 |
| CO6440524A2 (es) | 2012-05-15 |
| IL216463A (en) | 2017-09-28 |
| AU2010249380A1 (en) | 2011-12-08 |
| BRPI1012159A2 (pt) | 2020-09-15 |
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