ECSP13012703A - Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak - Google Patents
Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jakInfo
- Publication number
- ECSP13012703A ECSP13012703A ECSP13012703A ECSP13012703A EC SP13012703 A ECSP13012703 A EC SP13012703A EC SP13012703 A ECSP13012703 A EC SP13012703A EC SP13012703 A ECSP13012703 A EC SP13012703A
- Authority
- EC
- Ecuador
- Prior art keywords
- cyclobutyl
- pyrrolopyridine
- derivatives substituted
- jak inhibitors
- pyrrolopyrimidine derivatives
- Prior art date
Links
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 title abstract 2
- XWIYUCRMWCHYJR-UHFFFAOYSA-N 1h-pyrrolo[3,2-b]pyridine Chemical group C1=CC=C2NC=CC2=N1 XWIYUCRMWCHYJR-UHFFFAOYSA-N 0.000 title 1
- 229940122245 Janus kinase inhibitor Drugs 0.000 title 1
- KCTZOTUQSGYWLV-UHFFFAOYSA-N N1C=NC=C2N=CC=C21 Chemical group N1C=NC=C2N=CC=C21 KCTZOTUQSGYWLV-UHFFFAOYSA-N 0.000 title 1
- 102000015617 Janus Kinases Human genes 0.000 abstract 3
- 108010024121 Janus Kinases Proteins 0.000 abstract 3
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 2
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000005255 pyrrolopyridines Chemical class 0.000 abstract 1
- 150000004944 pyrrolopyrimidines 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
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/90—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
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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
- A61K31/495—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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- 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
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Wood Science & Technology (AREA)
- Environmental Sciences (AREA)
- Ophthalmology & Optometry (AREA)
- Pest Control & Pesticides (AREA)
- Zoology (AREA)
- Dentistry (AREA)
- Plant Pathology (AREA)
- Agronomy & Crop Science (AREA)
- Transplantation (AREA)
- Neurosurgery (AREA)
Abstract
La presente invención provee pirrolopirimidinas y pirrolopiridinas sustituidas con ciclobutilo de la fórmula I:en donde X, Y, Z, L, A, R5, n y m se definen con anterioridad, así como sus composiciones y métodos de uso que modulan la actividad de Janus quinasas (JAKs) y son de utilidad en el tratamiento de enfermedades relacionadas con la actividad de JAKs que incluyen, por ejemplo, trastornos inflamatorios, trastornos autoinmunes, cáncer y otras enfermedades.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41570510P | 2010-11-19 | 2010-11-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP13012703A true ECSP13012703A (es) | 2013-08-30 |
Family
ID=45094278
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP13012703 ECSP13012703A (es) | 2010-11-19 | 2013-06-19 | Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US8933085B2 (es) |
| EP (1) | EP2640723A1 (es) |
| JP (1) | JP5917545B2 (es) |
| KR (1) | KR20140019300A (es) |
| CN (1) | CN103415515B (es) |
| AR (1) | AR083933A1 (es) |
| AU (1) | AU2011329734B2 (es) |
| BR (1) | BR112013012502A2 (es) |
| CA (1) | CA2818542A1 (es) |
| CL (1) | CL2013001412A1 (es) |
| CO (1) | CO6761386A2 (es) |
| CR (1) | CR20130280A (es) |
| EA (1) | EA026201B1 (es) |
| EC (1) | ECSP13012703A (es) |
| IL (1) | IL226407A (es) |
| MX (1) | MX344478B (es) |
| NZ (1) | NZ611151A (es) |
| PE (1) | PE20140146A1 (es) |
| PH (1) | PH12013501001A1 (es) |
| SG (1) | SG190839A1 (es) |
| TW (1) | TW201249845A (es) |
| UA (1) | UA113156C2 (es) |
| WO (1) | WO2012068450A1 (es) |
Families Citing this family (116)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103214484B (zh) | 2005-12-13 | 2016-07-06 | 因塞特控股公司 | 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶 |
| 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. |
| HUE029236T2 (en) | 2007-06-13 | 2017-02-28 | Incyte Holdings Corp | (R) -3- (4- (7H-Pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl) -3-cyclopentylpropanenitrile Crystalline salts of Janus kinase inhibitor |
| PE20211639A1 (es) | 2009-01-15 | 2021-08-24 | Incyte Holdings Corp | Procesos para preparar inhibidores de jak y compuestos intermediarios relacionado |
| MY156727A (en) * | 2009-05-22 | 2016-03-15 | 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 |
| EP2432472B1 (en) | 2009-05-22 | 2019-10-02 | Incyte Holdings Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| EP2845856A1 (en) | 2009-06-29 | 2015-03-11 | Incyte Corporation | Pyrimidinones as PI3K inhibitors |
| TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| EP3354652B1 (en) * | 2010-03-10 | 2020-05-06 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| AR084691A1 (es) | 2010-05-21 | 2013-06-05 | Incyte Corp | Formulacion de uso topico para un inhibidor de jak y metodo para tratar trastorno de la piel |
| WO2012068440A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
| CA2818542A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| TW201249844A (en) | 2010-12-20 | 2012-12-16 | Incyte Corp | N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors |
| WO2012112847A1 (en) | 2011-02-18 | 2012-08-23 | Novartis Pharma Ag | mTOR/JAK INHIBITOR COMBINATION THERAPY |
| MY165963A (en) | 2011-06-20 | 2018-05-18 | Incyte Holdings Corp | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| 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 |
| AU2012300567B2 (en) * | 2011-09-02 | 2016-03-10 | Purdue Pharma L.P. | Pyrimidines as sodium channel blockers |
| UA121539C2 (uk) | 2011-09-02 | 2020-06-25 | Інсайт Холдинґс Корпорейшн | Гетероцикліламіни як інгібітори рі3к |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| 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 |
| JP6359546B2 (ja) | 2012-11-01 | 2018-07-18 | 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阻害薬としての三環式縮合チオフェン誘導体 |
| TWI761825B (zh) | 2012-11-15 | 2022-04-21 | 美商英塞特控股公司 | 盧梭利替尼之緩釋性劑型 |
| RU2654486C2 (ru) * | 2012-11-16 | 2018-05-21 | Ф. Хоффманн-Ля Рош Аг | Способ получения 2-трифторметилизоникотиновой кислоты и ее эфиров |
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-
2011
- 2011-11-18 CA CA2818542A patent/CA2818542A1/en not_active Abandoned
- 2011-11-18 KR KR1020137015801A patent/KR20140019300A/ko not_active Ceased
- 2011-11-18 UA UAA201307763A patent/UA113156C2/uk unknown
- 2011-11-18 TW TW100142377A patent/TW201249845A/zh unknown
- 2011-11-18 CN CN201180065119.1A patent/CN103415515B/zh not_active Expired - Fee Related
- 2011-11-18 PH PH1/2013/501001A patent/PH12013501001A1/en unknown
- 2011-11-18 EA EA201390736A patent/EA026201B1/ru not_active IP Right Cessation
- 2011-11-18 PE PE2013001220A patent/PE20140146A1/es not_active Application Discontinuation
- 2011-11-18 US US13/300,094 patent/US8933085B2/en active Active
- 2011-11-18 AR ARP110104324A patent/AR083933A1/es not_active Application Discontinuation
- 2011-11-18 WO PCT/US2011/061374 patent/WO2012068450A1/en not_active Ceased
- 2011-11-18 EP EP11791155.2A patent/EP2640723A1/en not_active Withdrawn
- 2011-11-18 JP JP2013540049A patent/JP5917545B2/ja active Active
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- 2011-11-18 SG SG2013038740A patent/SG190839A1/en unknown
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- 2013-05-31 CO CO13134023A patent/CO6761386A2/es unknown
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| TW201249845A (en) | 2012-12-16 |
| CL2013001412A1 (es) | 2013-12-20 |
| WO2012068450A1 (en) | 2012-05-24 |
| IL226407A (en) | 2017-04-30 |
| JP5917545B2 (ja) | 2016-05-18 |
| MX344478B (es) | 2016-12-16 |
| JP2014500260A (ja) | 2014-01-09 |
| MX2013005603A (es) | 2013-06-13 |
| IL226407A0 (en) | 2013-07-31 |
| EA026201B1 (ru) | 2017-03-31 |
| US20120149681A1 (en) | 2012-06-14 |
| CO6761386A2 (es) | 2013-09-30 |
| US20150087632A1 (en) | 2015-03-26 |
| EA201390736A1 (ru) | 2013-11-29 |
| KR20140019300A (ko) | 2014-02-14 |
| PE20140146A1 (es) | 2014-02-06 |
| CA2818542A1 (en) | 2012-05-24 |
| CN103415515A (zh) | 2013-11-27 |
| AR083933A1 (es) | 2013-04-10 |
| EP2640723A1 (en) | 2013-09-25 |
| US8933085B2 (en) | 2015-01-13 |
| US20190135813A1 (en) | 2019-05-09 |
| PH12013501001A1 (en) | 2019-09-02 |
| AU2011329734B2 (en) | 2015-05-28 |
| NZ611151A (en) | 2015-06-26 |
| AU2011329734A1 (en) | 2013-05-02 |
| CR20130280A (es) | 2013-08-09 |
| UA113156C2 (xx) | 2016-12-26 |
| BR112013012502A2 (pt) | 2019-03-06 |
| US10640506B2 (en) | 2020-05-05 |
| CN103415515B (zh) | 2015-08-26 |
| SG190839A1 (en) | 2013-07-31 |
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