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)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Environmental Sciences (AREA)
- Dentistry (AREA)
- Plant Pathology (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Agronomy & Crop Science (AREA)
- Pest Control & Pesticides (AREA)
- Ophthalmology & Optometry (AREA)
- Emergency Medicine (AREA)
- Gastroenterology & Hepatology (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 |
|---|---|---|---|---|
| SG10202003901UA (en) | 2005-12-13 | 2020-05-28 | Incyte Holdings Corp | Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors |
| KR20150036210A (ko) | 2007-06-13 | 2015-04-07 | 인사이트 코포레이션 | 야누스 키나제 억제제(R)―3―(4―(7H―피롤로[2,3-d]피리미딘―4―일)―1H―피라졸―1―일)―3―사이클로펜틸프로판니트릴의 염 |
| 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. |
| TWI720517B (zh) | 2009-01-15 | 2021-03-01 | 美商英塞特公司 | 製造jak抑制劑之方法及相關中間化合物 |
| AR076794A1 (es) | 2009-05-22 | 2011-07-06 | Incyte Corp | Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen |
| SI2432472T1 (sl) * | 2009-05-22 | 2019-11-29 | Incyte Holdings Corp | 3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK |
| KR101763656B1 (ko) | 2009-06-29 | 2017-08-01 | 인사이트 홀딩스 코포레이션 | Pi3k 저해물질로서의 피리미디논 |
| 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 |
| PE20130216A1 (es) | 2010-05-21 | 2013-02-27 | Incyte Corp | Formulacion topica para un inhibidor de jak |
| US9034884B2 (en) | 2010-11-19 | 2015-05-19 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors |
| PE20140146A1 (es) | 2010-11-19 | 2014-02-06 | Incyte Corp | Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak |
| EP3660016A1 (en) | 2010-12-20 | 2020-06-03 | Incyte Holdings Corporation | N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors |
| ES2547916T3 (es) | 2011-02-18 | 2015-10-09 | Novartis Pharma Ag | Terapia de combinación de inhibidores de mTOR/JAK |
| CN103797010B (zh) | 2011-06-20 | 2016-02-24 | 因塞特控股公司 | 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物 |
| EP2741747A1 (en) | 2011-08-10 | 2014-06-18 | Novartis Pharma AG | JAK P13K/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 |
| PT3513793T (pt) | 2011-09-02 | 2021-05-10 | Incyte Holdings Corp | Heterociclilaminas como inibidores de pi3k |
| EP3255041A1 (en) * | 2011-09-02 | 2017-12-13 | Purdue Pharma L.P. | Pyrimidines as sodium channel blockers |
| 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 |
| TWI646099B (zh) | 2012-11-01 | 2019-01-01 | 英塞特控股公司 | 作爲jak抑制劑之三環稠合噻吩衍生物 |
| PH12020551186B1 (en) | 2012-11-15 | 2024-03-20 | Incyte Holdings Corp | Sustained-release dosage forms of ruxolitinib |
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-
2011
- 2011-11-18 PE PE2013001220A patent/PE20140146A1/es not_active Application Discontinuation
- 2011-11-18 EP EP11791155.2A patent/EP2640723A1/en not_active Withdrawn
- 2011-11-18 CN CN201180065119.1A patent/CN103415515B/zh not_active Expired - Fee Related
- 2011-11-18 AU AU2011329734A patent/AU2011329734B2/en not_active Ceased
- 2011-11-18 SG SG2013038740A patent/SG190839A1/en unknown
- 2011-11-18 KR KR1020137015801A patent/KR20140019300A/ko not_active Ceased
- 2011-11-18 WO PCT/US2011/061374 patent/WO2012068450A1/en not_active Ceased
- 2011-11-18 PH PH1/2013/501001A patent/PH12013501001A1/en unknown
- 2011-11-18 AR ARP110104324A patent/AR083933A1/es not_active Application Discontinuation
- 2011-11-18 UA UAA201307763A patent/UA113156C2/uk unknown
- 2011-11-18 CA CA2818542A patent/CA2818542A1/en not_active Abandoned
- 2011-11-18 MX MX2013005603A patent/MX344478B/es active IP Right Grant
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- 2011-11-18 BR BR112013012502-0A patent/BR112013012502A2/pt not_active IP Right Cessation
- 2011-11-18 US US13/300,094 patent/US8933085B2/en active Active
- 2011-11-18 JP JP2013540049A patent/JP5917545B2/ja active Active
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- 2013-05-17 CL CL2013001412A patent/CL2013001412A1/es unknown
- 2013-05-31 CO CO13134023A patent/CO6761386A2/es unknown
- 2013-06-10 CR CR20130280A patent/CR20130280A/es unknown
- 2013-06-19 EC ECSP13012703 patent/ECSP13012703A/es unknown
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2014
- 2014-12-01 US US14/556,775 patent/US20150087632A1/en not_active Abandoned
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| AU2011329734A1 (en) | 2013-05-02 |
| CR20130280A (es) | 2013-08-09 |
| US20150087632A1 (en) | 2015-03-26 |
| US20120149681A1 (en) | 2012-06-14 |
| TW201249845A (en) | 2012-12-16 |
| MX2013005603A (es) | 2013-06-13 |
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| CN103415515B (zh) | 2015-08-26 |
| JP2014500260A (ja) | 2014-01-09 |
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| CA2818542A1 (en) | 2012-05-24 |
| CN103415515A (zh) | 2013-11-27 |
| PH12013501001A1 (en) | 2019-09-02 |
| US20190135813A1 (en) | 2019-05-09 |
| NZ611151A (en) | 2015-06-26 |
| CO6761386A2 (es) | 2013-09-30 |
| SG190839A1 (en) | 2013-07-31 |
| AU2011329734B2 (en) | 2015-05-28 |
| US10640506B2 (en) | 2020-05-05 |
| EA026201B1 (ru) | 2017-03-31 |
| IL226407A0 (en) | 2013-07-31 |
| BR112013012502A2 (pt) | 2019-03-06 |
| JP5917545B2 (ja) | 2016-05-18 |
| WO2012068450A1 (en) | 2012-05-24 |
| MX344478B (es) | 2016-12-16 |
| EA201390736A1 (ru) | 2013-11-29 |
| UA113156C2 (xx) | 2016-12-26 |
| US8933085B2 (en) | 2015-01-13 |
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