EA201290894A1 - Азетидиновые производные пиперидин-4-ила как ингибиторы jak1 - Google Patents
Азетидиновые производные пиперидин-4-ила как ингибиторы jak1Info
- Publication number
- EA201290894A1 EA201290894A1 EA201290894A EA201290894A EA201290894A1 EA 201290894 A1 EA201290894 A1 EA 201290894A1 EA 201290894 A EA201290894 A EA 201290894A EA 201290894 A EA201290894 A EA 201290894A EA 201290894 A1 EA201290894 A1 EA 201290894A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- piperidin
- ila
- azetidine derivatives
- jak1
- jak1 inhibitors
- Prior art date
Links
- 229940116839 Janus kinase 1 inhibitor Drugs 0.000 title 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical class C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 title 1
- 102000002295 Janus Kinase 1 Human genes 0.000 abstract 3
- 108010000837 Janus Kinase 1 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
- 150000001539 azetidines Chemical class 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
Classifications
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- 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
- A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
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- A—HUMAN NECESSITIES
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- 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
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- 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
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- 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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- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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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
- 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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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Physics & Mathematics (AREA)
- Condensed Matter Physics & Semiconductors (AREA)
- Crystallography & Structural Chemistry (AREA)
- General Physics & Mathematics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
В изобретении представлены азетидиновые производные пиперидин-4-ила, а также их композиции и способы их применения, которые модулируют активность Янус-киназы 1 (JAK1) и являются полезными для лечения заболеваний, связанных с активностью JAK1, включая, например, воспалительные нарушения, аутоиммунные нарушения, рак и другие заболевания.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US31258810P | 2010-03-10 | 2010-03-10 | |
US41560210P | 2010-11-19 | 2010-11-19 | |
PCT/US2011/027665 WO2011112662A1 (en) | 2010-03-10 | 2011-03-09 | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201290894A1 true EA201290894A1 (ru) | 2013-04-30 |
EA030376B1 EA030376B1 (ru) | 2018-07-31 |
Family
ID=44065466
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201290894A EA030376B1 (ru) | 2010-03-10 | 2011-03-09 | Азетидиновые производные пиперидин-4-ила как ингибиторы jak1 |
Country Status (38)
Country | Link |
---|---|
US (6) | US8765734B2 (ru) |
EP (6) | EP2545045B1 (ru) |
JP (6) | JP5858484B2 (ru) |
KR (7) | KR102283091B1 (ru) |
CN (1) | CN102985417B (ru) |
AR (1) | AR081315A1 (ru) |
AU (1) | AU2011224484A1 (ru) |
BR (1) | BR112012022513A2 (ru) |
CA (1) | CA2792508C (ru) |
CL (1) | CL2012002501A1 (ru) |
CO (1) | CO6602158A2 (ru) |
CR (1) | CR20120510A (ru) |
CY (2) | CY1120154T1 (ru) |
DK (3) | DK3354652T3 (ru) |
EA (1) | EA030376B1 (ru) |
EC (1) | ECSP12012218A (ru) |
ES (5) | ES2982015T3 (ru) |
HK (2) | HK1177741A1 (ru) |
HR (3) | HRP20160326T1 (ru) |
HU (3) | HUE028723T2 (ru) |
IL (1) | IL221823A (ru) |
LT (2) | LT3050882T (ru) |
ME (2) | ME02386B (ru) |
MX (5) | MX364636B (ru) |
MY (2) | MY175156A (ru) |
NO (1) | NO3050882T3 (ru) |
NZ (1) | NZ602313A (ru) |
PE (1) | PE20130038A1 (ru) |
PH (1) | PH12015502575A1 (ru) |
PL (3) | PL3050882T3 (ru) |
PT (2) | PT3354652T (ru) |
RS (3) | RS60680B1 (ru) |
SG (1) | SG183551A1 (ru) |
SI (3) | SI2545045T1 (ru) |
SM (1) | SMT201600085B (ru) |
TW (6) | TWI592413B (ru) |
WO (1) | WO2011112662A1 (ru) |
ZA (1) | ZA201207420B (ru) |
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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. |
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. |
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TWI484962B (zh) | 2009-05-22 | 2015-05-21 | Incyte Corp | 作為jak抑制劑之3-〔4-(7h-吡咯并〔2,3-d〕嘧啶-4-基)-1h-吡唑-1-基〕辛烷或庚腈 |
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EP2448938B9 (en) | 2009-06-29 | 2015-06-10 | Incyte Corporation | Pyrimidinones as pi3k inhibitors |
WO2011028685A1 (en) | 2009-09-01 | 2011-03-10 | Incyte Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
HUE028723T2 (en) | 2010-03-10 | 2016-12-28 | Incyte Holdings Corp | Piperidin-4-yl azetidine derivatives as JAK-1 inhibitors |
EA035981B1 (ru) | 2010-05-21 | 2020-09-09 | Инсайт Холдингс Корпорейшн | Композиция ингибитора jak для местного применения |
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 |
CA2822070C (en) | 2010-12-20 | 2019-09-17 | Incyte Corporation | N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors |
EA026317B1 (ru) | 2011-02-18 | 2017-03-31 | Новартис Фарма Аг | КОМБИНИРОВАННОЕ ЛЕЧЕНИЕ С ПРИМЕНЕНИЕМ ИНГИБИТОРОВ mTOR/JAK |
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WO2013023119A1 (en) | 2011-08-10 | 2013-02-14 | 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 |
SI2751109T1 (sl) | 2011-09-02 | 2017-03-31 | Incyte Holdings Corporation | Heterociklilamini kot inhibitorji pi3k |
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