CL2012002501A1 - Compuestos derivados de 4-(1-(1-(piperidin-4-il)azetidin-3-il)-h-pirazol-4-il)-(1h-pirrolo[2,3-b]piridina o pirimidina); forma cristalina; composicion farmaceutica; util para el tratamiento de una enfermedad autoinmune, cancer, trastorno mieloproliferativo, enfermedad inflamatoria, de resorcion osea o rechazo al trasplante. - Google Patents
Compuestos derivados de 4-(1-(1-(piperidin-4-il)azetidin-3-il)-h-pirazol-4-il)-(1h-pirrolo[2,3-b]piridina o pirimidina); forma cristalina; composicion farmaceutica; util para el tratamiento de una enfermedad autoinmune, cancer, trastorno mieloproliferativo, enfermedad inflamatoria, de resorcion osea o rechazo al trasplante.Info
- Publication number
- CL2012002501A1 CL2012002501A1 CL2012002501A CL2012002501A CL2012002501A1 CL 2012002501 A1 CL2012002501 A1 CL 2012002501A1 CL 2012002501 A CL2012002501 A CL 2012002501A CL 2012002501 A CL2012002501 A CL 2012002501A CL 2012002501 A1 CL2012002501 A1 CL 2012002501A1
- Authority
- CL
- Chile
- Prior art keywords
- piperidin
- cancer
- useful
- pharmaceutical composition
- treatment
- Prior art date
Links
- 208000023275 Autoimmune disease Diseases 0.000 title abstract 2
- 208000014767 Myeloproliferative disease Diseases 0.000 title abstract 2
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 title abstract 2
- 206010028980 Neoplasm Diseases 0.000 title abstract 2
- 206010052779 Transplant rejections Diseases 0.000 title abstract 2
- 201000011510 cancer Diseases 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 208000027866 inflammatory disease Diseases 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- MVXVYAKCVDQRLW-UHFFFAOYSA-N 1h-pyrrolo[2,3-b]pyridine Chemical compound C1=CN=C2NC=CC2=C1 MVXVYAKCVDQRLW-UHFFFAOYSA-N 0.000 title 2
- -1 1- (piperidin-4-yl) azetidin-3-yl Chemical group 0.000 title 1
- 208000006386 Bone Resorption Diseases 0.000 title 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 230000024279 bone resorption Effects 0.000 title 1
- 229940116839 Janus kinase 1 inhibitor Drugs 0.000 abstract 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 abstract 1
- 208000019664 bone resorption disease Diseases 0.000 abstract 1
- 210000000056 organ Anatomy 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
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- 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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- 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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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
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- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- C—CHEMISTRY; METALLURGY
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- 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
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- 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
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (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)
- Neurosurgery (AREA)
- Biomedical Technology (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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31258810P | 2010-03-10 | 2010-03-10 | |
| US41560210P | 2010-11-19 | 2010-11-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CL2012002501A1 true CL2012002501A1 (es) | 2012-12-14 |
Family
ID=44065466
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2012002501A CL2012002501A1 (es) | 2010-03-10 | 2012-09-10 | Compuestos derivados de 4-(1-(1-(piperidin-4-il)azetidin-3-il)-h-pirazol-4-il)-(1h-pirrolo[2,3-b]piridina o pirimidina); forma cristalina; composicion farmaceutica; util para el tratamiento de una enfermedad autoinmune, cancer, trastorno mieloproliferativo, enfermedad inflamatoria, de resorcion osea o rechazo al trasplante. |
Country Status (37)
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10961228B2 (en) | 2017-01-17 | 2021-03-30 | Astrazeneca Ab | JAK1 selective inhibitors |
Families Citing this family (132)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101391900B1 (ko) * | 2005-12-13 | 2014-05-02 | 인사이트 코포레이션 | 야누스 키나아제 억제제로서의 헤테로아릴 치환된 피롤로[2,3-b]피리딘 및 피롤로[2,3-b]피리미딘 |
| 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. |
| WO2008157208A2 (en) | 2007-06-13 | 2008-12-24 | Incyte Corporation | Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| 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 |
| DK2432472T3 (da) | 2009-05-22 | 2019-11-18 | Incyte Holdings Corp | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octan- eller heptan-nitril som jak-inhibitorer |
| 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 |
| HRP20140754T2 (hr) | 2009-06-29 | 2015-07-17 | Incyte Corporation | Pirimidinoni kao inhibitori pi3k |
| 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 |
| PH12015502575A1 (en) * | 2010-03-10 | 2017-04-24 | Incyte Corp | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| EP3087972A1 (en) | 2010-05-21 | 2016-11-02 | Incyte Holdings Corporation | Topical formulation for a jak inhibitor |
| CA2818545C (en) | 2010-11-19 | 2019-04-16 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
| CN103415515B (zh) | 2010-11-19 | 2015-08-26 | 因塞特公司 | 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物 |
| WO2012087881A1 (en) | 2010-12-20 | 2012-06-28 | Incyte Corporation | N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors |
| PL2675451T3 (pl) | 2011-02-18 | 2016-05-31 | Novartis Pharma Ag | Terapia skojarzona z inhibitorem mTOR/JAK |
| US8691807B2 (en) | 2011-06-20 | 2014-04-08 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors |
| 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 |
| LT3196202T (lt) | 2011-09-02 | 2019-07-10 | Incyte Holdings Corporation | Heterociklilaminai, kaip pi3k slopikliai |
| UA111854C2 (uk) * | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| ES2633793T3 (es) * | 2011-09-22 | 2017-09-25 | Merck Sharp & Dohme Corp. | Pirazol carboxamidas como inhibidores de quinasa Janus |
| 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 |
| MX2015003959A (es) | 2012-10-02 | 2015-11-16 | Epitherapeutics Aps | Inhibidores de histona demetilasas. |
| CA2888816A1 (en) | 2012-11-01 | 2014-05-08 | Incyte Corporation | Tricyclic fused thiophene derivatives as jak inhibitors |
| EP3949953A1 (en) | 2012-11-15 | 2022-02-09 | Incyte Holdings Corporation | Sustained-release dosage forms of ruxolitinib |
| JP6437452B2 (ja) | 2013-01-14 | 2018-12-12 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Pimキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物 |
| LT2945939T (lt) | 2013-01-15 | 2020-07-27 | Incyte Holdings Corporation | Triazolkarboksamidai ir piridinkarboksamido junginiai, naudotini kaip pim kinazės inhibitoriai |
| ES2670864T3 (es) | 2013-02-27 | 2018-06-01 | Gilead Sciences, Inc. | Inhibidores de histonas desmetilasas |
| BR112015021458B1 (pt) * | 2013-03-06 | 2022-06-07 | Incyte Holdings Corporation | "processos e intermediários para preparar {1-{1-[3-flúor2-(trifluormetil)isonicotinoil] piperidin-4-il}-3-[4-(7hpirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]azetidin-3-il}acetonitrila, útil no tratamento de doenças relacionadas com a atividade de janus quinases |
| US8669281B1 (en) | 2013-03-14 | 2014-03-11 | Alkermes Pharma Ireland Limited | Prodrugs of fumarates and their use in treating various diseases |
| UA116648C2 (uk) | 2013-03-14 | 2018-04-25 | Алкермес Фарма Айерленд Лімітед | Фумарати як проліки та їх застосування при лікуванні різних захворювань |
| WO2014146246A1 (en) * | 2013-03-19 | 2014-09-25 | Merck Sharp & Dohme Corp. | Cycloalkyl nitrile pyrazolo pyridones as janus kinase inhibitors |
| WO2014146249A1 (en) * | 2013-03-19 | 2014-09-25 | Merck Sharp & Dohme Corp. | Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors |
| KR20150132170A (ko) | 2013-03-19 | 2015-11-25 | 머크 샤프 앤드 돔 코포레이션 | 야누스 키나제 억제제로서의 비-시클릭 시아노에틸피라졸로 피리돈 |
| US9957265B2 (en) | 2013-03-19 | 2018-05-01 | Merck Sharp & Dohme Corp. | N-(2-cyano heterocyclyl) pyrazolo pyridones as janus kinase inhibitors |
| WO2014161046A1 (en) * | 2013-04-04 | 2014-10-09 | The Walter And Eliza Hall Institute Of Medical Research | Methods of treating diseases characterized by excessive wnt signalling |
| UA117830C2 (uk) | 2013-05-17 | 2018-10-10 | Інсайт Корпорейшн | Похідні біпіразолу як інгібітори jak |
| WO2015021153A1 (en) | 2013-08-07 | 2015-02-12 | Incyte Corporation | Sustained release dosage forms for a jak1 inhibitor |
| TW201529074A (zh) * | 2013-08-20 | 2015-08-01 | Incyte Corp | 在c-反應蛋白含量較高之實體腫瘤患者中的存活益處 |
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| JP6367545B2 (ja) * | 2013-12-17 | 2018-08-01 | コンサート ファーマシューティカルズ インコーポレイテッド | ルキソリチニブの重水素化誘導体 |
| US9604922B2 (en) | 2014-02-24 | 2017-03-28 | Alkermes Pharma Ireland Limited | Sulfonamide and sulfinamide prodrugs of fumarates and their use in treating various diseases |
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| NZ763326A (en) * | 2014-04-08 | 2023-04-28 | Incyte Holdings Corp | Treatment of b-cell malignancies by a combination jak and pi3k inhibitor |
| CR20160553A (es) | 2014-04-30 | 2017-04-25 | Incyte Corp | Procesos para preparar un inhibidor de jak1 y nuevas formas de este |
| WO2015184305A1 (en) * | 2014-05-30 | 2015-12-03 | Incyte Corporation | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 |
| US10077277B2 (en) | 2014-06-11 | 2018-09-18 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors |
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- 2024-11-20 JP JP2024201971A patent/JP2025019114A/ja active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10961228B2 (en) | 2017-01-17 | 2021-03-30 | Astrazeneca Ab | JAK1 selective inhibitors |
| US11897869B2 (en) | 2017-01-17 | 2024-02-13 | Astazeneca Ab | JAK1 selective inhibitors |
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