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
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- A—HUMAN NECESSITIES
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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
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- 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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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
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- A61K9/0048—Eye, e.g. artificial tears
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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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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- 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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- 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
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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)
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- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
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- Pulmonology (AREA)
- Immunology (AREA)
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- Rheumatology (AREA)
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- 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)
Abstract
Compuestos derivados de piperidin-4-IL azetidina, inhibidores de JAK1; composición farmacéutica; útil para el tratamiento de una enfermedad autoinmune, un cáncer, un trastorno mieloproliferativo, una enfermedad inflamatoria, una enfermedad de resorción ósea o rechazo al trasplante de órganos.
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)
| Country | Link |
|---|---|
| US (6) | US8765734B2 (es) |
| EP (6) | EP3354652B1 (es) |
| JP (7) | JP5858484B2 (es) |
| KR (7) | KR20180117206A (es) |
| CN (1) | CN102985417B (es) |
| AR (1) | AR081315A1 (es) |
| AU (1) | AU2011224484A1 (es) |
| BR (1) | BR112012022513A2 (es) |
| CA (1) | CA2792508C (es) |
| CL (1) | CL2012002501A1 (es) |
| CO (1) | CO6602158A2 (es) |
| CR (1) | CR20120510A (es) |
| CY (2) | CY1120154T1 (es) |
| DK (3) | DK2545045T3 (es) |
| EA (1) | EA030376B1 (es) |
| EC (1) | ECSP12012218A (es) |
| ES (5) | ES2569539T3 (es) |
| HR (3) | HRP20160326T1 (es) |
| HU (3) | HUE028723T2 (es) |
| IL (1) | IL221823A (es) |
| LT (2) | LT3354652T (es) |
| ME (2) | ME02386B (es) |
| MX (5) | MX380755B (es) |
| MY (2) | MY175156A (es) |
| NO (1) | NO3050882T3 (es) |
| NZ (1) | NZ602313A (es) |
| PE (1) | PE20130038A1 (es) |
| PH (2) | PH12015502575A1 (es) |
| PL (3) | PL2545045T3 (es) |
| PT (2) | PT3354652T (es) |
| RS (3) | RS54823B1 (es) |
| SG (1) | SG183551A1 (es) |
| SI (3) | SI3354652T1 (es) |
| SM (3) | SMT202000373T1 (es) |
| TW (6) | TWI531572B (es) |
| WO (1) | WO2011112662A1 (es) |
| ZA (1) | ZA201207420B (es) |
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 (133)
| 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 |
| 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. |
| 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 |
| 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 |
| EP2758389B1 (en) | 2011-09-22 | 2017-06-07 | Merck Sharp & Dohme Corp. | Pyrazole carboxamides as janus kinase inhibitors |
| 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 |
| BR112015007083A2 (pt) | 2012-10-02 | 2017-07-04 | Epitherapeutics Aps | inibidores de histona demetilases |
| 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 |
| EP2943485B1 (en) | 2013-01-14 | 2017-09-20 | Incyte Holdings Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
| ME03780B (me) | 2013-01-15 | 2021-04-20 | Incyte Holdings Corp | Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze |
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| MX384910B (es) | 2013-03-06 | 2025-03-14 | Incyte Holdings Corp | Procesos e intermedios para hacer un inhibidor de jak. |
| CN105452213B (zh) | 2013-03-14 | 2017-09-22 | 阿尔克梅斯制药爱尔兰有限公司 | 富马酸酯前体药物及其在治疗多种疾病中的应用 |
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| PE20200527A1 (es) | 2013-05-17 | 2020-03-09 | Incyte Corp | Derivados del bipirazol como inhibidores jak |
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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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