MA32684B1 - Dérivés de picolinamide en tant qu'inhibiteurs de kinase - Google Patents
Dérivés de picolinamide en tant qu'inhibiteurs de kinaseInfo
- Publication number
- MA32684B1 MA32684B1 MA33733A MA33733A MA32684B1 MA 32684 B1 MA32684 B1 MA 32684B1 MA 33733 A MA33733 A MA 33733A MA 33733 A MA33733 A MA 33733A MA 32684 B1 MA32684 B1 MA 32684B1
- Authority
- MA
- Morocco
- Prior art keywords
- kinase
- compositions
- compounds
- kinase inhibitors
- inhibiting
- Prior art date
Links
- IBBMAWULFFBRKK-UHFFFAOYSA-N picolinamide Chemical class NC(=O)C1=CC=CC=N1 IBBMAWULFFBRKK-UHFFFAOYSA-N 0.000 title abstract 2
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 239000000203 mixture Substances 0.000 abstract 3
- 102100036077 Serine/threonine-protein kinase pim-1 Human genes 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 2
- 230000002401 inhibitory effect Effects 0.000 abstract 2
- 208000005623 Carcinogenesis Diseases 0.000 abstract 1
- 101001059454 Homo sapiens Serine/threonine-protein kinase MARK2 Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 102000004278 Receptor Protein-Tyrosine Kinases Human genes 0.000 abstract 1
- 108090000873 Receptor Protein-Tyrosine Kinases Proteins 0.000 abstract 1
- 102100028904 Serine/threonine-protein kinase MARK2 Human genes 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000036952 cancer formation Effects 0.000 abstract 1
- 231100000504 carcinogenesis Toxicity 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 230000010469 pro-virus integration Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
-
- 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
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La présente invention concerne de nouveaux composés de picolinamide, des compositions et des procédés d'inhibition de l'activité kinase d'intégration de provirus de Maloney (kinase PIM) associée à la cancérogenèse chez un sujet humain ou animal. Dans certains modes de réalisation, les composés et compositions sont efficaces pour inhiber l'activité d'au moins une kinase PIM. Les nouveaux composés et compositions peuvent être utilisés seuls ou en combinaison avec au moins un agent additionnel pour le traitement d'un trouble véhiculé par une sérine/thréonine kinase ou un récepteur tyrosine kinase, tel que le cancer.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9366608P | 2008-09-02 | 2008-09-02 | |
| US22566009P | 2009-07-15 | 2009-07-15 | |
| PCT/EP2009/061205 WO2010026124A1 (fr) | 2008-09-02 | 2009-08-31 | Dérivés de picolinamide en tant qu’inhibiteurs de kinase |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MA32684B1 true MA32684B1 (fr) | 2011-10-02 |
Family
ID=41228825
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MA33733A MA32684B1 (fr) | 2008-09-02 | 2011-04-01 | Dérivés de picolinamide en tant qu'inhibiteurs de kinase |
Country Status (38)
| Country | Link |
|---|---|
| US (4) | US8329732B2 (fr) |
| EP (1) | EP2344474B1 (fr) |
| JP (2) | JP5412519B2 (fr) |
| KR (1) | KR101345920B1 (fr) |
| CN (3) | CN102203079B (fr) |
| AU (1) | AU2009289319C1 (fr) |
| BR (1) | BRPI0918268B1 (fr) |
| CA (1) | CA2734415C (fr) |
| CL (1) | CL2011000454A1 (fr) |
| CO (1) | CO6351725A2 (fr) |
| CR (1) | CR20110114A (fr) |
| DK (1) | DK2344474T3 (fr) |
| DO (1) | DOP2011000067A (fr) |
| EA (1) | EA020136B1 (fr) |
| EC (1) | ECSP11010859A (fr) |
| ES (1) | ES2551900T3 (fr) |
| GE (1) | GEP20135849B (fr) |
| HN (1) | HN2011000629A (fr) |
| HR (1) | HRP20151410T1 (fr) |
| HU (1) | HUE026381T2 (fr) |
| IL (1) | IL211291A (fr) |
| MA (1) | MA32684B1 (fr) |
| ME (1) | ME01291A (fr) |
| MX (1) | MX2011002365A (fr) |
| MY (1) | MY150136A (fr) |
| NI (1) | NI201100052A (fr) |
| NZ (1) | NZ591449A (fr) |
| PE (1) | PE20110298A1 (fr) |
| PL (1) | PL2344474T3 (fr) |
| PT (1) | PT2344474E (fr) |
| RS (1) | RS54506B1 (fr) |
| SI (1) | SI2344474T1 (fr) |
| SM (1) | SMT201600005B (fr) |
| SV (1) | SV2011003849A (fr) |
| TW (1) | TWI434843B (fr) |
| UY (1) | UY32085A (fr) |
| WO (1) | WO2010026124A1 (fr) |
| ZA (1) | ZA201101118B (fr) |
Families Citing this family (91)
| 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 |
| US20140249135A1 (en) * | 2007-03-01 | 2014-09-04 | Novartis Ag | Pim kinase inhibitors and methods of their use |
| WO2008157208A2 (fr) | 2007-06-13 | 2008-12-24 | Incyte Corporation | Sels de l'inhibiteur (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile de la janus kinase |
| BRPI0918268B1 (pt) | 2008-09-02 | 2021-08-03 | Novartis Ag | Derivados de picolinamida, seu uso, e composição farmacêutica |
| MX2011002367A (es) * | 2008-09-02 | 2011-04-04 | Novartis Ag | Inhibidores de cinasa biciclicos. |
| 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 |
| 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 |
| CA2794801C (fr) * | 2010-04-07 | 2019-01-15 | F. Hoffmann-La Roche Ag | Composes pyrazol-4-yl-heterocyclyle-carboxamide et leurs procedes d'utilisation |
| EP3087972A1 (fr) | 2010-05-21 | 2016-11-02 | Incyte Holdings Corporation | Formulation topique pour un inhibiteur jak |
| WO2012004217A1 (fr) * | 2010-07-06 | 2012-01-12 | Novartis Ag | Composés éthers cycliques utiles comme inhibiteurs de kinase |
| CA2818545C (fr) | 2010-11-19 | 2019-04-16 | Incyte Corporation | Pyrrolopyridines et pyrrolopyrimidines a substitution heterocyclique utilisees en tant qu'inhibiteurs des jak |
| 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 |
| EP2675816A4 (fr) | 2011-02-14 | 2014-08-13 | Univ Alberta | Catalyseurs à base d'acide boronique et procédés d'utilisation associés pour l'activation et la transformation d'acides carboxyliques |
| EP2681197A1 (fr) * | 2011-03-04 | 2014-01-08 | Novartis AG | Composés de cyclohexyle tétrasubstitués à titre d'inhibiteurs de kinases |
| UY33930A (es) * | 2011-03-04 | 2012-10-31 | Novartis Ag | Inhibidores novedosos de quinasas |
| CA2834166A1 (fr) | 2011-04-29 | 2012-11-01 | Amgen Inc. | Composes pyridazines bicycliques en tant qu'inhibiteurs de pim |
| US8691807B2 (en) | 2011-06-20 | 2014-04-08 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors |
| US9416132B2 (en) | 2011-07-21 | 2016-08-16 | Tolero Pharmaceuticals, Inc. | Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors |
| US9458151B2 (en) * | 2011-08-11 | 2016-10-04 | Jikai Biosciences, Inc. | Isothiazole derivatives as PIM kinase inhibitors and preparation methods and use in medicinal manufacture thereof |
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| 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 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
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| WO2013175388A1 (fr) * | 2012-05-21 | 2013-11-28 | Novartis Ag | Nouveaux n-pyridinylamides substitués par un cycle à titre d'inhibiteurs de kinase |
| WO2014033631A1 (fr) | 2012-08-31 | 2014-03-06 | Novartis Ag | N- (3-pyridyl)-biarylamides en tant qu'inhibiteurs de kinase |
| WO2014033630A1 (fr) | 2012-08-31 | 2014-03-06 | Novartis Ag | Nouveaux carboxamides d'aminothiazole en tant qu'inhibiteurs de kinase |
| SI2900657T1 (sl) | 2012-09-26 | 2020-07-31 | F. Hoffmann-La Roche Ag | Ciklični eter pirazol-4-il-heterociklil-karboksamidne spojine in načini uporabe |
| CN103724301A (zh) * | 2012-10-10 | 2014-04-16 | 上海特化医药科技有限公司 | (2r)-2-脱氧-2,2-二取代-1,4-核糖内酯及其制备方法和用途 |
| EP3949953A1 (fr) | 2012-11-15 | 2022-02-09 | Incyte Holdings Corporation | Formes posologiques à libération prolongée de ruxolitinibe |
| US20150336960A1 (en) | 2012-12-19 | 2015-11-26 | Novartis Ag | Aryl-substituted fused bicyclic pyridazine compounds |
| 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 |
| 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 |
| US9113629B2 (en) * | 2013-03-15 | 2015-08-25 | Dow Agrosciences Llc | 4-amino-6-(4-substituted-phenyl)-picolinates and 6-amino-2-(4-substituted-phenyl)-pyrimidine-4-carboxylates and their use as herbicides |
| WO2015021153A1 (fr) | 2013-08-07 | 2015-02-12 | Incyte Corporation | Formes galéniques à libération prolongée pour un inhibiteur jak1 |
| MX2016001683A (es) * | 2013-08-08 | 2016-05-02 | Novartis Ag | Combinaciones de inhibidores de quinasa pim. |
| EP3036238A1 (fr) | 2013-08-23 | 2016-06-29 | Incyte Corporation | Composés de furo- et thiéno-pyridinecarboxamide utiles en tant qu'inhibiteurs de kinases pim |
| EP3757130A1 (fr) | 2013-09-26 | 2020-12-30 | Costim Pharmaceuticals Inc. | Méthodes de traitement de cancers hématologiques |
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| JOP20200094A1 (ar) | 2014-01-24 | 2017-06-16 | Dana Farber Cancer Inst Inc | جزيئات جسم مضاد لـ pd-1 واستخداماتها |
| JOP20200096A1 (ar) | 2014-01-31 | 2017-06-16 | Children’S Medical Center Corp | جزيئات جسم مضاد لـ tim-3 واستخداماتها |
| ME03558B (fr) | 2014-03-14 | 2020-07-20 | Novartis Ag | Molécules d'anticorps anti-lag-3 et leurs utilisations |
| CA2939848A1 (fr) | 2014-03-18 | 2015-09-24 | F. Hoffmann-La Roche Ag | Composes oxepan-2-yl-pyrazol-4-yl-heterocyclyle-carboxamide et leurs methodes d'utilisation |
| WO2015184305A1 (fr) | 2014-05-30 | 2015-12-03 | Incyte Corporation | Traitement de la leucémie neutrophile chronique (cnl) et de la leucémie myéloïde chronique atypique (acml) par des inhibiteurs de jak1 |
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