PE20110298A1 - Derivados de picolinamida como inhibidores de cinasa - Google Patents
Derivados de picolinamida como inhibidores de cinasaInfo
- Publication number
- PE20110298A1 PE20110298A1 PE2011000444A PE2011000444A PE20110298A1 PE 20110298 A1 PE20110298 A1 PE 20110298A1 PE 2011000444 A PE2011000444 A PE 2011000444A PE 2011000444 A PE2011000444 A PE 2011000444A PE 20110298 A1 PE20110298 A1 PE 20110298A1
- Authority
- PE
- Peru
- Prior art keywords
- picolinamide
- cyclohexyl
- phenyl
- amino
- difluoro
- 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
- -1 CYCLOHEXYL Chemical class 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 101000595531 Homo sapiens Serine/threonine-protein kinase pim-1 Proteins 0.000 abstract 2
- 102100036077 Serine/threonine-protein kinase pim-1 Human genes 0.000 abstract 2
- 101001064870 Homo sapiens Lon protease homolog, mitochondrial Proteins 0.000 abstract 1
- 101001001648 Homo sapiens Serine/threonine-protein kinase pim-2 Proteins 0.000 abstract 1
- 101001001645 Homo sapiens Serine/threonine-protein kinase pim-3 Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 102100036120 Serine/threonine-protein kinase pim-2 Human genes 0.000 abstract 1
- 102100036119 Serine/threonine-protein kinase pim-3 Human genes 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical group [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000010354 integration Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
Classifications
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- 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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (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)
- Hematology (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (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
REFERIDA A UN COMPUESTO DERIVADO DE PICOLINAMIDA DE FORMULA (II), DONDE Y ES CICLOHEXILO; R1 ES H, -NH2 O HALOGENO; R12 ES H O HALOGENO; R5 ES CICLOHEXILO, FENILO O PIRIDILO OPCIONALMENTE SUSTITUIDOS CON HALOGENO, OH, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-(4-((3S,5S)-3-AMINO-5-METIL-CICLOHEXIL)-PIRIDIN-3-IL)-6-(2,6-DIFLUORO-FENIL)-5-FLUORO-PICOLINAMIDA, 3-AMINO-N-(4-((1R,3R,4S,5S)-3-AMINO-4-HIDROXI-5-METIL-CICLOHEXIL)-PIRIDIN-3-IL)-6-(2,6-DIFLUORO-FENIL)-PICOLINAMIDA, N-(4-((3R,4R,5S)-3-AMINO-4-HIDROXI-5-METIL-PIPERIDIN-1-IL)-PIRIDIN-3-IL)-6-(2,6-DIFLUORO-FENIL)-5-FLUORO-PICOLINAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS TIENEN ACTIVIDAD INHIBITORIA DE LA INTEGRACION DEL PROVIRUS DE LA CINASA MALONEY (CINASA PIM) QUE PUEDE SER PIM1, PIM2 O PIM3, Y SON UTILES EN EL TRATAMIENTO DEL CANCER
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9366608P | 2008-09-02 | 2008-09-02 | |
| US22566009P | 2009-07-15 | 2009-07-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20110298A1 true PE20110298A1 (es) | 2011-05-21 |
Family
ID=41228825
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2011000444A PE20110298A1 (es) | 2008-09-02 | 2009-08-31 | Derivados de picolinamida como inhibidores de cinasa |
Country Status (38)
| Country | Link |
|---|---|
| US (4) | US8329732B2 (es) |
| EP (1) | EP2344474B1 (es) |
| JP (2) | JP5412519B2 (es) |
| KR (1) | KR101345920B1 (es) |
| CN (3) | CN102203079B (es) |
| AU (1) | AU2009289319C1 (es) |
| BR (1) | BRPI0918268B1 (es) |
| CA (1) | CA2734415C (es) |
| CL (1) | CL2011000454A1 (es) |
| CO (1) | CO6351725A2 (es) |
| CR (1) | CR20110114A (es) |
| DK (1) | DK2344474T3 (es) |
| DO (1) | DOP2011000067A (es) |
| EA (1) | EA020136B1 (es) |
| EC (1) | ECSP11010859A (es) |
| ES (1) | ES2551900T3 (es) |
| GE (1) | GEP20135849B (es) |
| HN (1) | HN2011000629A (es) |
| HR (1) | HRP20151410T1 (es) |
| HU (1) | HUE026381T2 (es) |
| IL (1) | IL211291A (es) |
| MA (1) | MA32684B1 (es) |
| ME (1) | ME01291A (es) |
| MX (1) | MX2011002365A (es) |
| MY (1) | MY150136A (es) |
| NI (1) | NI201100052A (es) |
| NZ (1) | NZ591449A (es) |
| PE (1) | PE20110298A1 (es) |
| PL (1) | PL2344474T3 (es) |
| PT (1) | PT2344474E (es) |
| RS (1) | RS54506B1 (es) |
| SI (1) | SI2344474T1 (es) |
| SM (1) | SMT201600005B (es) |
| SV (1) | SV2011003849A (es) |
| TW (1) | TWI434843B (es) |
| UY (1) | UY32085A (es) |
| WO (1) | WO2010026124A1 (es) |
| ZA (1) | ZA201101118B (es) |
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 (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 |
| 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 (en) * | 2010-04-07 | 2019-01-15 | F. Hoffmann-La Roche Ag | Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use |
| EP3087972A1 (en) | 2010-05-21 | 2016-11-02 | Incyte Holdings Corporation | Topical formulation for a jak inhibitor |
| WO2012004217A1 (en) * | 2010-07-06 | 2012-01-12 | Novartis Ag | Cyclic ether compounds useful as kinase inhibitors |
| 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 |
| EP2675816A4 (en) | 2011-02-14 | 2014-08-13 | Univ Alberta | BORIC ACID CATALYSTS AND USE METHOD FOR THE ACTIVATION AND TRANSFORMATION OF CARBOXYLIC ACIDS |
| EP2681197A1 (en) * | 2011-03-04 | 2014-01-08 | Novartis AG | Tetrasubstituted cyclohexyl compounds as kinase inhibitors |
| UY33930A (es) * | 2011-03-04 | 2012-10-31 | Novartis Ag | Inhibidores novedosos de quinasas |
| CA2834166A1 (en) | 2011-04-29 | 2012-11-01 | Amgen Inc. | Bicyclic pyridazine compounds as pim inhibitors |
| 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 |
| US9453003B2 (en) * | 2011-08-11 | 2016-09-27 | Jikai Biosciences, Inc. | Pyrimidine derivatives as PIM kinase inhibitors and preparation methods and use in medicinal manufacture thereof |
| 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 |
| 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 |
| WO2013175388A1 (en) * | 2012-05-21 | 2013-11-28 | Novartis Ag | Novel ring-substituted n-pyridinyl amides as kinase inhibitors |
| WO2014033631A1 (en) | 2012-08-31 | 2014-03-06 | Novartis Ag | N-(3-pyridyl) biarylamides as kinase inhibitors |
| WO2014033630A1 (en) | 2012-08-31 | 2014-03-06 | Novartis Ag | Novel aminothiazole carboxamides as kinase inhibitors |
| 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 (en) | 2012-11-15 | 2022-02-09 | Incyte Holdings Corporation | Sustained-release dosage forms of ruxolitinib |
| 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 (en) | 2013-08-07 | 2015-02-12 | Incyte Corporation | Sustained release dosage forms for a jak1 inhibitor |
| MX2016001683A (es) * | 2013-08-08 | 2016-05-02 | Novartis Ag | Combinaciones de inhibidores de quinasa pim. |
| EP3036238A1 (en) | 2013-08-23 | 2016-06-29 | Incyte Corporation | Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors |
| EP3757130A1 (en) | 2013-09-26 | 2020-12-30 | Costim Pharmaceuticals Inc. | Methods for treating hematologic cancers |
| WO2015081083A1 (en) * | 2013-11-27 | 2015-06-04 | Novartis Ag | Combination therapy comprising an inhibitor of jak, cdk and pim |
| 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 (me) | 2014-03-14 | 2020-07-20 | Novartis Ag | Molekuli anti-lag-3 antiтela i njihove upotrebe |
| CA2939848A1 (en) | 2014-03-18 | 2015-09-24 | F. Hoffmann-La Roche Ag | Oxepan-2-yl-pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use |
| 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 |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9822124B2 (en) | 2014-07-14 | 2017-11-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors |
| JO3589B1 (ar) | 2014-08-06 | 2020-07-05 | Novartis Ag | مثبطات كيناز البروتين c وطرق استخداماتها |
| KR20170060042A (ko) | 2014-09-13 | 2017-05-31 | 노파르티스 아게 | Alk 억제제의 조합 요법 |
| EA201790737A1 (ru) | 2014-10-03 | 2017-08-31 | Новартис Аг | Комбинированная терапия |
| MA41044A (fr) | 2014-10-08 | 2017-08-15 | Novartis Ag | Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer |
| MX389663B (es) | 2014-10-14 | 2025-03-20 | Novartis Ag | Moleculas de anticuerpo que se unen a pd-l1 y usos de las mismas. |
| US10449211B2 (en) | 2015-03-10 | 2019-10-22 | Aduro Biotech, Inc. | Compositions and methods for activating “stimulator of interferon gene”—dependent signalling |
| US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
| US20180222982A1 (en) | 2015-07-29 | 2018-08-09 | Novartis Ag | Combination therapies comprising antibody molecules to pd-1 |
| EP3878465A1 (en) | 2015-07-29 | 2021-09-15 | Novartis AG | Combination therapies comprising antibody molecules to tim-3 |
| DK3317301T3 (da) | 2015-07-29 | 2021-06-28 | Immutep Sas | Kombinationsterapier omfattende antistofmolekyler mod lag-3 |
| AR105967A1 (es) | 2015-09-09 | 2017-11-29 | Incyte Corp | Sales de un inhibidor de pim quinasa |
| CN105254624B (zh) * | 2015-09-18 | 2019-08-09 | 上海吉铠医药科技有限公司 | 异噻唑衍生物pim激酶抑制剂及其制备方法与在制药中的应用 |
| CN105130959B (zh) * | 2015-09-18 | 2018-08-03 | 上海吉铠医药科技有限公司 | 嘧啶衍生物pim激酶抑制剂及其制备方法与在制药中的应用 |
| WO2017059251A1 (en) | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| SI3370768T1 (sl) | 2015-11-03 | 2022-04-29 | Janssen Biotech, Inc. | Protitelesa, ki se specifično vežejo na PD-1, in njihove uporabe |
| EP3389712B1 (en) | 2015-12-17 | 2024-04-10 | Novartis AG | Antibody molecules to pd-1 and uses thereof |
| CN107522696B (zh) | 2016-06-21 | 2019-02-19 | 上海方予健康医药科技有限公司 | 一种嘧啶类化合物的盐酸盐及其制备方法和用途 |
| CN107522695B (zh) * | 2016-06-21 | 2018-09-14 | 上海方予健康医药科技有限公司 | 一种pim激酶抑制剂的盐酸盐及其制备方法和用途 |
| CN107519175A (zh) * | 2016-06-21 | 2017-12-29 | 上海方予健康医药科技有限公司 | 一种嘧啶化合物或其盐在制备用于预防和/或治疗与flt3相关的疾病或障碍的药物中的应用 |
| US11098077B2 (en) | 2016-07-05 | 2021-08-24 | Chinook Therapeutics, Inc. | Locked nucleic acid cyclic dinucleotide compounds and uses thereof |
| UY37695A (es) | 2017-04-28 | 2018-11-30 | Novartis Ag | Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo |
| WO2018237173A1 (en) | 2017-06-22 | 2018-12-27 | Novartis Ag | Antibody molecules to cd73 and uses thereof |
| WO2019006292A1 (en) * | 2017-06-30 | 2019-01-03 | Bristol-Myers Squibb Company | SUBSTITUTED QUINOLINYCYCLOHEXYLPROPANAMIDE COMPOUNDS AND IMPROVED PROCESSES FOR THE PREPARATION THEREOF |
| TW201924683A (zh) | 2017-12-08 | 2019-07-01 | 美商英塞特公司 | 用於治療骨髓增生性贅瘤的低劑量組合療法 |
| US12398209B2 (en) | 2018-01-22 | 2025-08-26 | Janssen Biotech, Inc. | Methods of treating cancers with antagonistic anti-PD-1 antibodies |
| DK3746429T3 (da) | 2018-01-30 | 2022-05-02 | Incyte Corp | Fremgangsmåder til fremstilling af (1-(3-fluor-2-(trifluormethyl)isonicotinyl)piperidin-4-on) |
| PT3762368T (pt) | 2018-03-08 | 2022-05-06 | Incyte Corp | Compostos de aminopirazina diol como inibidores de pi3k-y |
| CN112423759A (zh) | 2018-03-30 | 2021-02-26 | 因赛特公司 | 使用jak抑制剂治疗化脓性汗腺炎 |
| EP3773560A4 (en) | 2018-04-13 | 2022-01-19 | Sumitomo Dainippon Pharma Oncology, Inc. | PIM KINASE INHIBITORS FOR THE TREATMENT OF MYELOPROLIFERATIVE NEOPLASMS AND CANCER-ASSOCIATED FIBROSIS |
| TWI869346B (zh) | 2018-05-30 | 2025-01-11 | 瑞士商諾華公司 | Entpd2抗體、組合療法、及使用該等抗體和組合療法之方法 |
| IL279152B2 (en) | 2018-06-05 | 2024-09-01 | Crinetics Pharmaceuticals Inc | Melanocortin subtype-2 receptor antagonists and uses thereof |
| WO2020010003A1 (en) | 2018-07-02 | 2020-01-09 | Incyte Corporation | AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS |
| CA3127502A1 (en) | 2019-02-12 | 2020-08-20 | Sumitomo Dainippon Pharma Oncology, Inc. | Formulations comprising heterocyclic protein kinase inhibitors |
| CN110078706B (zh) * | 2019-05-31 | 2022-02-01 | 浙江师范大学 | 一种伊马替尼衍生物及其制备方法和用途 |
| CN110452164B (zh) * | 2019-09-10 | 2022-07-22 | 上海皓鸿生物医药科技有限公司 | Pim447关键中间体的制备方法 |
| US20220348651A1 (en) | 2019-09-18 | 2022-11-03 | Novartis Ag | Entpd2 antibodies, combination therapies, and methods of using the antibodies and combination therapies |
| EP4054583A4 (en) | 2019-11-07 | 2023-10-25 | Crinetics Pharmaceuticals, Inc. | MELANOCORTIN SUBTYPE 2 RECEPTOR (MC2R) ANTAGONISTS AND THEIR USES |
| DK4077307T3 (da) | 2019-12-18 | 2025-05-26 | Crinetics Pharmaceuticals Inc | Gem-disubstituerede piperidinmelanocortin subtype-2-receptor- (mc2r)-antagonister og anvendelser deraf |
| ES3032933T3 (en) | 2019-12-23 | 2025-07-29 | Crinetics Pharmaceuticals Inc | Spirocyclic piperidine melanocortin subtype-2 receptor (mc2r) antagonists and uses thereof |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| CN112915086B (zh) * | 2021-01-27 | 2022-04-12 | 广州市力鑫药业有限公司 | 一种含有Akt靶向激酶抑制剂的药物组合物 |
| US12280046B2 (en) | 2021-03-19 | 2025-04-22 | Crinetics Pharmaceuticals, Inc. | Melanocortin subtype-2 receptor (MC2R) antagonist for the treatment of disease |
| AU2023372386A1 (en) | 2022-10-31 | 2025-05-08 | Sumitomo Pharma America, Inc. | Pim1 inhibitor for treating myeloproliferative neoplasms |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1251134A4 (en) | 2000-01-26 | 2003-01-29 | Meiji Seika Kaisha | NEW CARBAPENEM DERIVATIVES OF THE QUATERNARY SALT TYPE |
| JP2003520854A (ja) * | 2000-01-27 | 2003-07-08 | サイトビア インコーポレイテッド | カスパーゼのアクチベーターおよびアポトーシスのインデューサーとしての置換ニコチンアミドおよび類似物およびそれらの使用 |
| US8618085B2 (en) | 2000-04-28 | 2013-12-31 | Koasn Biosciences Incorporated | Therapeutic formulations of desoxyepothilones |
| MXPA03008560A (es) | 2001-03-22 | 2004-06-30 | Abbot Gmbh & Co Kg | Pirazolopirimidinas como agentes terapeuticos. |
| KR100557093B1 (ko) | 2003-10-07 | 2006-03-03 | 한미약품 주식회사 | 다약제 내성 저해 활성을 갖는 테트라졸 유도체 및 그의제조방법 |
| PE20050444A1 (es) | 2003-10-31 | 2005-08-09 | Takeda Pharmaceutical | Compuestos de piridina como inhibidores de la peptidasa |
| CA2548172A1 (en) | 2003-12-04 | 2005-06-23 | Vertex Pharmaceuticals Incorporated | Quinoxalines useful as inhibitors of protein kinases |
| US7459562B2 (en) | 2004-04-23 | 2008-12-02 | Bristol-Myers Squibb Company | Monocyclic heterocycles as kinase inhibitors |
| US20060004197A1 (en) | 2004-07-02 | 2006-01-05 | Thomas Thrash | Sulfonamide-based compounds as protein tyrosine kinase inhibitors |
| CR9465A (es) | 2005-03-25 | 2008-06-19 | Surface Logix Inc | Compuestos mejorados farmacocineticamente |
| AU2006278504B2 (en) | 2005-08-04 | 2013-01-17 | Sirtris Pharmaceuticals, Inc. | Imidazopyridine derivatives as sirtuin modulating agents |
| AU2006302174B2 (en) | 2005-10-06 | 2013-06-20 | Exelixis, Inc. | Pyridopyrimidinone Inhibitors of PIM-1 and/or PIM-3 |
| GB0520657D0 (en) * | 2005-10-11 | 2005-11-16 | Ludwig Inst Cancer Res | Pharmaceutical compounds |
| HRPK20050957B3 (en) * | 2005-11-11 | 2008-09-30 | Džanko Nikša | Collapsible hanger |
| AU2007314342B2 (en) * | 2006-10-31 | 2013-02-21 | Merck Sharp & Dohme Corp. | Anilinopiperazine Derivatives and methods of use thereof |
| AU2007314305B2 (en) | 2006-10-31 | 2013-01-24 | Merck Sharp & Dohme Corp. | 2-aminothiazole-4-carboxylic amides as protein kinase inhibitors |
| EA019951B1 (ru) * | 2007-03-01 | 2014-07-30 | Новартис Аг | Ингибиторы киназы pim и способы их применения |
| CN101801958B (zh) * | 2007-07-19 | 2014-01-29 | 默沙东公司 | 作为蛋白质激酶抑制剂的杂环酰胺化合物 |
| NZ583790A (en) | 2007-09-10 | 2012-04-27 | Cipla Ltd | Process for the preparation the raf kinase inhibitor sorafenib and intermediates for use in the process |
| AR070531A1 (es) * | 2008-03-03 | 2010-04-14 | Novartis Ag | Inhibidores de cinasa pim y metodos para su uso |
| BRPI0918268B1 (pt) * | 2008-09-02 | 2021-08-03 | Novartis Ag | Derivados de picolinamida, seu uso, e composição farmacêutica |
| US8809380B2 (en) | 2009-08-04 | 2014-08-19 | Raqualia Pharma Inc. | Picolinamide derivatives as TTX-S blockers |
| CN103380117A (zh) | 2011-01-21 | 2013-10-30 | Abbvie公司 | 激酶的吡啶酰胺抑制剂 |
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