PE20100087A1 - Compuestos y composiciones como inhibidores de cinasa - Google Patents
Compuestos y composiciones como inhibidores de cinasaInfo
- Publication number
- PE20100087A1 PE20100087A1 PE2009000902A PE2009000902A PE20100087A1 PE 20100087 A1 PE20100087 A1 PE 20100087A1 PE 2009000902 A PE2009000902 A PE 2009000902A PE 2009000902 A PE2009000902 A PE 2009000902A PE 20100087 A1 PE20100087 A1 PE 20100087A1
- Authority
- PE
- Peru
- Prior art keywords
- methyl
- amino
- alkyl
- compounds
- pyrimidin
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- -1 PYRIDIN-2-ONYL Chemical group 0.000 abstract 2
- 102000009465 Growth Factor Receptors Human genes 0.000 abstract 1
- 108010009202 Growth Factor Receptors Proteins 0.000 abstract 1
- 206010025323 Lymphomas Diseases 0.000 abstract 1
- 208000034578 Multiple myelomas Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 206010035226 Plasma cell myeloma Diseases 0.000 abstract 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 201000001441 melanoma Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 206010042863 synovial sarcoma Diseases 0.000 abstract 1
Classifications
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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
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE PIRIMIDINA DE FORMULA (1) DONDE EL ANILLO E OPCIONALMENTE POSEE UN DOBLE ENLACE; UNO DE Z1, Z2 Y Z3 ES NR6, N(R6)+-O- Y LOS OTROS SON CR2, EN DONDE R6 ES H, ALQUILO(C1-C6), ALQUENILO(C2-C6), ENTRE OTROS; R1 ES HALOGENO O ALQUILO(C1-C6) OPCIONALMENTE HALOGENADO; R2 ES PIRIDIN-2-ONILO, AZEPAN-2-ONILO O HETEROARILO DE 5 A 6 MIEMBROS OPCIONALMENTE SUSTITUIDO CON R9, DONDE R9 ES ALQUILO(C1-C6), HALOALQUILO(C1-C6) O CICLOALQUILO(C3-C7); R3 Y R4 SON CADA UNO H; R5 ES HALOGENO, OH, ALQUILO(C1-C6), ALCOXILO(C1-C6), ENTRE OTROS; m ES DE 2 A 4. SON COMPUESTOS PREFERIDOS: 5-CLORO-N2-(2-FLUORO-5-METIL-4-(1-METIL-PIPERIDIN-4-IL)-FENIL)-N4-(5-METIL-1H-PIRAZOL-3-IL)-PIRIMIDIN-2,4-DIAMINA, 1-(4-(4-(5-CLORO-4-(5-METIL-1H-PIRAZOL-3-IL-AMINO)-PIRIMIDIN-2-IL-AMINO)-2,5-DIMETIL-FENIL)-PIPERIDIN-1-IL)-3-MORFOLINO-PROPAN-1-ONA, 3-(4-(4-(5-CLORO-4-(5-METIL-1H-PIRAZOL-3-IL-AMINO)-PIRIMIDIN-2-IL-AMINO)-5-FLUORO-2-METIL-FENIL)-PIPERIDIN-1-IL)-PIRROLIDIN-1-CARBOXILATO DE TERBUTILO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DEL RECEPTOR DEL FACTOR DE CRECIMIENTO TIPO INSULINA (IGF-1R) Y DE LA CINASA DE LINFOMA ANAPLASICO (ALK) SIENDO UTILES EN EL TRATAMIENTO DE MIELOMA MULTIPLE, SARCOMA SINOVIAL, MELANOMA, TUMOR DE MAMA
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US7558308P | 2008-06-25 | 2008-06-25 | |
| US15543409P | 2009-02-25 | 2009-02-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20100087A1 true PE20100087A1 (es) | 2010-02-08 |
Family
ID=41349515
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2009000902A PE20100087A1 (es) | 2008-06-25 | 2009-06-23 | Compuestos y composiciones como inhibidores de cinasa |
Country Status (29)
| Country | Link |
|---|---|
| US (2) | US8519129B2 (es) |
| EP (1) | EP2318392A2 (es) |
| JP (1) | JP5508412B2 (es) |
| KR (1) | KR101432352B1 (es) |
| CN (1) | CN102112467B (es) |
| AR (1) | AR072787A1 (es) |
| AU (1) | AU2009264934B2 (es) |
| BR (1) | BRPI0914652A2 (es) |
| CA (1) | CA2729495C (es) |
| CL (1) | CL2009001476A1 (es) |
| CO (1) | CO6351787A2 (es) |
| CR (1) | CR20110028A (es) |
| DO (1) | DOP2010000397A (es) |
| EA (1) | EA020730B1 (es) |
| EC (1) | ECSP11010784A (es) |
| GE (1) | GEP20125564B (es) |
| HN (1) | HN2010002733A (es) |
| IL (1) | IL210124A0 (es) |
| MA (1) | MA32497B1 (es) |
| MX (1) | MX2010014039A (es) |
| NI (1) | NI201000219A (es) |
| NZ (1) | NZ590602A (es) |
| PA (1) | PA8834001A1 (es) |
| PE (1) | PE20100087A1 (es) |
| SV (1) | SV2010003776A (es) |
| TW (1) | TW201000466A (es) |
| UY (1) | UY31929A (es) |
| WO (1) | WO2010002655A2 (es) |
| ZA (1) | ZA201100344B (es) |
Families Citing this family (49)
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|---|---|---|---|---|
| AU2008296545B2 (en) | 2007-08-28 | 2011-09-29 | Irm Llc | 2 -biphenylamino-4 -aminopyrimidine derivatives as kinase inhibitors |
| US8445505B2 (en) | 2008-06-25 | 2013-05-21 | Irm Llc | Pyrimidine derivatives as kinase inhibitors |
| UY31929A (es) * | 2008-06-25 | 2010-01-05 | Irm Llc | Compuestos y composiciones como inhibidores de cinasa |
| JP5539518B2 (ja) | 2009-08-14 | 2014-07-02 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ２−アミノ−５−トリフルオロメチルピリミジン誘導体の位置選択的調製 |
| US8933227B2 (en) | 2009-08-14 | 2015-01-13 | Boehringer Ingelheim International Gmbh | Selective synthesis of functionalized pyrimidines |
| EP2544672A1 (en) | 2010-03-09 | 2013-01-16 | OSI Pharmaceuticals, LLC | Combination anti-cancer therapy |
| WO2011144742A1 (en) | 2010-05-21 | 2011-11-24 | Chemilia Ab | Novel pyrimidine derivatives |
| EP2576541B1 (en) | 2010-06-04 | 2016-04-06 | F.Hoffmann-La Roche Ag | Aminopyrimidine derivatives as lrrk2 modulators |
| AU2011328139A1 (en) | 2010-11-10 | 2013-04-04 | F. Hoffmann-La Roche Ag | Pyrazole aminopyrimidine derivatives as LRRK2 modulators |
| WO2012097479A1 (en) * | 2011-01-21 | 2012-07-26 | Abbott Laboratories | Bicyclic inhibitors of anaphastic lymphoma kinase |
| ES2587864T3 (es) | 2011-03-24 | 2016-10-27 | Noviga Research Ab | Derivados de pirimidina |
| PT2699553T (pt) | 2011-04-22 | 2024-01-24 | Signal Pharm Llc | Diaminocarboxamida e diaminocarbonitrila pirimidinas substituídas, as suas composições e métodos de tratamento com as mesmas |
| EP2554544A1 (en) * | 2011-08-01 | 2013-02-06 | Almirall, S.A. | Pyridin-2(1h)-one derivatives as jak inhibitors |
| WO2013030750A1 (en) | 2011-09-01 | 2013-03-07 | Lupin Limited | Antiviral compounds |
| ES2621257T3 (es) * | 2012-04-20 | 2017-07-03 | Annji Pharmaceutical Co., Ltd. | Ésteres de ciclopropanocarboxilato de análogos de purinas |
| SG11201408324QA (en) | 2012-06-12 | 2015-01-29 | Abbvie Inc | Pyridinone and pyridazinone derivatives |
| BR112015010221B1 (pt) | 2012-11-06 | 2022-09-13 | Shanghai Fochon Pharmaceutical Co., Ltd. | Inibidores de quinase alk, seus usos, composição farmacêutica, e método para fabricação de medicamento |
| CN104109149B (zh) * | 2013-04-22 | 2018-09-28 | 苏州泽璟生物制药有限公司 | 氘代的二氨基嘧啶化合物以及包含该化合物的药物组合物 |
| WO2015094803A1 (en) * | 2013-12-16 | 2015-06-25 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| JOP20200094A1 (ar) | 2014-01-24 | 2017-06-16 | Dana Farber Cancer Inst Inc | جزيئات جسم مضاد لـ pd-1 واستخداماتها |
| NZ715903A (en) | 2014-01-30 | 2017-06-30 | Signal Pharm Llc | Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use |
| JOP20200096A1 (ar) | 2014-01-31 | 2017-06-16 | Children’S Medical Center Corp | جزيئات جسم مضاد لـ tim-3 واستخداماتها |
| MY187246A (en) | 2014-03-14 | 2021-09-14 | Novartis Ag | Antibody molecules to lag-3 and uses thereof |
| CN105294654B (zh) * | 2014-05-30 | 2018-01-09 | 北京浦润奥生物科技有限责任公司 | Alk激酶抑制剂及其制备方法和应用 |
| 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 |
| CU20170052A7 (es) | 2014-10-14 | 2017-11-07 | Dana Farber Cancer Inst Inc | Moléculas de anticuerpo que se unen a pd-l1 |
| US9796685B2 (en) | 2014-12-16 | 2017-10-24 | Signal Pharmaceuticals, Llc | Formulations of 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-Methylcyclohexylamino)-pyrimidine-5-carboxamide |
| EP3233808B1 (en) | 2014-12-16 | 2021-07-14 | Signal Pharmaceuticals, LLC | Medical uses comprising methods for measurement of inhibition of c-jun n-terminal kinase in skin |
| WO2016100882A1 (en) | 2014-12-19 | 2016-06-23 | Novartis Ag | Combination therapies |
| CN105777616B (zh) * | 2014-12-26 | 2018-12-07 | 上海医药工业研究院 | 色瑞替尼的合成中间体及其制备方法 |
| CA2975260C (en) | 2015-01-29 | 2024-05-21 | Signal Pharmaceuticals Llc | Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide |
| KR20170129802A (ko) | 2015-03-10 | 2017-11-27 | 아두로 바이오테크, 인코포레이티드 | ＂인터페론 유전자의 자극인자＂-의존적 신호전달을 활성화하는 조성물 및 방법 |
| EP3795553B1 (en) | 2015-07-24 | 2024-05-15 | Celgene Corporation | Methods of synthesis of (1r,2r,5r)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein |
| JP6878405B2 (ja) | 2015-07-29 | 2021-05-26 | ノバルティス アーゲー | Ｐｄ−１に対する抗体分子を含む組み合わせ治療 |
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| EP3964528A1 (en) | 2015-07-29 | 2022-03-09 | Novartis AG | Combination therapies comprising antibody molecules to lag-3 |
| SG11201803520PA (en) | 2015-11-03 | 2018-05-30 | Janssen Biotech Inc | Antibodies specifically binding pd-1 and their uses |
| EP4424322A3 (en) | 2015-12-17 | 2025-04-16 | Novartis AG | Antibody molecules to pd-1 and uses thereof |
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| US20200172628A1 (en) | 2017-06-22 | 2020-06-04 | Novartis Ag | Antibody molecules to cd73 and uses thereof |
| 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 |
| WO2020069208A1 (en) * | 2018-09-27 | 2020-04-02 | The Regents Of The University Of California | Prevention and treatment of osteoarthritis by inhibition of insulin growth factor-1 signaling |
| ES2966807T3 (es) | 2019-05-10 | 2024-04-24 | Deciphera Pharmaceuticals Llc | Inhibidores de la autofagia de fenilaminopirimidina amida y métodos de uso de los mismos |
| PT3985000T (pt) * | 2019-06-28 | 2025-01-03 | Chengdu Zenitar Biomedical Tech Co Ltd | Derivado de pirimidina 2,4-dissubstituída, método de preparação para o mesmo e suas utilizações |
| WO2021053559A1 (en) | 2019-09-18 | 2021-03-25 | Novartis Ag | Entpd2 antibodies, combination therapies, and methods of using the antibodies and combination therapies |
| GB201915618D0 (en) | 2019-10-28 | 2019-12-11 | Univ Oslo | ALK inhibitors for treatment of ALK-negative cancer and antibody-mediated diseases |
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