AR058624A1 - PIRIMIDINE DERIVATIVES AS INHIBITORS OF PIRIMIDIN QUINASA SUBSTITUTES. PROCESSES OF OBTAINING AND PHARMACEUTICAL COMPOSITIONS. - Google Patents
PIRIMIDINE DERIVATIVES AS INHIBITORS OF PIRIMIDIN QUINASA SUBSTITUTES. PROCESSES OF OBTAINING AND PHARMACEUTICAL COMPOSITIONS.Info
- Publication number
- AR058624A1 AR058624A1 ARP060105731A ARP060105731A AR058624A1 AR 058624 A1 AR058624 A1 AR 058624A1 AR P060105731 A ARP060105731 A AR P060105731A AR P060105731 A ARP060105731 A AR P060105731A AR 058624 A1 AR058624 A1 AR 058624A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- aryl
- amino
- heteroaryl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 14
- 125000003545 alkoxy group Chemical group 0.000 abstract 11
- 125000003118 aryl group Chemical group 0.000 abstract 7
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 5
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 5
- 125000001072 heteroaryl group Chemical group 0.000 abstract 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 125000004104 aryloxy group Chemical group 0.000 abstract 3
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000005553 heteroaryloxy group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 208000030090 Acute Disease Diseases 0.000 abstract 1
- 208000017667 Chronic Disease Diseases 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 230000004075 alteration Effects 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- -1 aryl amido Chemical group 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 230000001684 chronic effect Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 125000006517 heterocyclyl carbonyl group Chemical group 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Su síntesis y uso para tratar, prevenir o mejorar una enfermedad, trastorno o alteracion cronica o aguda intermediada por proteinquinasas. Reivindicacion 1: Un compuesto de formula (1) y formas de éste, donde L está seleccionado entre un enlace, alquilo C1-6 o halo-alquilo C1-6; Ar está seleccionado entre arilo, heteroarilo, heterociclilo benzofusionado o cicloalquilo C3-12 benzofusionado, donde la porcion de anillo benceno del sistema de anillo benzofusionado está unida a la variable L; RA está seleccionado entre C=N-O-R1 o ciano; R1 está seleccionado entre H, alquilo C1-8, alquenilo C1-8, alcoxi C1-8, alcoxi C1-8-alquilo C1-8, hidroxi-alquilo C1-8, hidroxi-alcoxi C1-8, amino-alquilo C1-8, alquilo C1-8-amino-alquilo C1-8, alcoxi C1-8- alquilo C1-8-amino-alquilo C1-8, alquilo C1-8-sulfonil-alquilo C1-8, alquilo C1-8-sulfoniloxi-alquilo C1-8, arilo, aril-alquilo C1-8, ariloxi-alquilo C1-8, heterociclil-alquilo C1-8, heterociclil-carbonil-alquilo C1-8 o heteroaril-alquilo C1-8; donde aril-alquilo C1-8 está opcionalmente sustituido en el arilo con 1, 2, 3, 4 o 5 sustituyentes cada uno seleccionado entre hidroxi, alquilo C1-8, alcoxi C1-8, amino, alquilo C1-8-amino o alcoxicarbonilo C1-8, y donde hetrociclil-alquilo C1-8 está opcionalmente sustituido en el heterociclilo con 1, 2, 3 o 4 sustituyentes cada uno seleccionado entre hidroxi, alquilo C1-8, alcoxi C1-8, amino, alquilo C1-8-amino o alcoxicarbonilo C1-8; R2 esta selecionado de H, alquilo C1-8 o alcoxi C1-8; y R3, R4, R5, R6 y R7 está cada uno seleccionado de H, halogeno, hidroxi, alquilo C1-8, alcoxi C1-8, alcoxi C1-8-alquilo C1-8, hidroxi-alquilo C1-8, halo-alquilo C1-8, hidroxi-alcoxi C1-8, halo-alcoxi C1-8, amino, alquilo C1-8-amino, amino-alquilo C1- 8, alquilo C1-8-amino-alquilo C1-8, carboxi, acilo C1-8, alcoxicarbonilo C1-8, cicloalquilo C3-12, arilo, ariloxi, aril-alquilo C1-8, aril-alcoxi C1-8, aril-amido, heteroarilo, heteroariloxi, hteroaril-C1-8-alcoxi o heterociclilo, donde arilo, ariloxi, aril-alquilo C1-8 y aril-alcoxi C1-8 están cada uno opcionalmente sustituidos en el arilo con 1, 2, 3, 4 o 5 sustituyentes cada uno seleccionado entre ciano, halogeno, hidroxi, alquilo C1-8, alcoxi C1-8, amino, alquilo C1-8-amino, amino- alquilo C1-8, alquilo C1-8-amino-alquilo C1-8 o alcoxicarbonilo C1-8 y donde el heteroarilo y el heteroariloxi está cada uno opcionalmente sustituido en el heteroarilo con 1, 2, 3, 4 o 5 sustituyentes cada uno seleccionado entre alquilo C1-8, amino- alquilo C1-8, alquilo C1-8-amino-alquilo C1-8, carboxi C1-8 o alcoxicarbonilo C1-8.Its synthesis and use to treat, prevent or improve a chronic or acute disease, disorder or alteration mediated by protein kinases. Claim 1: A compound of formula (1) and forms thereof, wherein L is selected from a bond, C1-6 alkyl or halo- C1-6 alkyl; Ar is selected from aryl, heteroaryl, benzofused heterocyclyl or benzofused C3-12 cycloalkyl, where the benzene ring portion of the benzofused ring system is linked to the variable L; RA is selected from C = N-O-R1 or cyano; R 1 is selected from H, C 1-8 alkyl, C 1-8 alkenyl, C 1-8 alkoxy, C 1-8 alkoxy-C 1-8 alkyl, hydroxyC 1-8 alkyl, hydroxyC 1-8 alkoxy, aminoC 1-6 alkyl 8, C1-8-amino-C1-8-alkyl, C1-8-alkoxy-C1-8-alkyl-C1-8-alkyl, C1-8-sulfonyl-C1-8-alkyl, C1-8-sulfonyloxy-alkyl C 1-8 alkyl, aryl, aryl C 1-8 alkyl, aryloxy C 1-8 alkyl, heterocyclyl C 1-8 alkyl, heterocyclyl carbonyl C 1-8 alkyl or heteroaryl C 1-8 alkyl; where aryl-C1-8 alkyl is optionally substituted in the aryl with 1, 2, 3, 4 or 5 substituents each selected from hydroxy, C1-8 alkyl, C1-8 alkoxy, amino, C1-8-amino alkyl or alkoxycarbonyl C1-8, and where hetrocyclyl-C1-8 alkyl is optionally substituted in the heterocyclyl with 1, 2, 3 or 4 substituents each selected from hydroxy, C1-8 alkyl, C1-8 alkoxy, amino, C1-8 alkyl amino or C1-8 alkoxycarbonyl; R2 is selected from H, C1-8 alkyl or C1-8 alkoxy; and R3, R4, R5, R6 and R7 are each selected from H, halogen, hydroxy, C1-8 alkyl, C1-8 alkoxy, C1-8 alkoxy-C1-8 alkyl, hydroxy-C1-8 alkyl, halo- C1-8 alkyl, hydroxy-C1-8 alkoxy, halo-C1-8 alkoxy, amino, C1-8-amino alkyl, amino-C1-8 alkyl, C1-8-amino-C1-8 alkyl, carboxy, acyl C1-8, C1-8 alkoxycarbonyl, C3-12 cycloalkyl, aryl, aryloxy, aryl-C1-8 alkyl, aryl-C1-8 alkoxy, aryl amido, heteroaryl, heteroaryloxy, heteroaryl-C1-8-alkoxy or heterocyclyl, where aryl, aryloxy, aryl-C1-8 alkyl and aryl-C1-8 alkoxy are each optionally substituted in the aryl with 1, 2, 3, 4 or 5 substituents each selected from cyano, halogen, hydroxy, C1- alkyl 8, C 1-8 alkoxy, amino, C 1-8 alkyl, amino C 1-8 alkyl, C 1-8 alkyl-C 1-8 alkyl or C 1-8 alkoxycarbonyl and where the heteroaryl and heteroaryloxy are each optionally substituted in the heteroaryl with 1, 2, 3, 4 or 5 substituents each selected from C 1-8 alkyl, amino-alkyl C1-8 yl, C1-8 alkyl-amino- C1-8 alkyl, C1-8 carboxy or C1-8 alkoxycarbonyl.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US75263305P | 2005-12-21 | 2005-12-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR058624A1 true AR058624A1 (en) | 2008-02-13 |
Family
ID=38256842
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060105731A AR058624A1 (en) | 2005-12-21 | 2006-12-21 | PIRIMIDINE DERIVATIVES AS INHIBITORS OF PIRIMIDIN QUINASA SUBSTITUTES. PROCESSES OF OBTAINING AND PHARMACEUTICAL COMPOSITIONS. |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR058624A1 (en) |
| TW (1) | TW200800919A (en) |
| WO (1) | WO2007081630A2 (en) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI475996B (en) | 2007-10-19 | 2015-03-11 | Celgene Avilomics Res Inc | Heteroaryl compounds and uses thereof |
| US7989465B2 (en) | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| WO2009055299A1 (en) * | 2007-10-23 | 2009-04-30 | Janssen Pharmaceutica N.V. | Substituted pyrimidine-5-carboxamide and 5-carboxylic ester kinase inhibitors |
| JP5918264B2 (en) | 2010-12-22 | 2016-05-18 | アッヴィ・インコーポレイテッド | Hepatitis C inhibitor and use thereof |
| EP2678021A4 (en) * | 2011-02-24 | 2015-07-01 | Jiangsu Hansoh Pharmaceutical | Phosphorus containing compounds as protein kinase inhibitors |
| WO2012127441A1 (en) | 2011-03-23 | 2012-09-27 | Semorex Technologies Ltd. | Treatment of proliferative disorders with a chemiluminescent agent |
| CN103058935B (en) * | 2013-01-15 | 2015-05-06 | 四川大学 | Pyrimidine compound as well as preparation method and use for same |
| BR112015021985B1 (en) | 2013-03-15 | 2022-12-13 | Global Blood Therapeutics, Inc | PHARMACEUTICALLY ACCEPTABLE COMPOUNDS OR SALTS THEREOF, THEIR USES AND COMPOSITION |
| TW201534597A (en) | 2013-06-20 | 2015-09-16 | Ab Science | Benzimidazole derivatives as selective proteine kinase inhibitors |
| EA202092627A1 (en) | 2013-11-18 | 2021-09-30 | Глобал Блад Терапьютикс, Инк. | COMPOUNDS AND THEIR APPLICATIONS FOR HEMOGLOBIN MODULATION |
| CN104744446B (en) * | 2013-12-30 | 2019-06-25 | 广东东阳光药业有限公司 | Heteroaryl compound and its application in drug |
| US9840474B2 (en) | 2014-04-24 | 2017-12-12 | Sichuan University | Pyrimidine compounds and use as anti-cervical cancer thereof |
| AU2019255310B2 (en) | 2018-04-18 | 2022-11-24 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| EP3797108B1 (en) | 2018-05-21 | 2022-07-20 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| EP4003532B1 (en) | 2019-07-24 | 2024-09-04 | Constellation Pharmaceuticals, Inc. | Crystalline forms of 7-chloro-2-(4-(3-methoxyazetidin-1-yl)cyclohexyl)-2,4-dimethyl-n-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)benzo[d][1,3]dioxole-5-carboxamide |
| WO2021038419A1 (en) * | 2019-08-23 | 2021-03-04 | Insilico Medicine Ip Limited | Kinase inhibitors and methods of synthesis and treatment |
| US12293809B2 (en) | 2019-08-23 | 2025-05-06 | Insilico Medicine Ip Limited | Workflow for generating compounds with biological activity against a specific biological target |
| KR102889687B1 (en) * | 2020-11-03 | 2025-11-21 | 주식회사 엘지화학 | Novel Compound for Crop Protection |
| TWI750905B (en) * | 2020-11-19 | 2021-12-21 | 財團法人國家衛生研究院 | Thiazole compounds as protein kinase inhibitors |
| WO2024131772A1 (en) * | 2022-12-20 | 2024-06-27 | 杭州中美华东制药有限公司 | Oxime-containing compound having sting inhibitory effect, pharmaceutical composition thereof, and use thereof |
| EP4644373A1 (en) * | 2022-12-28 | 2025-11-05 | Nippon Soda Co., Ltd. | Hydrazide compound and agricultural/horticultural bactericidal agent |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6878714B2 (en) * | 2001-01-12 | 2005-04-12 | Amgen Inc. | Substituted alkylamine derivatives and methods of use |
| JP4049742B2 (en) * | 2001-06-01 | 2008-02-20 | エフ．ホフマン−ラ ロシュ アーゲー | Pyrimidine, triazine and pyrazine derivatives as glutamate receptors |
| EP1406875B1 (en) * | 2001-06-26 | 2013-07-31 | Bristol-Myers Squibb Company | N-heterocyclic inhibitors of tnf-alpha expression |
-
2006
- 2006-12-12 WO PCT/US2006/061890 patent/WO2007081630A2/en not_active Ceased
- 2006-12-20 TW TW095147765A patent/TW200800919A/en unknown
- 2006-12-21 AR ARP060105731A patent/AR058624A1/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| WO2007081630A3 (en) | 2007-12-21 |
| TW200800919A (en) | 2008-01-01 |
| WO2007081630A2 (en) | 2007-07-19 |
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Legal Events
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| FA | Abandonment or withdrawal |