AR056556A1 - Imidazo(1,2-a)piridina con actividad antiproliferacion celular - Google Patents
Imidazo(1,2-a)piridina con actividad antiproliferacion celularInfo
- Publication number
- AR056556A1 AR056556A1 ARP060104322A ARP060104322A AR056556A1 AR 056556 A1 AR056556 A1 AR 056556A1 AR P060104322 A ARP060104322 A AR P060104322A AR P060104322 A ARP060104322 A AR P060104322A AR 056556 A1 AR056556 A1 AR 056556A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- carbamoyl
- methylsulphonyloxy
- halo
- amino
- Prior art date
Links
- 230000001028 anti-proliverative effect Effects 0.000 title 1
- 230000001413 cellular effect Effects 0.000 title 1
- 230000000694 effects Effects 0.000 title 1
- -1 cyano, hydroxy, amino, mesyl Chemical group 0.000 abstract 21
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 8
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 8
- 125000005843 halogen group Chemical group 0.000 abstract 7
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 4
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 3
- 125000001589 carboacyl group Chemical group 0.000 abstract 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 125000004434 sulfur atom Chemical group 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- 125000006594 (C1-C3) alkylsulfony group Chemical group 0.000 abstract 1
- 125000002861 (C1-C4) alkanoyl group Chemical group 0.000 abstract 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 abstract 1
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 125000005137 alkenylsulfonyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Dermatology (AREA)
- Transplantation (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Procesos, composicion farmacéutica, uso para tratar cáncer. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1) donde: R1 se selecciona entre halo, amino, C1-3 alquilo, C1-3 alcoxi, N-(C1-3 alquil)amino, N,N-(C1-3 alquil)2amino y un anillo saturado de entre 4 y 7 miembros unido por N que contiene opcionalmente un átomo de N, O o S adicional; m es 0-4; donde los valores de R1 pueden ser iguales o diferentes; R2 se selecciona entre H, halo, amino, C1-3 alquilo y C1-3 alcoxi; R3 es H o halo; R4 es H, etinilo, halo, ciano, hidroxi, amino, mesilo, trifluorometilo, trifluorometoxi, metilo, etilo o metoxi; El anillo A es un anillo saturado de entre 4 y 7 miembros unido por N que contiene opcionalmente un átomo e N, O o S adicional; donde si dicho anillo contiene un átomo de N adicional ese N puede estar opcionalmente sustituido con R6; R5 es un sustituyente sobre C y se selecciona entre halo, ciano, hidroxi, trifluorometoxi, amino, carboxi, carbamoílo, sulfamoilo, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C1-6 alcanoilo, N(C1-6 alquil)carbamoilo, N,N-(C1-6 alquil)2carbamoilo, C1-6 alquilS(O)a donde a es entre 0 y 2, C1-6 alcoxicarbonilo, N-(C1-6 alquil)sulfamoilo, y N,N-(C1-6 alquil)2sulfamoilo; donde R5 en forma independiente puede estar opcionalmente sustituido sobre C con uno o más R7, o R5 es -NHR8, -NR9R10 o -O-R11; n es 0-4; donde los valores de R5 pueden ser iguales o diferentes; R6 se selecciona entre C1-6 alquilo, C1-6 alcanoilo, C1-6 alquilsulfonilo, C1-6 alcoxicarbonilo, carbamoílo, N-(C1-6 alquil)carbamoílo y N,N-(C1-6 alquil)carbamoílo; donde R6 puede estar opcionalmente sustituido sobre C con uno o más R12; R8, R9, R10 y R11 se seleccionan en forma independiente entre C1-34 alquilo, C1-4 alcanoílo, C1-4 alquilsulfonilo, C2-4 alquenilsulfonilo, C2-4 alquinilsulfonilo, C1-4 alcoxicarbonilo, carbamoílo, N-(C1-4 alquil)carbamoílo, N,N-(C1-4 alquil)carbamoílo, carbociclilo y heterociclilo; donde R8, R9, R10 y R11 pueden estar opcionalmente sustituidos en forma independiente sobre C con un grupo seleccionado entre R13; y donde si dicho heterociclilo contiene una porcion -NH- ese N puede estar opcionalmente sustituido con R14; R13 se selecciona entre halo, ciano, hidroxi, amino, trifluorometilo, trifluorometoxi, C1-3 alquilo y C1-3 alcoxi; R14 se selecciona entre C1-3 alquilo, C1-3 alcanoílo, C1-3 alquilsulfonilo, C1-3 alcoxicarbonilo, carbamoílo, N-(C1-3 alquil)carbamoílo y N,N- (C1-3 alquil)carbamoílo; y R7 y R12 se seleccionan en forma independiente entre halo, ciano, hidroxi, trifluorometoxi, trifluorometilo, amino, carboxi, carbamoílo, sulfamoilo, metilo, etilo, metoxi, etoxi, acetilo, acetoxi, metilamino, etilamino, dimetilamino, dietilamino, N-metil-N-etilamino, acetilamino, N-metilcarbamoílo, N-etilcarbamoílo, N,N-dimetilcarbamoílo, N,N-dietilcarbamoílo, N-metil-N-etilcarbamoílo, metiltio, etiltio, metilsulfinilo, etilsulfinilo, mesilo, etilsulfonilo, metoxicarbonilo, etoxicarbonilo, N-metilsulfamoílo, N-etilsulfamoílo, N,N-dimetilsulfamoílo, N,N-dietilsulfamoílo y N-metil-N-etilsulfamoílo; o una sal aceptable para uso farmacéutico o un éster hidrolizable in vivo del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US72228105P | 2005-09-30 | 2005-09-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR056556A1 true AR056556A1 (es) | 2007-10-10 |
Family
ID=37670759
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060104322A AR056556A1 (es) | 2005-09-30 | 2006-09-29 | Imidazo(1,2-a)piridina con actividad antiproliferacion celular |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US7745428B2 (es) |
| EP (1) | EP1934213A1 (es) |
| JP (1) | JP2009512636A (es) |
| KR (1) | KR20080049130A (es) |
| CN (1) | CN101277956A (es) |
| AR (1) | AR056556A1 (es) |
| AU (1) | AU2006296386A1 (es) |
| BR (1) | BRPI0616722A2 (es) |
| CA (1) | CA2623374A1 (es) |
| IL (1) | IL189916A0 (es) |
| NO (1) | NO20081162L (es) |
| TW (1) | TW200728290A (es) |
| UY (1) | UY29826A1 (es) |
| WO (1) | WO2007036732A1 (es) |
| ZA (1) | ZA200802497B (es) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0205690D0 (en) | 2002-03-09 | 2002-04-24 | Astrazeneca Ab | Chemical compounds |
| GB0205688D0 (en) | 2002-03-09 | 2002-04-24 | Astrazeneca Ab | Chemical compounds |
| US7442697B2 (en) | 2002-03-09 | 2008-10-28 | Astrazeneca Ab | 4-imidazolyl substituted pyrimidine derivatives with CDK inhibitory activity |
| GB0205693D0 (en) | 2002-03-09 | 2002-04-24 | Astrazeneca Ab | Chemical compounds |
| GB0311274D0 (en) | 2003-05-16 | 2003-06-18 | Astrazeneca Ab | Chemical compounds |
| GB0311276D0 (en) | 2003-05-16 | 2003-06-18 | Astrazeneca Ab | Chemical compounds |
| TW200811169A (en) * | 2006-05-26 | 2008-03-01 | Astrazeneca Ab | Chemical compounds |
| CN101679408B (zh) | 2006-12-22 | 2016-04-27 | Astex治疗学有限公司 | 作为fgfr抑制剂的双环杂环化合物 |
| US8513276B2 (en) | 2006-12-22 | 2013-08-20 | Astex Therapeutics Limited | Imidazo[1,2-a]pyridine compounds for use in treating cancer |
| BRPI0811898A2 (pt) * | 2007-06-01 | 2019-09-24 | Glaxosmithkline Llc | composto, composição farmacêutica, métodos para tratar um neoplasma suscetível e um câncer em um mamífero, processo para preparar um composto, e, uso de um composto. |
| GB0720038D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New compounds |
| GB0720041D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New Compounds |
| GB0810902D0 (en) | 2008-06-13 | 2008-07-23 | Astex Therapeutics Ltd | New compounds |
| NZ590320A (en) * | 2008-07-14 | 2012-12-21 | Gilead Sciences Inc | Fused heterocyclyc inhibitors of histone deacetylase and/or cyclin-dependent kinases |
| WO2010009166A1 (en) | 2008-07-14 | 2010-01-21 | Gilead Colorado, Inc. | Oxindolyl inhibitor compounds |
| US8134000B2 (en) | 2008-07-14 | 2012-03-13 | Gilead Sciences, Inc. | Imidazolyl pyrimidine inhibitor compounds |
| CA2731323A1 (en) | 2008-07-28 | 2010-02-04 | Gilead Sciences, Inc. | Cycloalkylidene and heterocycloalkylidene histone deacetylase inhibitor compounds |
| US20100105655A1 (en) * | 2008-10-29 | 2010-04-29 | Astrazeneca Ab | Novel compounds 515 |
| GB0906470D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| GB0906472D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| WO2010144371A1 (en) | 2009-06-08 | 2010-12-16 | Gilead Colorado, Inc. | Alkanoylamino benzamide aniline hdac inihibitor compounds |
| AU2010259042A1 (en) | 2009-06-08 | 2011-12-15 | Gilead Sciences, Inc. | Cycloalkylcarbamate benzamide aniline HDAC inhibitor compounds |
| PE20170003A1 (es) | 2009-08-17 | 2017-03-15 | Intellikine Llc | Compuestos heterociclicos y usos de los mismos |
| KR101774035B1 (ko) | 2009-10-30 | 2017-09-01 | 얀센 파마슈티카 엔.브이. | 이미다조［１，２―ｂ］피리다진 유도체 및 ＰＤＥ１０ 저해제로서의 그의 용도 |
| AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
| US10604523B2 (en) | 2011-06-27 | 2020-03-31 | Janssen Pharmaceutica Nv | 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline derivatives |
| WO2013071272A1 (en) * | 2011-11-11 | 2013-05-16 | Intellikine, Llc | Kinase inhibitor polymorphs |
| JP6426603B2 (ja) | 2012-06-26 | 2018-11-21 | ヤンセン ファーマシューティカ エヌ．ベー． | 神経障害または代謝障害の治療に使用するための、１−アリール−４−メチル−［１，２，４］トリアゾロ［４，３−ａ］−キノキサリン化合物などのＰＤＥ２阻害剤とＰＤＥ１０阻害剤との組合せ |
| EP2869822B1 (en) | 2012-07-09 | 2016-09-14 | Janssen Pharmaceutica, N.V. | Inhibitors of phosphodiesterase 10 enzyme |
| GB201220157D0 (en) * | 2012-11-08 | 2012-12-26 | Selvita Sa | Substitute tricyclic benzimidazoles as kinase inhibitors |
| US20160000787A1 (en) * | 2013-02-26 | 2016-01-07 | Senex Biotechnology, Inc. | Inhibitors of cdk8/19 for use in treating estrogen receptor positive breast cancer |
| CN111566100B (zh) * | 2018-02-12 | 2023-10-27 | 恩瑞生物医药科技（上海）有限公司 | 嘧啶类化合物、其制备方法及其医药用途 |
| CA3102279A1 (en) | 2018-06-01 | 2019-12-05 | Cornell University | Combination therapy for pi3k-associated disease or disorder |
| CN111303128B (zh) * | 2020-04-07 | 2020-10-27 | 苏州信诺维医药科技有限公司 | 一种多环类化合物、其制备方法及应用 |
| WO2026024674A1 (en) | 2024-07-22 | 2026-01-29 | Genesis Therapeutics, Inc. | Methods of treating skp2-associated cancers |
Family Cites Families (82)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4659363A (en) | 1983-07-25 | 1987-04-21 | Ciba-Geigy Corporation | N-(2-nitrophenyl)-2-aminopyrimidine derivatives, the preparation and use thereof |
| US4946956A (en) | 1988-09-21 | 1990-08-07 | Uniroyal Chemical Company, Inc. | Arylenediamine substituted pyrimidines |
| HU206337B (en) | 1988-12-29 | 1992-10-28 | Mitsui Petrochemical Ind | Process for producing pyrimidine derivatives and pharmaceutical compositions |
| US4983608A (en) | 1989-09-05 | 1991-01-08 | Hoechst-Roussell Pharmaceuticals, Inc. | N-substituted-4-pyrimidinamines and pyrimidinediamines |
| GB9012592D0 (en) | 1990-06-06 | 1990-07-25 | Smithkline Beecham Intercredit | Compounds |
| EP0584222B1 (en) | 1991-05-10 | 1997-10-08 | Rhone-Poulenc Rorer International (Holdings) Inc. | Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase |
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| US5516775A (en) | 1992-08-31 | 1996-05-14 | Ciba-Geigy Corporation | Further use of pyrimidine derivatives |
| US5610303A (en) | 1992-10-05 | 1997-03-11 | Ube Industries, Ltd. | Arylamino pyrimidine compound |
| US5543520A (en) | 1993-10-01 | 1996-08-06 | Ciba-Geigy Corporation | Pyrimidine derivatives |
| WO1995009847A1 (en) | 1993-10-01 | 1995-04-13 | Ciba-Geigy Ag | Pyrimidineamine derivatives and processes for the preparation thereof |
| DK0672041T3 (da) | 1993-10-01 | 2002-02-25 | Novartis Ag | Farmakologisk aktive pyridinderivater og fremgangsmåder til fremstilling deraf |
| US5705502A (en) | 1993-10-01 | 1998-01-06 | Novartis Corporation | Pharmacologically active pyrimidineamine derivatives and processes for the preparation thereof |
| GB9325217D0 (en) | 1993-12-09 | 1994-02-09 | Zeneca Ltd | Pyrimidine derivatives |
| AU688087B2 (en) | 1994-08-13 | 1998-03-05 | Yuhan Corporation | Novel pyrimidine derivatives and processes for the preparation thereof |
| PT813525E (pt) | 1995-03-10 | 2004-02-27 | Berlex Lab | Derivados de benzamidina e sua utilizacao como anticoagulantes |
| US5739143A (en) | 1995-06-07 | 1998-04-14 | Smithkline Beecham Corporation | Imidazole compounds and compositions |
| US5658903A (en) | 1995-06-07 | 1997-08-19 | Smithkline Beecham Corporation | Imidazole compounds, compositions and use |
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| WO1997035856A1 (en) | 1996-03-25 | 1997-10-02 | Smithkline Beecham Corporation | Novel treatment for cns injuries |
| AU2381397A (en) | 1996-04-19 | 1997-11-12 | Novo Nordisk A/S | Modulators of molecules with phosphotyrosine recognition units |
| TW440563B (en) | 1996-05-23 | 2001-06-16 | Hoffmann La Roche | Aryl pyrimidine derivatives and a pharmaceutical composition thereof |
| AU708883B2 (en) | 1996-06-10 | 1999-08-12 | Merck & Co., Inc. | Substituted imidazoles having cytokine inhibitory activity |
| GB9619284D0 (en) | 1996-09-16 | 1996-10-30 | Celltech Therapeutics Ltd | Chemical compounds |
| WO1998016230A1 (en) | 1996-10-17 | 1998-04-23 | Smithkline Beecham Corporation | Methods for reversibly inhibiting myelopoiesis in mammalian tissue |
| GB9622363D0 (en) | 1996-10-28 | 1997-01-08 | Celltech Therapeutics Ltd | Chemical compounds |
| ZA9711092B (en) | 1996-12-11 | 1999-07-22 | Smithkline Beecham Corp | Novel compounds. |
| BR9807305A (pt) | 1997-02-05 | 2000-05-02 | Warner Lambert Co | Pirido [2,3-d] pirimidinas e 4-aminopirimidinas como inibidores de proliferação celular. |
| DE19710435A1 (de) | 1997-03-13 | 1998-09-17 | Hoechst Ag | Verwendung von Pyrimidinderivaten zur Prävention von Krebs allein oder in Kombination mit anderen therapeutischen Maßnahmen |
| GB9705361D0 (en) | 1997-03-14 | 1997-04-30 | Celltech Therapeutics Ltd | Chemical compounds |
| CA2291709A1 (en) | 1997-05-30 | 1998-12-03 | Merck & Co., Inc. | Novel angiogenesis inhibitors |
| JP4380803B2 (ja) | 1997-06-12 | 2009-12-09 | アベンテイス・フアルマ・リミテツド | イミダゾリル−環式アセタール |
| TW517055B (en) | 1997-07-02 | 2003-01-11 | Smithkline Beecham Corp | Novel substituted imidazole compounds |
| AU9781098A (en) | 1997-10-02 | 1999-04-27 | Merck & Co., Inc. | Inhibitors of prenyl-protein transferase |
| JP2001519381A (ja) | 1997-10-10 | 2001-10-23 | インペリアル・カレッジ・イノベイションズ・リミテッド | 子宮収縮管理のためのｃｓａｉｄｔｍ化合物の使用 |
| JP4135318B2 (ja) | 1997-12-15 | 2008-08-20 | アステラス製薬株式会社 | 新規なピリミジン−５−カルボキサミド誘導体 |
| JP2001526230A (ja) | 1997-12-19 | 2001-12-18 | スミスクライン・ビーチャム・コーポレイション | ヘテロアリール置換イミダゾール化合物、その医薬組成物および使用 |
| KR20010041015A (ko) | 1998-02-17 | 2001-05-15 | 윌리엄 제이. 리플린 | 항바이러스성 피리미딘 유도체 |
| CZ299380B6 (cs) | 1998-03-27 | 2008-07-09 | Janssen Pharmaceutica N. V. | Pyrimidinová sloucenina, použití této slouceniny pro prípravu léciva, farmaceutický prostredek tutoslouceninu obsahující, zpusob prípravy tohoto prostredku a uvedené slouceniny a kombinace a produktuvedenou slouceninu obsahující |
| GB9806739D0 (en) | 1998-03-28 | 1998-05-27 | Univ Newcastle Ventures Ltd | Cyclin dependent kinase inhibitors |
| JP2002523498A (ja) | 1998-08-29 | 2002-07-30 | アストラゼネカ・アクチエボラーグ | ピリミジン化合物 |
| JP2002523497A (ja) | 1998-08-29 | 2002-07-30 | アストラゼネカ・アクチエボラーグ | ピリミジン化合物 |
| WO2000017202A1 (en) | 1998-09-18 | 2000-03-30 | Basf Aktiengesellschaft | 4-aminopyrrolopyrimidines as kinase inhibitors |
| CA2344249A1 (en) | 1998-09-18 | 2000-03-30 | Basf Aktiengesellschaft | Pyrrolopyrimidines as protein kinase inhibitors |
| US6531477B1 (en) | 1998-10-13 | 2003-03-11 | Dupont Pharmaceuticals Company | 6-substituted pyrazolo [3,4-d] pyrimidin-4-ones useful as cyclin dependent kinase inhibitors |
| JP2002528499A (ja) | 1998-10-29 | 2002-09-03 | ブリストル−マイヤーズ スクイブ カンパニー | Ｉｍｐｄｈ酵素のインヒビターであるアミノ核誘導化合物 |
| WO2000026209A1 (en) | 1998-11-03 | 2000-05-11 | Novartis Ag | Anti-inflammatory 4-phenyl-5-pyrimidinyl-imidazoles |
| GB9828511D0 (en) | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
| NZ513371A (en) | 1999-02-01 | 2003-08-29 | Cv Therapeutics Inc | 2,6,9 trisubstituted purine inhibitors of cyclin dependant kinase 2 and IkappaB-alpha |
| GB9903762D0 (en) | 1999-02-18 | 1999-04-14 | Novartis Ag | Organic compounds |
| GB9905075D0 (en) | 1999-03-06 | 1999-04-28 | Zeneca Ltd | Chemical compounds |
| US6627633B2 (en) | 1999-03-17 | 2003-09-30 | Albany Molecular Research, Inc. | 6-substituted biaryl purine derivatives as potent cyclin/CDK inhibitors and antiproliferative agents |
| GB9907658D0 (en) | 1999-04-06 | 1999-05-26 | Zeneca Ltd | Chemical compounds |
| GB9914258D0 (en) | 1999-06-18 | 1999-08-18 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9919778D0 (en) | 1999-08-21 | 1999-10-27 | Zeneca Ltd | Chemical compounds |
| GB9924862D0 (en) | 1999-10-20 | 1999-12-22 | Celltech Therapeutics Ltd | Chemical compounds |
| JP2003512467A (ja) | 1999-10-27 | 2003-04-02 | ノバルティス アクチエンゲゼルシャフト | チアゾールおよびイミダゾ（４，５−ｂ）ピリジン化合物ならびにそれらの医薬用途 |
| MXPA02005106A (es) | 1999-11-22 | 2002-11-07 | Smithkline Beecham Plc | Compuestos novedosos. |
| US7101869B2 (en) | 1999-11-30 | 2006-09-05 | Pfizer Inc. | 2,4-diaminopyrimidine compounds useful as immunosuppressants |
| IL150420A0 (en) | 1999-12-28 | 2002-12-01 | Pharmacopeia Inc | Pyrimidine and triazine kinase inhibitors |
| AU2001237041B9 (en) | 2000-02-17 | 2005-07-28 | Amgen Inc. | Kinase inhibitors |
| GB0004887D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004886D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004888D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0007371D0 (en) | 2000-03-28 | 2000-05-17 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0016877D0 (en) | 2000-07-11 | 2000-08-30 | Astrazeneca Ab | Chemical compounds |
| GB0021726D0 (en) | 2000-09-05 | 2000-10-18 | Astrazeneca Ab | Chemical compounds |
| US7122544B2 (en) | 2000-12-06 | 2006-10-17 | Signal Pharmaceuticals, Llc | Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto |
| US7129242B2 (en) | 2000-12-06 | 2006-10-31 | Signal Pharmaceuticals, Llc | Anilinopyrimidine derivatives as JNK pathway inhibitors and compositions and methods related thereto |
| GB0103926D0 (en) | 2001-02-17 | 2001-04-04 | Astrazeneca Ab | Chemical compounds |
| MEP13408A (en) | 2001-05-29 | 2010-06-10 | Bayer Schering Pharma Ag | Cdk inhibiting pyrimidines, production thereof and their use as medicaments |
| GB0113041D0 (en) | 2001-05-30 | 2001-07-18 | Astrazeneca Ab | Chemical compounds |
| BR0213899A (pt) | 2001-11-07 | 2004-08-31 | Hoffmann La Roche | Aminopirimidinas e aminopiridinas |
| GB0215844D0 (en) | 2002-07-09 | 2002-08-14 | Novartis Ag | Organic compounds |
| DE10349423A1 (de) | 2003-10-16 | 2005-06-16 | Schering Ag | Sulfoximinsubstituierte Parimidine als CDK- und/oder VEGF-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel |
| JP2007517825A (ja) | 2004-01-09 | 2007-07-05 | ノバルティス アクチエンゲゼルシャフト | Ｉｇｆ−ｉｒ阻害剤としてのフェニル−［４−（３−フェニル−１ｈ−ピラゾル−４−イル）−ピリミジン−２−イル］−アミン誘導体 |
| JP2008514571A (ja) | 2004-09-29 | 2008-05-08 | バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト | 細胞周期−キナーゼまたはレセプター−チロシン−キナーゼインヒビターとしての置換２−置換アニリノピリミジン類、それらの製造および薬剤としての使用 |
| CN101039919A (zh) | 2004-10-13 | 2007-09-19 | 惠氏公司 | 经n－苯磺酰基取代的苯胺基嘧啶类似物 |
| CN101321531A (zh) | 2005-10-03 | 2008-12-10 | 阿斯利康(瑞典)有限公司 | 嘧啶衍生物在制备用于预防和/或治疗阿尔茨海默病的药物中的用途 |
| TW200815418A (en) | 2006-06-27 | 2008-04-01 | Astrazeneca Ab | New compounds I |
| TW200815417A (en) | 2006-06-27 | 2008-04-01 | Astrazeneca Ab | New compounds II |
-
2006
- 2006-09-29 US US12/088,678 patent/US7745428B2/en not_active Expired - Fee Related
- 2006-09-29 EP EP06779577A patent/EP1934213A1/en not_active Withdrawn
- 2006-09-29 AR ARP060104322A patent/AR056556A1/es not_active Application Discontinuation
- 2006-09-29 UY UY29826A patent/UY29826A1/es not_active Application Discontinuation
- 2006-09-29 CN CNA2006800361639A patent/CN101277956A/zh active Pending
- 2006-09-29 JP JP2008532872A patent/JP2009512636A/ja active Pending
- 2006-09-29 BR BRPI0616722-5A patent/BRPI0616722A2/pt not_active Application Discontinuation
- 2006-09-29 KR KR1020087009591A patent/KR20080049130A/ko not_active Withdrawn
- 2006-09-29 TW TW095136339A patent/TW200728290A/zh unknown
- 2006-09-29 AU AU2006296386A patent/AU2006296386A1/en not_active Abandoned
- 2006-09-29 CA CA002623374A patent/CA2623374A1/en not_active Abandoned
- 2006-09-29 WO PCT/GB2006/003623 patent/WO2007036732A1/en not_active Ceased
-
2008
- 2008-03-04 IL IL189916A patent/IL189916A0/en unknown
- 2008-03-05 NO NO20081162A patent/NO20081162L/no not_active Application Discontinuation
- 2008-03-18 ZA ZA200802497A patent/ZA200802497B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2007036732A1 (en) | 2007-04-05 |
| NO20081162L (no) | 2008-04-23 |
| UY29826A1 (es) | 2007-04-30 |
| BRPI0616722A2 (pt) | 2012-12-25 |
| TW200728290A (en) | 2007-08-01 |
| EP1934213A1 (en) | 2008-06-25 |
| AU2006296386A1 (en) | 2007-04-05 |
| ZA200802497B (en) | 2009-03-25 |
| CN101277956A (zh) | 2008-10-01 |
| JP2009512636A (ja) | 2009-03-26 |
| IL189916A0 (en) | 2008-08-07 |
| KR20080049130A (ko) | 2008-06-03 |
| US20090054409A1 (en) | 2009-02-26 |
| US7745428B2 (en) | 2010-06-29 |
| CA2623374A1 (en) | 2007-04-05 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR056556A1 (es) | Imidazo(1,2-a)piridina con actividad antiproliferacion celular | |
| AR041594A1 (es) | Derivados de 1,4 piperidina disustituida y su uso como inhibidores de 11-beta hidroxiesteroide dehidrogenasa tipo 1 | |
| AR055249A1 (es) | Derivados de quinazolinas, procesos de obtencion y composiciones farmaceuticas | |
| AR056210A1 (es) | 4-(3-aminopirazol)pirimidina para uso como inhibidores de tirosina-quinasa | |
| AR050545A1 (es) | Derivados de quinazolinonas y su uso como inhibidores de b-raf | |
| AR064208A1 (es) | Derivados de piridin-3-il-quinazolinas como inhibidores de b-raf. procesos de obtencion y composiciones farmaceuticas. | |
| AR052170A1 (es) | Derivados de pirimidina utiles por su actividad anti-proliferacion celular | |
| AR070493A1 (es) | Derivados heterociclicos de urea, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de infecciones bacterianas. | |
| AR072047A1 (es) | Compuestos heterociclicos utiles para inhibir la adn girasa | |
| AR054183A1 (es) | Derivados de piridincarboxamida y su uso como agentes anticancerigenos. procesos de obtencion y composiciones farmaceuticas. | |
| AR033836A1 (es) | Compuesto 2-anilino-(imidazol-5-il)-pirimidina, composicion farmaceutica que lo comprende, su uso en la fabricacion de un medicamento que produce un efecto inhibitorio del ciclo celular y un proceso para su preparacion | |
| AR053683A1 (es) | Derivados de piperidina con actividad antibacteriana | |
| AR046779A1 (es) | Derivados de pirazol, metodos para su preparacion y usos de los mismos en la fabricacion de composiciones farmaceuticas y medicamentos que los contienen con actividad inhibitoria de trk para el tratamiento o profilaxis del cancer. | |
| AR053992A1 (es) | Compuestos quimicos con actividad anticancerosa, un procedimiento para su preparacion, su uso en la preparacion de medicamentos y composicion farmaceutica. | |
| AR046615A1 (es) | Pirrolidinas 3-(benzoil)-n-aciladas, como inhibidores de 11-beta-hsd1, utiles en el tratamiento de desordenes metabolicos | |
| AR046616A1 (es) | Piperidinas sustituidas utiles en el tratamiento de sindrome metabolico | |
| AR061653A1 (es) | Compuestos inhibidores de gsk3(glucogeno sintasa quinasa 3) | |
| AR056354A1 (es) | DERIVADOS DE PIRAZOL, UN MÉTODO DE PREPARACIoN DEL COMPUESTO, COMPOSICIoN FARMACÉUTICA Y PREPARACIoN DE UN MEDICAMENTO | |
| AR031075A1 (es) | Compuesto derivado de pirimidina, proceso para prepararlo, composicion farmaceutica que lo comprende y el uso de dicho compuesto en la fabricacion de un medicamento util en el tratamiento de cancer | |
| AR064130A1 (es) | Derivados de tiazoles y piridinas como antibacterianos. composiciones farmaceuticas. | |
| AR056184A1 (es) | Compuestos derivados de pirazol, composicion farmaceutica en base a aquellos y su uso para la fabricacion de medicamentos | |
| UY29058A1 (es) | Compuestos de isoindolona y su uso como potenciadores del receptor metabotropico de glutamato | |
| AR031251A1 (es) | Derivado de pirimidina, composicion farmaceutica que lo comprende, su uso en la fabricacion de un medicamento y proceso de preparacion | |
| AR072045A1 (es) | Derivados heterociclicos de urea y metodos para utilizarlos | |
| AR061118A1 (es) | Derivados de pirimidina, un proceso para su preparacion, composiciones farmaceuticas que los comprenden y el uso de los mismos en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la inhibicion de cdk2. |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |