AR056025A1 - Compuestos de imidazol sustituidos como inhibidores de ksp - Google Patents
Compuestos de imidazol sustituidos como inhibidores de kspInfo
- Publication number
- AR056025A1 AR056025A1 ARP060103489A ARP060103489A AR056025A1 AR 056025 A1 AR056025 A1 AR 056025A1 AR P060103489 A ARP060103489 A AR P060103489A AR P060103489 A ARP060103489 A AR P060103489A AR 056025 A1 AR056025 A1 AR 056025A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- heterocyclic
- group
- alkyl
- aryl
- Prior art date
Links
- RAXXELZNTBOGNW-UHFFFAOYSA-N 1H-imidazole Chemical class C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 14
- 125000001072 heteroaryl group Chemical group 0.000 abstract 7
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 4
- 125000003107 substituted aryl group Chemical group 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 3
- 125000004442 acylamino group Chemical group 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000005017 substituted alkenyl group Chemical group 0.000 abstract 2
- 125000004426 substituted alkynyl group Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000000266 alpha-aminoacyl group Chemical group 0.000 abstract 1
- 239000002246 antineoplastic agent Substances 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- -1 carboxylester Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000005415 substituted alkoxy group Chemical group 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
-
- 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
- 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
- C07D403/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Abstract
Composiciones farmacéuticas que los contienen y usos terapéuticos como agentes anticáncer. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1) en donde: R1 se selecciona del grupo formado por aminoacilo, acilamino, carboxilo, carboxiléster, alquilo, y alquilo sustituido, con la salvedad de que alquilo sustituido no está sustituido con arilo o arilo sustituido; R2 se selecciona del grupo formado por H, alquilo, y arilo; R3 y R4 se seleccionan en forma independiente del grupo formado por H, hidroxi, alquilo, alquilo sustituido, cicloalquilo, cicloalquilo sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, heterocíclico, y heterocíclico sustituido, con la salvedad de que solo 1 de R3 o R4 es hidroxi; o R3 y R4 junto con el átomo de N al cual están unidos se unen para formar un heterocíclico o heterocíclico sustituido; R5 se selecciona del grupo formado por H, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, cicloalquilo, cicloalquilo sustituido, heterocíclico, heterocíclico sustituido, arilo, arilo sustituido, heteroarilo y heteroarilo sustituido; o R1 y R5, junto con los átomos de C y N unidos respectivamente a los mismos se unen para formar un grupo heterocíclico o heterocíclico sustituido; o cuando R1 y R5, junto con los átomos de C y N unidos respectivamente a los mismos, no forman un grupo heterocíclico, entonces R4 y R5, junto con los átomos unidos a los mismos, forman un grupo heterocíclico o heterocíclico sustituido; R8 se selecciona del grupo formado por L-A1, en donde L se selecciona del grupo formado por -S(O)q- donde q es uno o dos, y alquileno C1-5 opcionalmente sustituido con hidroxi, halo, o acilamino; y A1 se selecciona del grupo formado por arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, heterocíclico, heterocíclico sustituido, cicloalquilo, y cicloalquilo sustituido; y uno de cualquiera de R6 o R7 se selecciona del grupo formado por cicloalquilo, heterocíclico, arilo y heteroarilo, todos los cuales pueden estar opcionalmente sustituidos con -(R9)m donde R9 tiene los valores que se han definido y m es un entero entre 1 y 4, y el otro de R6 o R7 se selecciona del grupo formado por H, halo, y alquilo; R9 se selecciona del grupo formado por ciano, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, -CF3, alcoxi, alcoxi sustituido, halo, y hidroxi; y cuando m es un entero entre 2 y 4, entonces cada R9 pueden ser iguales o diferentes; o sus sales, ésteres o prodrogas aceptables para uso farmacéutico.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US70690105P | 2005-08-09 | 2005-08-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR056025A1 true AR056025A1 (es) | 2007-09-12 |
Family
ID=37421032
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060103489A AR056025A1 (es) | 2005-08-09 | 2006-08-09 | Compuestos de imidazol sustituidos como inhibidores de ksp |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US7626040B2 (es) |
| EP (1) | EP1912972B1 (es) |
| JP (1) | JP4975745B2 (es) |
| KR (1) | KR20080036611A (es) |
| CN (1) | CN101253167A (es) |
| AR (1) | AR056025A1 (es) |
| AT (1) | ATE526324T1 (es) |
| AU (1) | AU2006279991B2 (es) |
| BR (1) | BRPI0614547A2 (es) |
| CA (1) | CA2618747A1 (es) |
| ES (1) | ES2374449T3 (es) |
| GT (1) | GT200600366A (es) |
| HK (1) | HK1111995A1 (es) |
| MY (1) | MY147188A (es) |
| PE (1) | PE20070352A1 (es) |
| PL (1) | PL1912972T3 (es) |
| PT (1) | PT1912972E (es) |
| RU (1) | RU2413721C9 (es) |
| TW (1) | TW200800951A (es) |
| WO (1) | WO2007021794A1 (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2091926B1 (en) * | 2006-11-13 | 2015-10-21 | Novartis AG | Substituted pyrazole and triazole compounds as ksp inhibitors |
| JP2010515687A (ja) * | 2007-01-05 | 2010-05-13 | ノバルティス アーゲー | キネシンスピンドルタンパク質阻害剤（ｅｇ−５）としてのイミダゾール誘導体 |
| TW200934785A (en) | 2007-10-19 | 2009-08-16 | Schering Corp | Compounds for inhibiting KSP kinesin activity |
| US8252832B2 (en) * | 2007-12-14 | 2012-08-28 | Novartis Ag | Kinesin inhibitors as cancer therapeutics |
| CA2794406A1 (en) | 2010-04-15 | 2011-10-20 | Novartis Ag | Triazole compounds as ksp inhibitors |
| US9498540B2 (en) | 2013-03-15 | 2016-11-22 | Novartis Ag | Cell proliferation inhibitors and conjugates thereof |
| CN105451773A (zh) * | 2013-03-15 | 2016-03-30 | 诺华股份有限公司 | 细胞增殖抑制剂及其缀合物 |
| ES2815098T3 (es) * | 2013-12-23 | 2021-03-29 | Bayer Pharma AG | Conjugados de ligadores (ADCs) con inhibidores de KSP |
| WO2016020791A1 (en) | 2014-08-05 | 2016-02-11 | Novartis Ag | Ckit antibody drug conjugates |
| CN114917361A (zh) * | 2015-06-22 | 2022-08-19 | 拜耳医药股份有限公司 | 具有酶可裂解基团的抗体药物缀合物（adc）和抗体前药缀合物（apdc） |
| EP3919518A1 (en) | 2016-06-15 | 2021-12-08 | Bayer Pharma Aktiengesellschaft | Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies |
| EP3558387B1 (de) | 2016-12-21 | 2021-10-20 | Bayer Pharma Aktiengesellschaft | Spezifische antikörper-wirkstoff-konjugate (adcs) mit ksp-inhibitoren |
| PE20191235A1 (es) | 2016-12-21 | 2019-09-11 | Bayer Pharma AG | Conjugados de ligando-farmaco (adcs) con grupos escindibles enzimaticamente |
| EP3806908A1 (de) | 2018-06-18 | 2021-04-21 | Bayer Aktiengesellschaft | Gegen cxcr5 gerichtete binder-wirkstoff-konjugate mit enzymatisch spaltbaren linkern und verbessertem wirkungsprofil |
| CN109481436A (zh) * | 2018-08-21 | 2019-03-19 | 广东医科大学 | 血栓素a2合成酶抑制剂奥扎格雷在制备治疗吸烟所致肺癌药物中的应用 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4235871A (en) | 1978-02-24 | 1980-11-25 | Papahadjopoulos Demetrios P | Method of encapsulating biologically active materials in lipid vesicles |
| US4501728A (en) | 1983-01-06 | 1985-02-26 | Technology Unlimited, Inc. | Masking of liposomes from RES recognition |
| US4837028A (en) | 1986-12-24 | 1989-06-06 | Liposome Technology, Inc. | Liposomes with enhanced circulation time |
| US5011472A (en) | 1988-09-06 | 1991-04-30 | Brown University Research Foundation | Implantable delivery system for biological factors |
| EP0946587A2 (en) | 1996-12-16 | 1999-10-06 | Fujisawa Pharmaceutical Co., Ltd. | New amide compounds |
| US6117940A (en) | 1997-10-17 | 2000-09-12 | Mjalli; Adnan M. M. | Amino-ketone solid support templates |
| IL139835A (en) * | 1998-06-12 | 2005-11-20 | Sod Conseils Rech Applic | Imidazolyl derivatives and their use as somatostatin receptor ligands |
| MXPA02004162A (es) * | 1999-10-27 | 2003-08-20 | Cytokinetics Inc | Metodo y composiciones que utilizan quinazolinonas. |
| US6545004B1 (en) * | 1999-10-27 | 2003-04-08 | Cytokinetics, Inc. | Methods and compositions utilizing quinazolinones |
| AU2001227812A1 (en) | 2000-05-02 | 2001-11-12 | Advanced Syntech, Llc A Kentucky Limited Liability Corporation | A novel solid support template for preparation of highly functionalized heterocycle compounds |
| IL154222A0 (en) * | 2000-08-01 | 2003-07-31 | Sod Conseils Rech Applic | Imidazolyl derivatives |
| DE10211770A1 (de) | 2002-03-14 | 2003-10-02 | Boehringer Ingelheim Pharma | Neue substituierte Piperidine, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung |
| US7026312B2 (en) | 2002-03-14 | 2006-04-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Substituted piperidines, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof |
| WO2004071448A2 (en) | 2003-02-12 | 2004-08-26 | Transtech Pharma Inc. | Substituted azole derivatives as inhibitors of protein tyrosine phosphatases |
| WO2004100873A2 (en) * | 2003-05-07 | 2004-11-25 | Cytokinetics, Inc. | Compounds, compositions, and methods |
| EP1622878A4 (en) * | 2003-05-15 | 2008-04-09 | Cytokinetics Inc | COMPOUNDS, COMPOSITIONS AND METHODS |
| WO2005100322A1 (en) | 2004-04-14 | 2005-10-27 | Pfizer Limited | Sulphur-linked imidazole compounds for the treament of hiv |
| US7618981B2 (en) | 2004-05-06 | 2009-11-17 | Cytokinetics, Inc. | Imidazopyridinyl-benzamide anti-cancer agents |
| KR101170925B1 (ko) * | 2004-06-18 | 2012-08-07 | 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 | 암 치료용 키네신 방추 단백질 (ｋｓｐ) 억제제로서의ｎ-(1-(1-벤질-4-페닐-1ｈ-이미다졸-2-일)-2,2-디메틸프로필)벤자미드 유도체 및 관련 화합물 |
-
2006
- 2006-08-08 TW TW095129062A patent/TW200800951A/zh unknown
- 2006-08-08 MY MYPI20063824A patent/MY147188A/en unknown
- 2006-08-09 WO PCT/US2006/031129 patent/WO2007021794A1/en active Application Filing
- 2006-08-09 AR ARP060103489A patent/AR056025A1/es not_active Application Discontinuation
- 2006-08-09 CA CA002618747A patent/CA2618747A1/en not_active Abandoned
- 2006-08-09 JP JP2008526175A patent/JP4975745B2/ja not_active Expired - Fee Related
- 2006-08-09 ES ES06789653T patent/ES2374449T3/es active Active
- 2006-08-09 GT GT200600366A patent/GT200600366A/es unknown
- 2006-08-09 AT AT06789653T patent/ATE526324T1/de active
- 2006-08-09 BR BRPI0614547-7A patent/BRPI0614547A2/pt not_active IP Right Cessation
- 2006-08-09 KR KR1020087003946A patent/KR20080036611A/ko not_active Application Discontinuation
- 2006-08-09 RU RU2008108939/04A patent/RU2413721C9/ru not_active IP Right Cessation
- 2006-08-09 PL PL06789653T patent/PL1912972T3/pl unknown
- 2006-08-09 PE PE2006000968A patent/PE20070352A1/es not_active Application Discontinuation
- 2006-08-09 CN CNA2006800293472A patent/CN101253167A/zh active Pending
- 2006-08-09 AU AU2006279991A patent/AU2006279991B2/en not_active Ceased
- 2006-08-09 PT PT06789653T patent/PT1912972E/pt unknown
- 2006-08-09 EP EP06789653A patent/EP1912972B1/en active Active
- 2006-08-09 US US11/502,303 patent/US7626040B2/en not_active Expired - Fee Related
-
2008
- 2008-06-26 HK HK08107126.4A patent/HK1111995A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| WO2007021794A1 (en) | 2007-02-22 |
| US7626040B2 (en) | 2009-12-01 |
| KR20080036611A (ko) | 2008-04-28 |
| TW200800951A (en) | 2008-01-01 |
| ATE526324T1 (de) | 2011-10-15 |
| JP4975745B2 (ja) | 2012-07-11 |
| ES2374449T3 (es) | 2012-02-16 |
| EP1912972A1 (en) | 2008-04-23 |
| PT1912972E (pt) | 2012-01-06 |
| HK1111995A1 (en) | 2008-08-22 |
| JP2009504664A (ja) | 2009-02-05 |
| CN101253167A (zh) | 2008-08-27 |
| PE20070352A1 (es) | 2007-05-30 |
| RU2413721C9 (ru) | 2011-05-20 |
| EP1912972B1 (en) | 2011-09-28 |
| AU2006279991A1 (en) | 2007-02-22 |
| RU2008108939A (ru) | 2009-09-20 |
| US20070037853A1 (en) | 2007-02-15 |
| BRPI0614547A2 (pt) | 2011-03-29 |
| MY147188A (en) | 2012-11-14 |
| AU2006279991B2 (en) | 2011-09-29 |
| CA2618747A1 (en) | 2007-02-22 |
| RU2413721C2 (ru) | 2011-03-10 |
| PL1912972T3 (pl) | 2012-02-29 |
| GT200600366A (es) | 2007-05-10 |
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