PE20070352A1 - Compuestos de imidazol sustituidos como inhibidores de ksp - Google Patents
Compuestos de imidazol sustituidos como inhibidores de kspInfo
- Publication number
- PE20070352A1 PE20070352A1 PE2006000968A PE2006000968A PE20070352A1 PE 20070352 A1 PE20070352 A1 PE 20070352A1 PE 2006000968 A PE2006000968 A PE 2006000968A PE 2006000968 A PE2006000968 A PE 2006000968A PE 20070352 A1 PE20070352 A1 PE 20070352A1
- Authority
- PE
- Peru
- Prior art keywords
- substituted
- alkyl
- imidazol
- aminopropyl
- carboxamide
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- RAXXELZNTBOGNW-UHFFFAOYSA-N 1H-imidazole Chemical group C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 title 1
- -1 AMINO Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- WGYKZJWCGVVSQN-UHFFFAOYSA-N propylamine Chemical class CCCN WGYKZJWCGVVSQN-UHFFFAOYSA-N 0.000 abstract 3
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical class O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 102000010638 Kinesin Human genes 0.000 abstract 1
- 108010063296 Kinesin Proteins 0.000 abstract 1
- 210000000481 breast Anatomy 0.000 abstract 1
- 208000020816 lung neoplasm Diseases 0.000 abstract 1
- 208000025113 myeloid leukemia Diseases 0.000 abstract 1
- 210000000496 pancreas Anatomy 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- JSPCTNUQYWIIOT-UHFFFAOYSA-N piperidine-1-carboxamide Chemical compound NC(=O)N1CCCCC1 JSPCTNUQYWIIOT-UHFFFAOYSA-N 0.000 abstract 1
- 210000002784 stomach Anatomy 0.000 abstract 1
- 150000003573 thiols Chemical class 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
SE REFIERE A UN COMPUESTO DE FORMULA I DONDE R1 ES AMINOACILO, CARBOXILO, ALQUILO C1-C6, ENTRE OTROS; R2 ES H, ALQUILO C1-C6, ARILO C6-C14; R3 Y R4 SON CADA UNO H, OH, ALQUILO C1-C6 OPCIONALMENTE SUSTITUIDO CON NH2, CN, HALOGENO, NITRO, ENTRE OTROS, CICLOALQUILO C3-C10 OPCIONALMENTE SUSTITUIDO CON OXO, TIOXO, NH2, ENTRE OTROS; R5 ES H, ALQUILO C1-C6 SUSTITUIDO O NO CON NH2, CN, HALOGENO, NITRO, ENTRE OTROS, ALQUENILO C2-C6 SUSTITUIDO O NO, ENTRE OTROS; R6 Y R7 SON CADA UNO CICLOALQUILO C3-C10, ARILO C6-C14, HETEROARILO, ENTRE OTROS; R8 ES L-A1; L ES ALQUILENO C1-C5 SUSTITUIDO O NO CON OH, HALO, ACILAMINO, S(O)q; q ES 1-4; A1 ES ARILO C6-C14, HETEROARILO, HETEROCICLICO, CICLOALQUILO C3-C10 SUSTITUIDO O NO CON OH, NH2, CN, TIOL, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-(3-AMINOPROPIL)-N-{(1R)-1-[1-BENCIL-4-(3-CLOROFENIL)-1H-IMIDAZOL-2-IL]-2-METILPROPIL}MORFOLIN-4-CARBOXAMIDA; N-(3-AMINOPROPIL)-N-{(1R)-1-[1-BENCIL-4-(3-CLOROFENIL)-1H-IMIDAZOL-2-IL]-2-METILPROPIL}PIPERIDIN-1-CARBOXAMIDA; N-(3-AMINOPROPIL)-N-[(1R)-1-(1-BENCIL-4-FENIL-1H-IMIDAZOL-2-IL)-2,2-DIMETILPROPIL]PIPERIDIN-1-CARBOXAMIDA; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA PROTEINA QUINESINA DEL HUSO (KSP) SIENDO UTILES EN EL TRATAMIENTO DE CANCER DE PULMON, DE MAMA, DE PANCREAS, DE ESTOMAGO, LEUCEMIA MIELOIDE
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US70690105P | 2005-08-09 | 2005-08-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20070352A1 true PE20070352A1 (es) | 2007-05-30 |
Family
ID=37421032
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2006000968A PE20070352A1 (es) | 2005-08-09 | 2006-08-09 | Compuestos de imidazol sustituidos como inhibidores de ksp |
Country Status (19)
| 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) |
| 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 (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2007323998B2 (en) * | 2006-11-13 | 2011-09-22 | Novartis Ag | Substituted pyrazole and triazole compounds as KSP inhibitors |
| GEP20125415B (en) * | 2007-01-05 | 2012-03-12 | Novartis Ag | Imidazole derivatives as kinesin spindle protein inhibitors (eg-5) |
| MX2010004312A (es) | 2007-10-19 | 2010-07-05 | Schering Corp | Derivados de 1,3,4-tiadiazol espiro-condensados para inhibir la actividad de quinesina de la proteina de quinesina del huso. |
| US8252832B2 (en) * | 2007-12-14 | 2012-08-28 | Novartis Ag | Kinesin inhibitors as cancer therapeutics |
| EA201201404A1 (ru) | 2010-04-15 | 2013-04-30 | Новартис Аг | Триазолы как ингибиторы кбв (кинезин-белок веретена) |
| US9498540B2 (en) | 2013-03-15 | 2016-11-22 | Novartis Ag | Cell proliferation inhibitors and conjugates thereof |
| EP2968591A1 (en) * | 2013-03-15 | 2016-01-20 | Novartis AG | Cell proliferation inhibitors and conjugates thereof |
| KR102329024B1 (ko) * | 2013-12-23 | 2021-11-19 | 바이엘 파마 악티엔게젤샤프트 | 키네신 스핀들 단백질(ksp)과의 항체 약물 접합체 (adcs) |
| US10786578B2 (en) | 2014-08-05 | 2020-09-29 | Novartis Ag | CKIT antibody drug conjugates |
| EP3310440A1 (de) * | 2015-06-22 | 2018-04-25 | Bayer Pharma Aktiengesellschaft | Binder-wirkstoff-konjugate (adcs) und binder-prodrug-konjugate (apdcs) mit enzymatisch spaltbaren gruppen |
| CA2990398A1 (en) * | 2015-06-23 | 2016-12-29 | Bayer Pharma Aktiengesellschaft | Antibody drug conjugates of kinesin spindel protein (ksp) inhibitors with anti-cd123-antibodies |
| US11001636B2 (en) | 2016-06-15 | 2021-05-11 | Bayer Pharma Aktiengesellschaft | Specific antibody-drug-conjugates (ADCs) with KSP inhibitors and anti-CD123-antibodies |
| JP7030811B2 (ja) | 2016-12-21 | 2022-03-07 | バイエル・ファルマ・アクティエンゲゼルシャフト | Ｋｓｐ阻害剤を有する特異的抗体－薬物コンジュゲート（ａｄｃ） |
| CN116327974A (zh) | 2016-12-21 | 2023-06-27 | 拜耳制药股份公司 | 具有酶促可裂解基团的抗体-药物-缀合物(adc) |
| CN112601553A (zh) | 2018-06-18 | 2021-04-02 | 拜耳股份有限公司 | 具有可酶切的接头和改善的活性谱的针对cxcr5的结合剂-药物缀合物 |
| 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 (20)
| Publication number | Priority date | Publication date | Assignee | Title |
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| 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 |
| WO1998027108A2 (en) | 1996-12-16 | 1998-06-25 | Fujisawa Pharmaceutical Co., Ltd. | New amide compounds and their use as nitric oxide synthase inhibitors |
| US6117940A (en) | 1997-10-17 | 2000-09-12 | Mjalli; Adnan M. M. | Amino-ketone solid support templates |
| CN1319094A (zh) * | 1998-06-12 | 2001-10-24 | 研究及应用科学协会股份有限公司 | 咪唑基衍生物 |
| WO2001030768A1 (en) * | 1999-10-27 | 2001-05-03 | Cytokinetics, Inc. | Methods and compositions utilizing quinazolinones |
| US6545004B1 (en) * | 1999-10-27 | 2003-04-08 | Cytokinetics, Inc. | Methods and compositions utilizing quinazolinones |
| WO2001083575A1 (en) | 2000-05-02 | 2001-11-08 | Advanced Syntech, Llc A Kentucky Limited Liability Corporation | A novel solid support template for preparation of highly functionalized heterocycle compounds |
| EP1305294B1 (en) * | 2000-08-01 | 2007-04-25 | Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) | 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 |
| RU2005100783A (ru) * | 2002-06-14 | 2005-07-20 | Мерк энд Ко., Инк. (US) | Ингибиторы митотического кинезина |
| WO2004071448A2 (en) | 2003-02-12 | 2004-08-26 | Transtech Pharma Inc. | Substituted azole derivatives as inhibitors of protein tyrosine phosphatases |
| US20080021079A1 (en) * | 2003-05-07 | 2008-01-24 | Han-Jie Zhou | Compounds, Compositions, and Methods |
| US20070032536A1 (en) * | 2003-05-15 | 2007-02-08 | Xianping Qian | Compounds, compositions and methods |
| MXPA06011884A (es) | 2004-04-14 | 2006-12-14 | Pfizer | Compuestos de imidazol unidos a azufre para el tratamiento del virus de inmunodeficiencia humana. |
| US7618981B2 (en) | 2004-05-06 | 2009-11-17 | Cytokinetics, Inc. | Imidazopyridinyl-benzamide anti-cancer agents |
| JP4836280B2 (ja) * | 2004-06-18 | 2011-12-14 | ノバルティス バクシンズ アンド ダイアグノスティックス，インコーポレーテッド | 癌を治療するためのキネシンスピンドルタンパク質（ｋｓｐ）阻害剤としてのｎ−（１−（１−ベンジル−４−フェニル−１ｈ−イミダゾール−２−イル）−２，２−ジメチルプロピル）ベンズアミド誘導体および関連化合物 |
-
2006
- 2006-08-08 MY MYPI20063824A patent/MY147188A/en unknown
- 2006-08-08 TW TW095129062A patent/TW200800951A/zh unknown
- 2006-08-09 PE PE2006000968A patent/PE20070352A1/es not_active Application Discontinuation
- 2006-08-09 AU AU2006279991A patent/AU2006279991B2/en not_active Ceased
- 2006-08-09 JP JP2008526175A patent/JP4975745B2/ja not_active Expired - Fee Related
- 2006-08-09 AR ARP060103489A patent/AR056025A1/es not_active Application Discontinuation
- 2006-08-09 KR KR1020087003946A patent/KR20080036611A/ko not_active Ceased
- 2006-08-09 PL PL06789653T patent/PL1912972T3/pl unknown
- 2006-08-09 BR BRPI0614547-7A patent/BRPI0614547A2/pt not_active IP Right Cessation
- 2006-08-09 US US11/502,303 patent/US7626040B2/en not_active Expired - Fee Related
- 2006-08-09 PT PT06789653T patent/PT1912972E/pt unknown
- 2006-08-09 GT GT200600366A patent/GT200600366A/es unknown
- 2006-08-09 WO PCT/US2006/031129 patent/WO2007021794A1/en not_active Ceased
- 2006-08-09 AT AT06789653T patent/ATE526324T1/de active
- 2006-08-09 ES ES06789653T patent/ES2374449T3/es active Active
- 2006-08-09 RU RU2008108939/04A patent/RU2413721C9/ru not_active IP Right Cessation
- 2006-08-09 CA CA002618747A patent/CA2618747A1/en not_active Abandoned
- 2006-08-09 CN CNA2006800293472A patent/CN101253167A/zh active Pending
- 2006-08-09 EP EP06789653A patent/EP1912972B1/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US20070037853A1 (en) | 2007-02-15 |
| KR20080036611A (ko) | 2008-04-28 |
| AR056025A1 (es) | 2007-09-12 |
| AU2006279991B2 (en) | 2011-09-29 |
| RU2413721C9 (ru) | 2011-05-20 |
| MY147188A (en) | 2012-11-14 |
| PL1912972T3 (pl) | 2012-02-29 |
| JP4975745B2 (ja) | 2012-07-11 |
| GT200600366A (es) | 2007-05-10 |
| BRPI0614547A2 (pt) | 2011-03-29 |
| AU2006279991A1 (en) | 2007-02-22 |
| US7626040B2 (en) | 2009-12-01 |
| EP1912972B1 (en) | 2011-09-28 |
| CN101253167A (zh) | 2008-08-27 |
| RU2008108939A (ru) | 2009-09-20 |
| JP2009504664A (ja) | 2009-02-05 |
| EP1912972A1 (en) | 2008-04-23 |
| HK1111995A1 (en) | 2008-08-22 |
| ATE526324T1 (de) | 2011-10-15 |
| WO2007021794A1 (en) | 2007-02-22 |
| ES2374449T3 (es) | 2012-02-16 |
| PT1912972E (pt) | 2012-01-06 |
| TW200800951A (en) | 2008-01-01 |
| RU2413721C2 (ru) | 2011-03-10 |
| CA2618747A1 (en) | 2007-02-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |