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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (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 (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 |
|---|---|---|---|---|
| MX2009005071A (es) * | 2006-11-13 | 2009-05-25 | Novartis Ag | Compuestos de pirazol y triazol sustituidos como inhibidores de ksp. |
| US7820646B2 (en) * | 2007-01-05 | 2010-10-26 | Novartis Vaccines And Diagnostics, Inc. | Cyclized derivatives as Eg-5 inhibitors |
| BRPI0818605A2 (pt) | 2007-10-19 | 2015-04-22 | Schering Corp | Derivados de 1,3,4-tiadiazl espiro-condensados para inibir a atividade de ksp cinesima |
| US8252832B2 (en) * | 2007-12-14 | 2012-08-28 | Novartis Ag | Kinesin inhibitors as cancer therapeutics |
| US8546434B2 (en) | 2010-04-15 | 2013-10-01 | Novartis Ag | Triazole compounds as KSP inhibitors |
| US9498540B2 (en) | 2013-03-15 | 2016-11-22 | Novartis Ag | Cell proliferation inhibitors and conjugates thereof |
| WO2014151030A1 (en) * | 2013-03-15 | 2014-09-25 | Novartis Ag | Cell proliferation inhibitors and conjugates thereof |
| NZ720736A (en) * | 2013-12-23 | 2020-08-28 | Bayer Pharma AG | Antibody drug conjugates (adcs) with kinesin spindel protein (ksp) |
| WO2016020791A1 (en) | 2014-08-05 | 2016-02-11 | Novartis Ag | Ckit antibody drug conjugates |
| CN108025084A (zh) * | 2015-06-22 | 2018-05-11 | 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） |
| JP7022707B2 (ja) | 2016-06-15 | 2022-02-18 | バイエル・ファルマ・アクティエンゲゼルシャフト | Ｋｓｐ阻害剤および抗ｃｄ１２３抗体を含む特異的抗体－薬物－コンジュゲート（ａｄｃ） |
| KR102583006B1 (ko) | 2016-12-21 | 2023-09-27 | 바이엘 파마 악티엔게젤샤프트 | 효소적으로 절단가능한 기를 갖는 항체 약물 접합체 (adc) |
| CN110072556B (zh) | 2016-12-21 | 2023-05-02 | 拜耳制药股份公司 | 具有ksp抑制剂的特异性抗体药物缀合物(adc) |
| SG11202012608VA (en) | 2018-06-18 | 2021-02-25 | Bayer Ag | Binder/active agent conjugates directed against cxcr5, having enzymatically cleavable linkers and improved activity profile |
| 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 |
| JP2001505585A (ja) | 1996-12-16 | 2001-04-24 | 藤沢薬品工業株式会社 | 新規アミド化合物およびそれらの一酸化窒素シンターゼ阻害剤としての用途 |
| US6117940A (en) | 1997-10-17 | 2000-09-12 | Mjalli; Adnan M. M. | Amino-ketone solid support templates |
| PT1086086E (pt) * | 1998-06-12 | 2005-02-28 | Sod Conseils Rech Applic | Derivados imidazolilo e sua utilizacao como ligandos de receptores da somatostatina |
| US6545004B1 (en) * | 1999-10-27 | 2003-04-08 | Cytokinetics, Inc. | Methods and compositions utilizing quinazolinones |
| ES2263501T3 (es) * | 1999-10-27 | 2006-12-16 | Cytokinetics, Inc. | Procedimiento y composiciones que utilizan quinazolinonas. |
| 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 |
| JP2004518613A (ja) * | 2000-08-01 | 2004-06-24 | ソシエテ・ドゥ・コンセイユ・ドゥ・ルシェルシュ・エ・ダプリカーション・シャンティフィック・エス・ア・エス | イミダゾリル誘導体 |
| 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 |
| DE10211770A1 (de) | 2002-03-14 | 2003-10-02 | Boehringer Ingelheim Pharma | Neue substituierte Piperidine, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung |
| 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 |
| WO2004103282A2 (en) * | 2003-05-15 | 2004-12-02 | 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 |
| EP1765789B1 (en) * | 2004-06-18 | 2013-02-27 | Novartis AG | N-(1-(1-benzyl-4-phenyl-1h-imidazol-2-yl)-2,2-dimethylpropyl)benzamide derivatives and related compounds as kinesin spindle protein (ksp) inhibitors for the treatment of cancer |
-
2006
- 2006-08-08 MY MYPI20063824A patent/MY147188A/en unknown
- 2006-08-08 TW TW095129062A patent/TW200800951A/zh unknown
- 2006-08-09 AU AU2006279991A patent/AU2006279991B2/en not_active Ceased
- 2006-08-09 WO PCT/US2006/031129 patent/WO2007021794A1/en active Application Filing
- 2006-08-09 KR KR1020087003946A patent/KR20080036611A/ko not_active Application Discontinuation
- 2006-08-09 EP EP06789653A patent/EP1912972B1/en active Active
- 2006-08-09 CA CA002618747A patent/CA2618747A1/en not_active Abandoned
- 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 ES ES06789653T patent/ES2374449T3/es active Active
- 2006-08-09 PT PT06789653T patent/PT1912972E/pt unknown
- 2006-08-09 PE PE2006000968A patent/PE20070352A1/es not_active Application Discontinuation
- 2006-08-09 AR ARP060103489A patent/AR056025A1/es not_active Application Discontinuation
- 2006-08-09 GT GT200600366A patent/GT200600366A/es unknown
- 2006-08-09 JP JP2008526175A patent/JP4975745B2/ja not_active Expired - Fee Related
- 2006-08-09 RU RU2008108939/04A patent/RU2413721C9/ru not_active IP Right Cessation
- 2006-08-09 AT AT06789653T patent/ATE526324T1/de active
- 2006-08-09 CN CNA2006800293472A patent/CN101253167A/zh active Pending
- 2006-08-09 PL PL06789653T patent/PL1912972T3/pl unknown
-
2008
- 2008-06-26 HK HK08107126.4A patent/HK1111995A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| AU2006279991B2 (en) | 2011-09-29 |
| AR056025A1 (es) | 2007-09-12 |
| AU2006279991A1 (en) | 2007-02-22 |
| CA2618747A1 (en) | 2007-02-22 |
| ATE526324T1 (de) | 2011-10-15 |
| PT1912972E (pt) | 2012-01-06 |
| PL1912972T3 (pl) | 2012-02-29 |
| BRPI0614547A2 (pt) | 2011-03-29 |
| KR20080036611A (ko) | 2008-04-28 |
| US20070037853A1 (en) | 2007-02-15 |
| MY147188A (en) | 2012-11-14 |
| CN101253167A (zh) | 2008-08-27 |
| RU2413721C9 (ru) | 2011-05-20 |
| HK1111995A1 (en) | 2008-08-22 |
| RU2413721C2 (ru) | 2011-03-10 |
| EP1912972B1 (en) | 2011-09-28 |
| JP4975745B2 (ja) | 2012-07-11 |
| US7626040B2 (en) | 2009-12-01 |
| TW200800951A (en) | 2008-01-01 |
| WO2007021794A1 (en) | 2007-02-22 |
| JP2009504664A (ja) | 2009-02-05 |
| RU2008108939A (ru) | 2009-09-20 |
| EP1912972A1 (en) | 2008-04-23 |
| ES2374449T3 (es) | 2012-02-16 |
| GT200600366A (es) | 2007-05-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |