AR036175A1 - Derivados de la dolastatina 10, composiciones farmaceuticas que los comprenden, el uso de dichos compuestos en la preparacion de medicamentos, procesos para la preparacion de dichos compuestos, e intermediarios utiles en la preparacion de dichos compuestos - Google Patents
Derivados de la dolastatina 10, composiciones farmaceuticas que los comprenden, el uso de dichos compuestos en la preparacion de medicamentos, procesos para la preparacion de dichos compuestos, e intermediarios utiles en la preparacion de dichos compuestosInfo
- Publication number
- AR036175A1 AR036175A1 ARP020102678A ARP020102678A AR036175A1 AR 036175 A1 AR036175 A1 AR 036175A1 AR P020102678 A ARP020102678 A AR P020102678A AR P020102678 A ARP020102678 A AR P020102678A AR 036175 A1 AR036175 A1 AR 036175A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- compounds
- dioxolyl
- alkoxy
- amino
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/05—Dipeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0205—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Biochemistry (AREA)
- Engineering & Computer Science (AREA)
- Crystallography & Structural Chemistry (AREA)
- Epidemiology (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Derivados de la dolastatina 10 de la fórmula (1), en donde R1, R2 y R3 son cada uno independientemente hidrógeno ó alquilo C1-4; R4 es hidrógeno; alquilo sustituido opcionalmente con uno a tres sustituyentes seleccionados del grupo consistente en hidroxilo, alcoxilo, amino, mono- o dialquilamino, carboxilo, alcoxicarbonilo, carbamoiloxilo, alquilcarboniloxilo, carbamoilo o halógeno; alquenilo; alquinilo; cicloalquilo C3-7; arilo sustituido opcionalmente con uno a tres sustituyentes seleccionados del grupo consistente en halógeno, alcoxicarbonilo, carbamoilo, sulfamoilo, alquilcarboniloxilo, ciano, mono- o dialquilamino, alquilo, alcoxilo, fenilo, fenoxilo, trifluorometilo, trifluorometoxilo, tioalquilo, hidroxilo, alquilcarbonilamino, heterociclilo, 1,3-dioxolilo, 1,4-dioxolilo, amino o bencilo; aralquilo con el grupo arilo sustituido opcionalmente con uno a tres sustituyentes seleccionados del grupo consistente en halógeno, alcoxicarbonilo, sulfamoilo, alquilcarboniloxilo, ciano, mono- o dialquilamino, alquilo, alcoxilo, fenilo, fenoxilo, trifluorometilo, trifluorometoxilo, tioalquilo, hidroxilo, alquilcarbonilamino, heterociclilo, 1,3-dioxolilo, 1,4-dioxolilo, amino o bencilo; o heterociclilalquilo; R5 es alquil C1-6-amino; hidroxilo; cicloalquil C3-7-amino sustituido opcionalmente por fenilo o bencilo; arilamino; aralquilamino con alquileno C1-4 y el grupo arilo sustituido opcionalmente con uno a tres sustituyentes seleccionados del grupo consistente en halógeno, alcoxicarbonilo, sulfamoilo, alquilcarboniloxilo, carbamoiloxilo, ciano, mono- o dialquilamino, alquilo, alcoxilo, fenilo, fenoxilo, trifluorometilo, trifluorometoxilo, tioalquilo, hidroxilo, alquilcarbonilamino, heterociclilo, 1,3-dioxolilo, 1,4-dioxolilo, amino o bencilo; alcoxilo C1-4; benzhidrazino; heterociclilo sustituido opcionalmente con uno a tres sustituyentes seleccionados del grupo consistente en bencilo, benzhidrilo, alquilo, hidroxilo, alcoxilo, alquilcarbamoiloxilo, amino, mono- o dialquilamino, acilamino, alcoxicarbonilamino, fenilo o halógeno; heterociclilamino; heterocicloalquilamino con el grupo heterociclilo sustituido opcionalmente con uno a tres sustituyentes seleccionados del grupo consistente en bencilo, benzhidrilo, alquilo, hidroxilo, alcoxilo, alquilcarbamoiloxilo, amino, dialquilamino, acilamino, alcoxicarbonilamino o halógeno; aralquiloxilo y aralquilo ambos sustituidos opcionalmente con uno a tres sustituyentes del grupo consistente en halógeno, alcoxicarbonilo, sulfamoilo, alquilcarboniloxilo, ciano, mono- o dialquilamino, alquilo, alcoxilo, fenilo, fenoxilo, trifluorometilo, trifluorometoxilo, tioalquilo, hidroxilo, alquilcarbonilamino, heterociclilo, 1,3-dioxolilo, 1,4-dioxolilo, amino, aminosulfonilo o bencilo; y n es un número entero de 0, 1 ó 2; y las sales farmacéuticamente aceptables de los mismos. Dichos compuestos tienen actividad antitumoral y son útiles para el tratamiento de enfermedades malignas, particularmente cáncer colorrectal, cáncer de pulmón, cáncer de mama, cáncer de estómago, cáncer cervical y cáncer de vejiga. Composiciones farmacéuticas que los comprenden, uso de dichos compuestos en la preparación de medicamentos, procesos para la preparación de dichos compuestos e intermediarios útiles en la preparación de dichos compuestos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01117410 | 2001-07-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR036175A1 true AR036175A1 (es) | 2004-08-18 |
Family
ID=8178073
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020102678A AR036175A1 (es) | 2001-07-19 | 2002-07-17 | Derivados de la dolastatina 10, composiciones farmaceuticas que los comprenden, el uso de dichos compuestos en la preparacion de medicamentos, procesos para la preparacion de dichos compuestos, e intermediarios utiles en la preparacion de dichos compuestos |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US6737409B2 (es) |
| EP (1) | EP1412328B1 (es) |
| JP (1) | JP2004534859A (es) |
| KR (2) | KR100611540B1 (es) |
| CN (1) | CN1553897A (es) |
| AR (1) | AR036175A1 (es) |
| AT (1) | ATE341537T1 (es) |
| BR (1) | BR0211289A (es) |
| CA (1) | CA2453987A1 (es) |
| CO (1) | CO5550462A2 (es) |
| DE (1) | DE60215179T2 (es) |
| DK (1) | DK1412328T3 (es) |
| ES (1) | ES2272763T3 (es) |
| GT (1) | GT200200154A (es) |
| HR (1) | HRP20040043A2 (es) |
| HU (1) | HUP0401253A2 (es) |
| IL (1) | IL159890A0 (es) |
| MX (1) | MXPA04000577A (es) |
| MY (1) | MY127718A (es) |
| NO (1) | NO20040198L (es) |
| NZ (1) | NZ530655A (es) |
| PA (1) | PA8551001A1 (es) |
| PE (1) | PE20030258A1 (es) |
| PL (1) | PL367682A1 (es) |
| PT (1) | PT1412328E (es) |
| RU (1) | RU2296750C2 (es) |
| SI (1) | SI1412328T1 (es) |
| UY (1) | UY27388A1 (es) |
| WO (1) | WO2003008378A1 (es) |
| ZA (1) | ZA200400334B (es) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7256257B2 (en) | 2001-04-30 | 2007-08-14 | Seattle Genetics, Inc. | Pentapeptide compounds and uses related thereto |
| NZ555951A (en) * | 2002-03-22 | 2009-01-31 | Eisai Co Ltd | Hemiasterlin derivatives and uses thereof |
| US7064211B2 (en) | 2002-03-22 | 2006-06-20 | Eisai Co., Ltd. | Hemiasterlin derivatives and uses thereof |
| ES2556641T3 (es) | 2002-07-31 | 2016-01-19 | Seattle Genetics, Inc. | Conjugados de fármacos y su uso para tratar cáncer, una enfermedad autoinmune o una enfermedad infecciosa |
| SG195524A1 (en) | 2003-11-06 | 2013-12-30 | Seattle Genetics Inc | Monomethylvaline compounds capable of conjugation to ligands |
| WO2005118525A1 (en) * | 2004-06-02 | 2005-12-15 | F.Hoffmann-La Roche Ag | Synthesis of amino-alkoxy-heptanoic alkyl ester |
| JP2008519863A (ja) | 2004-11-12 | 2008-06-12 | シアトル ジェネティクス インコーポレイティッド | Ｎ末端にアミノ安息香酸単位を有するオーリスタチン |
| RU2007126358A (ru) * | 2004-12-13 | 2009-01-20 | Ф.Хоффманн-Ля Рош Аг (Ch) | Новая фармацевтическая композиция, содержащая по меньшей мере одно производное доластатина 10 |
| EP1828117A1 (en) * | 2004-12-13 | 2007-09-05 | F. Hoffmann-Roche AG | Novel process for the manufacture of 3-pyrrolidin-2-yl-propionic acid derivatives |
| US20060189893A1 (en) * | 2005-01-06 | 2006-08-24 | Diamics, Inc. | Systems and methods for detecting abnormal cells |
| US20060161076A1 (en) * | 2005-01-06 | 2006-07-20 | Diamics, Inc. | Systems and methods for collection of cell clusters |
| AU2006205909A1 (en) * | 2005-01-13 | 2006-07-20 | F. Hoffmann-La Roche Ag | New one-step synthesis of useful disubstituted amines |
| US7772177B2 (en) | 2005-05-18 | 2010-08-10 | Aegera Therapeutics, Inc. | BIR domain binding compounds |
| US8871720B2 (en) | 2005-07-07 | 2014-10-28 | Seattle Genetics, Inc. | Monomethylvaline compounds having phenylalanine carboxy modifications at the C-terminus |
| ES2708763T3 (es) | 2005-07-07 | 2019-04-11 | Seattle Genetics Inc | Compuestos de monometilvalina que tienen modificaciones de la cadena lateral de fenilalanina en el extremo C |
| US7750116B1 (en) | 2006-02-18 | 2010-07-06 | Seattle Genetics, Inc. | Antibody drug conjugate metabolites |
| NZ572836A (en) | 2006-05-16 | 2011-12-22 | Pharmascience Inc | Iap bir domain binding compounds |
| US20080003652A1 (en) * | 2006-06-28 | 2008-01-03 | Hans Iding | Novel enzymatic process for the manufacture of Boc-Dap-Oh priority to related application(s) |
| PE20090481A1 (es) | 2007-07-16 | 2009-05-18 | Genentech Inc | Anticuerpos anti-cd79b e inmunoconjugados humanizados y metodos de uso |
| RS52305B (en) | 2007-07-16 | 2012-12-31 | Genentech Inc. | ANTI-CD79B ANTIBODIES AND IMMUNOCONCULATES AND METHODS OF USE |
| ES2587392T3 (es) | 2008-01-31 | 2016-10-24 | Genentech, Inc. | Anticuerpos anti-CD79b e inmunoconjugados y métodos de uso |
| US8609105B2 (en) | 2008-03-18 | 2013-12-17 | Seattle Genetics, Inc. | Auristatin drug linker conjugates |
| CN102933231B (zh) | 2010-02-10 | 2015-07-29 | 伊缪诺金公司 | Cd20抗体及其用途 |
| SG182724A1 (en) | 2010-02-12 | 2012-08-30 | Pharmascience Inc | Iap bir domain binding compounds |
| EP2579887B1 (de) | 2010-06-10 | 2014-11-12 | Seattle Genetics, Inc. | Neue auristatin-derivate und ihre verwendung |
| US8987209B2 (en) | 2010-09-29 | 2015-03-24 | Seattle Genetics, Inc. | N-carboxyalkyl-auristatin and the use thereof |
| US9029406B2 (en) | 2011-03-16 | 2015-05-12 | Seattle Genetics, Inc | N-carboxyalkylauristatins and use thereof |
| KR102356286B1 (ko) * | 2011-05-27 | 2022-02-08 | 암브룩스, 인코포레이티드 | 비-천연 아미노산 연결된 돌라스타틴 유도체를 함유하는 조성물, 이를 수반하는 방법, 및 용도 |
| DK3170821T3 (da) * | 2011-05-27 | 2021-10-11 | Ambrx Inc | Sammensætninger som indeholder, fremgangsmåder som involverer, og anvendelser af ikke-naturlige aminosyrebundne dolastatinderivater |
| US9278996B2 (en) | 2012-09-20 | 2016-03-08 | Celltrion, Inc. | Dolastatin-10 derivative, method of producing the same and anticancer drug composition containing the same |
| EP3086815B1 (en) | 2013-12-27 | 2022-02-09 | Zymeworks Inc. | Sulfonamide-containing linkage systems for drug conjugates |
| EP3262071B8 (en) | 2014-09-23 | 2022-05-18 | F. Hoffmann-La Roche AG | Method of using anti-cd79b immunoconjugates |
| CN105949277B (zh) * | 2015-05-05 | 2019-03-01 | 成都永泰诺科技有限公司 | 一种抗肿瘤化合物及其用途 |
| WO2017170637A1 (ja) * | 2016-03-29 | 2017-10-05 | 東レ株式会社 | ペプチド誘導体及びその用途 |
| CN109021065B (zh) * | 2017-06-08 | 2021-10-01 | 复旦大学 | 一种制备海兔毒素Dolastatin10的方法 |
| JPWO2023033129A1 (es) | 2021-09-03 | 2023-03-09 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6323315B1 (en) | 1999-09-10 | 2001-11-27 | Basf Aktiengesellschaft | Dolastatin peptides |
-
2002
- 2002-07-15 US US10/195,698 patent/US6737409B2/en not_active Expired - Fee Related
- 2002-07-17 DK DK02764710T patent/DK1412328T3/da active
- 2002-07-17 PT PT02764710T patent/PT1412328E/pt unknown
- 2002-07-17 BR BR0211289-2A patent/BR0211289A/pt not_active IP Right Cessation
- 2002-07-17 RU RU2004105145/04A patent/RU2296750C2/ru not_active IP Right Cessation
- 2002-07-17 CN CNA028177622A patent/CN1553897A/zh active Pending
- 2002-07-17 DE DE60215179T patent/DE60215179T2/de not_active Expired - Fee Related
- 2002-07-17 KR KR1020047000854A patent/KR100611540B1/ko not_active IP Right Cessation
- 2002-07-17 ES ES02764710T patent/ES2272763T3/es not_active Expired - Lifetime
- 2002-07-17 PL PL02367682A patent/PL367682A1/xx not_active Application Discontinuation
- 2002-07-17 CA CA002453987A patent/CA2453987A1/en not_active Abandoned
- 2002-07-17 KR KR1020067008692A patent/KR20060057652A/ko not_active Application Discontinuation
- 2002-07-17 SI SI200230447T patent/SI1412328T1/sl unknown
- 2002-07-17 JP JP2003513938A patent/JP2004534859A/ja active Pending
- 2002-07-17 MY MYPI20022704A patent/MY127718A/en unknown
- 2002-07-17 MX MXPA04000577A patent/MXPA04000577A/es active IP Right Grant
- 2002-07-17 NZ NZ530655A patent/NZ530655A/en unknown
- 2002-07-17 AT AT02764710T patent/ATE341537T1/de not_active IP Right Cessation
- 2002-07-17 EP EP02764710A patent/EP1412328B1/en not_active Expired - Lifetime
- 2002-07-17 IL IL15989002A patent/IL159890A0/xx unknown
- 2002-07-17 HU HU0401253A patent/HUP0401253A2/hu unknown
- 2002-07-17 AR ARP020102678A patent/AR036175A1/es not_active Application Discontinuation
- 2002-07-17 WO PCT/EP2002/007931 patent/WO2003008378A1/en active IP Right Grant
- 2002-07-17 UY UY27388A patent/UY27388A1/es not_active Application Discontinuation
- 2002-07-18 PA PA20028551001A patent/PA8551001A1/es unknown
- 2002-07-18 GT GT200200154A patent/GT200200154A/es unknown
- 2002-07-19 PE PE2002000643A patent/PE20030258A1/es not_active Application Discontinuation
-
2004
- 2004-01-15 ZA ZA2004/00334A patent/ZA200400334B/en unknown
- 2004-01-16 NO NO20040198A patent/NO20040198L/no not_active Application Discontinuation
- 2004-01-19 HR HR20040043A patent/HRP20040043A2/hr not_active Application Discontinuation
- 2004-01-20 CO CO04003736A patent/CO5550462A2/es not_active Application Discontinuation
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Legal Events
| Date | Code | Title | Description |
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| FA | Abandonment or withdrawal |