ATE228132T1 - Trifluoromethylpyrroloindolcarbonsäure und dessen esterderivat sowie ein verfahren zu seiner herstellung - Google Patents
Trifluoromethylpyrroloindolcarbonsäure und dessen esterderivat sowie ein verfahren zu seiner herstellungInfo
- Publication number
- ATE228132T1 ATE228132T1 AT94908108T AT94908108T ATE228132T1 AT E228132 T1 ATE228132 T1 AT E228132T1 AT 94908108 T AT94908108 T AT 94908108T AT 94908108 T AT94908108 T AT 94908108T AT E228132 T1 ATE228132 T1 AT E228132T1
- Authority
- AT
- Austria
- Prior art keywords
- trifluoromethylpyrroloindole
- production
- carboxylic acid
- ester derivative
- arylsulfonyloxy
- Prior art date
Links
- ALRWGSAXZMCLHO-UHFFFAOYSA-N 3-(trifluoromethyl)pyrrolo[2,3-e]indole-2-carboxylic acid Chemical compound C1=CC2=C(C(F)(F)F)C(C(=O)O)=NC2=C2C=CN=C21 ALRWGSAXZMCLHO-UHFFFAOYSA-N 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003275 alpha amino acid group Chemical group 0.000 abstract 1
- 230000000259 anti-tumor effect Effects 0.000 abstract 1
- 125000005279 aryl sulfonyloxy group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/10—Spiro-condensed systems
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Laminated Bodies (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP22286292 | 1992-08-21 | ||
| JP20425593A JP3514490B2 (ja) | 1992-08-21 | 1993-08-18 | トリフルオロメチルピロロインドールカルボン酸エステル誘導体及びその製造方法 |
| PCT/JP1993/001159 WO1994004535A1 (fr) | 1992-08-21 | 1993-08-19 | Derive d'ester carboxylique de trifluoromethylpyrroloindole et procede pour sa fabrication |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE228132T1 true ATE228132T1 (de) | 2002-12-15 |
Family
ID=26514369
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT94908108T ATE228132T1 (de) | 1992-08-21 | 1993-08-19 | Trifluoromethylpyrroloindolcarbonsäure und dessen esterderivat sowie ein verfahren zu seiner herstellung |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US5629430A (de) |
| EP (1) | EP0656360B1 (de) |
| JP (1) | JP3514490B2 (de) |
| KR (2) | KR100312444B1 (de) |
| AT (1) | ATE228132T1 (de) |
| CA (1) | CA2142869C (de) |
| DE (1) | DE69332504T2 (de) |
| DK (1) | DK0656360T3 (de) |
| ES (1) | ES2188608T3 (de) |
| HU (1) | HU221041B1 (de) |
| PT (1) | PT656360E (de) |
| TW (1) | TW394774B (de) |
| WO (1) | WO1994004535A1 (de) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1051552C (zh) * | 1994-11-29 | 2000-04-19 | 杏林制药株式会社 | 丙烯酰胺衍生物及其制造方法 |
| WO1998003509A1 (en) * | 1996-07-23 | 1998-01-29 | Kyowa Hakko Kogyo Co., Ltd. | Dc-89 derivatives |
| AU5576098A (en) * | 1997-01-24 | 1998-08-18 | Kyorin Pharmaceutical Co. Ltd. | Pyrroloindole derivatives and intermediates in producing the same |
| NZ504884A (en) * | 1997-12-08 | 2002-10-25 | Scripps Research Inst | Synthesis of the dihydroindole C-ring of CC-1065/duocarmycin analogs and certain intermediates |
| US6989452B2 (en) * | 2001-05-31 | 2006-01-24 | Medarex, Inc. | Disulfide prodrugs and linkers and stabilizers useful therefor |
| WO2004035571A1 (en) * | 2002-10-15 | 2004-04-29 | Rigel Pharmaceuticals, Inc. | Substituted indoles and their use as hcv inhibitors |
| GB0403038D0 (en) | 2004-02-11 | 2004-03-17 | Novartis Ag | Organic compounds |
| US7691962B2 (en) * | 2004-05-19 | 2010-04-06 | Medarex, Inc. | Chemical linkers and conjugates thereof |
| JP4806680B2 (ja) * | 2004-05-19 | 2011-11-02 | メダレックス インコーポレイテッド | 自己犠牲リンカー及び薬剤複合体 |
| US7781478B2 (en) | 2004-07-14 | 2010-08-24 | Ptc Therapeutics, Inc. | Methods for treating hepatitis C |
| JP2008529556A (ja) * | 2005-02-18 | 2008-08-07 | メダレックス, インク. | 前立腺特異的膜抗原(psma)に対するヒトモノクローナル抗体 |
| US7714016B2 (en) * | 2005-04-08 | 2010-05-11 | Medarex, Inc. | Cytotoxic compounds and conjugates with cleavable substrates |
| EP2354163A3 (de) * | 2005-09-26 | 2013-04-24 | Medarex, Inc. | Konjugate von Duocarmycin und Anti-CD70 oder Anti-PSMA Antikörpern |
| RS52100B (sr) | 2005-10-26 | 2012-06-30 | Medarex, Inc. | Postupci i jedinjenja za pripremu analoga cc-1065 |
| WO2007059404A2 (en) | 2005-11-10 | 2007-05-24 | Medarex, Inc. | Duocarmycin derivatives as novel cytotoxic compounds and conjugates |
| TWI412367B (zh) | 2006-12-28 | 2013-10-21 | 梅達雷克斯有限責任公司 | 化學鏈接劑與可裂解基質以及其之綴合物 |
| AR065404A1 (es) | 2007-02-21 | 2009-06-03 | Medarex Inc | Conjugados farmaco-ligando, los que se unen a citotoxinas potentes, composicion farmaceutica que los contienen y su uso para retardar o detener el crecimiento de un tumor en un mamifero |
| US9901567B2 (en) | 2007-08-01 | 2018-02-27 | Syntarga B.V. | Substituted CC-1065 analogs and their conjugates |
| CA2706378C (en) * | 2007-11-20 | 2017-09-12 | Lankenau Institute For Medical Research | Disulfide chemotherapeutic agents and methods of use thereof |
| ES2647317T3 (es) * | 2008-11-03 | 2017-12-20 | Syntarga B.V. | Análogos de CC-1065 y sus conjugados |
| US8697391B2 (en) | 2009-05-15 | 2014-04-15 | Lankenau Institute For Medical Research | Method of determining cell number or viability using hydroxyethyldisulfide |
| PT3056203T (pt) | 2010-04-21 | 2018-02-15 | Syntarga Bv | Conjugados de análogos de cc-1065 e ligantes bifuncionais |
| CA2891280C (en) | 2012-11-24 | 2018-03-20 | Hangzhou Dac Biotech Co., Ltd. | Hydrophilic linkers and their uses for conjugation of drugs to cell binding molecules |
| CA2935433C (en) | 2014-01-10 | 2019-04-02 | Synthon Biopharmaceuticals B.V. | Duocarmycin anti-her2 antibody drug conjucates with activity against her2 expressing malignancies |
| RU2680404C2 (ru) | 2014-01-10 | 2019-02-21 | Синтон Байофармасьютикалс Б. В. | Способ очистки cys-связанных конъюгатов антитело-лекарственное средство |
| RU2686085C2 (ru) | 2014-01-10 | 2019-04-24 | Синтон Байофармасьютикалс Б. В. | Конъюгаты антитело-лекарственное средство (adc) с дуокармицином, применяемые для лечения рака эндометрия |
| US10464955B2 (en) | 2014-02-28 | 2019-11-05 | Hangzhou Dac Biotech Co., Ltd. | Charged linkers and their uses for conjugation |
| NZ739830A (en) | 2015-07-12 | 2021-12-24 | Hangzhou Dac Biotech Co Ltd | Bridge linkers for conjugation of cell-binding molecules |
| US9839687B2 (en) | 2015-07-15 | 2017-12-12 | Suzhou M-Conj Biotech Co., Ltd. | Acetylenedicarboxyl linkers and their uses in specific conjugation of a cell-binding molecule |
| KR20220150408A (ko) | 2016-11-14 | 2022-11-10 | 항저우 디에이씨 바이오테크 씨오, 엘티디 | 결합 링커, 그러한 결합 링커를 함유하는 세포 결합 분자-약물 결합체, 링커를 갖는 그러한 결합체의 제조 및 사용 |
| KR20230067637A (ko) * | 2020-09-11 | 2023-05-16 | 더 리전트 오브 더 유니버시티 오브 캘리포니아 | 근이영양증을 치료하기 위한 조성물 및 방법 |
| CN112724068A (zh) * | 2020-12-30 | 2021-04-30 | 蔡桂坡 | 具有hdac抑制活性的吲哚类衍生物的合成方法及肿瘤应用 |
| EP4426727A2 (de) | 2021-11-03 | 2024-09-11 | Hangzhou Dac Biotech Co., Ltd. | Spezifische konjugation eines antikörpers |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4978757A (en) * | 1984-02-21 | 1990-12-18 | The Upjohn Company | 1,2,8,8a-tetrahydrocyclopropa (C) pyrrolo [3,2-e)]-indol-4(5H)-ones and related compounds |
| JP2598116B2 (ja) * | 1988-12-28 | 1997-04-09 | 協和醗酵工業株式会社 | 新規物質dc113 |
| JP2510335B2 (ja) * | 1989-07-03 | 1996-06-26 | 協和醗酵工業株式会社 | Dc―88a誘導体 |
| JP3037965B2 (ja) * | 1990-06-20 | 2000-05-08 | 財団法人相模中央化学研究所 | 2―アルコキシカルボニル―2―メチル―1―オキソ―1,2,3,6,7,8―ヘキサヒドロ―ベンゾ〔1,2―b;4,3―b´〕ジピロール誘導体 |
| JPH0499774A (ja) * | 1990-08-14 | 1992-03-31 | Sagami Chem Res Center | 2―エピデュオカルマイシンaおよびその製造中間体 |
-
1993
- 1993-08-18 JP JP20425593A patent/JP3514490B2/ja not_active Expired - Fee Related
- 1993-08-19 PT PT94908108T patent/PT656360E/pt unknown
- 1993-08-19 HU HU9500494A patent/HU221041B1/hu not_active IP Right Cessation
- 1993-08-19 EP EP94908108A patent/EP0656360B1/de not_active Expired - Lifetime
- 1993-08-19 KR KR1019950700666A patent/KR100312444B1/ko not_active Expired - Fee Related
- 1993-08-19 DE DE69332504T patent/DE69332504T2/de not_active Expired - Fee Related
- 1993-08-19 CA CA002142869A patent/CA2142869C/en not_active Expired - Fee Related
- 1993-08-19 DK DK94908108T patent/DK0656360T3/da active
- 1993-08-19 AT AT94908108T patent/ATE228132T1/de not_active IP Right Cessation
- 1993-08-19 US US08/381,981 patent/US5629430A/en not_active Expired - Fee Related
- 1993-08-19 WO PCT/JP1993/001159 patent/WO1994004535A1/ja not_active Ceased
- 1993-08-19 ES ES94908108T patent/ES2188608T3/es not_active Expired - Lifetime
- 1993-10-04 TW TW082108171A patent/TW394774B/zh not_active IP Right Cessation
-
2001
- 2001-04-13 KR KR1020017004709A patent/KR100312445B1/ko not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| DE69332504T2 (de) | 2003-10-02 |
| US5629430A (en) | 1997-05-13 |
| EP0656360A1 (de) | 1995-06-07 |
| ES2188608T3 (es) | 2003-07-01 |
| EP0656360A4 (de) | 1995-08-30 |
| AU4761893A (en) | 1994-03-15 |
| EP0656360B1 (de) | 2002-11-20 |
| PT656360E (pt) | 2003-02-28 |
| DE69332504D1 (de) | 2003-01-02 |
| KR100312445B1 (ko) | 2001-11-09 |
| HU9500494D0 (en) | 1995-04-28 |
| DK0656360T3 (da) | 2003-03-17 |
| CA2142869C (en) | 2002-01-01 |
| CA2142869A1 (en) | 1994-03-03 |
| JP3514490B2 (ja) | 2004-03-31 |
| AU689443B2 (en) | 1998-04-02 |
| HU221041B1 (hu) | 2002-07-29 |
| KR100312444B1 (ko) | 2002-02-28 |
| JPH06116269A (ja) | 1994-04-26 |
| TW394774B (en) | 2000-06-21 |
| HUT71493A (en) | 1995-11-28 |
| WO1994004535A1 (fr) | 1994-03-03 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| UEP | Publication of translation of european patent specification |
Ref document number: 0656360 Country of ref document: EP |
|
| REN | Ceased due to non-payment of the annual fee |