NO952366L - Dolostatin-analog - Google Patents
Dolostatin-analogInfo
- Publication number
- NO952366L NO952366L NO952366A NO952366A NO952366L NO 952366 L NO952366 L NO 952366L NO 952366 A NO952366 A NO 952366A NO 952366 A NO952366 A NO 952366A NO 952366 L NO952366 L NO 952366L
- Authority
- NO
- Norway
- Prior art keywords
- hydrogen
- alkyl
- alkoxy
- benzyl
- hydroxy
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/02—Linear peptides containing at least one abnormal peptide link
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Crystallography & Structural Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Cephalosporin Compounds (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Measurement And Recording Of Electrical Phenomena And Electrical Characteristics Of The Living Body (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Window Of Vehicle (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Nye peptider med formelen \ N-CHX-CO-(A) -NR3-CHB-CHD-CHE-CO-(R7) -(M) ,-Q hvor H1 er alkoksy; alkyl; cykloalkyl; alkylsulfonyl; trifluor- etyl; fluoretyl; difluoretyl; trifluoracetyl; amidino; ureyl; piperidinosulfonyl; aorfolinosulfonyl; benzyloksy- karbonyl; alkoksykarbonyl; aninosulfonyl son kan veie substituert ned alkyl; hydroksy; fenylsulfonyl som kan v«re substituert ned en eller flere substituenter uavhen- gig valgt fra alkyl, -N(CH.,) , nitro, halogen og CF3: eller NR8B9 hvor R8 og R9 hver kan v«e enten hydrogen eller alkyl; R2 er hydrogen; alkyl; cykloalkyl; acyl; benioyl eller ben- zyl BOB kan vcre substituert ned opp til tre substitu- enter uavhengig valgt fra nitro, halogen, CFa, alkyl og alkoksy (fortrinnsvis C. ); eller R1-N-R2 tilsanaen kan vcre en 5- eller e-leddet heterocyklus son kan vcre usubstituert eller substituert ned en eller flere substituenter uavhengig valgt fra fenyl, benzyl, alkyl, H(CH ) , okso, nitro, tienyl, CONH-, COOMe og COOEt; X er hydrogen, alkyl, cykloalkyl, -CH -cykloheskyl eller benzyl; A er valgt fra gruppen bestående av valyl, isoleucyl, leu- cyl, allo-isoleucyl, a-aninoisobutanoyl, 3-tert.-butyl- alanyl, 2-tert.-butylglycyl, 3-cykloheksylal«nyl, 2-etyl- glycyl eller 2-cykloheKsylglycyl-rester; R3 er hydrogen eller alkyl: B er hydrogen eller alkyl, cykloalkyl, -CH,-cykloheksyl eller benzyl; D er hydrogen, hydroksy, acetoksy eller alkoksy; E er hydrogen eller alkyl; eller B og E tilsanmen er -(CH2)3-, -(CH,),-, -CH(CH )CH,CH,-, -CH(CH )CH2-, -C(CH3)2CH2CM2- eller C(CH.,)2CH2-: H7 er -NR -CHG-CHK-CHL-CO-, eller M er valgt fra gruppen bestående av 1-aninopentyl-l-karbon- yl, valyl, 2-tert.-butylglycyl, prolyl, hydroksyprolyl, isoleucyl, leucyl, }-cykloheksylalanyl, fenylalanyl, tetrahydroisokinolyl-2-karbonyl, 3-tiazolylalanyl, 3- tienylalanyl, histidyl, 2-aninoindyl-2-karbonyl, tyrosyl, 3-pyridylalanyl, 3-tert.-butylalanyl, 2-cykloheksylglycyl eller 3-naftylalanyl-rester: eller R1R2N-CHX-CO- og A tilsamnen er R' r u co- eller hvor T er hydrogen eller lavere alkyl; u er hydrogen eller lave- re alkyl; n er l, 2 eller 3; v er oksygen eller svovel; v er hydrogen; Z er hydrogen eller lavere alkyl: eller y og Z tilsamnen kan danne en binding; w er hydrogen, lavere alkyl eller fenyl; a, b og d uavhengig er o eller 1; Q er hydroksy, alkoksy, fenoksy, benzyloksy eller en sub- stituert eller usubstituert aninogruppe; forutsatt at hvor b og d er o, skal Q ikke v«re en hydroy.sy- eller alkoksygruppe; og saltene derav med fysiologisk aksepterbare syrer. De nye substanser har anti-neoplastisk effekt. hvor V er oksygen eller svovel; YA er hydrogen; Z er hydrogen eller lavere alkyl; eller Y1 og Zl tilaaanen kan danne en binding; w1 er hydrogen, alkyl eller fenyl; R4 er hydrogen eller alkyl: C er hydrogen, alkyl, cykloheksyl, CH -cykloheksyl eller benzyl; K er hydrogen, hydroksy, acetoksy eller alkoksy; L er hydrogen eller alkyl; eller R* og C tllsammen er -(CH,) -, -(CH,),-, eller -CH2,-CH(OH)-CH2 -;
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US99130992A | 1992-12-16 | 1992-12-16 | |
PCT/EP1993/003410 WO1994013695A1 (en) | 1992-12-16 | 1993-12-04 | Dolostatin analog |
Publications (2)
Publication Number | Publication Date |
---|---|
NO952366L true NO952366L (no) | 1995-06-15 |
NO952366D0 NO952366D0 (no) | 1995-06-15 |
Family
ID=25537082
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
NO952366A NO952366D0 (no) | 1992-12-16 | 1995-06-15 | Dolostatin-analog |
Country Status (24)
Country | Link |
---|---|
US (1) | US5502032A (no) |
EP (1) | EP0674652B1 (no) |
JP (1) | JPH08504415A (no) |
CN (1) | CN1057095C (no) |
AT (1) | ATE196296T1 (no) |
AU (1) | AU679479B2 (no) |
BR (1) | BR1100019A (no) |
CA (1) | CA2151953A1 (no) |
CZ (1) | CZ286752B6 (no) |
DE (1) | DE69329425T2 (no) |
ES (1) | ES2151921T3 (no) |
FI (1) | FI952961A0 (no) |
HR (1) | HRP931504B1 (no) |
HU (1) | HUT72067A (no) |
IL (1) | IL107987A (no) |
NO (1) | NO952366D0 (no) |
NZ (1) | NZ258882A (no) |
PL (1) | PL178766B1 (no) |
RU (1) | RU2132334C1 (no) |
SG (1) | SG67935A1 (no) |
SI (1) | SI9300661A (no) |
TW (1) | TW400335B (no) |
WO (1) | WO1994013695A1 (no) |
ZA (1) | ZA939389B (no) |
Families Citing this family (32)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5599902A (en) * | 1994-11-10 | 1997-02-04 | Arizona Board Of Regents Acting On Behalf Of Arizona State University | Cancer inhibitory peptides |
US5663149A (en) * | 1994-12-13 | 1997-09-02 | Arizona Board Of Regents Acting On Behalf Of Arizona State University | Human cancer inhibitory pentapeptide heterocyclic and halophenyl amides |
US5807984A (en) * | 1995-11-09 | 1998-09-15 | Basf Aktienegesellschaft | Oligopeptides, the preparation and use thereof |
TW474946B (en) * | 1995-12-15 | 2002-02-01 | Basf Ag | Novel compounds, the preparation and use thereof |
US20010009901A1 (en) * | 1996-12-11 | 2001-07-26 | Basf Aktiengesellschaft Germany | Antineoplastic peptides |
US5741892A (en) * | 1996-07-30 | 1998-04-21 | Basf Aktiengesellschaft | Pentapeptides as antitumor agents |
US5939527A (en) * | 1996-07-30 | 1999-08-17 | Basf Aktiengesellschaft | Tetrapeptides as antitumor agents |
US5965537A (en) * | 1997-03-10 | 1999-10-12 | Basf Aktiengesellschaft | Dolastatin 15 derivatives with carbonyl and heterocyclic functionalities at the C-terminus |
US6103698A (en) * | 1997-03-13 | 2000-08-15 | Basf Aktiengesellschaft | Dolastatin-15 derivatives in combination with taxanes |
US6143721A (en) * | 1997-07-18 | 2000-11-07 | Basf Aktiengesellschaft | Dolastatin 15 derivatives |
US6015790A (en) * | 1997-10-06 | 2000-01-18 | Basf Aktiengesellschaft | Methods and compositions for treating rheumatoid arthritis |
US5985837A (en) * | 1998-07-08 | 1999-11-16 | Basf Aktiengesellschaft | Dolastatin 15 derivatives |
EP1156803A4 (en) | 1999-02-09 | 2004-03-17 | Bristol Myers Squibb Co | FXA LACTAM INHIBITORS AND METHOD |
US6323315B1 (en) | 1999-09-10 | 2001-11-27 | Basf Aktiengesellschaft | Dolastatin peptides |
CA2385528C (en) | 1999-10-01 | 2013-12-10 | Immunogen, Inc. | Compositions and methods for treating cancer using immunoconjugates and chemotherapeutic agents |
US6511973B2 (en) | 2000-08-02 | 2003-01-28 | Bristol-Myers Squibb Co. | Lactam inhibitors of FXa and method |
CA2436774A1 (en) * | 2001-01-30 | 2002-08-08 | R. Michael Lawrence | Sulfonamide lactam inhibitors of factor xa |
EP1446110A2 (en) * | 2001-10-16 | 2004-08-18 | Structural Bioinformatics Inc. | Organosulfur inhibitors of tyrosine phosphatases |
US7087604B2 (en) | 2002-03-08 | 2006-08-08 | Bristol-Myers Squibb Company | Cyclic derivatives as modulators of chemokine receptor activity |
JP2006525990A (ja) * | 2003-05-12 | 2006-11-16 | ファイザー・プロダクツ・インク | 神経変性障害の処置のためのイソオキサゾール化合物およびイソチアゾール化合物 |
JP2008503490A (ja) * | 2004-06-17 | 2008-02-07 | センジェント・セラピューティクス・インコーポレイテッド | チロシンホスファターゼの三置換窒素調節物質 |
EP1786421A2 (en) * | 2004-07-09 | 2007-05-23 | Cengent Therapeutics, Inc. | Oxygen/nitrogen heterocycle inhibitors of tyrosine phosphatases |
EP1841749A1 (en) | 2004-09-02 | 2007-10-10 | Metabasis Therapeutics, Inc. | Derivatives of thiazole and thiadiazole inhibitors of tyrosine phosphatases |
EP2722051B1 (en) | 2005-07-07 | 2018-11-07 | Seattle Genetics, Inc. | Monomethylvaline compounds having phenylalanine side-chain modifications at the C-terminus |
RU2617402C2 (ru) | 2011-06-10 | 2017-04-25 | Мерсана Терапьютикс, Инк. | Конъюгаты белок-полимер-лекарственное средство |
EP2928503B1 (en) | 2012-12-10 | 2019-02-20 | Mersana Therapeutics, Inc. | Conjugates of auristatin compounds |
CN105358174B (zh) | 2013-03-15 | 2019-03-15 | 酵活有限公司 | 具细胞毒性和抗有丝分裂的化合物以及其使用方法 |
PL3086815T3 (pl) | 2013-12-27 | 2022-06-13 | Zymeworks Inc. | Układy łącznikowe dla koniugatów leków zawierające ugrupowanie sulfonamidowe |
US10675355B2 (en) | 2013-12-27 | 2020-06-09 | Var2 Pharmaceuticals Aps | VAR2CSA-drug conjugates |
WO2016041082A1 (en) | 2014-09-17 | 2016-03-24 | CDRD Ventures, Inc. | Cytotoxic and anti-mitotic compounds, and methods of using the same |
US10517958B2 (en) | 2016-10-04 | 2019-12-31 | Zymeworks Inc. | Compositions and methods for the treatment of platinum-drug resistant cancer |
JPWO2023033129A1 (no) | 2021-09-03 | 2023-03-09 |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3540495A1 (de) * | 1985-11-15 | 1987-05-21 | Merck Patent Gmbh | Aminosaeurederivate |
ES2058070T3 (es) * | 1986-05-09 | 1994-11-01 | Pulverer Gerhard | Utilizacion de monosacaridos especificos para la preparacion de un medicamento para impedir metastasis de tumores malignos. |
JP2714402B2 (ja) * | 1988-07-13 | 1998-02-16 | 日清製粉株式会社 | 癌転移抑制剤 |
EP0357332A3 (en) * | 1988-08-24 | 1991-07-31 | Merck & Co. Inc. | Renin inhibitors useful for the treatment of aids by inhibition of hiv protease |
US4978744A (en) * | 1989-01-27 | 1990-12-18 | Arizona Board Of Regents | Synthesis of dolastatin 10 |
US5138036A (en) * | 1989-11-13 | 1992-08-11 | Arizona Board Of Regents Acting On Behalf Of Arizona State University | Isolation and structural elucidation of the cytostatic cyclodepsipeptide dolastatin 14 |
SG87056A1 (en) * | 1991-08-09 | 2002-03-19 | Teikoku Hormone Mfg Co Ltd | Novel tetrapeptide derivative |
-
1993
- 1993-12-04 AT AT94902676T patent/ATE196296T1/de active
- 1993-12-04 NZ NZ258882A patent/NZ258882A/en unknown
- 1993-12-04 SG SG1996009255A patent/SG67935A1/en unknown
- 1993-12-04 HU HU9501754A patent/HUT72067A/hu unknown
- 1993-12-04 ES ES94902676T patent/ES2151921T3/es not_active Expired - Lifetime
- 1993-12-04 EP EP94902676A patent/EP0674652B1/en not_active Expired - Lifetime
- 1993-12-04 AU AU56959/94A patent/AU679479B2/en not_active Ceased
- 1993-12-04 JP JP6513752A patent/JPH08504415A/ja active Pending
- 1993-12-04 RU RU95115135A patent/RU2132334C1/ru active
- 1993-12-04 PL PL93309353A patent/PL178766B1/pl not_active IP Right Cessation
- 1993-12-04 CA CA002151953A patent/CA2151953A1/en not_active Abandoned
- 1993-12-04 WO PCT/EP1993/003410 patent/WO1994013695A1/en active IP Right Grant
- 1993-12-04 DE DE69329425T patent/DE69329425T2/de not_active Expired - Fee Related
- 1993-12-04 CZ CZ19951575A patent/CZ286752B6/cs not_active IP Right Cessation
- 1993-12-10 IL IL10798793A patent/IL107987A/en active IP Right Grant
- 1993-12-14 TW TW082110574A patent/TW400335B/zh not_active IP Right Cessation
- 1993-12-15 ZA ZA939389A patent/ZA939389B/xx unknown
- 1993-12-16 CN CN93112646A patent/CN1057095C/zh not_active Expired - Fee Related
- 1993-12-16 SI SI9300661A patent/SI9300661A/sl unknown
- 1993-12-16 HR HR931504A patent/HRP931504B1/xx not_active IP Right Cessation
-
1994
- 1994-01-05 US US08/178,529 patent/US5502032A/en not_active Expired - Fee Related
-
1995
- 1995-06-15 NO NO952366A patent/NO952366D0/no not_active Application Discontinuation
- 1995-06-15 FI FI952961A patent/FI952961A0/fi unknown
-
1996
- 1996-07-26 BR BR1100019-8A patent/BR1100019A/pt active IP Right Grant
Also Published As
Publication number | Publication date |
---|---|
CZ157595A3 (en) | 1996-01-17 |
SI9300661A (en) | 1994-06-30 |
ES2151921T3 (es) | 2001-01-16 |
HRP931504A2 (en) | 1997-02-28 |
HU9501754D0 (en) | 1995-08-28 |
EP0674652B1 (en) | 2000-09-13 |
CN1095724A (zh) | 1994-11-30 |
US5502032A (en) | 1996-03-26 |
RU2132334C1 (ru) | 1999-06-27 |
CZ286752B6 (en) | 2000-06-14 |
AU5695994A (en) | 1994-07-04 |
JPH08504415A (ja) | 1996-05-14 |
PL178766B1 (pl) | 2000-06-30 |
TW400335B (en) | 2000-08-01 |
CN1057095C (zh) | 2000-10-04 |
PL309353A1 (en) | 1995-10-02 |
FI952961A (fi) | 1995-06-15 |
FI952961A0 (fi) | 1995-06-15 |
IL107987A (en) | 1999-10-28 |
ZA939389B (en) | 1995-06-15 |
NZ258882A (en) | 1997-06-24 |
HRP931504B1 (en) | 2001-04-30 |
DE69329425D1 (de) | 2000-10-19 |
ATE196296T1 (de) | 2000-09-15 |
HUT72067A (en) | 1996-03-28 |
NO952366D0 (no) | 1995-06-15 |
CA2151953A1 (en) | 1994-06-23 |
RU95115135A (ru) | 1997-06-10 |
DE69329425T2 (de) | 2001-01-18 |
IL107987A0 (en) | 1994-04-12 |
SG67935A1 (en) | 1999-10-19 |
BR1100019A (pt) | 2000-07-25 |
AU679479B2 (en) | 1997-07-03 |
EP0674652A1 (en) | 1995-10-04 |
WO1994013695A1 (en) | 1994-06-23 |
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Legal Events
Date | Code | Title | Description |
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FC2A | Withdrawal, rejection or dismissal of laid open patent application |