PE20000009A1 - Conjugados de 4-desacetilvinblastina - Google Patents
Conjugados de 4-desacetilvinblastinaInfo
- Publication number
- PE20000009A1 PE20000009A1 PE1998001170A PE00117098A PE20000009A1 PE 20000009 A1 PE20000009 A1 PE 20000009A1 PE 1998001170 A PE1998001170 A PE 1998001170A PE 00117098 A PE00117098 A PE 00117098A PE 20000009 A1 PE20000009 A1 PE 20000009A1
- Authority
- PE
- Peru
- Prior art keywords
- oligopeptide
- ser
- zero
- refers
- proteolitically
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
- C07K5/1002—Tetrapeptides with the first amino acid being neutral
- C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
- C07K5/1013—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
- A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
- C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
- C07K5/1002—Tetrapeptides with the first amino acid being neutral
- C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
-
- 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)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Toxicology (AREA)
- Zoology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Urology & Nephrology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
SE REFIERE A UN AGENTE CITOTOXICO DEL ALCALOIDE VINCAPERVINCA QUE EN LA POSICION 4 ESTA UNIDO POR UN ENLAZADOR QUIMICO A UN OLIGOPEPTIDO EL QUE SE CARACTERIZA POR UNA SECUENCIA DE AMINOACIDOS QUE SE DIVIDEN PROTEOLITICAMENTE POR UN ANTIGENO PROSTATICO ESPECIFICO LIBRE (PROTEASA). EL OLIGOPEPTIDO ES DE PREFERENCIA AsnLysIleSerTyrGln/Ser, LysIleSerTyrGln/Ser, AsnLysIleSerTyrTyr/Ser, ENTRE OTROS. EL AGENTE CITOTOXICO ES DE PREFERECIA VINBLASTINA, 4-DESACETILVINBLASTINA, VINCRISTINA, LEUROSIDINA, VINDESINA. TAMBIEN SE REFIERE A UN CONJUGADO DE FORMULA Ia, DONDE EL OLIGOPEPTIDO ES RECONOCIDO POR EL ANTIGENO PROSTATICO ESPECIFICO LIBRE Y SE PUEDE DIVIDIR PROTEOLITICAMENTE POR LA ACTIVIDAD ENZIMATICA, DONDE XL ES UN ENLACE, -C(O)-(CH2)u-W-(CH2)u-O- Y -C(O)-(CH2)u-W-(CH2)u-NH-; R ES H, -(C=O)R1a, GRUPO c, d, e, ETOXIESCUARATO, COTININILO, R1 Y R2 SON H, OH, ALQUILO C1-C6, ENTRE OTROS; W ES ALQUILO C1-C6, CICLOPENTILO, CICLOHEXILO, ENTRE OTROS; n ES 1-4, p ES CERO-100, q ES 0-1, SI p ES CERO q ES 1, r ES 1-3, t ES 3 o 4, u ES CERO-3. UN COMPUESTO PREFERIDO DE FORMULA II. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. EL COMPUESTO I PUEDE SER UTIL PARA TRATAR EL CANCER DE PROSTATA, HIPERPLASIA PROSTATICA BENIGNA
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US6711097P | 1997-12-02 | 1997-12-02 | |
| GBGB9804399.5A GB9804399D0 (en) | 1998-03-02 | 1998-03-02 | Conjugates useful in the treatment of prostate cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20000009A1 true PE20000009A1 (es) | 2000-01-27 |
Family
ID=26313204
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE1998001170A PE20000009A1 (es) | 1997-12-02 | 1998-12-01 | Conjugados de 4-desacetilvinblastina |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US20060148718A1 (es) |
| EP (1) | EP1036093A1 (es) |
| JP (1) | JP2001525337A (es) |
| KR (1) | KR100580137B1 (es) |
| CN (1) | CN1181092C (es) |
| AR (1) | AR016427A1 (es) |
| AU (1) | AU744652B2 (es) |
| BG (1) | BG65486B1 (es) |
| BR (1) | BR9815116A (es) |
| CA (1) | CA2311615A1 (es) |
| DZ (1) | DZ2665A1 (es) |
| EA (1) | EA002745B1 (es) |
| EE (1) | EE200000333A (es) |
| HR (1) | HRP20000367A2 (es) |
| HU (1) | HUP0100350A3 (es) |
| ID (1) | ID24735A (es) |
| IL (1) | IL136167A0 (es) |
| IS (1) | IS5502A (es) |
| NO (1) | NO20002804L (es) |
| NZ (1) | NZ504615A (es) |
| PE (1) | PE20000009A1 (es) |
| PL (1) | PL197006B1 (es) |
| SK (1) | SK8282000A3 (es) |
| TR (1) | TR200002260T2 (es) |
| TW (1) | TW577897B (es) |
| WO (1) | WO1999028345A1 (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ512171A (en) * | 1998-12-11 | 2004-07-30 | Medarex Inc | Prodrug compound comprising a therapeutic agent, an oligopeptide with a non-genetically encoded amino acid, a stabilizing group and optionally a linker group |
| GB9924759D0 (en) | 1999-10-19 | 1999-12-22 | Merck Sharp & Dohme | Process for preparing peptide intermediates |
| US7842581B2 (en) | 2003-03-27 | 2010-11-30 | Samsung Electronics Co., Ltd. | Methods of forming metal layers using oxygen gas as a reaction source and methods of fabricating capacitors using such metal layers |
| SI2187965T1 (sl) | 2007-08-17 | 2020-03-31 | Purdue Research Foundation Office Of Technology Commercialization | Konjugati vezalca ligand-veznika PSMA in metode za uporabo |
| US9951324B2 (en) | 2010-02-25 | 2018-04-24 | Purdue Research Foundation | PSMA binding ligand-linker conjugates and methods for using |
| WO2014028057A1 (en) * | 2012-08-15 | 2014-02-20 | Visen Medical, Inc. | Prostate specific antigen agents and methods of using same for prostate cancer imaging |
| CN104884056A (zh) * | 2012-11-12 | 2015-09-02 | 雷德伍德生物科技股份有限公司 | 用于制备缀合物的化合物和方法 |
| EA201590783A1 (ru) | 2012-11-15 | 2015-11-30 | Эндосайт, Инк. | Конъюгаты для доставки лекарственных средств и способы лечения заболеваний, вызванных клетками, экспрессирующими psma |
| WO2014178839A1 (en) | 2013-04-30 | 2014-11-06 | Hewlett-Packard Development Company, L.P. | Memory access rate |
| DE202014011593U1 (de) | 2013-10-18 | 2023-08-23 | Novartis Ag | Markierte Inhibitoren des prostataspezifischen Membranantigens (PSMA), deren Verwendung als bildgebende Mittel und pharmazeutische Wirkstoffe für die Behandlung von Prostatakrebs |
| EP3777898B1 (en) | 2013-11-14 | 2025-01-01 | Endocyte, Inc. | Compounds for positron emission tomography |
| US10188759B2 (en) | 2015-01-07 | 2019-01-29 | Endocyte, Inc. | Conjugates for imaging |
| CA3097381A1 (en) | 2018-04-17 | 2019-10-24 | Endocyte, Inc. | Methods of treating cancer |
| CN116635054A (zh) | 2020-12-22 | 2023-08-22 | 科比欧尔斯公司 | 包括四肽部分的化合物 |
| WO2022167664A1 (en) | 2021-02-07 | 2022-08-11 | Cobiores Nv | Compounds comprising a tetrapeptidic moiety |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4203898A (en) * | 1977-08-29 | 1980-05-20 | Eli Lilly And Company | Amide derivatives of VLB, leurosidine, leurocristine and related dimeric alkaloids |
| US4296105A (en) * | 1978-08-03 | 1981-10-20 | Institut International De Pathologie Cellulaire Et Moleculaire | Derivatives of doxorubicine, their preparation and use |
| US4719312A (en) * | 1978-10-02 | 1988-01-12 | Merck & Co., Inc. | Lysosometropic detergent therapeutic agents |
| US4376765A (en) * | 1980-03-31 | 1983-03-15 | Institut International De Pathologie Cellulaire Et Moleculaire | Medicaments, their preparation and compositions containing same |
| US4639456A (en) * | 1980-06-10 | 1987-01-27 | Omnichem S.A. | Vinblastin-23-oyl amino acid derivatives |
| ATE64396T1 (de) * | 1983-04-29 | 1991-06-15 | Omnichem Sa | Konjugierte vinblastin-verbindungen und ihre derivate, verfahren zu ihrer herstellung und diese enthaltende pharmazeutische zusammensetzungen. |
| FR2546163B1 (fr) * | 1983-05-16 | 1987-10-09 | Centre Nat Rech Scient | Nouveaux derives acyles hydrosolubles de peptides ou d'amino-acides, leur preparation et leur application |
| FR2626882B1 (fr) * | 1988-02-08 | 1991-11-08 | Ire Celltarg Sa | Conjugues de derives de vinca comportant une chaine detergente en position c-3 |
| US5391723A (en) * | 1989-05-31 | 1995-02-21 | Neorx Corporation | Oligonucleotide conjugates |
| EP0647450A1 (en) * | 1993-09-09 | 1995-04-12 | BEHRINGWERKE Aktiengesellschaft | Improved prodrugs for enzyme mediated activation |
| US5866679A (en) * | 1994-06-28 | 1999-02-02 | Merck & Co., Inc. | Peptides |
| US6143864A (en) * | 1994-06-28 | 2000-11-07 | Merck & Co., Inc. | Peptides |
| US5599686A (en) * | 1994-06-28 | 1997-02-04 | Merck & Co., Inc. | Peptides |
| WO1997014416A1 (en) * | 1995-10-18 | 1997-04-24 | Merck & Co., Inc. | Conjugates useful in the treatment of benign prostatic hyperplasia |
| US5998362A (en) * | 1996-09-12 | 1999-12-07 | Merck & Co., Inc. | Conjugates useful in the treatment of prostate cancer |
| CA2265476A1 (en) * | 1996-09-12 | 1998-03-19 | Merck & Co., Inc. | Conjugates useful in the treatment of prostate cancer |
| HRP970566A2 (en) * | 1996-10-30 | 1998-08-31 | Jones Deborah Defeo | Conjugates useful in the treatment of prostate canser |
-
1998
- 1998-11-25 TR TR2000/02260T patent/TR200002260T2/xx unknown
- 1998-11-25 EP EP98960550A patent/EP1036093A1/en not_active Withdrawn
- 1998-11-25 WO PCT/US1998/025358 patent/WO1999028345A1/en active IP Right Grant
- 1998-11-25 SK SK828-2000A patent/SK8282000A3/sk unknown
- 1998-11-25 KR KR1020007005969A patent/KR100580137B1/ko not_active IP Right Cessation
- 1998-11-25 BR BR9815116-9A patent/BR9815116A/pt not_active Application Discontinuation
- 1998-11-25 EE EEP200000333A patent/EE200000333A/xx unknown
- 1998-11-25 NZ NZ504615A patent/NZ504615A/en unknown
- 1998-11-25 CA CA002311615A patent/CA2311615A1/en not_active Abandoned
- 1998-11-25 JP JP2000523236A patent/JP2001525337A/ja active Pending
- 1998-11-25 AU AU16123/99A patent/AU744652B2/en not_active Ceased
- 1998-11-25 PL PL340768A patent/PL197006B1/pl not_active IP Right Cessation
- 1998-11-25 HU HU0100350A patent/HUP0100350A3/hu unknown
- 1998-11-25 CN CNB988132826A patent/CN1181092C/zh not_active Expired - Fee Related
- 1998-11-25 IL IL13616798A patent/IL136167A0/xx not_active IP Right Cessation
- 1998-11-25 EA EA200000603A patent/EA002745B1/ru not_active IP Right Cessation
- 1998-11-25 ID IDW20001039A patent/ID24735A/id unknown
- 1998-11-30 DZ DZ980275A patent/DZ2665A1/xx active
- 1998-12-01 PE PE1998001170A patent/PE20000009A1/es not_active Application Discontinuation
- 1998-12-01 AR ARP980106090A patent/AR016427A1/es active IP Right Grant
- 1998-12-02 TW TW087119985A patent/TW577897B/zh not_active IP Right Cessation
-
2000
- 2000-05-19 IS IS5502A patent/IS5502A/is unknown
- 2000-05-31 NO NO20002804A patent/NO20002804L/no not_active Application Discontinuation
- 2000-06-02 HR HR20000367A patent/HRP20000367A2/hr not_active Application Discontinuation
- 2000-06-27 BG BG104563A patent/BG65486B1/bg unknown
-
2006
- 2006-02-24 US US11/362,251 patent/US20060148718A1/en not_active Abandoned
- 2006-09-26 US US11/481,999 patent/US20070021350A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| WO1999028345A1 (en) | 1999-06-10 |
| PL340768A1 (en) | 2001-02-26 |
| AU744652B2 (en) | 2002-02-28 |
| HRP20000367A2 (en) | 2000-12-31 |
| SK8282000A3 (en) | 2000-11-07 |
| CN1181092C (zh) | 2004-12-22 |
| NO20002804D0 (no) | 2000-05-31 |
| IS5502A (is) | 2000-05-19 |
| PL197006B1 (pl) | 2008-02-29 |
| KR20010032687A (ko) | 2001-04-25 |
| TR200002260T2 (tr) | 2000-12-21 |
| CN1284086A (zh) | 2001-02-14 |
| AR016427A1 (es) | 2001-07-04 |
| HUP0100350A3 (en) | 2001-09-28 |
| HUP0100350A2 (hu) | 2001-08-28 |
| KR100580137B1 (ko) | 2006-05-16 |
| ID24735A (id) | 2000-08-03 |
| EA002745B1 (ru) | 2002-08-29 |
| BG65486B1 (bg) | 2008-09-30 |
| US20060148718A1 (en) | 2006-07-06 |
| BR9815116A (pt) | 2000-10-10 |
| JP2001525337A (ja) | 2001-12-11 |
| AU1612399A (en) | 1999-06-16 |
| IL136167A0 (en) | 2001-05-20 |
| TW577897B (en) | 2004-03-01 |
| BG104563A (en) | 2001-04-30 |
| NO20002804L (no) | 2000-07-21 |
| NZ504615A (en) | 2003-05-30 |
| EP1036093A1 (en) | 2000-09-20 |
| CA2311615A1 (en) | 1999-06-10 |
| US20070021350A1 (en) | 2007-01-25 |
| EA200000603A1 (ru) | 2000-12-25 |
| EE200000333A (et) | 2001-08-15 |
| DZ2665A1 (fr) | 2003-03-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |