ES2572183T3 - Conjugados de disorazoles y sus derivados con moléculas de unión celular, nuevos derivados de disorazol, procesos de preparación y usos de los mismos - Google Patents
Conjugados de disorazoles y sus derivados con moléculas de unión celular, nuevos derivados de disorazol, procesos de preparación y usos de los mismosInfo
- Publication number
- ES2572183T3 ES2572183T3 ES07803270T ES07803270T ES2572183T3 ES 2572183 T3 ES2572183 T3 ES 2572183T3 ES 07803270 T ES07803270 T ES 07803270T ES 07803270 T ES07803270 T ES 07803270T ES 2572183 T3 ES2572183 T3 ES 2572183T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- group
- aryl
- independently selected
- heterocyclyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
- C12P17/00—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
- C12P17/18—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin
- C12P17/188—Heterocyclic compound containing in the condensed system at least one hetero ring having nitrogen atoms and oxygen atoms as the only ring heteroatoms
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
-
- 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
- C07K14/575—Hormones
- C07K14/655—Somatostatins
- C07K14/6555—Somatostatins at least 1 amino acid in D-form
-
- 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
- C07K7/23—Luteinising hormone-releasing hormone [LHRH]; Related peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Zoology (AREA)
- Genetics & Genomics (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Wood Science & Technology (AREA)
- Endocrinology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Microbiology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Toxicology (AREA)
- Pharmacology & Pharmacy (AREA)
- Gastroenterology & Hepatology (AREA)
- General Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Abstract
Un compuesto de formula (I) o (IV) C1 -B1 -A-B2-C2 (I), C1 - B1 -A (IV), en las que para (I) y (IV): A es un resto disorazol de acuerdo con la formula (III)**Fórmula** en la que: Rio, Rjo, Rkp, Rmp, R28, R30, R31, R32, R33, R34, R35, R36, R38, R40, R41, R42, R43, R44 son hidrogeno; Rlp, Rnp juntos forman un doble enlace o se seleccionan independientemente entre el grupo que consiste en "hidrogeno, alcoxilo"; R27, R29 juntos forman un doble enlace o un epoxido (oxirano); R37, R39 juntos forman un doble enlace o un epoxido (oxirano); R25, R26 se seleccionan independientemente entre si entre el grupo que consiste en: "alquilo" que esta opcionalmente sustituido en el grupo alquilo con 1, 2 o 3 sustituyentes seleccionados independientemente entre si entre el grupo que consiste en "alquilo, cicloalquilo, cicloalquil-alquilo, arilo, heteroarilo, aril-alquilo, heteroaril-alquilo, heterociclilo, heterociclil-alquilo, alquilsulfonilo, arilsulfonilo, aril-alquilsulfonilo, -F, -Cl, -Br, -I, -N3, -NO2, >=O, >=S, >=S(O)2, hidroxilo, acetilo, carboxilo, carboxilester, amida, carbonato, carbamato, restos de alfa-aminoacido, restos de beta-aminoacido, alcoxilo, amino, hidroxilamino, mono-alquilamino, di-alquilamino, hidrazinilo, ciano, ciano-alquilo, sulfhidrilo, disulfidilalquilo y/o alquil-sulfidilo"; B1 y/o B2 se seleccionan independientemente entre si entre el grupo que consiste en "conector de resto de acido dicarbonico, succinilo, glutarilo"; C1 y/o C2 se seleccionan independientemente entre si entre el grupo que consiste en "LHRH, [D-Lys6] - LHRH, somatostatina, analogos de somatostatina, albumina de suero humano (HSA)"; o es 1 o 2; p es 1 o 2; en donde el termino "alquilo" incluye hidrocarburos aciclicos saturados, parcialmente insaturados o insaturados que tienen C1-C12 atomos de carbono, que pueden ser de cadena lineal o ramificada y que pueden contener uno o mas dobles enlaces y/o uno o mas triples enlaces; en donde el termino "alcoxilo" se refiere a radicales en los que un grupo "alquilo", "cicloalquilo", "cicloalquilalquilo", "arilo", "aril-alquilo", "heteroarilo", "heteroaril-alquilo", "heterociclilo" y/o "heterociclil-alquilo" esta unido a traves de un atomo de oxigeno (grupo -O-).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US84235706P | 2006-09-06 | 2006-09-06 | |
| EP06018750A EP1900742A1 (en) | 2006-09-07 | 2006-09-07 | Conjugates of disorazoles and their derivatives with cell-binding molecules, novel disorazole derivatives, processes of manufacturing and uses thereof |
| PCT/EP2007/059310 WO2008028934A1 (en) | 2006-09-06 | 2007-09-06 | Conjugates of disorazoles and their derivatives with cell-binding molecules, novel disorazole derivatives, processes of manufacturing and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2572183T3 true ES2572183T3 (es) | 2016-05-30 |
Family
ID=37670733
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES07803270T Active ES2572183T3 (es) | 2006-09-06 | 2007-09-06 | Conjugados de disorazoles y sus derivados con moléculas de unión celular, nuevos derivados de disorazol, procesos de preparación y usos de los mismos |
Country Status (16)
| Country | Link |
|---|---|
| US (3) | US7741277B2 (es) |
| EP (2) | EP1900742A1 (es) |
| KR (1) | KR101532966B1 (es) |
| AR (1) | AR062685A1 (es) |
| AU (1) | AU2007293650B2 (es) |
| CA (1) | CA2662308C (es) |
| DK (1) | DK2066679T3 (es) |
| ES (1) | ES2572183T3 (es) |
| HU (1) | HUE028061T2 (es) |
| MX (2) | MX337358B (es) |
| NZ (1) | NZ575032A (es) |
| PL (1) | PL2066679T3 (es) |
| RS (1) | RS54857B1 (es) |
| SI (1) | SI2066679T1 (es) |
| TW (1) | TWI346116B (es) |
| WO (1) | WO2008028934A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1900742A1 (en) * | 2006-09-07 | 2008-03-19 | AEterna Zentaris GmbH | Conjugates of disorazoles and their derivatives with cell-binding molecules, novel disorazole derivatives, processes of manufacturing and uses thereof |
| EP2340047A1 (en) * | 2008-09-19 | 2011-07-06 | Nektar Therapeutics | Polymer conjugates of kiss1 peptides |
| WO2010033207A1 (en) * | 2008-09-19 | 2010-03-25 | Nektar Therapeutics | Polymer conjugates of therapeutic peptides |
| AU2010216372B2 (en) * | 2009-02-20 | 2013-06-20 | Ipsen Pharma S.A.S. | Cytotoxic conjugates having neuropeptide Y receptor binding compound |
| US20120004182A1 (en) * | 2010-07-02 | 2012-01-05 | Carsten Gruendker | Pharmaceutical compositions and methods for induction and enhancement of apoptosis in tumor cells |
| CN110133300B (zh) * | 2012-03-18 | 2022-02-25 | 镜株式会社 | 疾病样品分析装置、分析系统及分析方法 |
| KR101974583B1 (ko) | 2012-08-29 | 2019-05-02 | 삼성전자주식회사 | 링커 폴리펩티드 및 이를 이용한 표적 물질 분석 방법 |
| US11465997B2 (en) | 2017-06-22 | 2022-10-11 | William Marsh Rice University | Synthesis of disorazoles and analogs thereof as potent anticancer agents |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6214969B1 (en) | 1988-10-21 | 2001-04-10 | The Administrators Of The Tulane Educational Fund | Luteinizing hormone releasing hormone analogs with cytotoxic moiety |
| US5866679A (en) | 1994-06-28 | 1999-02-02 | Merck & Co., Inc. | Peptides |
| US5843903A (en) | 1995-11-27 | 1998-12-01 | The Administrators Of The Tulane Educational Fund | Targeted cytotoxic anthracycline analogs |
| AU715632B2 (en) | 1996-09-12 | 2000-02-03 | Merck & Co., Inc. | Conjugates useful in the treatment of prostate cancer |
| DE19728737C1 (de) | 1997-07-04 | 1999-02-11 | Johannes Christian Groeninghen | Verfahren zur Erkennung und Bestimmung von GnRH-Rezeptoren und die Verwendung von GnRH-Agonisten und GnRH-Antagonisten zur Behandlung eines Tumors ausgehend vom Hirn und/oder Nervensystem und/oder den Hirnhäuten |
| WO1999002175A1 (en) | 1997-07-10 | 1999-01-21 | Merck & Co., Inc. | Conjugates useful in the treatment of prostate cancer |
| UA79480C2 (en) * | 2002-08-24 | 2007-06-25 | Zentaris Gmbh | Disorazol containing drug for treating benign and malignant tumors |
| US7364877B2 (en) | 2002-12-06 | 2008-04-29 | Kosan Biosciences, Inc. | Polynucleotides encoding disorazole polyketide synthase polypeptides |
| AU2005244980B2 (en) * | 2004-05-19 | 2011-09-15 | E. R. Squibb & Sons, L.L.C. | Chemical linkers and conjugates thereof |
| JP2008526246A (ja) | 2005-01-13 | 2008-07-24 | ヘルムホルツ−ツェントルム フュア インフェクツィオンスフォルシュンク ゲーエムベーハー | ジソラゾールの産生のための合成経路をコードする遺伝子 |
| US20060199252A1 (en) | 2005-01-13 | 2006-09-07 | Herbert Irschik | Genes encoding the synthetic pathway for the production of disorazole |
| WO2006135371A1 (en) * | 2005-06-09 | 2006-12-21 | Kosan Biosciences Incorporated | Conjugates with reduced adverse systemic effects |
| EP1743897A1 (en) * | 2005-07-15 | 2007-01-17 | Gesellschaft für Biotechnologische Forschung mbH | Biologically active compounds obtainable from Sorangium cellulosum |
| EP1900742A1 (en) | 2006-09-07 | 2008-03-19 | AEterna Zentaris GmbH | Conjugates of disorazoles and their derivatives with cell-binding molecules, novel disorazole derivatives, processes of manufacturing and uses thereof |
-
2006
- 2006-09-07 EP EP06018750A patent/EP1900742A1/en not_active Withdrawn
-
2007
- 2007-09-06 PL PL07803270.3T patent/PL2066679T3/pl unknown
- 2007-09-06 MX MX2011010178A patent/MX337358B/es unknown
- 2007-09-06 US US11/850,747 patent/US7741277B2/en not_active Expired - Fee Related
- 2007-09-06 EP EP07803270.3A patent/EP2066679B1/en active Active
- 2007-09-06 MX MX2009002483A patent/MX2009002483A/es active IP Right Grant
- 2007-09-06 TW TW096133272A patent/TWI346116B/zh not_active IP Right Cessation
- 2007-09-06 RS RS20160412A patent/RS54857B1/sr unknown
- 2007-09-06 CA CA2662308A patent/CA2662308C/en not_active Expired - Fee Related
- 2007-09-06 WO PCT/EP2007/059310 patent/WO2008028934A1/en active Application Filing
- 2007-09-06 AU AU2007293650A patent/AU2007293650B2/en not_active Ceased
- 2007-09-06 KR KR1020097007093A patent/KR101532966B1/ko not_active IP Right Cessation
- 2007-09-06 DK DK07803270.3T patent/DK2066679T3/en active
- 2007-09-06 AR ARP070103942A patent/AR062685A1/es not_active Application Discontinuation
- 2007-09-06 SI SI200731775A patent/SI2066679T1/sl unknown
- 2007-09-06 HU HUE07803270A patent/HUE028061T2/en unknown
- 2007-09-06 NZ NZ575032A patent/NZ575032A/en not_active IP Right Cessation
- 2007-09-06 ES ES07803270T patent/ES2572183T3/es active Active
-
2010
- 2010-03-19 US US12/728,050 patent/US8470776B2/en not_active Expired - Fee Related
- 2010-03-19 US US12/728,075 patent/US20100323963A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US20100323963A1 (en) | 2010-12-23 |
| WO2008028934A8 (en) | 2008-05-02 |
| CA2662308C (en) | 2014-10-28 |
| CA2662308A1 (en) | 2008-03-13 |
| EP2066679B1 (en) | 2016-03-09 |
| KR20090064436A (ko) | 2009-06-18 |
| AR062685A1 (es) | 2008-11-26 |
| MX2009002483A (es) | 2009-03-23 |
| US8470776B2 (en) | 2013-06-25 |
| AU2007293650B2 (en) | 2012-06-14 |
| SI2066679T1 (sl) | 2016-06-30 |
| EP2066679A1 (en) | 2009-06-10 |
| HUE028061T2 (en) | 2016-11-28 |
| RU2009112546A (ru) | 2010-10-20 |
| RS54857B1 (sr) | 2016-10-31 |
| WO2008028934A1 (en) | 2008-03-13 |
| NZ575032A (en) | 2011-02-25 |
| PL2066679T3 (pl) | 2016-09-30 |
| US20080090758A1 (en) | 2008-04-17 |
| AU2007293650A1 (en) | 2008-03-13 |
| US20100317580A1 (en) | 2010-12-16 |
| KR101532966B1 (ko) | 2015-07-02 |
| DK2066679T3 (en) | 2016-06-27 |
| MX337358B (es) | 2016-02-29 |
| TWI346116B (en) | 2011-08-01 |
| TW200823228A (en) | 2008-06-01 |
| EP1900742A1 (en) | 2008-03-19 |
| US7741277B2 (en) | 2010-06-22 |
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