AR038712A1 - Uso de epotilonas en el tratamiento de enfermedades cerebrales asociados con procesos proliferativos - Google Patents
Uso de epotilonas en el tratamiento de enfermedades cerebrales asociados con procesos proliferativosInfo
- Publication number
- AR038712A1 AR038712A1 ARP030100696A ARP030100696A AR038712A1 AR 038712 A1 AR038712 A1 AR 038712A1 AR P030100696 A ARP030100696 A AR P030100696A AR P030100696 A ARP030100696 A AR P030100696A AR 038712 A1 AR038712 A1 AR 038712A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- group
- aralkyl
- aryl
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/423—Oxazoles condensed with carbocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
) Uso de una epotilona que presenta un coeficiente de distribución promedio entre plasma y cerebro que comprende entre 0,3 y 1,5 en el ensayo de inyección de bolo intravenoso en ratón, en la preparación de un medicamento para el tratamiento de una enfermedad cerebral asociada con procesos proliferativos. Reivindicación 4: El uso de un compuesto, caracterizado porque dicho compuesto responde a la fórmula general (1) donde: R1a, R1b son, independientemente entre sí, hidrógeno, alquilo C1-10, arilo aralquilo; o forman juntos un grupo -(CH2)m-, donde m comprende entre 2 y 5; R2a, R2b son, independientemente entre sí, hidrógeno, alquilo C1-10, arilo, aralquilo; o forman juntos un grupo -(CH2)n, donde n comprende entre 2 y 5; o alquenilo C2-10; R3 es hidrógeno, alquilo C1-0, arilo, aralquilo; R4a, R4b son, independientemente entre sí, hidrógeno, alquilo C1-10, arilo, aralquilo; o forman juntos un grupo -(CH2)p, donde p comprende entre 2 y 5; R5 es hidrógeno, alquilo C1-10, arilo, aralquilo, CO2H, CO2 alquilo, CH2OH, CH2O alquilo, CH2O acilo, CN, CH2NH2, CH2N(alquilo, acilo)1,2 o CH2Hal; R6, R7 son, cada uno, hidrógeno; o forman juntos un enlace adicional o forman juntos una función epoxi; G es O ó CH2; D-E es un grupo H2C-CH2, HC=CH, C?C, CH(OH)-CH(OH); CH(OH)-CH2, CH2-CH(OH), CH2-O, O-CH2; o un resto de fórmula (2); W es un grupo C(=X)R8 o es un radical aromático o heteroaromático bi- o tricíclico; X es O ó dos grupos OR20 o un grupo alquilen(C2-10)-dioxi (que puede ser de cadena lineal o ramificada) o H/OR9 o un grupo CR10R11; R8 es hidrógeno, alquilo C1-10, arilo, aralquilo, halógeno, CN; R9 es hidrógeno o un grupo protector PGx; R10, R11 son, independientemente entre sí, hidrógeno, alquilo C1-20, arilo, aralquilo; o junto con el carbono del metileno forman un anillo carbocíclico de 5 a 7 miembros; Z es O ó H/OR12; R12 es hidrógeno o un grupo protector PGz; A-Y es un grupo O-C(=O), O-CH2, CH2-C(=O), NR21-C(=O), o NR21-SO2; R20 es un grupo alquilo C1-20; R21 es hidrógeno o alquilo C1-10; PGx, PGz es alquilo C1-20, cicloalquilo C4-7, que puede contener un átomo de oxígeno en el anillo, arilo, aralquilo, acilo C1-20, aroílo, alquilsulfonilo C1-20, arilsulfonilo, tri(alquil C1-20)sililo, di(alquil C1-20)arilsililo, (alquil C1-20)diarilsililo o tri(aralquil)sililo; como un estereoisómero único o una mezcla de distintos estereoisómeros y/o como una sal aceptable para uso farmacéutico del mismo, para la preparación de un medicamento destinado al tratamiento de una enfermedad cerebral asociada con procesos proliferativos.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36106202P | 2002-03-01 | 2002-03-01 | |
| EP02004745A EP1340498A1 (en) | 2002-03-01 | 2002-03-01 | Use of epothilones in the treatment of brain diseases associated with proliferative processes |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR038712A1 true AR038712A1 (es) | 2005-01-26 |
Family
ID=27675676
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030100696A AR038712A1 (es) | 2002-03-01 | 2003-03-03 | Uso de epotilonas en el tratamiento de enfermedades cerebrales asociados con procesos proliferativos |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US20040019088A1 (es) |
| EP (2) | EP1340498A1 (es) |
| JP (1) | JP2005525360A (es) |
| KR (1) | KR20040095244A (es) |
| CN (1) | CN100473381C (es) |
| AR (1) | AR038712A1 (es) |
| AU (1) | AU2003215618B2 (es) |
| BR (1) | BR0308154A (es) |
| CA (1) | CA2477403A1 (es) |
| CR (1) | CR7444A (es) |
| EC (1) | ECSP045340A (es) |
| HK (1) | HK1079998A1 (es) |
| HR (1) | HRP20040892A2 (es) |
| IL (1) | IL163752A0 (es) |
| MX (1) | MXPA04008450A (es) |
| NO (1) | NO20044175L (es) |
| NZ (1) | NZ546617A (es) |
| PL (1) | PL370768A1 (es) |
| RU (1) | RU2351330C2 (es) |
| UA (1) | UA83798C2 (es) |
| WO (1) | WO2003074053A1 (es) |
| YU (1) | YU76404A (es) |
| ZA (1) | ZA200407905B (es) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0977563B1 (en) | 1996-12-03 | 2005-10-12 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| CA2299608A1 (en) * | 1997-08-09 | 1999-02-18 | Schering Aktiengesellschaft | New epothilone derivatives, method for producing same and their pharmaceutical use |
| BR0008206A (pt) * | 1999-02-11 | 2002-02-19 | Schering Ag | Derivados de epotilon, processos para a sua preparação e sua aplicação farmacêutica |
| US7125893B1 (en) * | 1999-04-30 | 2006-10-24 | Schering Ag | 6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations |
| CN102532120A (zh) | 2002-08-23 | 2012-07-04 | 索隆-基特林癌症研究协会 | 埃坡霉素(epothilone)，合成埃坡霉素的中间体，其类似物及其用途 |
| US7649006B2 (en) | 2002-08-23 | 2010-01-19 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| DE10331004A1 (de) * | 2003-07-03 | 2005-02-24 | Schering Ag | Verfahren für die Herstellung von C1-C15-Fragmenten von Epothilonen und deren Derivaten |
| EP1559447A1 (en) * | 2004-01-30 | 2005-08-03 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Use of epothilones in the treatment of neuronal connectivity defects such as schizophrenia and autism |
| US20060069136A1 (en) * | 2004-09-24 | 2006-03-30 | Ulrich Klar | Use of Epothilones in the treatment of bone metastasis |
| US20060121511A1 (en) | 2004-11-30 | 2006-06-08 | Hyerim Lee | Biomarkers and methods for determining sensitivity to microtubule-stabilizing agents |
| EP1674098A1 (en) * | 2004-12-23 | 2006-06-28 | Schering Aktiengesellschaft | Stable and tolerable parental formulations of highly reactive organic drug substances with low or no solubility in water |
| EP1700596A1 (en) * | 2005-03-09 | 2006-09-13 | Max-Planck-Gesellschaft Zur Förderung Der Wissenschaften E.V. | Use of microtubule stabilizing compounds for the treatment of lesions of CNS axons |
| DE102007016046A1 (de) * | 2007-03-30 | 2008-10-23 | Bayer Schering Pharma Aktiengesellschaft | Verfahren zur Herstellung von Epothilonderivaten durch selektive katalytische Epoxidierung |
| TWI472329B (zh) | 2008-04-24 | 2015-02-11 | 必治妥美雅史谷比公司 | 埃坡徽素ｄ於治療包括阿茲海默症之ｔａｕ相關疾病的用途 |
| EP2793947B1 (en) | 2011-12-23 | 2021-02-03 | Innate Pharma | Enzymatic conjugation of polypeptides |
| US10132799B2 (en) | 2012-07-13 | 2018-11-20 | Innate Pharma | Screening of conjugated antibodies |
| EP2916872B1 (en) | 2012-11-09 | 2019-02-27 | Innate Pharma | Recognition tags for tgase-mediated conjugation |
| WO2014140300A1 (en) | 2013-03-15 | 2014-09-18 | Innate Pharma | Solid phase tgase-mediated conjugation of antibodies |
| US10071169B2 (en) | 2013-06-20 | 2018-09-11 | Innate Pharma | Enzymatic conjugation of polypeptides |
| KR20160042871A (ko) | 2013-06-21 | 2016-04-20 | 이나뜨 파르마, 에스.아. | 폴리펩티드의 효소적 콘쥬게이션 |
| WO2019092148A1 (en) | 2017-11-10 | 2019-05-16 | Innate Pharma | Antibodies with functionalized glutamine residues |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3226545B2 (ja) * | 1995-06-09 | 2001-11-05 | ノバルティス・アクチエンゲゼルシャフト | ラパマイシン誘導体 |
| US6515016B2 (en) * | 1996-12-02 | 2003-02-04 | Angiotech Pharmaceuticals, Inc. | Composition and methods of paclitaxel for treating psoriasis |
| US6495579B1 (en) * | 1996-12-02 | 2002-12-17 | Angiotech Pharmaceuticals, Inc. | Method for treating multiple sclerosis |
| BR9807418A (pt) * | 1997-02-18 | 2002-01-22 | Canji Inc | Terapia de gene supressor de tumor combinado e quimioterapia no tratamento de neoplasmas |
| GB9801231D0 (en) * | 1997-06-05 | 1998-03-18 | Merck & Co Inc | A method of treating cancer |
| US6605599B1 (en) * | 1997-07-08 | 2003-08-12 | Bristol-Myers Squibb Company | Epothilone derivatives |
| CA2299608A1 (en) * | 1997-08-09 | 1999-02-18 | Schering Aktiengesellschaft | New epothilone derivatives, method for producing same and their pharmaceutical use |
| JP4434484B2 (ja) * | 1997-12-04 | 2010-03-17 | ブリストル−マイヤーズ スクイブ カンパニー | オキシラニルエポチロン化合物のオレフィン性エポチロン化合物への還元法 |
| FR2775187B1 (fr) * | 1998-02-25 | 2003-02-21 | Novartis Ag | Utilisation de l'epothilone b pour la fabrication d'une preparation pharmaceutique antiproliferative et d'une composition comprenant l'epothilone b comme agent antiproliferatif in vivo |
| US6302838B1 (en) * | 1998-02-25 | 2001-10-16 | Novartis Ag | Cancer treatment with epothilones |
| AU4775299A (en) * | 1998-06-22 | 2000-01-10 | Nicolaou, Kyriacos Costa | Desmethyl epothilones |
| ES2291194T3 (es) * | 1999-02-18 | 2008-03-01 | Bayer Schering Pharma Aktiengesellschaft | Derivados de 16-halogeno-epotilones, procedimiento acerca de su preparacion y su utilizacion farmaceutica. |
| AR023792A1 (es) * | 1999-04-30 | 2002-09-04 | Bayer Schering Pharma Ag | Derivados 6-alquenilo- y 6-alquinilo-epotilona, los procedimientos para prepararlos y su empleo en productos farmaceuticos |
| EP2289549A3 (en) * | 1999-10-01 | 2011-06-15 | Immunogen, Inc. | Immunoconjugates for treating cancer |
| DE10020517A1 (de) * | 2000-04-19 | 2001-10-25 | Schering Ag | Neue Epothilon-Derivate, Verfahren zu deren Herstellung und ihre pharmazeutische Verwendung |
| WO2001092255A2 (en) * | 2000-05-26 | 2001-12-06 | Kosan Biosciences, Inc. | Epothilone derivatives and methods for making and using the same |
| GB0013643D0 (en) * | 2000-05-31 | 2000-07-26 | Unilever Plc | Targeted moieties for use in bleach catalysts |
| CA2449077A1 (en) * | 2001-06-01 | 2002-12-12 | Gregory D. Vite | Epothilone derivatives |
-
2002
- 2002-03-01 EP EP02004745A patent/EP1340498A1/en not_active Withdrawn
-
2003
- 2003-02-28 BR BR0308154-0A patent/BR0308154A/pt not_active Withdrawn
- 2003-02-28 RU RU2004129325/15A patent/RU2351330C2/ru active
- 2003-02-28 US US10/375,043 patent/US20040019088A1/en not_active Abandoned
- 2003-02-28 CN CNB038097613A patent/CN100473381C/zh not_active Expired - Fee Related
- 2003-02-28 IL IL16375203A patent/IL163752A0/xx unknown
- 2003-02-28 NZ NZ546617A patent/NZ546617A/en unknown
- 2003-02-28 EP EP03743360A patent/EP1480643A1/en not_active Withdrawn
- 2003-02-28 CA CA002477403A patent/CA2477403A1/en not_active Abandoned
- 2003-02-28 PL PL03370768A patent/PL370768A1/xx not_active Application Discontinuation
- 2003-02-28 AU AU2003215618A patent/AU2003215618B2/en not_active Expired - Fee Related
- 2003-02-28 KR KR10-2004-7013549A patent/KR20040095244A/ko not_active Application Discontinuation
- 2003-02-28 WO PCT/EP2003/002085 patent/WO2003074053A1/en active Application Filing
- 2003-02-28 MX MXPA04008450A patent/MXPA04008450A/es not_active Application Discontinuation
- 2003-02-28 YU YU76404A patent/YU76404A/sh unknown
- 2003-02-28 JP JP2003572570A patent/JP2005525360A/ja active Pending
- 2003-02-28 UA UA20040907817A patent/UA83798C2/ru unknown
- 2003-03-03 AR ARP030100696A patent/AR038712A1/es unknown
-
2004
- 2004-09-01 CR CR7444A patent/CR7444A/es not_active Application Discontinuation
- 2004-09-28 HR HRP20040892 patent/HRP20040892A2/hr not_active Application Discontinuation
- 2004-09-30 ZA ZA200407905A patent/ZA200407905B/en unknown
- 2004-09-30 NO NO20044175A patent/NO20044175L/no not_active Application Discontinuation
- 2004-09-30 EC EC2004005340A patent/ECSP045340A/es unknown
-
2006
- 2006-01-04 HK HK06100157.3A patent/HK1079998A1/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ECSP045340A (es) | 2004-11-26 |
| US20040019088A1 (en) | 2004-01-29 |
| NO20044175L (no) | 2004-12-01 |
| EP1340498A1 (en) | 2003-09-03 |
| YU76404A (sh) | 2006-08-17 |
| BR0308154A (pt) | 2005-01-04 |
| IL163752A0 (en) | 2005-12-18 |
| EP1480643A1 (en) | 2004-12-01 |
| RU2351330C2 (ru) | 2009-04-10 |
| UA83798C2 (ru) | 2008-08-26 |
| AU2003215618A1 (en) | 2003-09-16 |
| AU2003215618B2 (en) | 2009-06-04 |
| CA2477403A1 (en) | 2003-09-12 |
| WO2003074053A1 (en) | 2003-09-12 |
| PL370768A1 (en) | 2005-05-30 |
| ZA200407905B (en) | 2006-04-26 |
| HRP20040892A2 (en) | 2004-12-31 |
| CR7444A (es) | 2005-10-05 |
| NZ546617A (en) | 2007-12-21 |
| MXPA04008450A (es) | 2005-07-13 |
| CN100473381C (zh) | 2009-04-01 |
| HK1079998A1 (zh) | 2006-04-21 |
| CN1649587A (zh) | 2005-08-03 |
| RU2004129325A (ru) | 2005-07-10 |
| KR20040095244A (ko) | 2004-11-12 |
| JP2005525360A (ja) | 2005-08-25 |
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