AR050947A1 - Derivados de 3,4-dihidro-3-metil-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazina-8-carboxilato - Google Patents
Derivados de 3,4-dihidro-3-metil-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazina-8-carboxilatoInfo
- Publication number
- AR050947A1 AR050947A1 ARP050103949A ARP050103949A AR050947A1 AR 050947 A1 AR050947 A1 AR 050947A1 AR P050103949 A ARP050103949 A AR P050103949A AR P050103949 A ARP050103949 A AR P050103949A AR 050947 A1 AR050947 A1 AR 050947A1
- Authority
- AR
- Argentina
- Prior art keywords
- composition
- oxoimidazo
- tetrazine
- dihydro
- branched
- Prior art date
Links
- VVTMIOYTNALQAW-UHFFFAOYSA-N 3-methyl-4-oxoimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxylic acid Chemical class O=C1N(C)N=NC2=C(C(O)=O)N=CN21 VVTMIOYTNALQAW-UHFFFAOYSA-N 0.000 title 1
- 239000000203 mixture Substances 0.000 abstract 6
- 238000000034 method Methods 0.000 abstract 3
- -1 3,4-dihydro-3-methyl-4-oxoimidazo [5,1-d] -1,2,3,5-tetrazine-8-carboxylate compound Chemical class 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 1
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 1
- 230000002378 acidificating effect Effects 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 230000000259 anti-tumor effect Effects 0.000 abstract 1
- 239000000729 antidote Substances 0.000 abstract 1
- 229940075522 antidotes Drugs 0.000 abstract 1
- 239000012059 conventional drug carrier Substances 0.000 abstract 1
- 239000002552 dosage form Substances 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 229910052736 halogen Chemical group 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 239000006186 oral dosage form Substances 0.000 abstract 1
- 150000003333 secondary alcohols Chemical class 0.000 abstract 1
- 150000003509 tertiary alcohols Chemical class 0.000 abstract 1
- 238000011200 topical administration Methods 0.000 abstract 1
- 239000006211 transdermal dosage form Substances 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
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente describe el compuesto de 3,4-dihidro-3-metil-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazina-8-carboxilato de la formula general (1), un procedimiento para producirlo, una composicion farmacéutica que lo comprende y el uso del compuesto y su composicion en la fabricacion de un medicamento para el tratamiento de un tumor. Dicha composicion comprende uno o más compuestos de temozolomida-8-carboxilato de formula (1) como el ingrediente activo y portadores farmacéuticos convencionales. Dicha composicion puede también comprender uno o más componentes ácidos farmacéuticamente aceptables y opcionalmente un alcohol secundario o alcohol terciario o derivados éster del mismo. Además, dicha composicion puede ser preparada en todos los tipos de formas de dosificacion convencional, en particular las formas de dosificacion oral y una forma de dosificacion transdérmica para administracion topica. Adicionalmente, la presente describe un método para utilizar estos compuestos y composiciones para el tratamiento de un tumor. Métodos para prepararlos, composiciones farmacéuticas que los contienen y usos de los derivados y composiciones en la fabricacion de medicamentos que poseen antídotos antitumorales. Reivindicacion 1: Un compuesto de 3,4-dihidro-3-metil-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazina-8-carboxilato de la formula general (1), en donde X es O o S; R es un alquilo C3-10 lineal o ramificado sustituido o no sustituido, cicloalquilo C3-10, alquenilo C3-10 lineal o ramificado o una cadena alquinilo C3-10 lineal o ramificada; y si R tiene un grupo sustituyente, dicho grupo sustituyente puede ser alquilo C1-6, alcoxi C1-6, grupo alquiltio C1-6, grupo alquil amino C1-6, fenilo o fenilo sustituido con halogeno.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2004100720564A CN1752088A (zh) | 2004-09-22 | 2004-09-22 | 含有替莫唑胺酯的药用组合物 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR050947A1 true AR050947A1 (es) | 2006-12-06 |
Family
ID=36089840
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050103949A AR050947A1 (es) | 2004-09-22 | 2005-09-21 | Derivados de 3,4-dihidro-3-metil-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazina-8-carboxilato |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US7579336B2 (es) |
| EP (1) | EP1798234B1 (es) |
| JP (2) | JP5620046B2 (es) |
| KR (1) | KR101065984B1 (es) |
| CN (1) | CN1752088A (es) |
| AR (1) | AR050947A1 (es) |
| AU (1) | AU2005287799B2 (es) |
| BR (1) | BRPI0515555A (es) |
| CA (1) | CA2580910C (es) |
| DK (1) | DK1798234T3 (es) |
| ES (1) | ES2389376T3 (es) |
| IL (1) | IL182027A (es) |
| MX (1) | MX2007003366A (es) |
| MY (1) | MY153713A (es) |
| NZ (1) | NZ554609A (es) |
| PL (1) | PL1798234T3 (es) |
| RU (1) | RU2393160C2 (es) |
| UA (1) | UA89795C2 (es) |
| WO (1) | WO2006032190A1 (es) |
| ZA (1) | ZA200702801B (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1727340B (zh) * | 2004-07-29 | 2011-05-18 | 天津帝士力投资控股集团有限公司 | 一种替莫唑胺-8-羧酸酯及其组合物 |
| EP1808173A1 (en) * | 2006-01-12 | 2007-07-18 | Matthias Dormeyer | Use of CNS penetrating anticancer compounds for the treatment of protozan diseases |
| US8558511B2 (en) * | 2009-04-07 | 2013-10-15 | Battelle Memorial Institute | Method and apparatus for smart battery charging including a plurality of controllers each monitoring input variables |
| KR20140087846A (ko) * | 2012-12-31 | 2014-07-09 | 주식회사 삼양바이오팜 | 테모졸로미드를 포함하는 안정성이 개선된 약제학적 조성물 및 이의 제조방법 |
| RU2527258C1 (ru) * | 2013-02-19 | 2014-08-27 | Автономная Некоммерческая Организация "Научно-Исследовательский Центр Биотехнологии Антибиотиков И Других Биологически Активных Веществ "Биоан" | 6-ЗАМЕЩЕННЫЕ 3-АЗОЛИЛИМИДАЗО[1,2-b][1,2,4,5]ТЕТРАЗИНЫ, ПРОЯВЛЯЮЩИЕ ПРОТИВООПУХОЛЕВУЮ АКТИВНОСТЬ |
| US10709715B2 (en) * | 2017-12-03 | 2020-07-14 | Cipla Limited | Method of treating hypertension |
| EP3833342A4 (en) | 2018-08-09 | 2022-07-13 | The Board of Trustees of the University of Illinois | IMIDAZOTETRAZINE COMPOUNDS |
| CN114014862A (zh) * | 2021-06-28 | 2022-02-08 | 烟台大学 | 一种治疗脑胶质瘤的新化合物及其制备和应用 |
| CN115260107B (zh) * | 2022-06-23 | 2023-11-24 | 烟台邦杰生物科技有限公司 | 一种抗肿瘤药物前药、药物组合物及在肿瘤靶向治疗领域的应用 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8616125D0 (en) * | 1986-07-02 | 1986-08-06 | May & Baker Ltd | Compositions of matter |
| EP0922458A1 (en) * | 1993-01-14 | 1999-06-16 | Cancer Research Campaign Technology Limited | Potentiation of temozolomide by an ATase inhibitor |
| CN1244583C (zh) | 2002-09-29 | 2006-03-08 | 天津天士力集团有限公司 | 替莫唑胺－8－羧酸脂和－8－酰胺衍生物，它们的合成方法以及它们在制备抗癌制剂中的应用 |
| CN1742723A (zh) * | 2004-09-02 | 2006-03-08 | 天津倍方科技发展有限公司 | 含有替莫唑胺－8－羧酸酯的药物组合物以及该类化合物用于制备抗肿瘤药物的用途 |
-
2004
- 2004-09-22 CN CNA2004100720564A patent/CN1752088A/zh active Pending
-
2005
- 2005-09-15 NZ NZ554609A patent/NZ554609A/en not_active IP Right Cessation
- 2005-09-15 PL PL05785075T patent/PL1798234T3/pl unknown
- 2005-09-15 US US11/575,849 patent/US7579336B2/en not_active Expired - Fee Related
- 2005-09-15 CA CA2580910A patent/CA2580910C/en not_active Expired - Fee Related
- 2005-09-15 EP EP05785075A patent/EP1798234B1/en not_active Expired - Lifetime
- 2005-09-15 AU AU2005287799A patent/AU2005287799B2/en not_active Ceased
- 2005-09-15 BR BRPI0515555-0A patent/BRPI0515555A/pt not_active IP Right Cessation
- 2005-09-15 KR KR1020077009054A patent/KR101065984B1/ko not_active Expired - Fee Related
- 2005-09-15 DK DK05785075.2T patent/DK1798234T3/da active
- 2005-09-15 WO PCT/CN2005/001477 patent/WO2006032190A1/zh not_active Ceased
- 2005-09-15 MX MX2007003366A patent/MX2007003366A/es active IP Right Grant
- 2005-09-15 RU RU2007114948/04A patent/RU2393160C2/ru not_active IP Right Cessation
- 2005-09-15 UA UAA200704418A patent/UA89795C2/ru unknown
- 2005-09-15 ES ES05785075T patent/ES2389376T3/es not_active Expired - Lifetime
- 2005-09-15 JP JP2007532748A patent/JP5620046B2/ja not_active Expired - Fee Related
- 2005-09-21 AR ARP050103949A patent/AR050947A1/es not_active Application Discontinuation
- 2005-09-22 MY MYPI20054428A patent/MY153713A/en unknown
-
2007
- 2007-03-19 IL IL182027A patent/IL182027A/en not_active IP Right Cessation
- 2007-04-03 ZA ZA200702801A patent/ZA200702801B/xx unknown
-
2012
- 2012-09-24 JP JP2012209183A patent/JP2013028630A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| CN1752088A (zh) | 2006-03-29 |
| US20080044457A1 (en) | 2008-02-21 |
| EP1798234A4 (en) | 2009-04-29 |
| EP1798234A1 (en) | 2007-06-20 |
| DK1798234T3 (da) | 2012-08-27 |
| IL182027A (en) | 2014-05-28 |
| JP2013028630A (ja) | 2013-02-07 |
| MX2007003366A (es) | 2008-03-05 |
| KR20070062569A (ko) | 2007-06-15 |
| UA89795C2 (ru) | 2010-03-10 |
| JP2008513523A (ja) | 2008-05-01 |
| NZ554609A (en) | 2010-06-25 |
| KR101065984B1 (ko) | 2011-09-19 |
| ES2389376T3 (es) | 2012-10-25 |
| IL182027A0 (en) | 2007-07-24 |
| AU2005287799A1 (en) | 2006-03-30 |
| CA2580910C (en) | 2011-10-25 |
| HK1100440A1 (en) | 2007-09-21 |
| WO2006032190A1 (en) | 2006-03-30 |
| JP5620046B2 (ja) | 2014-11-05 |
| MY153713A (en) | 2015-03-13 |
| BRPI0515555A (pt) | 2008-07-29 |
| RU2393160C2 (ru) | 2010-06-27 |
| RU2007114948A (ru) | 2008-10-27 |
| US7579336B2 (en) | 2009-08-25 |
| EP1798234B1 (en) | 2012-06-13 |
| ZA200702801B (en) | 2008-08-27 |
| CA2580910A1 (en) | 2006-03-30 |
| PL1798234T3 (pl) | 2012-11-30 |
| AU2005287799B2 (en) | 2009-03-26 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |