BR0009449A - Compound, process for preparing a compound, composition, use of a compound, and methods for treating or preventing a disease in a mammal where a phosphodiesterase isoenzyme inhibitor and / or a bronchodilator should be expected to be beneficial for the treatment or prevention of asthma in a mammal and for the treatment or prevention of chronic obstructive pulmonary disease (copd) in a mammal - Google Patents
Compound, process for preparing a compound, composition, use of a compound, and methods for treating or preventing a disease in a mammal where a phosphodiesterase isoenzyme inhibitor and / or a bronchodilator should be expected to be beneficial for the treatment or prevention of asthma in a mammal and for the treatment or prevention of chronic obstructive pulmonary disease (copd) in a mammalInfo
- Publication number
- BR0009449A BR0009449A BR0009449-8A BR0009449A BR0009449A BR 0009449 A BR0009449 A BR 0009449A BR 0009449 A BR0009449 A BR 0009449A BR 0009449 A BR0009449 A BR 0009449A
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- treatment
- mammal
- prevention
- alkyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
"COMPOSTO, PROCESSO PARA PREPARAR UM COMPOSTO, COMPOSIçãO, USO DE UM COMPOSTO, E, MéTODOS PARA O TRATAMENTO OU PREVENçãO DE UMA DOENçA EM UM MAMìFERO ONDE DEVE-SE ESPERAR QUE UM INIBIDOR DA ISOENZIMA DE FOSFODIESTERASE E/OU UM BRONCODILATADOR SEJAM BENéFICOS, PARA O TRATAMENTO OU PREVENçãO DA ASMA EM UM MAMìFERO E PARA O TRATAMENTO OU PREVENçãO DA DOENçA PULMONAR OBSTRUTIVA CRÈNICA (COPD) EM UM MAMìFERO". Os compostos da fórmula geral (I) em que cada um de R^ 1^ e R^ 2^ representa independentemente um grupo alquila C~ 1-6~ ou acila C~ 2-7~; X representa OCH~ 2~ ou um grupo CR^ 3^R^ 4^, em que cada um de R^ 3^ ou R^ 4^ representa independentemente um átomo de hidrogênio ou um grupo alquila C~ 1-3~; R^ 5^ representa um átomo de hidrogênio ou um grupo alquila C~ 1-3~, alquenila C~ 2-3~ ou alquinila C~ 2-3~; R^ 3^ representa um átomo de hidrogênio ou um grupo alquila C~ 1-6~, alquenila C~ 2-6~, alquinila C~ 2-6~, amino, alquila C~ 1-6~ amino, dialquila (C~ 1-6~) amino ou acilamino C~ 2-7~; cada um de R^ 7^ e R^ 8^ representa independentemente um átomo de hidrogênio ou halógeno ou um hidróxi, trifluorometila, alquila C~ 1-6~, alquenila C~ 2-6~, alquinila C~ 2-6~, acila C~ 2-7~, alquiltio C~ 1-6~, alcóxi C~ 1-6~, cicloalquila C~ 3-6~; R^ 9^ representa um átomo de hidrogênio ou halógeno ou um grupo hidróxi, trifluorometila, alquila C~ 1-6~, alquenila C~ 2-6~, alquinila C~ 2-6~, acila C~ 2-7~, alquiltio C~ 1-6~, alcóxi C~ 1-6~ ou cicloalquila C~ 3-6~, ou sais destes são úteis para o tratamento de distúrbios respiratórios tais como a asma. Os compostos da invenção têm uma duração maior de ação do que o composto conhecido trequinsina (9,10-dimetóxi-3-metil-2-mesitilimino-2,3,6,7-tetra-hidro-4H-pirimido[6, 1-a]isoquinolin-4-ona) e a trequinsina não tem gosto muito amargo."COMPOUND, PROCESS TO PREPARE A COMPOUND, COMPOSITION, USE OF A COMPOUND, AND METHODS FOR THE TREATMENT OR PREVENTION OF A DISEASE IN A MAMMALIAN WHERE TO EXPOSE AN INHIBITOR OF PHOSPHODIESTERASE AND / OR A BRONCODYLOSIS, OR BRONZODYCHEMISTRY FOR THE TREATMENT OR PREVENTION OF ASTHMA IN A MAMMALIAN AND FOR THE TREATMENT OR PREVENTION OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) IN A MAMMALIAN ". The compounds of the general formula (I) in which each of R ^ 1 ^ ^ and R ^ 2 ^ ^ independently represents a C ~ 1-6 ~ alkyl or C ~ 2-7 ~ acyl group; X represents OCH ~ 2 ~ or a CR ^ 3 ^ R ^ 4 ^ group, each of R ^ 3 ^ or R ^ 4 ^ independently representing a hydrogen atom or a C ~ 1-3 ~ alkyl group; R5 represents a hydrogen atom or a C ~ 1-3 ~ alkyl, C ~ 2-3 ~ alkenyl or C ~ 2-3 ~ alkynyl group; R ^ 3 ^ represents a hydrogen atom or a C ~ 1-6 ~ alkyl, C ~ 2-6 ~ alkenyl, C ~ 2-6 ~ alkynyl, amino, C ~ 1-6 ~ amino, dialkyl (C ~ 1-6 ~) amino or C ~ 2-7 ~ acylamino; each of R ^ 7 ^ and R ^ 8 ^ independently represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C ~ 1-6 ~ alkyl, C ~ 2-6 ~ alkenyl, C ~ 2-6 ~ alkynyl, C ~ 2-7 ~ acyl, C ~ 1-6 ~ alkylthio, C ~ 1-6 ~ alkoxy, C ~ 3-6 ~ cycloalkyl; R ^ 9 ^ represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C ~ 1-6 ~ alkyl, C ~ 2-6 ~ alkenyl, C ~ 2-6 ~ alkynyl, C ~ 2-7 ~ acyl group, C ~ 1-6 ~ alkylthio, C ~ 1-6 ~ alkoxy or C ~ 3-6 ~ cycloalkyl, or salts thereof are useful for the treatment of respiratory disorders such as asthma. The compounds of the invention have a longer duration of action than the known compound trequininsin (9,10-dimethoxy-3-methyl-2-mesitylimino-2,3,6,7-tetrahydro-4H-pyrimido [6, 1 -a] isoquinolin-4-one) and threquinsin does not taste very bitter.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9907456.9A GB9907456D0 (en) | 1999-03-31 | 1999-03-31 | Compounds |
| GBGB9909803.0A GB9909803D0 (en) | 1999-04-28 | 1999-04-28 | Compounds |
| PCT/GB2000/001195 WO2000058309A1 (en) | 1999-03-31 | 2000-03-29 | Derivatives of pyrimido[6,1-a]isoquinolin-4-one |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR0009449A true BR0009449A (en) | 2002-01-08 |
Family
ID=26315370
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0009449-8A BR0009449A (en) | 1999-03-31 | 2000-03-29 | Compound, process for preparing a compound, composition, use of a compound, and methods for treating or preventing a disease in a mammal where a phosphodiesterase isoenzyme inhibitor and / or a bronchodilator should be expected to be beneficial for the treatment or prevention of asthma in a mammal and for the treatment or prevention of chronic obstructive pulmonary disease (copd) in a mammal |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP1165556A1 (en) |
| JP (1) | JP2002543046A (en) |
| CN (1) | CN1348452A (en) |
| AU (1) | AU3974700A (en) |
| BR (1) | BR0009449A (en) |
| CA (1) | CA2368460A1 (en) |
| MX (1) | MXPA01009847A (en) |
| NO (1) | NO20014729L (en) |
| NZ (1) | NZ514157A (en) |
| WO (1) | WO2000058309A1 (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR089284A1 (en) * | 2011-12-22 | 2014-08-13 | Galapagos Nv | DIHYDROPIRIMIDINOISOQUINOLINONES AND PHARMACEUTICAL COMPOSITIONS OF THE SAME FOR THE TREATMENT OF INFLAMMATORY DISORDERS |
-
2000
- 2000-03-29 CN CN00806771A patent/CN1348452A/en active Pending
- 2000-03-29 WO PCT/GB2000/001195 patent/WO2000058309A1/en not_active Application Discontinuation
- 2000-03-29 CA CA002368460A patent/CA2368460A1/en not_active Abandoned
- 2000-03-29 BR BR0009449-8A patent/BR0009449A/en not_active IP Right Cessation
- 2000-03-29 EP EP00918982A patent/EP1165556A1/en not_active Withdrawn
- 2000-03-29 AU AU39747/00A patent/AU3974700A/en not_active Abandoned
- 2000-03-29 MX MXPA01009847A patent/MXPA01009847A/en unknown
- 2000-03-29 JP JP2000608011A patent/JP2002543046A/en active Pending
- 2000-03-29 NZ NZ514157A patent/NZ514157A/en unknown
-
2001
- 2001-09-28 NO NO20014729A patent/NO20014729L/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| CA2368460A1 (en) | 2000-10-05 |
| NO20014729D0 (en) | 2001-09-28 |
| NZ514157A (en) | 2003-08-29 |
| AU3974700A (en) | 2000-10-16 |
| MXPA01009847A (en) | 2003-06-24 |
| WO2000058309A1 (en) | 2000-10-05 |
| NO20014729L (en) | 2001-11-23 |
| JP2002543046A (en) | 2002-12-17 |
| CN1348452A (en) | 2002-05-08 |
| EP1165556A1 (en) | 2002-01-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application fees: dismissal - article 86 of industrial property law |
Free format text: REFERENTE A 5A, 6A E 7A ANUIDADES. |
|
| B08K | Lapse as no evidence of payment of the annual fee has been furnished to inpi (acc. art. 87) |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 1925 DE 27/11/2007. |