BR0116347A - Derivados pirazinoquinoxalina substituìdos como agonistas e antagonistas do receptor de serotonina - Google Patents
Derivados pirazinoquinoxalina substituìdos como agonistas e antagonistas do receptor de serotoninaInfo
- Publication number
- BR0116347A BR0116347A BR0116347-7A BR0116347A BR0116347A BR 0116347 A BR0116347 A BR 0116347A BR 0116347 A BR0116347 A BR 0116347A BR 0116347 A BR0116347 A BR 0116347A
- Authority
- BR
- Brazil
- Prior art keywords
- disorders
- antagonists
- novel compounds
- receptor agonists
- serotonin receptor
- Prior art date
Links
- 239000003420 antiserotonin agent Substances 0.000 title abstract 3
- 239000000952 serotonin receptor agonist Substances 0.000 title abstract 3
- CVSGFMWKZVZOJD-UHFFFAOYSA-N pyrazino[2,3-f]quinoxaline Chemical class C1=CN=C2C3=NC=CN=C3C=CC2=N1 CVSGFMWKZVZOJD-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 208000018522 Gastrointestinal disease Diseases 0.000 abstract 1
- 206010019233 Headaches Diseases 0.000 abstract 1
- 208000019695 Migraine disease Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 208000028017 Psychotic disease Diseases 0.000 abstract 1
- 206010041250 Social phobia Diseases 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000004064 dysfunction Effects 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- 210000001035 gastrointestinal tract Anatomy 0.000 abstract 1
- 231100000869 headache Toxicity 0.000 abstract 1
- 206010027599 migraine Diseases 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000004899 motility Effects 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 208000012201 sexual and gender identity disease Diseases 0.000 abstract 1
- 208000015891 sexual disease Diseases 0.000 abstract 1
- 208000019116 sleep disease Diseases 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity 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
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Child & Adolescent Psychology (AREA)
- Anesthesiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Saccharide Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
"DERIVADOS PIRAZINOQUINOXALINA SUBSTITUìDOS COMO AGONISTAS E ANTAGONISTAS DO RECEPTOR DE SEROTONINA". A presente invenção direciona-se a novos compostos representados pelas Fórmulas estruturais (I) e (I-a) ou um sal farmaceuticamente aceitável destes, onde descreve-se R1, R4a, R4b, RS, R6, R7, R8, R9, n e X. A invenção também diz respeito a formulações farmacêuticas compreendendo esses novos compostos como ingredientes ativos e ao uso dos novos compostos e suas formulações no tratamento de alguns distúrbios. Os compostos desta invenção são agonistas e antagonistas de serotonina, sendo de utilidade no controle ou prevenção de distúrbios do sistema nervoso central, incluindo obesidade, ansiedade, depressão, psicose, esquizofrenia, distúrbios do sono e distúrbios sexuais, enxaqueca e outras condições associadas com dor cefálica, fobias sociais, e distúrbios gastrintestinais, como disfunção da motilidade do trato gastrintestinal.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25676500P | 2000-12-20 | 2000-12-20 | |
| PCT/US2001/049374 WO2002059127A2 (en) | 2000-12-20 | 2001-12-19 | Pyrazinoquinoxaline derivatives as serotonin agonists and antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR0116347A true BR0116347A (pt) | 2004-07-06 |
Family
ID=22973498
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0116347-7A BR0116347A (pt) | 2000-12-20 | 2001-12-19 | Derivados pirazinoquinoxalina substituìdos como agonistas e antagonistas do receptor de serotonina |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US6638934B2 (pt) |
| EP (1) | EP1345942B9 (pt) |
| JP (2) | JP4346307B2 (pt) |
| KR (1) | KR20030069192A (pt) |
| CN (1) | CN1505631A (pt) |
| AT (1) | ATE318819T1 (pt) |
| AU (1) | AU2002248216B2 (pt) |
| BG (1) | BG107864A (pt) |
| BR (1) | BR0116347A (pt) |
| CA (1) | CA2431970A1 (pt) |
| DE (1) | DE60117617T2 (pt) |
| EE (1) | EE200300301A (pt) |
| ES (1) | ES2260335T3 (pt) |
| HU (1) | HUP0303513A3 (pt) |
| IL (1) | IL156201A0 (pt) |
| IS (1) | IS6850A (pt) |
| MX (1) | MXPA03005437A (pt) |
| NO (1) | NO20032795L (pt) |
| PL (1) | PL366060A1 (pt) |
| RU (1) | RU2003121406A (pt) |
| SK (1) | SK7022003A3 (pt) |
| WO (1) | WO2002059127A2 (pt) |
| ZA (1) | ZA200304303B (pt) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002059127A2 (en) * | 2000-12-20 | 2002-08-01 | Bristol-Myers Squibb Pharma Company | Pyrazinoquinoxaline derivatives as serotonin agonists and antagonists |
| US7244843B2 (en) * | 2003-10-07 | 2007-07-17 | Bristol-Myers Squibb Company | Modulators of serotonin receptors |
| GB0417558D0 (en) * | 2004-08-06 | 2004-09-08 | Merck Sharp & Dohme | Novel combination therapy |
| EP2400300A1 (en) | 2004-08-25 | 2011-12-28 | Takeda Pharmaceutical Company Limited | Method of screening preventives/remedies for stress urinary incontinence |
| WO2007132841A1 (ja) | 2006-05-16 | 2007-11-22 | Takeda Pharmaceutical Company Limited | 縮合複素環化合物およびその用途 |
| WO2009063992A1 (ja) | 2007-11-15 | 2009-05-22 | Takeda Pharmaceutical Company Limited | 縮合ピリジン誘導体およびその用途 |
| JPWO2011071136A1 (ja) | 2009-12-11 | 2013-04-22 | アステラス製薬株式会社 | 線維筋痛症治療剤 |
| US20130267500A1 (en) | 2010-09-01 | 2013-10-10 | Arena Pharmaceuticals, Inc. | 5-ht2c receptor agonists in the treatment of disorders ameliorated by reduction of norepinephrine level |
| CA2891122C (en) | 2012-11-14 | 2021-07-20 | The Johns Hopkins University | Methods and compositions for treating schizophrenia |
| WO2015066344A1 (en) | 2013-11-01 | 2015-05-07 | Arena Pharmaceuticals, Inc. | 5-ht2c receptor agonists and compositions and methods of use |
| JPWO2019131902A1 (ja) | 2017-12-27 | 2020-12-10 | 武田薬品工業株式会社 | 腹圧性尿失禁および便失禁の治療薬 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3914421A (en) | 1972-06-19 | 1975-10-21 | Endo Lab | Pyridopyrrolobenzheterocycles for combatting depression |
| US4115577A (en) | 1972-06-19 | 1978-09-19 | Endo Laboratories, Inc. | Pyridopyrrolobenzheterocycles |
| US4183936A (en) | 1972-06-19 | 1980-01-15 | Endo Laboratories, Inc. | Pyridopyrrolobenzheterocycles |
| US4013652A (en) | 1972-06-19 | 1977-03-22 | Endo Laboratories, Inc. | Pyridopyrrolobenzoxazine |
| US4238607A (en) | 1972-06-19 | 1980-12-09 | Endo Laboratories Inc. | Pyridopyrrolo benzheterocycles |
| US4219550A (en) | 1978-11-09 | 1980-08-26 | E. I. Du Pont De Nemours And Company | Cis- and trans- octahydropyridopyrrolobenzheterocycles |
| HUT61548A (en) * | 1990-08-27 | 1993-01-28 | Sandoz Ag | Process for producing indolonaphthyridine derivatives and pharmaceutical compositions comprising such compounds |
| EA200100671A1 (ru) * | 1998-12-17 | 2001-12-24 | Американ Хоум Продактс Корпорейшн | ПРОИЗВОДНЫЕ 2,3,4,4a-ТЕТРАГИДРО-1H-ПИРАЗИНО [1,2a]ХИНОКСАЛИН-5(6H)-ОНА, ЯВЛЯЮЩИЕСЯ АГОНИСТАМИ 5HT2C |
| WO2002059127A2 (en) * | 2000-12-20 | 2002-08-01 | Bristol-Myers Squibb Pharma Company | Pyrazinoquinoxaline derivatives as serotonin agonists and antagonists |
-
2001
- 2001-12-19 WO PCT/US2001/049374 patent/WO2002059127A2/en active IP Right Grant
- 2001-12-19 SK SK702-2003A patent/SK7022003A3/sk unknown
- 2001-12-19 US US10/026,404 patent/US6638934B2/en not_active Expired - Lifetime
- 2001-12-19 DE DE60117617T patent/DE60117617T2/de not_active Expired - Lifetime
- 2001-12-19 BR BR0116347-7A patent/BR0116347A/pt not_active Application Discontinuation
- 2001-12-19 CN CNA01822704XA patent/CN1505631A/zh active Pending
- 2001-12-19 PL PL01366060A patent/PL366060A1/xx not_active Application Discontinuation
- 2001-12-19 AT AT01997097T patent/ATE318819T1/de active
- 2001-12-19 HU HU0303513A patent/HUP0303513A3/hu not_active Application Discontinuation
- 2001-12-19 ES ES01997097T patent/ES2260335T3/es not_active Expired - Lifetime
- 2001-12-19 CA CA002431970A patent/CA2431970A1/en not_active Abandoned
- 2001-12-19 RU RU2003121406/04A patent/RU2003121406A/ru not_active Application Discontinuation
- 2001-12-19 EE EEP200300301A patent/EE200300301A/xx unknown
- 2001-12-19 JP JP2002559429A patent/JP4346307B2/ja not_active Expired - Fee Related
- 2001-12-19 MX MXPA03005437A patent/MXPA03005437A/es unknown
- 2001-12-19 AU AU2002248216A patent/AU2002248216B2/en not_active Ceased
- 2001-12-19 KR KR10-2003-7008273A patent/KR20030069192A/ko not_active Application Discontinuation
- 2001-12-19 EP EP01997097A patent/EP1345942B9/en not_active Expired - Lifetime
- 2001-12-19 IL IL15620101A patent/IL156201A0/xx unknown
-
2003
- 2003-05-30 BG BG107864A patent/BG107864A/bg unknown
- 2003-06-02 ZA ZA200304303A patent/ZA200304303B/en unknown
- 2003-06-18 IS IS6850A patent/IS6850A/is unknown
- 2003-06-19 NO NO20032795A patent/NO20032795L/no not_active Application Discontinuation
-
2009
- 2009-05-11 JP JP2009114360A patent/JP5117440B2/ja not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| HUP0303513A2 (hu) | 2004-01-28 |
| KR20030069192A (ko) | 2003-08-25 |
| CN1505631A (zh) | 2004-06-16 |
| EE200300301A (et) | 2003-10-15 |
| JP2004524298A (ja) | 2004-08-12 |
| JP4346307B2 (ja) | 2009-10-21 |
| BG107864A (bg) | 2004-03-31 |
| US20020177596A1 (en) | 2002-11-28 |
| WO2002059127A3 (en) | 2002-10-03 |
| JP5117440B2 (ja) | 2013-01-16 |
| RU2003121406A (ru) | 2004-12-27 |
| US6638934B2 (en) | 2003-10-28 |
| ATE318819T1 (de) | 2006-03-15 |
| NO20032795L (no) | 2003-08-04 |
| DE60117617D1 (de) | 2006-04-27 |
| SK7022003A3 (en) | 2004-08-03 |
| NO20032795D0 (no) | 2003-06-19 |
| ZA200304303B (en) | 2004-09-02 |
| IS6850A (is) | 2003-06-18 |
| WO2002059127A2 (en) | 2002-08-01 |
| EP1345942A2 (en) | 2003-09-24 |
| JP2009215304A (ja) | 2009-09-24 |
| PL366060A1 (en) | 2005-01-24 |
| EP1345942B9 (en) | 2006-11-15 |
| EP1345942B1 (en) | 2006-03-01 |
| AU2002248216B2 (en) | 2007-03-01 |
| IL156201A0 (en) | 2003-12-23 |
| ES2260335T3 (es) | 2006-11-01 |
| DE60117617T2 (de) | 2007-01-25 |
| HUP0303513A3 (en) | 2005-12-28 |
| MXPA03005437A (es) | 2003-09-10 |
| CA2431970A1 (en) | 2002-08-01 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B11A | Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing | ||
| B11Y | Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette] |