AR022687A1 - Derivados de 2,3,4,4a-tetrahidro-1h-pirazino[1,2-a] quinoxalin-5(6h)ona, una composicion farmaceutica y el uso de los mismos para la manufactura de losmedicamentos. - Google Patents
Derivados de 2,3,4,4a-tetrahidro-1h-pirazino[1,2-a] quinoxalin-5(6h)ona, una composicion farmaceutica y el uso de los mismos para la manufactura de losmedicamentos.Info
- Publication number
- AR022687A1 AR022687A1 ARP990106455A ARP990106455A AR022687A1 AR 022687 A1 AR022687 A1 AR 022687A1 AR P990106455 A ARP990106455 A AR P990106455A AR P990106455 A ARP990106455 A AR P990106455A AR 022687 A1 AR022687 A1 AR 022687A1
- Authority
- AR
- Argentina
- Prior art keywords
- derivatives
- alkyl
- quinoxalin
- disorders
- manufacture
- Prior art date
Links
Classifications
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- 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
- 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
- A61P25/06—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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Psychiatry (AREA)
- Hematology (AREA)
- Child & Adolescent Psychology (AREA)
- Endocrinology (AREA)
- Anesthesiology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Derivados de 2,3,4,4A-tertahidro-1H-pirazino[1,2-A]quinoxalin-5(6H)ona que comprende compuestos de formula 1 en donde R, R1, R2, R3, R4, R y X tiene susignificado dado en la memoria descriptiva: R es hidrogeno, alquilo C1-6, acilo C2-7, o aroilo; R1,R2, R3 y R4 son cada uno independientemente hidrogeno,alquilo C1-6, alcoxi C1-6, halogeno, trifluoralquilo, -CN, alquilsulfonamida C1-6, alquil amida C1-6, amino, alquilamino C1-6, dialquilamino C1-6 por porcionalquilo, trifluoralcoxi C1-6 de carbono, acilo C2-7, o aroilo, X es CR5R6 o un grupo carbonilo; R5 y R6 son cada uno, independientemente, hidrogeno o alquiloC1-6; o una sal farmacéuticamente aceptable del mismo, con la condicion de que por lo menos dos de R1, R2, R3 o R4 no son hidrogeno. Estos compuestos sonagonistas receptores de 5HT2c utiles para el tratamiento de desordenes que involucran el sistema nervioso central tal como desordenes obsesivos, compulsivos,depresion, ansiedad, esquizofrenia, migrana, desordenes del sueno, desordenes de la alimentacion, obesidad, diabetes de tipo II, y epilepsia. Además sedescribe una composicion farmacéutica y el uso de dichos derivados para la manufactura de un medicamento.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US21347198A | 1998-12-17 | 1998-12-17 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR022687A1 true AR022687A1 (es) | 2002-09-04 |
Family
ID=22795247
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP990106455A AR022687A1 (es) | 1998-12-17 | 1999-12-16 | Derivados de 2,3,4,4a-tetrahidro-1h-pirazino[1,2-a] quinoxalin-5(6h)ona, una composicion farmaceutica y el uso de los mismos para la manufactura de losmedicamentos. |
Country Status (18)
Country | Link |
---|---|
EP (1) | EP1140940A1 (es) |
JP (1) | JP2002532504A (es) |
KR (1) | KR20010108025A (es) |
CN (1) | CN1240701C (es) |
AR (1) | AR022687A1 (es) |
AU (1) | AU3123400A (es) |
BR (1) | BR9916326A (es) |
CA (1) | CA2351385A1 (es) |
CZ (1) | CZ20012193A3 (es) |
EA (1) | EA200100671A1 (es) |
HU (1) | HUP0104773A3 (es) |
IL (1) | IL143323A0 (es) |
NO (1) | NO20013001L (es) |
NZ (1) | NZ512765A (es) |
PL (1) | PL348815A1 (es) |
SK (1) | SK8192001A3 (es) |
WO (1) | WO2000035922A1 (es) |
ZA (1) | ZA200104598B (es) |
Families Citing this family (52)
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US6960579B1 (en) | 1998-05-19 | 2005-11-01 | Alcon Manufacturing, Ltd. | Serotonergic 5HT7 receptor compounds for treating ocular and CNS disorders |
US6806285B1 (en) | 2000-03-17 | 2004-10-19 | Alcon, Inc. | 5-Hydroxyl indole derivatives for treating glaucoma |
US7012090B1 (en) | 2000-03-17 | 2006-03-14 | Alcon, Inc. | Pyranoindoles for treating glaucoma |
US6956036B1 (en) | 2000-03-17 | 2005-10-18 | Alcon, Inc. | 6-hydroxy-indazole derivatives for treating glaucoma |
WO2002010169A1 (en) * | 2000-07-31 | 2002-02-07 | F. Hoffmann-La Roche Ag | Piperazine derivatives |
US6759405B2 (en) | 2000-11-03 | 2004-07-06 | Wyeth | Cycloocta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives |
US6858604B2 (en) | 2000-11-03 | 2005-02-22 | Wyeth | Cyclohepta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives |
AR031197A1 (es) | 2000-11-03 | 2003-09-10 | Wyeth Corp | Procedimiento para la preparacion de derivados de 1,2,3,4,8,9,10,10a-octahidro-7bh-ciclopenta(b) diazepino(6,7,1-hi)indol |
DE60106641T2 (de) * | 2000-11-03 | 2005-12-01 | Wyeth | Cyclopenta[b][1,4] diazepino[6,7,1-hi]indole als 5ht2c antagonisten |
AR031202A1 (es) | 2000-11-03 | 2003-09-10 | Wyeth Corp | Ciclopenta(b) (1,4)diazepino(6,7,1-hi) indoles y derivados |
US6784172B2 (en) | 2000-11-03 | 2004-08-31 | Wyeth | Processes for preparation of cyclopenta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives |
AR031195A1 (es) | 2000-11-03 | 2003-09-10 | Wyeth Corp | Procedimiento para la preparacion de derivados de 1,2,3,4,8,9,10,10a-octahidro-7bh-ciclopenta (b) (1,4) diazepino (6,7,1) diazepino (6,7,1-hi) indol |
EP1337518B1 (en) | 2000-11-20 | 2009-06-17 | Biovitrum AB (publ) | Piperazinylpyrazines compounds as antagonists of serotonin 5-ht2 receptor |
SE0004245D0 (sv) | 2000-11-20 | 2000-11-20 | Pharmacia Ab | Novel compounds and their use |
GB0030710D0 (en) | 2000-12-15 | 2001-01-31 | Hoffmann La Roche | Piperazine derivatives |
WO2002059127A2 (en) * | 2000-12-20 | 2002-08-01 | Bristol-Myers Squibb Pharma Company | Pyrazinoquinoxaline derivatives as serotonin agonists and antagonists |
KR100539143B1 (ko) | 2000-12-27 | 2005-12-26 | 에프. 호프만-라 로슈 아게 | 인돌 유도체 및 그의 5-ht2b 및 5-ht2c 수용체리간드로서의 용도 |
WO2002074746A1 (fr) * | 2001-03-16 | 2002-09-26 | Yamanouchi Pharmaceutical Co., Ltd. | Derives de benzazepine |
BR0210238A (pt) | 2001-06-01 | 2004-07-20 | Alcon Inc | Novos análogos de aril-amino-propano e seu uso para o tratamento de glaucoma |
JP2004535418A (ja) | 2001-06-01 | 2004-11-25 | アルコン,インコーポレイテッド | ピラノインダゾールおよび緑内障治療への使用 |
EP1392658A4 (en) | 2001-06-01 | 2004-10-13 | Alcon Inc | NOVEL FUSED INDAZOLES AND INDOLES AND THEIR USE IN THE TREATMENT OF GLAUCOMES |
TW593302B (en) | 2001-12-20 | 2004-06-21 | Alcon Inc | Novel benzodifuranimidazoline and benzofuranimidazoline derivatives and their use for the treatment of glaucoma |
TW200307540A (en) | 2002-04-25 | 2003-12-16 | Wyeth Corp | [1, 4]Diazocino[7, 8, 1-hi] indole derivatives as antipsychotic and antiobesity agents |
TWI312781B (en) | 2002-04-25 | 2009-08-01 | [1,4]diazepino[6,7,1-ij]quinoline derivatives as antipsychotic and antiobesity agents | |
TW200307682A (en) | 2002-04-25 | 2003-12-16 | Wyeth Corp | 1,2,3,4,7,8-Hexahydro-6H-[1,4]diazepino[6,7,1-ij]quinoline derivatives as antipsychotic and antiobesity agents |
EP1513831B1 (en) | 2002-06-19 | 2010-01-06 | Biovitrum AB (publ) | Novel compounds, their use and preparation |
WO2004054572A2 (en) | 2002-12-13 | 2004-07-01 | Alcon, Inc. | Novel benzopyran analogs and their use for the treatment of glaucoma |
EP1581221B1 (en) | 2002-12-19 | 2011-05-18 | Bristol-Myers Squibb Company | Substituted tricyclic gamma-carbolines as serotonin receptor agonists and antagonists |
CL2004000826A1 (es) | 2003-04-25 | 2005-03-04 | Pfizer | Uso de un agonista para el receptor 5-ht2c para preparar un medicamento util en el tratamiento de la incontinencia urinaria provocada por estres, con la condicion de que el agonista no sea 1-[6-cloro-5-(trifluorometil)-2-piridinil]piperazina (org-129 |
CA2529750A1 (en) * | 2003-06-20 | 2005-02-24 | Arena Pharmaceuticals, Inc. | N-phenyl-piperazine derivatives and methods of prophylaxis or treatment of 5ht2c receptor associated diseases |
GB0314967D0 (en) | 2003-06-26 | 2003-07-30 | Hoffmann La Roche | Piperazine derivatives |
WO2005053688A1 (en) | 2003-11-26 | 2005-06-16 | Alcon, Inc. | Substituted furo[2,3-g] indazoles for the treatment of glaucoma |
US7129257B1 (en) | 2003-12-15 | 2006-10-31 | Alcon, Inc. | Pyrazolo[3,4- e]benzoxazoles for the treatment of glaucoma |
US7338972B1 (en) | 2003-12-15 | 2008-03-04 | Alcon, Inc. | Substituted 1-alkylamino-1H-indazoles for the treatment of glaucoma |
AR046890A1 (es) | 2003-12-15 | 2005-12-28 | Alcon Inc | [1,4] oxazino [2,3-g] indazoles sustituidos para el tratamiento del glaucoma. |
EP2248524A3 (en) | 2004-08-25 | 2011-03-09 | Takeda Pharmaceutical Company Limited | Preventives/remedies for stress urinary incontinence and method of screening the same |
JP2008514662A (ja) * | 2004-09-30 | 2008-05-08 | エフ.ホフマン−ラ ロシュ アーゲー | ベンゾオキサジン及びキノキサリン誘導体並びに使用 |
GT200500317A (es) | 2004-11-05 | 2006-10-27 | Proceso para preparar compuestos de quinolina y productos obtenidos de los mismos | |
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AR054849A1 (es) | 2005-07-26 | 2007-07-18 | Wyeth Corp | Diazepinoquinolinas, sintesis de las mismas, e intermediarios para obtenerlas |
EP2018863B9 (en) | 2006-05-16 | 2015-02-18 | Takeda Pharmaceutical Company Limited | Fused heterocyclic compound and use thereof |
EP2216023A4 (en) | 2007-11-15 | 2013-03-13 | Takeda Pharmaceutical | CONDENSED PYRIDINE DERIVATIVE AND USE THEREOF |
KR101062376B1 (ko) | 2008-04-10 | 2011-09-06 | 한국화학연구원 | 신규 인돌 카르복실산 비스피리딜 카르복사마이드 유도체,이의 제조방법 및 이를 유효성분으로 함유하는 조성물 |
KR101110199B1 (ko) | 2009-05-18 | 2012-03-14 | 한국화학연구원 | 피페라진-퀴놀린 유도체, 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 중추신경계 질환의 예방 또는 치료용 약학적 조성물 |
US8575186B2 (en) | 2009-10-05 | 2013-11-05 | Albany Molecular Research, Inc. | Epiminocycloalkyl[b] indole derivatives as serotonin sub-type 6 (5-HT6) modulators and uses thereof |
US20120253036A1 (en) | 2009-12-11 | 2012-10-04 | Yukinori Nagakura | Agent for treating fibromyalgia |
EP2531485B1 (en) | 2010-02-04 | 2019-04-24 | The Board of Trustees of the University of Illionis | Highly selective 5-ht(2c) receptor agonists having antagonist activity at the 5-ht(2b) receptor |
WO2012030953A1 (en) | 2010-09-01 | 2012-03-08 | Arena Pharmaceuticals, Inc. | 5-ht2c receptor agonists in the treatment of disorders ameliorated by reduction of norepinephrine level |
WO2012099952A2 (en) | 2011-01-19 | 2012-07-26 | Albany Molecular Research, Inc. | Benzofuro[3,2-c] pyridines and related analogs as serotonin sub-type 6 (5-ht6) modulators for the treatment of obesity, metabolic syndrome, cognition and schizophrenia |
WO2015066344A1 (en) | 2013-11-01 | 2015-05-07 | Arena Pharmaceuticals, Inc. | 5-ht2c receptor agonists and compositions and methods of use |
WO2016123164A1 (en) | 2015-01-29 | 2016-08-04 | The Board Of Trustees Of The University Of Illinois | Cyclopropylmethanamines as selective 5-ht(2c) receptor agonists |
WO2019131902A1 (ja) | 2017-12-27 | 2019-07-04 | 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 (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4032639A (en) * | 1976-03-22 | 1977-06-28 | American Home Products Corporation | 2,3,4,4A-Tetrahydro-1H-pyrazino[1,2-a,]quinoxalin-5(6H)-ones and derivatives thereof for relieving hypertension |
US4089958A (en) * | 1976-12-20 | 1978-05-16 | American Home Products Corporation | 2,3,4,4A-Tetrahydro-1H-pyrazino[1,2]quinoxalin-5(6)-ones and derivatives thereof |
US4203987A (en) * | 1979-05-21 | 1980-05-20 | American Home Products Corporation | 3-[Pyridinylalkyl and piperidinylalkyl]-2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5(6H)-ones |
GB8917333D0 (en) * | 1989-07-28 | 1989-09-13 | Merck Sharp & Dohme | Therapeutic agents |
EP0539209A1 (en) * | 1991-10-24 | 1993-04-28 | The Upjohn Company | Benzo-isoquinoline derivatives and analogs and their use in therapeutics |
AU4547796A (en) * | 1995-02-03 | 1996-08-21 | Sankyo Company Limited | Hexahydropyrazinoquinoline derivatives |
-
1999
- 1999-12-16 JP JP2000588181A patent/JP2002532504A/ja not_active Withdrawn
- 1999-12-16 HU HU0104773A patent/HUP0104773A3/hu unknown
- 1999-12-16 AR ARP990106455A patent/AR022687A1/es not_active Application Discontinuation
- 1999-12-16 AU AU31234/00A patent/AU3123400A/en not_active Abandoned
- 1999-12-16 WO PCT/US1999/029894 patent/WO2000035922A1/en not_active Application Discontinuation
- 1999-12-16 CA CA002351385A patent/CA2351385A1/en not_active Abandoned
- 1999-12-16 CN CNB998144169A patent/CN1240701C/zh not_active Expired - Fee Related
- 1999-12-16 EP EP99965285A patent/EP1140940A1/en not_active Withdrawn
- 1999-12-16 IL IL14332399A patent/IL143323A0/xx unknown
- 1999-12-16 KR KR1020017007583A patent/KR20010108025A/ko not_active Application Discontinuation
- 1999-12-16 PL PL99348815A patent/PL348815A1/xx not_active Application Discontinuation
- 1999-12-16 SK SK819-2001A patent/SK8192001A3/sk unknown
- 1999-12-16 NZ NZ512765A patent/NZ512765A/en unknown
- 1999-12-16 CZ CZ20012193A patent/CZ20012193A3/cs unknown
- 1999-12-16 EA EA200100671A patent/EA200100671A1/ru unknown
- 1999-12-16 BR BR9916326-8A patent/BR9916326A/pt not_active IP Right Cessation
-
2001
- 2001-06-05 ZA ZA200104598A patent/ZA200104598B/en unknown
- 2001-06-15 NO NO20013001A patent/NO20013001L/no not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
PL348815A1 (en) | 2002-06-17 |
JP2002532504A (ja) | 2002-10-02 |
HUP0104773A2 (hu) | 2002-04-29 |
ZA200104598B (en) | 2002-09-05 |
CZ20012193A3 (cs) | 2001-12-12 |
KR20010108025A (ko) | 2001-12-07 |
IL143323A0 (en) | 2002-04-21 |
NO20013001D0 (no) | 2001-06-15 |
CN1240701C (zh) | 2006-02-08 |
SK8192001A3 (en) | 2001-12-03 |
AU3123400A (en) | 2000-07-03 |
BR9916326A (pt) | 2001-10-02 |
WO2000035922A1 (en) | 2000-06-22 |
HUP0104773A3 (en) | 2004-10-28 |
NO20013001L (no) | 2001-06-15 |
NZ512765A (en) | 2003-10-31 |
CA2351385A1 (en) | 2000-06-22 |
EP1140940A1 (en) | 2001-10-10 |
CN1330652A (zh) | 2002-01-09 |
EA200100671A1 (ru) | 2001-12-24 |
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