ZA200304267B - 8-{4-[3-(5-Fluoro-1H-indol-3-yl)-propyl]-piperazin-1-yl]-2-methyl-4H-benzo[1,4]oxazin-3-onmesylate with high affinity for the dopamine D2 receptor and the serotonin reuptake site. - Google Patents
8-{4-[3-(5-Fluoro-1H-indol-3-yl)-propyl]-piperazin-1-yl]-2-methyl-4H-benzo[1,4]oxazin-3-onmesylate with high affinity for the dopamine D2 receptor and the serotonin reuptake site. Download PDFInfo
- Publication number
- ZA200304267B ZA200304267B ZA200304267A ZA200304267A ZA200304267B ZA 200304267 B ZA200304267 B ZA 200304267B ZA 200304267 A ZA200304267 A ZA 200304267A ZA 200304267 A ZA200304267 A ZA 200304267A ZA 200304267 B ZA200304267 B ZA 200304267B
- Authority
- ZA
- South Africa
- Prior art keywords
- dopamine
- compound
- receptor
- serotonin reuptake
- indol
- Prior art date
Links
- 230000000697 serotonin reuptake Effects 0.000 title description 5
- 102000004980 Dopamine D2 Receptors Human genes 0.000 title description 2
- 108090001111 Dopamine D2 Receptors Proteins 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims description 19
- 238000000034 method Methods 0.000 claims description 6
- 239000000203 mixture Substances 0.000 claims description 6
- 239000000126 substance Substances 0.000 claims description 6
- 208000015114 central nervous system disease Diseases 0.000 claims 3
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 9
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 6
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 description 6
- 239000012458 free base Substances 0.000 description 5
- 229960003638 dopamine Drugs 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 208000024891 symptom Diseases 0.000 description 3
- -1 5-FLUORO- 1H-INDOL-3-YL Chemical class 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
- 208000020114 Schizophrenia and other psychotic disease Diseases 0.000 description 2
- 239000000935 antidepressant agent Substances 0.000 description 2
- 229940005513 antidepressants Drugs 0.000 description 2
- 239000000164 antipsychotic agent Substances 0.000 description 2
- 239000002249 anxiolytic agent Substances 0.000 description 2
- 230000000949 anxiolytic effect Effects 0.000 description 2
- 229940005530 anxiolytics Drugs 0.000 description 2
- 230000006399 behavior Effects 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- YZTJYBJCZXZGCT-UHFFFAOYSA-N phenylpiperazine Chemical class C1CNCCN1C1=CC=CC=C1 YZTJYBJCZXZGCT-UHFFFAOYSA-N 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
- 208000019901 Anxiety disease Diseases 0.000 description 1
- 206010003805 Autism Diseases 0.000 description 1
- 208000020706 Autistic disease Diseases 0.000 description 1
- 208000009132 Catalepsy Diseases 0.000 description 1
- 208000018737 Parkinson disease Diseases 0.000 description 1
- 241000283984 Rodentia Species 0.000 description 1
- 208000012886 Vertigo Diseases 0.000 description 1
- 206010047853 Waxy flexibility Diseases 0.000 description 1
- OCBFFGCSTGGPSQ-UHFFFAOYSA-N [CH2]CC Chemical compound [CH2]CC OCBFFGCSTGGPSQ-UHFFFAOYSA-N 0.000 description 1
- 230000016571 aggressive behavior Effects 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 229940005529 antipsychotics Drugs 0.000 description 1
- VMWNQDUVQKEIOC-CYBMUJFWSA-N apomorphine Chemical compound C([C@H]1N(C)CC2)C3=CC=C(O)C(O)=C3C3=C1C2=CC=C3 VMWNQDUVQKEIOC-CYBMUJFWSA-N 0.000 description 1
- 229960004046 apomorphine Drugs 0.000 description 1
- 230000003542 behavioural effect Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 239000012876 carrier material Substances 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 230000009194 climbing Effects 0.000 description 1
- 230000019771 cognition Effects 0.000 description 1
- 230000001143 conditioned effect Effects 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 238000002425 crystallisation Methods 0.000 description 1
- 230000008025 crystallization Effects 0.000 description 1
- 230000003291 dopaminomimetic effect Effects 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 229940098779 methanesulfonic acid Drugs 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 239000002464 receptor antagonist Substances 0.000 description 1
- 229940044551 receptor antagonist Drugs 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 230000000862 serotonergic effect Effects 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000011343 solid material Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 231100000889 vertigo Toxicity 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61P25/18—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
- A61P25/22—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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01200610 | 2001-02-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200304267B true ZA200304267B (en) | 2004-08-30 |
Family
ID=8179909
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200304267A ZA200304267B (en) | 2001-02-21 | 2003-05-30 | 8-{4-[3-(5-Fluoro-1H-indol-3-yl)-propyl]-piperazin-1-yl]-2-methyl-4H-benzo[1,4]oxazin-3-onmesylate with high affinity for the dopamine D2 receptor and the serotonin reuptake site. |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US6958396B2 (ja) |
| EP (1) | EP1366044B1 (ja) |
| JP (1) | JP4216072B2 (ja) |
| KR (1) | KR100859107B1 (ja) |
| CN (1) | CN1284780C (ja) |
| AR (1) | AR032712A1 (ja) |
| AT (1) | ATE472545T1 (ja) |
| AU (1) | AU2002250983B2 (ja) |
| BR (1) | BR0206162A (ja) |
| CA (1) | CA2430707C (ja) |
| CZ (1) | CZ20032171A3 (ja) |
| DE (1) | DE60236848D1 (ja) |
| DZ (1) | DZ3490A1 (ja) |
| ES (1) | ES2347321T3 (ja) |
| HK (1) | HK1078569A1 (ja) |
| HU (1) | HUP0303330A3 (ja) |
| IL (1) | IL155720A0 (ja) |
| MX (1) | MXPA03007430A (ja) |
| NO (1) | NO325298B1 (ja) |
| NZ (1) | NZ526018A (ja) |
| PL (1) | PL201176B1 (ja) |
| RU (1) | RU2281945C2 (ja) |
| SK (1) | SK10412003A3 (ja) |
| WO (1) | WO2002066473A1 (ja) |
| ZA (1) | ZA200304267B (ja) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TR200200460T2 (tr) * | 1999-08-23 | 2002-06-21 | Solvay Pharmaceuticals B.V. | Yeni fenilpiperazinler |
| AR032712A1 (es) * | 2001-02-21 | 2003-11-19 | Solvay Pharm Bv | Un mesilato de derivados de fenilpiperazina y composiciones farmaceuticas que lo contienen |
| BRPI0518370A2 (pt) * | 2004-12-07 | 2008-11-18 | Solvay Pharm Bv | composto, composiÇço farmacÊutica, mÉtodo para preparar uma composiÇço, e, uso de um composto |
| US7371769B2 (en) | 2004-12-07 | 2008-05-13 | Solvay Pharmaceuticals B.V. | Tetrahydropyridin-4-yl indoles with a combination of affinity for dopamine-D2 receptors and serotonin reuptake sites |
| US8101619B2 (en) | 2004-12-08 | 2012-01-24 | Solvay Pharmaceuticals B.V. | Phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake inhibition |
| GT200600416A (es) | 2005-09-12 | 2007-09-20 | Sales salicilato y gentisato de un compuesto de piperazina | |
| GT200600414A (es) * | 2005-09-12 | 2007-09-20 | Sal de glucuranato de compuesto de piperazine | |
| TW200800306A (en) * | 2005-09-12 | 2008-01-01 | Wyeth Corp | Sustained-release formulation and uses thereof |
| US9066903B2 (en) | 2006-02-28 | 2015-06-30 | The United States Of America As Represented By The Department Of Veterans Affairs | Pharmacological treatment of Parkinson's disease |
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| DE69819266T2 (de) | 1997-09-02 | 2004-07-29 | Duphar International Research B.V. | Piperidin- und Piperazin Derivate als 5-HT1-Rezeptor-Agonisten |
| US6125957A (en) * | 1998-02-10 | 2000-10-03 | Kauffmann; Ricardo M. | Prosthetic apparatus for supporting a user in sitting or standing positions |
| EP1089997A1 (en) | 1998-06-19 | 2001-04-11 | H.Lundbeck A/S | 4,5,6 and 7-indole and indoline derivatives, their preparation and use |
| AR020773A1 (es) | 1998-10-16 | 2002-05-29 | Duphar Int Res | Compuesto derivados de 3-(tetrahidropiridin-4-il)indol, metodo para prepararlo, una composicion farmaceutica que los contiene, metodo para preparar dicha composicion y uso del compuesto |
| US6223104B1 (en) * | 1998-10-21 | 2001-04-24 | Deka Products Limited Partnership | Fault tolerant architecture for a personal vehicle |
| US6302230B1 (en) * | 1999-06-04 | 2001-10-16 | Deka Products Limited Partnership | Personal mobility vehicles and methods |
| US6314896B1 (en) | 1999-06-10 | 2001-11-13 | L'air Liquide, Societe Anonyme Pour L'etude Et L'exploitation Des Procedes Georges Claude | Method for operating a boiler using oxygen-enriched oxidants |
| TR200200460T2 (tr) * | 1999-08-23 | 2002-06-21 | Solvay Pharmaceuticals B.V. | Yeni fenilpiperazinler |
| US6288505B1 (en) * | 2000-10-13 | 2001-09-11 | Deka Products Limited Partnership | Motor amplifier and control for a personal transporter |
| AR032711A1 (es) | 2001-02-21 | 2003-11-19 | Solvay Pharm Bv | Derivados de fenilpiperazina, un metodo para la preparacion de los mismos y una composicion farmaceutica que los contiene |
| AR032712A1 (es) * | 2001-02-21 | 2003-11-19 | Solvay Pharm Bv | Un mesilato de derivados de fenilpiperazina y composiciones farmaceuticas que lo contienen |
| EP1336406A1 (en) | 2002-02-14 | 2003-08-20 | Solvay Pharmaceuticals B.V. | Partial dopamine-D2 receptor agonist plus serotonin and/or noradrenaline inhibitory activity |
-
2002
- 2002-02-18 AR ARP020100548A patent/AR032712A1/es not_active Application Discontinuation
- 2002-02-19 SK SK1041-2003A patent/SK10412003A3/sk unknown
- 2002-02-19 CZ CZ20032171A patent/CZ20032171A3/cs unknown
- 2002-02-19 IL IL15572002A patent/IL155720A0/xx not_active IP Right Cessation
- 2002-02-19 PL PL362288A patent/PL201176B1/pl not_active IP Right Cessation
- 2002-02-19 CN CNB028029682A patent/CN1284780C/zh not_active Expired - Fee Related
- 2002-02-19 WO PCT/EP2002/001795 patent/WO2002066473A1/en active Application Filing
- 2002-02-19 US US10/432,225 patent/US6958396B2/en not_active Expired - Fee Related
- 2002-02-19 EP EP02719880A patent/EP1366044B1/en not_active Expired - Lifetime
- 2002-02-19 AU AU2002250983A patent/AU2002250983B2/en not_active Ceased
- 2002-02-19 KR KR1020037010907A patent/KR100859107B1/ko not_active IP Right Cessation
- 2002-02-19 HU HU0303330A patent/HUP0303330A3/hu unknown
- 2002-02-19 DZ DZ023490A patent/DZ3490A1/fr active
- 2002-02-19 JP JP2002565987A patent/JP4216072B2/ja not_active Expired - Fee Related
- 2002-02-19 RU RU2003114440/04A patent/RU2281945C2/ru not_active IP Right Cessation
- 2002-02-19 BR BR0206162-7A patent/BR0206162A/pt not_active Application Discontinuation
- 2002-02-19 MX MXPA03007430A patent/MXPA03007430A/es active IP Right Grant
- 2002-02-19 NZ NZ526018A patent/NZ526018A/en unknown
- 2002-02-19 CA CA2430707A patent/CA2430707C/en not_active Expired - Fee Related
- 2002-02-19 AT AT02719880T patent/ATE472545T1/de not_active IP Right Cessation
- 2002-02-19 ES ES02719880T patent/ES2347321T3/es not_active Expired - Lifetime
- 2002-02-19 DE DE60236848T patent/DE60236848D1/de not_active Expired - Lifetime
-
2003
- 2003-05-30 ZA ZA200304267A patent/ZA200304267B/en unknown
- 2003-06-24 NO NO20032914A patent/NO325298B1/no not_active IP Right Cessation
-
2005
- 2005-05-23 US US11/134,455 patent/US8106044B2/en not_active Expired - Fee Related
- 2005-11-18 HK HK05110338A patent/HK1078569A1/xx not_active IP Right Cessation
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