HUP0400772A2 - Eljárás piperazinszármazékok mezilátjainak előállítására és ezen vegyületek - Google Patents
Eljárás piperazinszármazékok mezilátjainak előállítására és ezen vegyületekInfo
- Publication number
- HUP0400772A2 HUP0400772A2 HU0400772A HUP0400772A HUP0400772A2 HU P0400772 A2 HUP0400772 A2 HU P0400772A2 HU 0400772 A HU0400772 A HU 0400772A HU P0400772 A HUP0400772 A HU P0400772A HU P0400772 A2 HUP0400772 A2 HU P0400772A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- general formula
- atom
- compounds
- formula
- Prior art date
Links
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 2
- 150000004885 piperazines Chemical class 0.000 title 1
- 229940066771 systemic antihistamines piperazine derivative Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 229910052799 carbon Inorganic materials 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000004432 carbon atom Chemical group C* 0.000 abstract 3
- 125000001153 fluoro group Chemical group F* 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- YZCKVEUIGOORGS-IGMARMGPSA-N Protium Chemical group [1H] YZCKVEUIGOORGS-IGMARMGPSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- -1 amine compound Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 229910052731 fluorine Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- IZDROVVXIHRYMH-UHFFFAOYSA-N methanesulfonic anhydride Chemical compound CS(=O)(=O)OS(C)(=O)=O IZDROVVXIHRYMH-UHFFFAOYSA-N 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000006413 ring segment Chemical group 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 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
- C07D413/02—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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
- C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurosurgery (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
A találmány tárgyát eljárás képezi az (1) általános képletű vegyületekmezilátjainak előállítására, ahol a képletben X jelentése (4)általános képletű csoport, ahol R1 jelentése hidrogénatom vagyfluoratom; R2 jelentése hidrogénatom, 1-4 szénatomos alkil-, 1-4szénatomos alkoxi- vagy oxocsoport; A jelentése 5-7 gyűrűatomból állóheterociklusos csoport, amelyek közül 1-3 heteroatomot képez O, N és Sközül választva; Y jelentése metil-, etil-, egy vagy több fluoratommalszubsztituált etil-, (3-7 szénatomos cikloalkil)-metil-csoport, amelyegy vagy több fluoratommal van szubsztituálva vagy (5) általánosképletű csoport, amelyben Z jelentése hidrogénatom, fenil-, 1-3csoporttal szubsztituált fenilcsoport, ahol a szubsztituensekválaszthatók hidroxilcsoport, halogénatom, 1-4 szénatomos alkil-, 1-4szénatomos alkoxi- vagy cianocsoport közül, továbbá R3 jelentésehidrogénatom vagy 1-3 szubsztituens, amelyek választhatók halogénatom,hidroxil-, 1-4 szénatomos alkil- vagy 1-4 szénatomos alkoxicsoportközül. Az (1) általános képletű vegyületek mezilátjainakelőállításánál úgy járnak el, hogy (2) általános képletű aminvegyületet (3) általános képletű vegyülettel és metánszulfonsav-anhidriddel reagáltatják, ahol a vegyületek képletében X és Yjelentése a tárgyi körben megadottal azonos. A találmány tárgyáhoztartoznak ezen kívül maguk az (1) általános képletű vegyületek is. Ó
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01200534 | 2001-02-16 | ||
| PCT/EP2002/001666 WO2002066449A2 (en) | 2001-02-16 | 2002-02-14 | Process for the preparation of mesylates of piperazine derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0400772A2 true HUP0400772A2 (hu) | 2004-08-30 |
| HUP0400772A3 HUP0400772A3 (en) | 2008-02-28 |
Family
ID=8179894
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0400772A HUP0400772A3 (en) | 2001-02-16 | 2002-02-14 | Process for the preparation of mesylates of piperazine derivatives |
Country Status (35)
| Country | Link |
|---|---|
| US (1) | US7030241B2 (hu) |
| EP (1) | EP1362040B1 (hu) |
| JP (1) | JP4328528B2 (hu) |
| KR (2) | KR101000733B1 (hu) |
| CN (1) | CN1176079C (hu) |
| AR (1) | AR034206A1 (hu) |
| AT (1) | ATE284875T1 (hu) |
| AU (1) | AU2002250962B2 (hu) |
| BG (1) | BG66101B1 (hu) |
| BR (1) | BR0205683A (hu) |
| CA (1) | CA2422703C (hu) |
| CZ (1) | CZ301780B6 (hu) |
| DE (1) | DE60202261T2 (hu) |
| DK (1) | DK1362040T3 (hu) |
| DZ (1) | DZ3489A1 (hu) |
| ES (1) | ES2230481T3 (hu) |
| HK (1) | HK1059934A1 (hu) |
| HR (1) | HRP20030610B1 (hu) |
| HU (1) | HUP0400772A3 (hu) |
| IL (1) | IL153509A (hu) |
| IS (1) | IS2417B (hu) |
| ME (1) | MEP37508A (hu) |
| MX (1) | MXPA03002359A (hu) |
| MY (1) | MY130687A (hu) |
| NO (1) | NO324460B1 (hu) |
| NZ (1) | NZ524632A (hu) |
| PL (1) | PL208363B1 (hu) |
| PT (1) | PT1362040E (hu) |
| RS (1) | RS51126B (hu) |
| RU (1) | RU2272036C2 (hu) |
| SI (1) | SI1362040T1 (hu) |
| SK (1) | SK286143B6 (hu) |
| UA (1) | UA75390C2 (hu) |
| WO (1) | WO2002066449A2 (hu) |
| ZA (1) | ZA200301590B (hu) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR045362A1 (es) * | 2003-08-18 | 2005-10-26 | Solvay Pharm Bv | Forma cristalina estable de mesilato de bifeprunox (monometansulfonato de 7-[4-([1,1- bifenil] -3- ilmetil) -1- piperazinil] - 2-(3h) -benzoxazolona |
| US7435738B2 (en) | 2003-08-18 | 2008-10-14 | Solvay Pharmaceuticals, Inc. | Stable crystalline form of bifeprunox mesylate (7-[4-([1,1′-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate) |
| US7405216B2 (en) | 2004-08-18 | 2008-07-29 | Solvay Pharmaceuticals, B.V. | Stable crystalline form of bifeprunox mesylate (7-[4-([1,1′-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate) |
| US7964604B2 (en) * | 2005-02-18 | 2011-06-21 | Solvay Pharmaceuticals B.V. | Bifeprunox mesylate maintenance dose compositions and methods for using the same |
| US7423040B2 (en) | 2005-02-18 | 2008-09-09 | Irene Eijgendaal | Stable crystalline form of bifeprunox mesylate, dosage forms thereof and methods for using same |
| US20070275977A1 (en) * | 2006-05-02 | 2007-11-29 | Van Aar Marcel P | N-oxides of pyridylmethyl -piperazine and -piperidine derivatives |
| US8106056B2 (en) * | 2006-06-16 | 2012-01-31 | Solvay Pharmaceuticals B.V. | Combination preparations comprising bifeprunox and a dopamine agonist |
| US7786126B2 (en) | 2006-06-16 | 2010-08-31 | Solvay Pharmaceuticals B.V. | Combination preparations comprising SLV308 and a dopamine agonist |
| US20080132520A1 (en) * | 2006-08-31 | 2008-06-05 | Winsemius Antje A | Compositions, kits and methods for administering a titration schedule comprising bifeprunox compounds |
| US20090068290A1 (en) * | 2006-08-31 | 2009-03-12 | Michel Bourin | Bifeprunox doses for treating schizophrenia |
| KR20090063228A (ko) | 2006-08-31 | 2009-06-17 | 솔베이 파마슈티칼스 비. 브이 | 정신분열증 치료용 비페프루녹스를 위한 적정 계획 및 이에사용하기 위한 키트 |
| JP2011511011A (ja) | 2008-02-05 | 2011-04-07 | ハーバー バイオサイエンシーズ，インコーポレイテッド | 医薬的固体状態形態 |
| WO2011023796A1 (en) | 2009-08-31 | 2011-03-03 | Abbott Healthcare Products B.V. | Bifeprunox for treating addiction |
| UY32934A (es) | 2009-10-12 | 2011-05-31 | Abbott Healthcare Products Bv | Monohidrato de pardoprunox |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0190472B1 (en) * | 1984-12-21 | 1989-07-12 | Duphar International Research B.V | New pharmaceutical compositions having anti-psychotic properties |
| EP0189612B1 (en) * | 1984-12-21 | 1992-11-04 | Duphar International Research B.V | New pharmaceutical compositions having a psychotropic activity |
| JPH0344383A (ja) * | 1989-07-12 | 1991-02-26 | Ihara Chem Ind Co Ltd | ５―トリフルオロメチル―２―ハロメチルベンゾチアゾール類の製造法 |
| JP3044383B2 (ja) * | 1990-05-22 | 2000-05-22 | コニカ株式会社 | 含窒素６員環化合物の製造方法 |
| ATE340173T1 (de) * | 1996-03-29 | 2006-10-15 | Duphar Int Res | Piperazin- und piperidin- derivate |
| SE9702799D0 (sv) * | 1997-07-25 | 1997-07-25 | Astra Ab | New compounds |
| UA71590C2 (en) | 1998-11-13 | 2004-12-15 | Duphar Int Res | Piperazine and piperidine derivatives |
| US7435738B2 (en) * | 2003-08-18 | 2008-10-14 | Solvay Pharmaceuticals, Inc. | Stable crystalline form of bifeprunox mesylate (7-[4-([1,1′-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate) |
-
2002
- 2002-02-12 AR ARP020100460A patent/AR034206A1/es active IP Right Grant
- 2002-02-14 CZ CZ20030697A patent/CZ301780B6/cs not_active IP Right Cessation
- 2002-02-14 DZ DZ023489A patent/DZ3489A1/fr active
- 2002-02-14 CN CNB028016858A patent/CN1176079C/zh not_active Expired - Fee Related
- 2002-02-14 DK DK02719858T patent/DK1362040T3/da active
- 2002-02-14 ES ES02719858T patent/ES2230481T3/es not_active Expired - Lifetime
- 2002-02-14 KR KR1020087015071A patent/KR101000733B1/ko not_active IP Right Cessation
- 2002-02-14 EP EP02719858A patent/EP1362040B1/en not_active Expired - Lifetime
- 2002-02-14 AU AU2002250962A patent/AU2002250962B2/en not_active Ceased
- 2002-02-14 IL IL153509A patent/IL153509A/en not_active IP Right Cessation
- 2002-02-14 WO PCT/EP2002/001666 patent/WO2002066449A2/en active IP Right Grant
- 2002-02-14 NZ NZ524632A patent/NZ524632A/en not_active IP Right Cessation
- 2002-02-14 DE DE60202261T patent/DE60202261T2/de not_active Expired - Lifetime
- 2002-02-14 UA UA2003098528A patent/UA75390C2/uk unknown
- 2002-02-14 AT AT02719858T patent/ATE284875T1/de active
- 2002-02-14 US US10/468,098 patent/US7030241B2/en not_active Expired - Fee Related
- 2002-02-14 BR BR0205683-6A patent/BR0205683A/pt not_active Application Discontinuation
- 2002-02-14 KR KR1020037000026A patent/KR100859106B1/ko not_active IP Right Cessation
- 2002-02-14 SK SK309-2003A patent/SK286143B6/sk not_active IP Right Cessation
- 2002-02-14 ME MEP-375/08A patent/MEP37508A/xx unknown
- 2002-02-14 CA CA2422703A patent/CA2422703C/en not_active Expired - Fee Related
- 2002-02-14 SI SI200230061T patent/SI1362040T1/xx unknown
- 2002-02-14 JP JP2002565965A patent/JP4328528B2/ja not_active Expired - Fee Related
- 2002-02-14 PT PT02719858T patent/PT1362040E/pt unknown
- 2002-02-14 RS YUP-644/03A patent/RS51126B/sr unknown
- 2002-02-14 MY MYPI20020505A patent/MY130687A/en unknown
- 2002-02-14 HU HU0400772A patent/HUP0400772A3/hu unknown
- 2002-02-14 MX MXPA03002359A patent/MXPA03002359A/es active IP Right Grant
- 2002-02-14 RU RU2003105902/04A patent/RU2272036C2/ru not_active IP Right Cessation
- 2002-02-14 PL PL369330A patent/PL208363B1/pl unknown
-
2003
- 2003-02-26 ZA ZA200301590A patent/ZA200301590B/en unknown
- 2003-04-15 NO NO20031754A patent/NO324460B1/no not_active IP Right Cessation
- 2003-07-17 IS IS6876A patent/IS2417B/is unknown
- 2003-07-28 HR HR20030610A patent/HRP20030610B1/xx not_active IP Right Cessation
- 2003-08-13 BG BG108090A patent/BG66101B1/bg unknown
-
2004
- 2004-04-22 HK HK04102835A patent/HK1059934A1/xx not_active IP Right Cessation
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA9A | Lapse of provisional patent protection due to relinquishment or protection considered relinquished |