FI114985B - Piperazinderivat som 5-HT1A antagonister - Google Patents
Piperazinderivat som 5-HT1A antagonister Download PDFInfo
- Publication number
- FI114985B FI114985B FI964815A FI964815A FI114985B FI 114985 B FI114985 B FI 114985B FI 964815 A FI964815 A FI 964815A FI 964815 A FI964815 A FI 964815A FI 114985 B FI114985 B FI 114985B
- Authority
- FI
- Finland
- Prior art keywords
- formula
- compound
- group
- methyl
- chr
- Prior art date
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
-
- 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)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Anesthesiology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Polymers With Sulfur, Phosphorus Or Metals In The Main Chain (AREA)
- Hydrogenated Pyridines (AREA)
Claims (5)
1. Förening eller ett farmaceutiskt godtagbart sy-5 raadditionssalt därav, kännetecknad därav, att nämnda förening har den allmänna formeln (A): /=*η (T^Jj ^ N— CHRaCHRb—N (A) W ^CO Ό 10 där Ra och Rb vardera är väte eller en metylgrupp. 2 . (R)-N-(l-metyl-2-(4-indolyl-l-piperazinyletyl)- N-(2-pyridyl)cyklohexankarboxamid eller ett farmaceutiskt godtagbart syraadditionssalt därav. 3. (R)-N-(2-metyl-2-(4-indolyl-l-piperazinyl)etyl)-15 N-(2-pyridyl)cyklohexankarboxamid eller ett farmaceutiskt t * i ,godtagbart syraadditionssalt därav. I I
4. N-[2-(4-(4-indolyl)-1-piperazinyl) etyl]-N-(2- ! pyridyl)cyklohexankarboxamid eller ett farmaceutiskt godtagbart syraadditionssalt därav.
5. Farmaceutiskt komposition, känneteck- ’·’ n a d därav, att den innefattar en förening enligt nägot av de föregäende patentkraven i kombination med ett farma-ceutiskt godtagbart spädningsmedel eller en farmaceutiskt • · » godtagbar bärare.
6. Användning av en förening enligt nägot av pa- >ii(. tentkraven 1 tili 4 vid framställningen av ett läkemedel » · . för behandling av CNS-störningar. ‘Λ; 7. Amin, kännetecknad därav, att den har formeln (B) : 114985 HN^ ^ V- CHR*CHRbHH (β) där Ra och Rb vardera är väte eller en metylgrupp. 5 8. Förfarande för framställning av en förening enligt patentkrav 1, kännetecknat därav, att a) en amin med formeln (B): ΗΝ/=Γ N\Z/N" (B) 10 (där Ra och Rb vardera är väte eller en metylgrupp) acyle-ras med cyklohexankarboxylsyra eller ett acyleringsderivat därav, b) en amid med formeln • 15 - X) :· HN ^ X; Xc0"O alkyleras med ett alkyleringsmedel med formeln: > ♦ Hl/ : />-N ^ N— CHR>CHRb— x' v_y : 20
1 U9 85 där Ra och Rb vardera är väte eller en metylgrupp och X1 är en lämnande grupp, säsom halogen eller en alkyl- eller arylsulfonyloxigrupp, c) en förening med formeln (C): 5 Hl/~ h=\ r~\ (C) (i VT alkyleras med en förening med formel jO x1- CHRaCHRbC N ίο N—' där Ra och Rb vardera är väte eller en metylgrupp och X1 är en lämnande grupp, säsom halogen eller en alkyl- eller arylsulfonyloxigrupp, eller • 15 d) ett Nind-skyddat derivat av en förening med for- » » meln Hl/~ *: ; ‘ N( /N~ CHR’CHRbNHC0 { , bringas att reagera med 2-fluorpyridin-N-oxid varefter ; skyddsgruppen och N-oxidgruppen avlägsnas. • · · » t . > t
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB9411099A GB9411099D0 (en) | 1994-06-03 | 1994-06-03 | Piperazine derivatives |
GB9411099 | 1994-06-03 | ||
PCT/GB1995/001263 WO1995033743A1 (en) | 1994-06-03 | 1995-06-01 | Piperazine derivatives as 5ht1a antagonists |
GB9501263 | 1995-06-01 |
Publications (3)
Publication Number | Publication Date |
---|---|
FI964815A FI964815A (sv) | 1996-12-02 |
FI964815A0 FI964815A0 (sv) | 1996-12-02 |
FI114985B true FI114985B (sv) | 2005-02-15 |
Family
ID=10756114
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
FI964815A FI114985B (sv) | 1994-06-03 | 1996-12-02 | Piperazinderivat som 5-HT1A antagonister |
Country Status (25)
Country | Link |
---|---|
US (1) | US5723464A (sv) |
EP (1) | EP0763031B1 (sv) |
JP (1) | JPH10500989A (sv) |
KR (1) | KR100359393B1 (sv) |
CN (2) | CN1048985C (sv) |
AT (1) | ATE192744T1 (sv) |
AU (1) | AU680147B2 (sv) |
BR (1) | BR9507910A (sv) |
CA (1) | CA2191871C (sv) |
CZ (1) | CZ287381B6 (sv) |
DE (1) | DE69516867T2 (sv) |
DK (1) | DK0763031T3 (sv) |
ES (1) | ES2145275T3 (sv) |
FI (1) | FI114985B (sv) |
GB (1) | GB9411099D0 (sv) |
GR (1) | GR3033449T3 (sv) |
HU (1) | HUT76466A (sv) |
IL (1) | IL113967A (sv) |
MX (1) | MX9605915A (sv) |
NZ (2) | NZ331452A (sv) |
PT (1) | PT763031E (sv) |
RU (1) | RU2165933C2 (sv) |
SK (1) | SK281418B6 (sv) |
WO (1) | WO1995033743A1 (sv) |
ZA (1) | ZA954525B (sv) |
Families Citing this family (32)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IL101722A (en) * | 1991-05-02 | 1996-05-14 | Wyeth John & Brother Ltd | History of piperazine, their preparation and pharmaceutical preparations containing them |
AU2622595A (en) * | 1994-06-03 | 1996-01-04 | John Wyeth & Brother Limited | Novel processes and intermediates for the preparation of piperazine derivatives |
EP0773942A1 (en) * | 1994-07-26 | 1997-05-21 | Pfizer Inc. | 4-indole derivatives as serotonin agonists and antagonists |
US5519025A (en) * | 1995-04-10 | 1996-05-21 | American Home Products Corporation | 4-indolylpiperazinyl derivatives |
US5486518A (en) * | 1995-04-10 | 1996-01-23 | American Home Products Corporation | 4-indolylpiperazinyl derivatives |
IT1282705B1 (it) * | 1996-02-28 | 1998-03-31 | Recordati Chem Pharm | Uso di antagonisti del recettore serotoninergico 5-ht|a per il trattamento dell'incontinenza urinaria |
US5990114A (en) * | 1996-02-28 | 1999-11-23 | Recordati, S.A., Chemical And Pharmaceutical Company | Use of 5-HT1A receptor antagonists for the treatment of urinary incontinence |
DE19615232A1 (de) * | 1996-04-18 | 1997-10-23 | Merck Patent Gmbh | Neue Carbamoylderivate und deren Verwendung als 5-HT ¶1¶¶A¶-Antagonisten |
DE19725664A1 (de) | 1997-06-18 | 1998-12-24 | Merck Patent Gmbh | 3-Benzylpiperidine |
US6399614B1 (en) | 1997-08-01 | 2002-06-04 | Recordati S.A. Chemical And Pharmaceutical Company | 1-(N-phenylaminoalkyl)piperazine derivatives substituted at position 2 of the phenyl ring |
AU9256498A (en) * | 1997-08-01 | 1999-02-22 | Recordati S.A. Chemical And Pharmaceutical Company | 1,4-disubstituted piperazines |
IT1293807B1 (it) * | 1997-08-01 | 1999-03-10 | Recordati Chem Pharm | Derivati 1- (n-fenilaminoalchil) piperazinici sostituiti alla posizione 2 dell'anello fenilico |
US6271234B1 (en) | 1997-08-01 | 2001-08-07 | Recordati S.A., Chemical And Pharmaceutical Company | 1,4-disubstituted piperazines |
IT1293804B1 (it) | 1997-08-01 | 1999-03-10 | Recordati Chem Pharm | Diarilalchilpiperazine attive sulle basse vie urinarie |
US6376494B1 (en) | 1998-06-15 | 2002-04-23 | American Home Products Corporation | Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents |
EP1087954A1 (en) * | 1998-06-15 | 2001-04-04 | American Home Products Corporation | Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents |
US20060287335A1 (en) | 2000-11-28 | 2006-12-21 | Wyeth | Serotonergic agents for treating sexual dysfunction |
US20060223824A1 (en) * | 2000-11-28 | 2006-10-05 | Wyeth | Serotonergic agents |
EP1367053A4 (en) * | 2001-02-27 | 2005-08-03 | Kaneka Corp | PROCESS FOR THE PRODUCTION OF OPTICALLY ACTIVE N-ARYL-1-AMINO-2-PROPANOL DERIVATIVES |
US7091349B2 (en) | 2002-03-12 | 2006-08-15 | Wyeth | Process for synthesizing N-aryl piperazines with chiral N′-1-[benzoyl(2-pyridyl)amino]-2-propane substitution |
US7361773B2 (en) | 2002-03-12 | 2008-04-22 | Wyeth | Preparation of N1-(2'-pyridyl)-1,2-propanediamine sulfamic acid and its use in the synthesis of biologically active piperazines |
IL163827A0 (en) * | 2002-03-12 | 2005-12-18 | Wyeth Corp | Process for synthesizing chiral n-aryl piperazines |
NZ535169A (en) | 2002-03-12 | 2006-03-31 | Wyeth Corp | Process for making chiral 1,4-disubstituted piperazines |
WO2003078396A1 (en) * | 2002-03-12 | 2003-09-25 | Wyeth | Preparation of n1-(2’-pyridyl)-1,2-propanediamine sulfamic acid and its use in the synthesis of biologically active piperazines |
US7179813B2 (en) | 2003-06-11 | 2007-02-20 | Wyeth | Bicyclic indolyl derivatives and methods for their use as serotonergic agents |
CN100436448C (zh) * | 2003-06-11 | 2008-11-26 | 惠氏公司 | 二环吲哚基衍生物以及其作为5-羟色胺能活性剂的应用 |
TW200800959A (en) | 2005-06-10 | 2008-01-01 | Wyeth Corp | Piperazine-piperidine antagonists and agonists of the 5-HT1a receptor |
WO2007146073A2 (en) * | 2006-06-09 | 2007-12-21 | Wyeth | Method for enhancing cognitive function |
BR112016028255A2 (pt) | 2014-06-06 | 2017-08-22 | Flexus Biosciences Inc | agentes imunorreguladores |
US11242319B2 (en) | 2014-11-05 | 2022-02-08 | Flexus Biosciences, Inc. | Immunoregulatory agents |
UY36390A (es) * | 2014-11-05 | 2016-06-01 | Flexus Biosciences Inc | Compuestos moduladores de la enzima indolamina 2,3-dioxigenasa (ido), sus métodos de síntesis y composiciones farmacéuticas que los contienen |
UY36391A (es) | 2014-11-05 | 2016-06-01 | Flexus Biosciences Inc | Compuestos moduladores de la enzima indolamina 2,3-dioxigenasa (ido1), sus métodos de síntesis y composiciones farmacèuticas que las contienen |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB8909209D0 (en) * | 1989-04-22 | 1989-06-07 | Wyeth John & Brother Ltd | Piperazine derivatives |
IE65362B1 (en) * | 1989-04-22 | 1995-10-18 | Wyeth John & Brother Ltd | Piperazine derivatives |
GB9021535D0 (en) * | 1990-10-03 | 1990-11-14 | Wyeth John & Brother Ltd | Piperazine derivatives |
IL101722A (en) * | 1991-05-02 | 1996-05-14 | Wyeth John & Brother Ltd | History of piperazine, their preparation and pharmaceutical preparations containing them |
SE9201138D0 (sv) * | 1992-04-09 | 1992-04-09 | Astra Ab | Novel phthalimidoalkylpiperazines |
GB9300195D0 (en) * | 1993-01-06 | 1993-03-03 | Wyeth John & Brother Ltd | Piperazine derivatives |
-
1994
- 1994-06-03 GB GB9411099A patent/GB9411099D0/en active Pending
-
1995
- 1995-06-01 EP EP95921017A patent/EP0763031B1/en not_active Expired - Lifetime
- 1995-06-01 ZA ZA954525A patent/ZA954525B/xx unknown
- 1995-06-01 DE DE69516867T patent/DE69516867T2/de not_active Expired - Fee Related
- 1995-06-01 AU AU26230/95A patent/AU680147B2/en not_active Ceased
- 1995-06-01 NZ NZ331452A patent/NZ331452A/xx unknown
- 1995-06-01 CA CA002191871A patent/CA2191871C/en not_active Expired - Fee Related
- 1995-06-01 MX MX9605915A patent/MX9605915A/es not_active IP Right Cessation
- 1995-06-01 IL IL11396795A patent/IL113967A/xx not_active IP Right Cessation
- 1995-06-01 SK SK1541-96A patent/SK281418B6/sk unknown
- 1995-06-01 BR BR9507910A patent/BR9507910A/pt not_active Application Discontinuation
- 1995-06-01 DK DK95921017T patent/DK0763031T3/da active
- 1995-06-01 CN CN95193383A patent/CN1048985C/zh not_active Expired - Fee Related
- 1995-06-01 CZ CZ19963507A patent/CZ287381B6/cs not_active IP Right Cessation
- 1995-06-01 AT AT95921017T patent/ATE192744T1/de not_active IP Right Cessation
- 1995-06-01 ES ES95921017T patent/ES2145275T3/es not_active Expired - Lifetime
- 1995-06-01 WO PCT/GB1995/001263 patent/WO1995033743A1/en active IP Right Grant
- 1995-06-01 KR KR1019960706880A patent/KR100359393B1/ko not_active IP Right Cessation
- 1995-06-01 NZ NZ287498A patent/NZ287498A/xx unknown
- 1995-06-01 PT PT95921017T patent/PT763031E/pt unknown
- 1995-06-01 RU RU97100151/04A patent/RU2165933C2/ru not_active IP Right Cessation
- 1995-06-01 HU HU9603315A patent/HUT76466A/hu unknown
- 1995-06-01 JP JP8500531A patent/JPH10500989A/ja not_active Withdrawn
- 1995-06-02 US US08/459,205 patent/US5723464A/en not_active Expired - Lifetime
-
1996
- 1996-12-02 FI FI964815A patent/FI114985B/sv active IP Right Grant
-
1998
- 1998-11-10 CN CN98122461A patent/CN1093122C/zh not_active Expired - Fee Related
-
2000
- 2000-05-19 GR GR20000401137T patent/GR3033449T3/el not_active IP Right Cessation
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