HK1023775A1 - Heteroarylpiperidines and piperazines and their use as antipsychotics and analgetics - Google Patents

Heteroarylpiperidines and piperazines and their use as antipsychotics and analgetics

Info

Publication number
HK1023775A1
HK1023775A1 HK00103040.4A HK00103040A HK1023775A1 HK 1023775 A1 HK1023775 A1 HK 1023775A1 HK 00103040 A HK00103040 A HK 00103040A HK 1023775 A1 HK1023775 A1 HK 1023775A1
Authority
HK
Hong Kong
Prior art keywords
heteroarylpiperidines
piperazines
compounds
analgetics
antipsychotics
Prior art date
Application number
HK00103040.4A
Other languages
Unknown language ( )
English (en)
Inventor
Joseph T Strupczewski
Grover C Helsley
Yulin Chiang
Kenneth J Bordeau
Edward J Glamkowski
Original Assignee
Aventisub Ii Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27120778&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HK1023775(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Aventisub Ii Inc filed Critical Aventisub Ii Inc
Publication of HK1023775A1 publication Critical patent/HK1023775A1/

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/24Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/25Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/30Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms
    • C07C233/33Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/49Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/54Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/22Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/45Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by condensation
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/673Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by change of size of the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/68Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
    • C07C45/70Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form
    • C07C45/71Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form being hydroxy groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/20Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D275/00Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/04Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D275/00Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/04Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D275/06Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • C07D277/68Benzothiazoles 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
    • C07D277/82Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/10Heterocyclic 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 carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
HK00103040.4A 1991-11-05 2000-05-22 Heteroarylpiperidines and piperazines and their use as antipsychotics and analgetics HK1023775A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US78826991A 1991-11-05 1991-11-05
US07/969,383 US5364866A (en) 1989-05-19 1992-10-30 Heteroarylpiperidines, pyrrolidines and piperazines and their use as antipsychotics and analetics

Publications (1)

Publication Number Publication Date
HK1023775A1 true HK1023775A1 (en) 2000-09-22

Family

ID=27120778

Family Applications (2)

Application Number Title Priority Date Filing Date
HK00103040.4A HK1023775A1 (en) 1991-11-05 2000-05-22 Heteroarylpiperidines and piperazines and their use as antipsychotics and analgetics
HK00103045A HK1023776A1 (en) 1991-11-05 2000-05-22 Heteroarylperidines and piperazines and their use as antipsychotics and analgetics

Family Applications After (1)

Application Number Title Priority Date Filing Date
HK00103045A HK1023776A1 (en) 1991-11-05 2000-05-22 Heteroarylperidines and piperazines and their use as antipsychotics and analgetics

Country Status (25)

Country Link
US (4) US5364866A (ru)
EP (8) EP1110954A1 (ru)
JP (1) JP2927551B2 (ru)
KR (1) KR100276764B1 (ru)
AT (3) ATE248825T1 (ru)
AU (1) AU674499B2 (ru)
CA (1) CA2121253C (ru)
CZ (1) CZ287611B6 (ru)
DE (3) DE69233189T2 (ru)
DK (3) DK0612318T3 (ru)
ES (3) ES2354407T3 (ru)
FI (2) FI942052A (ru)
GE (1) GEP19991706B (ru)
HK (2) HK1023775A1 (ru)
HU (1) HUT70855A (ru)
IL (1) IL103622A (ru)
NO (1) NO304979B1 (ru)
NZ (1) NZ245006A (ru)
PH (1) PH30432A (ru)
PT (2) PT542136E (ru)
RO (1) RO114447B1 (ru)
RU (1) RU2127731C1 (ru)
SK (1) SK283517B6 (ru)
UA (1) UA41289C2 (ru)
WO (1) WO1993009102A1 (ru)

Families Citing this family (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5776963A (en) * 1989-05-19 1998-07-07 Hoechst Marion Roussel, Inc. 3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility
US5364866A (en) 1989-05-19 1994-11-15 Hoechst-Roussel Pharmaceuticals, Inc. Heteroarylpiperidines, pyrrolidines and piperazines and their use as antipsychotics and analetics
US5561128A (en) * 1989-05-19 1996-10-01 Hoechst-Roussel Pharmaceuticals, Inc. N-[(4-(heteroaryl)-1-piperidinyl)alkyl]-10,11-dihydro-5H-dibenz[B,F]azepines and related compounds and their therapeutic utility
US5750542A (en) 1993-09-28 1998-05-12 Pfizer Benzisoxazole and benzisothizole derivatives as cholinesterase inhibitors
CA2149918A1 (en) * 1992-11-23 1994-06-09 Mark G. Palermo Substituted 3-(aminoalkylamino)-1,2-benzisoxazoles and related compounds
US5494908A (en) * 1992-11-23 1996-02-27 Hoechst-Roussel Pharmaceutical Incorporated Substituted 3-(aminoalkylamino)-1,2-benzisoxazoles and related compounds
GB9410031D0 (en) * 1994-05-19 1994-07-06 Merck Sharp & Dohme Therapeutic agents
WO1996039397A1 (en) * 1995-06-06 1996-12-12 Hoechst Marion Roussel, Inc. Benzisoxazole and indazole derivatives as antipsychotic agents
NZ334148A (en) * 1996-08-12 2001-12-21 Celgene Corp 3-Substituted phenyl-ethyl or ethenyl derivatives terminated with a nitrile, alkane, carboxyl or carbamoyl group useful to reduce cytokine levels
EP1632483B1 (en) * 2001-02-16 2008-10-29 Aventis Pharmaceuticals Inc. Heterocyclic substituted carbonyl derivatives and their use as dopamine d3 receptor ligands
GB0117577D0 (en) 2001-02-16 2001-09-12 Aventis Pharm Prod Inc Novel heterocyclic substituted carbonyl derivatives and their use as dopamine D receptor ligands
FR2827280B1 (fr) * 2001-07-13 2003-10-31 Servier Lab Nouveaux derives de benzene sulfonamide, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
EP2305656B1 (en) * 2001-08-31 2012-10-24 Novartis AG Optical isomers of an iloperidone metabolite
US7355042B2 (en) * 2001-10-16 2008-04-08 Hypnion, Inc. Treatment of CNS disorders using CNS target modulators
JP5067998B2 (ja) 2001-10-30 2012-11-07 ノバルティス アーゲー イロペリドンおよび星形ポリマーのデポー製剤
CA2476936A1 (en) * 2002-02-20 2003-08-28 Chih-Hung Lee Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (vr1) receptor
GB0216416D0 (en) 2002-07-15 2002-08-21 Novartis Ag Organic compounds
US6939877B2 (en) * 2002-09-12 2005-09-06 Wyeth Antidepressant piperidine derivatives of heterocycle-fused benzodioxans
WO2004026864A1 (en) * 2002-09-17 2004-04-01 Warner-Lambert Company Llc Heterocyclic substituted piperazines for the treatment of schizophrenia
WO2004029048A1 (en) * 2002-09-26 2004-04-08 Warner-Lambert Company Llc Heterocyclic substituted piperazines for the treatment of schizophrenia
US7157471B2 (en) * 2003-08-25 2007-01-02 Boehringer Ingelheim International Gmbh Haloalkyl- and piperidine-substituted benzimidazole-derivatives
GB0322994D0 (en) * 2003-10-01 2003-11-05 Novartis Ag Organic compounds
JP2007513197A (ja) * 2003-12-08 2007-05-24 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー 統合失調症の治療のための複素環式置換インダン誘導体および関連化合物
US20100063093A1 (en) * 2007-03-28 2010-03-11 Curt Wolfgang Methods for the administration of iloperidone
CA2582022C (en) 2004-09-30 2021-05-18 Vanda Pharmaceuticals, Inc. Methods for the administration of iloperidone
EP1877405B1 (en) * 2005-04-26 2010-03-03 Hypnion, Inc. Benzisoxazole piperidine compounds and methods of use thereof
CA2637531A1 (en) * 2006-02-17 2007-08-30 Memory Pharmaceuticals Corporation Compounds having 5-ht6 receptor affinity
RU2008150624A (ru) * 2006-05-22 2010-06-27 Ванда Фармасьютиклз, Инк. (Us) Лечение депрессивных расстройств
US20150259747A1 (en) 2007-03-29 2015-09-17 Vanda Pharmaceuticals Inc. Method of predicting a predisposition to qt prolongation
ES2542967T3 (es) 2007-03-29 2015-08-13 Vanda Pharmaceuticals Inc. Método de predecir una predisposición a la prolongación de QT
US8198305B2 (en) * 2007-04-13 2012-06-12 Concert Pharmaceuticals Inc. 1,2-benzisoxazol-3-yl compounds
ES2569480T3 (es) 2007-05-18 2016-05-11 Vanda Pharmaceuticals Inc. Marcadores genéticos de eficacia de iloperidona en el tratamiento de síntomas psicóticos
ES2498673T3 (es) * 2007-07-26 2014-09-25 F. Hoffmann-La Roche Ag Moduladores duales de los receptores 5-HT2a y D3
AU2008286760A1 (en) * 2007-08-15 2009-02-19 Memory Pharmaceuticals Corporation 3' substituted compounds having 5-HT6 receptor affinity
EP2198048A2 (en) * 2007-09-10 2010-06-23 Vanda Pharmaceuticals Inc. Prediction of qt prolongation based on snp genotype
WO2009076664A1 (en) 2007-12-13 2009-06-18 Vanda Pharmaceuticals Inc. Method and composition for treating a serotonin receptor-mediated condition
EP2222301B1 (en) 2007-12-13 2014-10-08 Vanda Pharmaceuticals Inc. Method and composition for treating an alpha adrenoceptor-mediated condition
US20100016297A1 (en) * 2008-06-24 2010-01-21 Memory Pharmaceuticals Corporation Alkyl-substituted 3' compounds having 5-ht6 receptor affinity
US20100029629A1 (en) * 2008-07-25 2010-02-04 Memory Pharmaceuticals Corporation Acyclic compounds having 5-ht6 receptor affinity
US20100056531A1 (en) * 2008-08-22 2010-03-04 Memory Pharmaceuticals Corporation Alkyl-substituted 3' compounds having 5-ht6 receptor affinity
CA2757723C (en) 2009-04-06 2018-07-24 Vanda Pharmaceuticals, Inc. Method of predicting a predisposition to qt prolongation based on abcc2 gene sequence or product thereof
SI2417267T1 (sl) 2009-04-06 2017-02-28 Vanda Pharmaceuticals Inc. Postopek zdravljenja na podlagi polimorfizmov gena KCNQ1
JP5881597B2 (ja) 2009-04-06 2016-03-09 ヴァンダ ファーマシューティカルズ インコーポレイテッド Qt延長に対する素因を予測する方法
JP5692872B2 (ja) 2009-04-06 2015-04-01 ヴァンダ ファーマシューティカルズ インコーポレイテッド Bai遺伝子の配列又はその産物に基づいてqt延長に対する素因を予測する方法
DE102009016996A1 (de) 2009-04-08 2010-10-14 Fleissner Gmbh Vorrichtung zum Verfestigen einer Faserbahn
DE102009017729A1 (de) 2009-04-11 2010-10-14 Fleissner Gmbh Vorrichtung zum Verfestigen einer Faserbahn
DE102009032343A1 (de) 2009-07-09 2011-01-20 Fleissner Gmbh Und Co. Vorrichtung zum Verfestigen einer Materialbahn
US8802855B2 (en) 2009-09-19 2014-08-12 Zhejiang Huahai Pharmaceutical Co., Ltd. Method for preparation of iloperidone and crystallization method thereof
WO2011055188A1 (en) * 2009-11-05 2011-05-12 Orchid Chemicals And Pharmaceuticals Limited An improved process for the preparation of iloperidone
WO2011061750A2 (en) * 2009-11-19 2011-05-26 Symed Labs Limited Process for the preparation of iloperidone using a novel intermediate
EP2515863A2 (en) 2009-12-23 2012-10-31 Lupin Limited Slow release pharmaceutical compositions of iloperidone
JP6076740B2 (ja) 2010-01-07 2017-02-08 アルカーメス ファーマ アイルランド リミテッド 第四級アンモニウム塩プロドラッグ
US8343706B2 (en) * 2010-01-25 2013-01-01 International Business Machines Corporation Fluorine-free fused ring heteroaromatic photoacid generators and resist compositions containing the same
DE102010009275A1 (de) 2010-02-25 2011-08-25 Trützschler Nonwovens GmbH, 63329 Vorrichtung zum Verfestigen einer Materialbahn
WO2011154860A1 (en) * 2010-06-08 2011-12-15 Alembic Pharmaceuticals Limited An improved process for preparing iloperidone
WO2012032532A1 (en) * 2010-09-07 2012-03-15 Symed Labs Limited "processes for the preparation of 4'-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino]propoxy]-3'-methoxyacetophenone and intermediates thereof"
WO2012090138A1 (en) * 2010-12-27 2012-07-05 Ranbaxy Laboratories Limited Processes for the preparation of iloperidone
WO2012123963A2 (en) 2011-02-24 2012-09-20 Megafine Pharma (P) Ltd. A process for preparation of iloperidone and amorphous co- precipitate of iloperidone with pharmaceutically acceptable excipient
JP2015510893A (ja) 2012-03-14 2015-04-13 ヴァンダ ファーマシューティカルズ インコーポレイテッド 精神障害の治療における使用のためのイロペリドン代謝物
US9375433B2 (en) * 2012-09-26 2016-06-28 Tangent Reprofiling Limited Modulators of androgen synthesis
JP6440625B2 (ja) 2012-11-14 2018-12-19 ザ・ジョンズ・ホプキンス・ユニバーシティー 精神分裂病を処置するための方法および組成物
CN103012387B (zh) * 2012-12-26 2015-08-12 浙江大学 伊潘立酮的制备方法
EP2968220B1 (en) 2013-03-15 2021-05-05 Agenebio, Inc. Methods and compositions for improving cognitive function
US10806717B2 (en) 2013-03-15 2020-10-20 The Johns Hopkins University Methods and compositions for improving cognitive function
CN103319472B (zh) * 2013-07-23 2016-07-06 河北科技大学 一种伊潘立酮的制备方法
US10925834B2 (en) 2015-05-22 2021-02-23 Agenebio, Inc. Extended release pharmaceutical compositions of levetiracetam
BR112021009265A2 (pt) 2018-12-04 2021-08-10 Vanda Pharmaceuticals Inc. métodos para preparar e administrar uma formulação de depósito injetável de iloperidona cristalina, e, formulação de depósito injetável de iloperidona cristalina
US11607408B2 (en) 2019-10-15 2023-03-21 Vanda Pharmaceuticals Inc. Method of treatment of schizophrenia
WO2023201182A1 (en) 2022-04-13 2023-10-19 Vanda Pharmaceuticals Inc. Treatment of parkinson's disease and parkinson's disease psychosis

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2258843B1 (ru) 1974-01-30 1977-09-09 Roussel Uclaf
US4335127A (en) * 1979-01-08 1982-06-15 Janssen Pharmaceutica, N.V. Piperidinylalkyl quinazoline compounds, composition and method of use
US4355037A (en) * 1981-11-12 1982-10-19 Hoechst-Roussel Pharmaceuticals 3-(4-Piperidyl)-1,2-benzisoxales
US4458076A (en) * 1983-05-31 1984-07-03 Hoechst-Roussel Pharmaceuticals 3-(4-Piperidinyl)-1,2-benzisothiazoles
HU198036B (en) * 1983-08-22 1989-07-28 Hoechst Roussel Pharma Process for production of derivatives of 3-piperidil-/1h/-indasole and medical preparatives containing them
US4670447A (en) * 1983-08-22 1987-06-02 Hoechst-Roussel Pharmaceuticals Inc. Antipsychotic 3-(piperidinyl)- and 3-(pyrrolidinyl)-1H-indazoles
US4590196A (en) 1984-08-23 1986-05-20 Bristol-Myers Company Analgesic 1,2-benzisothiazol-3-ylpiperazine derivatives
JPH0625181B2 (ja) 1985-03-27 1994-04-06 住友製薬株式会社 新規なイミド誘導体
AU593194B2 (en) * 1986-09-26 1990-02-01 Sumitomo Pharmaceuticals Company, Limited Imide derivatives ,and their production and use
US4999356A (en) * 1987-08-07 1991-03-12 Hoechst-Roussel Pharmaceuticals, Inc. 1-phenyl-3-(1-piperazinyl)-1H-indazoles
EP0302423A3 (en) 1987-08-07 1991-01-09 Hoechst-Roussel Pharmaceuticals Incorporated 1-phenyl-3-(1-piperazinyl)-1h-indazoles, a process and intermediates for their preparation, and the use thereof as medicaments
CA1335289C (en) * 1987-10-26 1995-04-18 Fujio Antoku Piperidinyl benzisoxazole derivatives, their production and pharmaceutical use
JPH01199967A (ja) * 1987-10-26 1989-08-11 Sumitomo Pharmaceut Co Ltd 新規なイミド誘導体
US4880930A (en) 1987-11-30 1989-11-14 New James S Psychotropic acyclic amide derivatives
US5001130A (en) * 1988-02-18 1991-03-19 Bristol-Myers Company Psychotropic heterobicycloalkylpiperazine derivatives
US4780466A (en) * 1988-03-17 1988-10-25 Hoechst-Roussel Pharmaceuticals, Inc. Arylpiperazinylalkoxy derivatives of cyclic imides
NZ230045A (en) * 1988-08-05 1990-11-27 Janssen Pharmaceutica Nv 3-piperazinylbenzazole derivatives and pharmaceutical compositions
IL90879A0 (en) 1988-09-02 1990-02-09 Janssen Pharmaceutica Nv 3-piperidinyl-indazole derivatives,their preparation and antihypertensive compositions containing them
FR2641278B1 (fr) * 1989-01-05 1991-03-22 Lipha Piperidines, procedes de preparation et medicaments les contenant
NZ233525A (en) 1989-05-15 1991-09-25 Janssen Pharmaceutica Nv Piperidinyl, pyrrolidinyl and piperazinyl alkylphenol ethers and pharmaceutical compositions
NZ233503A (en) 1989-05-15 1991-06-25 Janssen Pharmaceutica Nv Substituted (thio)morpholinyl and piperazinyl alkylphenol ethers
ES2076253T3 (es) * 1989-05-19 1995-11-01 Hoechst Roussel Pharma N-(ariloxialquil)-heteroarilpiperidinas y -heteroarilpiperazinas, un procedimiento para su preparacion y su uso como medicamentos.
US5364866A (en) 1989-05-19 1994-11-15 Hoechst-Roussel Pharmaceuticals, Inc. Heteroarylpiperidines, pyrrolidines and piperazines and their use as antipsychotics and analetics
US4954503A (en) * 1989-09-11 1990-09-04 Hoechst-Roussel Pharmaceuticals, Inc. 3-(1-substituted-4-piperazinyl)-1H-indazoles
US4968792A (en) * 1989-09-25 1990-11-06 American Home Products Corporation Psychotropic benzisothiazole derivatives
JP2800953B2 (ja) * 1990-07-06 1998-09-21 住友製薬株式会社 新規なイミド誘導体
EP0609361A1 (en) 1991-10-31 1994-08-10 AlliedSignal Inc. Electro-hydraulic brake system
GB9202915D0 (en) * 1992-02-12 1992-03-25 Wellcome Found Chemical compounds
GB9302622D0 (en) 1993-02-10 1993-03-24 Wellcome Found Heteroaromatic compounds

Also Published As

Publication number Publication date
CZ110294A3 (en) 1995-06-14
EP0542136B1 (en) 2002-10-16
FI942052A0 (fi) 1994-05-04
ES2283087T3 (es) 2007-10-16
ES2206450T3 (es) 2004-05-16
US5658911A (en) 1997-08-19
DK0959075T3 (da) 2011-02-07
NO941647D0 (no) 1994-05-04
HUT70855A (en) 1995-11-28
HK1023776A1 (en) 2000-09-22
WO1993009102A1 (en) 1993-05-13
DE69233189D1 (de) 2003-10-09
ATE485293T1 (de) 2010-11-15
EP0612318B1 (en) 2003-09-03
EP0963984B1 (en) 2009-03-18
AU709451B2 (en) 1999-08-26
ATE248825T1 (de) 2003-09-15
AU3057092A (en) 1993-06-07
EP0959075A1 (en) 1999-11-24
PT963984E (pt) 2009-06-01
DK0612318T3 (da) 2003-12-08
FI20100200A (fi) 2010-05-10
RO114447B1 (ro) 1999-04-30
NO941647L (no) 1994-05-04
AU1775497A (en) 1997-06-05
EP0542136A1 (en) 1993-05-19
UA41289C2 (ru) 2001-09-17
PT542136E (pt) 2003-03-31
DK0959076T3 (da) 2007-07-02
FI942052A (fi) 1994-06-30
JP2927551B2 (ja) 1999-07-28
DE69233189T2 (de) 2004-06-24
NZ245006A (en) 1995-11-27
GEP19991706B (en) 1999-08-05
ES2354407T3 (es) 2011-03-14
PH30432A (en) 1997-05-09
SK45694A3 (en) 1995-02-08
SK283517B6 (sk) 2003-08-05
EP1110954A1 (en) 2001-06-27
JPH07501055A (ja) 1995-02-02
EP1052255A1 (en) 2000-11-15
AU674499B2 (en) 1997-01-02
EP0959076B1 (en) 2007-03-07
DE69233686D1 (de) 2007-04-19
US5364866A (en) 1994-11-15
EP0957102A1 (en) 1999-11-17
ATE356123T1 (de) 2007-03-15
KR100276764B1 (ko) 2001-01-15
USRE39198E1 (en) 2006-07-18
IL103622A0 (en) 1993-04-04
HU9401316D0 (en) 1994-08-29
CA2121253A1 (en) 1993-05-13
CZ287611B6 (cs) 2001-01-17
CA2121253C (en) 2007-07-31
EP0612318A1 (en) 1994-08-31
NO304979B1 (no) 1999-03-15
DE69233796D1 (de) 2010-12-02
EP0959076A1 (en) 1999-11-24
USRE39265E1 (en) 2006-09-05
EP0963984A1 (en) 1999-12-15
DE69233686T2 (de) 2007-10-18
EP0959075B1 (en) 2010-10-20
RU2127731C1 (ru) 1999-03-20
IL103622A (en) 2000-12-06

Similar Documents

Publication Publication Date Title
HK1023776A1 (en) Heteroarylperidines and piperazines and their use as antipsychotics and analgetics
CA2175212A1 (en) Heteroarylpiperidines, pyrrolidines and piperazines and their use as antipsychotics and analgetics
RU94028105A (ru) Новые гетероарилпроизводные, промежуточные соединения для их получения, фармкомпозиция на их основе, способ лечения психозов и способ облегчения боли
GB9406857D0 (en) Improvements in or relating to organic compounds
DK0694545T3 (da) Substituerede dibenzoxazepinforbindelser, farmaceutiske sammensætninger og anvendelsesmetoder
ATE144253T1 (de) Methanoanthracene als dopaminantagonisten
ATE144254T1 (de) Methanoanthracene als dopaminantagonisten
IE894175L (en) N-pyridinyl-9h-carbazol-9-amines, a process for their¹preparation and their use as medicaments
GR3021399T3 (en) Methanoanthracenes as dopamine antagonists
IL98200A0 (en) Pharmaceutical composition containing a derivative of substituted-l-valyl-l-prolinamide
TW360651B (en) Heteroarylpiperidines, pyrrolidines and piperazines and their use as antipsychotics and analgesics and intermediates for their preparation
MX9909548A (es) Metodos para la reduccion de fibrinogenos.
DE69431118D1 (de) Fungizide, hautkosmetishe zusammensetzung
ES8706671A1 (es) Un procedimiento para la preparacion de acarbapenems

Legal Events

Date Code Title Description
PE Patent expired

Effective date: 20121103