DE2961740D1 - N-heterocyclyl-4-piperidinamines, methods for their preparation, pharmaceutical compositions comprising them, intermediates therefor, and method for the preparation of the intermediates - Google Patents

N-heterocyclyl-4-piperidinamines, methods for their preparation, pharmaceutical compositions comprising them, intermediates therefor, and method for the preparation of the intermediates

Info

Publication number
DE2961740D1
DE2961740D1 DE7979300525T DE2961740T DE2961740D1 DE 2961740 D1 DE2961740 D1 DE 2961740D1 DE 7979300525 T DE7979300525 T DE 7979300525T DE 2961740 T DE2961740 T DE 2961740T DE 2961740 D1 DE2961740 D1 DE 2961740D1
Authority
DE
Germany
Prior art keywords
preparation
intermediates
piperidinamines
heterocyclyl
methods
Prior art date
Legal status (The legal status 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 status listed.)
Expired
Application number
DE7979300525T
Other languages
German (de)
English (en)
Inventor
Frans Janssens
Raymond Stokbroekx
Joseph Torremans
Marcel Luyckx
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Janssen Pharmaceutica NV
Original Assignee
Janssen Pharmaceutica NV
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=26670178&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=DE2961740(D1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from US06/002,276 external-priority patent/US4219559A/en
Application filed by Janssen Pharmaceutica NV filed Critical Janssen Pharmaceutica NV
Application granted granted Critical
Publication of DE2961740D1 publication Critical patent/DE2961740D1/de
Expired legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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 to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 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 to ring carbon atoms
    • C07D211/54Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 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 to ring carbon atoms
    • C07D211/56Nitrogen atoms
    • C07D211/58Nitrogen atoms attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; Hydrogenated benzimidazoles 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
    • C07D235/26Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/341,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/361,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
DE7979300525T 1978-04-03 1979-03-30 N-heterocyclyl-4-piperidinamines, methods for their preparation, pharmaceutical compositions comprising them, intermediates therefor, and method for the preparation of the intermediates Expired DE2961740D1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US89253478A 1978-04-03 1978-04-03
US06/002,276 US4219559A (en) 1979-01-10 1979-01-10 N-Heterocyclyl-4-piperidinamines

Publications (1)

Publication Number Publication Date
DE2961740D1 true DE2961740D1 (en) 1982-02-25

Family

ID=26670178

Family Applications (1)

Application Number Title Priority Date Filing Date
DE7979300525T Expired DE2961740D1 (en) 1978-04-03 1979-03-30 N-heterocyclyl-4-piperidinamines, methods for their preparation, pharmaceutical compositions comprising them, intermediates therefor, and method for the preparation of the intermediates

Country Status (29)

Country Link
EP (1) EP0005318B1 (cg-RX-API-DMAC7.html)
JP (2) JPS54151982A (cg-RX-API-DMAC7.html)
AT (1) AT373887B (cg-RX-API-DMAC7.html)
AU (1) AU523352B2 (cg-RX-API-DMAC7.html)
BG (1) BG38164A3 (cg-RX-API-DMAC7.html)
CA (1) CA1140119A (cg-RX-API-DMAC7.html)
CS (1) CS256358B2 (cg-RX-API-DMAC7.html)
CY (1) CY1250A (cg-RX-API-DMAC7.html)
DE (1) DE2961740D1 (cg-RX-API-DMAC7.html)
DK (1) DK169325B1 (cg-RX-API-DMAC7.html)
EG (1) EG13913A (cg-RX-API-DMAC7.html)
ES (1) ES479206A1 (cg-RX-API-DMAC7.html)
FI (1) FI64801C (cg-RX-API-DMAC7.html)
GR (1) GR64907B (cg-RX-API-DMAC7.html)
HK (1) HK3184A (cg-RX-API-DMAC7.html)
HU (1) HU182965B (cg-RX-API-DMAC7.html)
IE (1) IE47818B1 (cg-RX-API-DMAC7.html)
IL (1) IL56992A (cg-RX-API-DMAC7.html)
MY (1) MY8500046A (cg-RX-API-DMAC7.html)
NO (2) NO154058C (cg-RX-API-DMAC7.html)
NZ (1) NZ189978A (cg-RX-API-DMAC7.html)
PH (1) PH15877A (cg-RX-API-DMAC7.html)
PL (1) PL123380B1 (cg-RX-API-DMAC7.html)
PT (1) PT69429A (cg-RX-API-DMAC7.html)
RO (1) RO79320A (cg-RX-API-DMAC7.html)
SG (1) SG29883G (cg-RX-API-DMAC7.html)
SU (1) SU1056902A3 (cg-RX-API-DMAC7.html)
YU (2) YU42484B (cg-RX-API-DMAC7.html)
ZA (1) ZA791557B (cg-RX-API-DMAC7.html)

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MA19091A1 (fr) * 1980-03-10 1981-10-01 Janssen Pharmaceutica Nv Nouveaux derives de i-(4-aryl-cyclohexyl)piperidine .
IN156065B (cg-RX-API-DMAC7.html) * 1982-07-12 1985-05-04 Janssen Pharmaceutica Nv
US4556660A (en) * 1982-07-12 1985-12-03 Janssen Pharmaceutica N.V. N-(Bicyclic heterocyclyl)-4-piperidinamines
US4634704A (en) * 1983-10-06 1987-01-06 Janssen Pharmaceutica, N.V. Anti-allergic five membered heterocyclic ring containing N-(bicyclic heterocycyl)-4-piperidinamines
DE3484096D1 (de) * 1983-11-30 1991-03-14 Janssen Pharmaceutica Nv Bizyklisches heterozyklyl aufveisende n-(bizyklisches heterozyklyl-4-piperidinamine.
PL144514B1 (en) * 1984-01-09 1988-06-30 Janssen Pharmaceutica Nv Method of obtaining novel derivatives of n-/4-piperidinolo/-2-imidazoloamine
KR930005004B1 (ko) * 1985-04-15 1993-06-11 쟈안센 파아마슈우티카 엔. 부이. 치환된 n-[(4-피페리디닐)알킬]이환 축합 옥사졸아민 및 티아졸아민의 제조방법
GB8515934D0 (en) * 1985-06-24 1985-07-24 Janssen Pharmaceutica Nv (4-piperidinomethyl and-hetero)purines
EG17993A (en) * 1986-02-03 1991-08-30 Janssen Pharmaceutica Nv Anti-histaminic compositions containing n-heterocyclyl-4-piperidinanines
NZ223654A (en) * 1987-03-09 1990-03-27 Janssen Pharmaceutica Nv 1-alkyl-substituted-benzimidazole-4-piperidinamines and pharmaceutical compositions
FR2618435B1 (fr) * 1987-07-23 1989-10-27 Synthelabo Derives de benzimidazole, leur preparation et leur application en therapeutique
US5210091A (en) * 1991-06-24 1993-05-11 Neurosearch A/S Imidazole compounds and their use
US5624948A (en) * 1993-05-20 1997-04-29 Kissei Pharmaceutical Co., Ltd. 1-(2-benzimidazolyl)-1,5-diazacyclooctane compounds
US5547966A (en) * 1993-10-07 1996-08-20 Bristol-Myers Squibb Company Aryl urea and related compounds
JP2002505277A (ja) * 1998-03-06 2002-02-19 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ グリシン輸送阻害剤
HRP20080390A2 (en) * 1999-06-28 2008-12-31 Janssen Pharmaceutica N.V. Respiratory syncytial virus replication inhibitors
AU779516B2 (en) 1999-06-28 2005-01-27 Janssen Pharmaceutica N.V. Respiratory syncytial virus replication inhibitors
AU778218B2 (en) 1999-06-28 2004-11-25 Janssen Pharmaceutica N.V. Respiratory syncytial virus replication inhibitors
ATE348808T1 (de) 2000-03-06 2007-01-15 Acadia Pharm Inc Azacyclische verbindungen zur verwendung in der behandlung von mit serotonin verwandten krankheiten
CZ20032351A3 (cs) 2001-02-02 2004-08-18 Tevaápharmaceuticaláindustriesáltd Způsob výroby substituovaných @@}@@pyridylmethylB sulfinyl @�H@benzimidazolů
US6911452B2 (en) 2001-12-28 2005-06-28 Acadia Pharmaceuticals Inc. Spiroazacyclic compounds as monoamine receptor modulators
IL163666A0 (en) 2002-02-22 2005-12-18 New River Pharmaceuticals Inc Active agent delivery systems and methods for protecting and administering active agents
US7253186B2 (en) 2002-06-24 2007-08-07 Carl-Magnus Andersson N-substituted piperidine derivatives as serotonin receptor agents
US7538222B2 (en) 2002-06-24 2009-05-26 Acadia Pharmaceuticals, Inc. N-substituted piperidine derivatives as serotonin receptor agents
AU2003247615B2 (en) 2002-06-24 2007-08-09 Acadia Pharmaceuticals Inc. N-substituted piperidine derivatives as serotonin receptor agents
NZ541146A (en) 2003-01-16 2009-04-30 Acadia Pharm Inc N-(1-methylpiperidin-4-yl)-N-(4-fluorophenylmethyl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamide, also known as ACP-103, and its tartrate salt as therapeutics for neurodegenerative diseases
PT1697343E (pt) 2003-12-18 2009-09-16 Tibotec Pharm Ltd Aminobenzimidazolos e benzimidazolos como inibidores da replicação do vírus sincicial respiratório
RU2369606C2 (ru) 2003-12-18 2009-10-10 Тиботек Фармасьютикалз Лтд. Производные 5- или 6-замещенных бензимидазолов в качестве ингибиторов репликации респираторного синцитиального вируса
AR046771A1 (es) * 2003-12-18 2005-12-21 Tibotec Pharm Ltd Derivados piperidina-amino-bencimidazol como inhibidores de la replicacion del virus sincitial respiratorio
US7820695B2 (en) 2004-05-21 2010-10-26 Acadia Pharmaceuticals, Inc. Selective serotonin receptor inverse agonists as therapeutics for disease
US20050261278A1 (en) 2004-05-21 2005-11-24 Weiner David M Selective serotonin receptor inverse agonists as therapeutics for disease
US7868176B2 (en) 2004-09-27 2011-01-11 Acadia Pharmaceuticals, Inc. Salts of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-y1)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and their preparation
US7790899B2 (en) 2004-09-27 2010-09-07 Acadia Pharmaceuticals, Inc. Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms
CN101677971A (zh) 2007-03-19 2010-03-24 阿卡蒂亚药品公司 5-ht2a反向激动剂和拮抗剂与抗精神病药物的组合
JP6850282B2 (ja) 2015-07-20 2021-03-31 アカディア ファーマシューティカルズ インコーポレーテッド N−(4−フルオロベンジル)−n−(1−メチルピペリジン−4−イル)−n’−(4−(2−メチルプロピルオキシ)フェニルメチル)カルバミドならびにその酒石酸塩および多形形態cを調製する方法
US10953000B2 (en) 2016-03-25 2021-03-23 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome P450 modulators
WO2017165635A1 (en) 2016-03-25 2017-09-28 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome p450 modulators
EP3558311A1 (en) 2016-12-20 2019-10-30 Acadia Pharmaceuticals Inc. Pimavanserin alone or in combination for use in the treatment of alzheimer's disease psychosis
US11135211B2 (en) 2017-04-28 2021-10-05 Acadia Pharmaceuticals Inc. Pimavanserin for treating impulse control disorder
EP3675827A1 (en) 2017-08-30 2020-07-08 Acadia Pharmaceuticals Inc. Formulations of pimavanserin

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US2857391A (en) * 1955-04-15 1958-10-21 Merck & Co Inc Aminomethylbenzimidazoles
US2971005A (en) * 1958-10-17 1961-02-07 Merck & Co Inc Nu-substituted derivatives of 2-benzylaminobenzimidazoles
BE788065A (fr) * 1971-08-26 1973-02-26 Degussa Nouvelles aza-benzimidazoles et procede pour leur preparation

Also Published As

Publication number Publication date
ATA242579A (de) 1983-07-15
DK129879A (da) 1979-10-04
BG38164A3 (bg) 1985-10-15
SU1056902A3 (ru) 1983-11-23
ZA791557B (en) 1980-11-26
CS256358B2 (en) 1988-04-15
RO79320A (ro) 1982-08-17
YU42484B (en) 1988-10-31
EP0005318A1 (en) 1979-11-14
IE790676L (en) 1979-10-03
AU4529679A (en) 1979-10-18
CS222779A2 (en) 1987-03-12
NO154090B (no) 1986-04-07
NO791097L (no) 1979-10-04
EG13913A (en) 1982-09-30
FI64801B (fi) 1983-09-30
IL56992A0 (en) 1979-07-25
NZ189978A (en) 1984-05-31
CA1140119A (en) 1983-01-25
CY1250A (en) 1984-08-31
FI791084A7 (fi) 1979-10-04
IE47818B1 (en) 1984-06-27
YU78479A (en) 1983-10-31
JPS641477B2 (cg-RX-API-DMAC7.html) 1989-01-11
PT69429A (pt) 1979-05-01
SG29883G (en) 1984-04-19
PL214648A1 (cg-RX-API-DMAC7.html) 1980-03-24
EP0005318B1 (en) 1982-01-06
MY8500046A (en) 1985-12-31
PL123380B1 (en) 1982-10-30
HU182965B (en) 1984-03-28
ES479206A1 (es) 1979-12-16
YU43158B (en) 1989-04-30
JPS54151982A (en) 1979-11-29
FI64801C (fi) 1984-01-10
AU523352B2 (en) 1982-07-22
JPH01117880A (ja) 1989-05-10
PH15877A (en) 1983-04-13
NO842563L (no) 1979-10-04
DK169325B1 (da) 1994-10-10
HK3184A (en) 1984-01-20
JPH0240666B2 (cg-RX-API-DMAC7.html) 1990-09-12
NO154058B (no) 1986-04-01
IL56992A (en) 1983-03-31
AT373887B (de) 1984-02-27
NO154090C (no) 1986-07-16
NO154058C (no) 1986-07-09
YU50283A (en) 1983-12-31
GR64907B (en) 1980-06-07

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