IE47818B1 - 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
IE47818B1
IE47818B1 IE676/79A IE67679A IE47818B1 IE 47818 B1 IE47818 B1 IE 47818B1 IE 676/79 A IE676/79 A IE 676/79A IE 67679 A IE67679 A IE 67679A IE 47818 B1 IE47818 B1 IE 47818B1
Authority
IE
Ireland
Prior art keywords
group
formula
alkyl
parts
benzimidazol
Prior art date
Application number
IE676/79A
Other languages
English (en)
Other versions
IE790676L (en
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=IE47818(B1) "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
Publication of IE790676L publication Critical patent/IE790676L/xx
Publication of IE47818B1 publication Critical patent/IE47818B1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/36—Heterocyclic 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
    • C07D211/54—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/36—Heterocyclic 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
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; 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
    • C07D235/26—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-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)
IE676/79A 1978-04-03 1979-08-08 N-heterocyclyl-4-piperidinamines,methods for their preparation,pharmaceutical compositions comprising them,intermediates therefor,and method for the preparation of the intermediates IE47818B1 (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 (2)

Publication Number Publication Date
IE790676L IE790676L (en) 1979-10-03
IE47818B1 true IE47818B1 (en) 1984-06-27

Family

ID=26670178

Family Applications (1)

Application Number Title Priority Date Filing Date
IE676/79A IE47818B1 (en) 1978-04-03 1979-08-08 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 (enExample)
JP (2) JPS54151982A (enExample)
AT (1) AT373887B (enExample)
AU (1) AU523352B2 (enExample)
BG (1) BG38164A3 (enExample)
CA (1) CA1140119A (enExample)
CS (1) CS256358B2 (enExample)
CY (1) CY1250A (enExample)
DE (1) DE2961740D1 (enExample)
DK (1) DK169325B1 (enExample)
EG (1) EG13913A (enExample)
ES (1) ES479206A1 (enExample)
FI (1) FI64801C (enExample)
GR (1) GR64907B (enExample)
HK (1) HK3184A (enExample)
HU (1) HU182965B (enExample)
IE (1) IE47818B1 (enExample)
IL (1) IL56992A (enExample)
MY (1) MY8500046A (enExample)
NO (2) NO154058C (enExample)
NZ (1) NZ189978A (enExample)
PH (1) PH15877A (enExample)
PL (1) PL123380B1 (enExample)
PT (1) PT69429A (enExample)
RO (1) RO79320A (enExample)
SG (1) SG29883G (enExample)
SU (1) SU1056902A3 (enExample)
YU (2) YU42484B (enExample)
ZA (1) ZA791557B (enExample)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
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MA19091A1 (fr) * 1980-03-10 1981-10-01 Janssen Pharmaceutica Nv Nouveaux derives de i-(4-aryl-cyclohexyl)piperidine .
IN156065B (enExample) * 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
EP0144101B1 (en) * 1983-11-30 1991-02-06 Janssen Pharmaceutica N.V. Bicyclic heterocyclyl containing n-(bicyclic heterocyclyl)-4-piperidinamines
JPS60174778A (ja) * 1984-01-09 1985-09-09 ジヤンセン・フア−マシユ−チカ・ナ−ムロ−ゼ・フエンノ−トシヤツプ Ｎ−ヘテロシクリル−４−ピペリジンアミン
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
CA1327579C (en) * 1986-02-03 1994-03-08 Frans Eduard Janssens Anti-histaminic compositions containing n-heterocyclyl-4-piperidinamines
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
CA2161876A1 (en) * 1993-05-20 1994-12-08 Den-Ichi Momose 1-(2-benzimidazolyl)-1,5-diazacyclooctane compounds
US5547966A (en) * 1993-10-07 1996-08-20 Bristol-Myers Squibb Company Aryl urea and related compounds
IL138228A0 (en) * 1998-03-06 2001-10-31 Janssen Pharmaceutica Nv Glycine transport inhibitors
US6924287B1 (en) * 1999-06-28 2005-08-02 Janssen Pharmacatica, N.V. Respiratory syncytial virus replication inhibitors
KR100731271B1 (ko) * 1999-06-28 2007-06-21 얀센 파마슈티카 엔.브이. 호흡기 신시티움 바이러스 복제 억제제
CZ20014573A3 (cs) * 1999-06-28 2002-05-15 Janssen Pharmaceutica N. V. Inhibitory replikace respiračně syncyciálního viru
KR100879647B1 (ko) 2000-03-06 2009-01-20 아카디아 파마슈티칼스 인코포레이티드 세로토닌 관련 질병의 치료에 사용되는 아자시클릭 화합물
EP1970374A1 (en) 2001-02-02 2008-09-17 Teva Pharmaceutical Industries Ltd. Process for the production of substituted 2-(pyridin-2-ylmethylsulfinyl)-1H-benzimidazoles
KR100974901B1 (ko) 2001-12-28 2010-08-10 아카디아 파마슈티칼스 인코포레이티드 모노아민 수용체 조정자로서의 스피로아자사이클릭 화합물
JP4625637B2 (ja) 2002-02-22 2011-02-02 シャイア エルエルシー 活性物質送達系及び活性物質を保護し投与する方法
US7253186B2 (en) 2002-06-24 2007-08-07 Carl-Magnus Andersson 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
US7538222B2 (en) 2002-06-24 2009-05-26 Acadia Pharmaceuticals, Inc. N-substituted piperidine derivatives as serotonin receptor agents
ES2367135T3 (es) 2003-01-16 2011-10-28 Acadia Pharmaceuticals Inc. Agonistas inversos selectivos de los receptores 2a o 2c de serotonina utilzados como agentes terapéuticos para enfermedades neurodegenerativas.
TWI356055B (en) 2003-12-18 2012-01-11 Tibotec Pharm Ltd Aminobenzimidazoles and benzimidazoles as inhibito
CN103450159A (zh) * 2003-12-18 2013-12-18 泰博特克药品有限公司 作为呼吸道合胞病毒复制的抑制剂的哌啶-氨基-苯并咪唑类衍生物
RU2369606C2 (ru) 2003-12-18 2009-10-10 Тиботек Фармасьютикалз Лтд. Производные 5- или 6-замещенных бензимидазолов в качестве ингибиторов репликации респираторного синцитиального вируса
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
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
RU2417986C2 (ru) 2004-09-27 2011-05-10 Акадиа Фармасьютикалз Инк. Синтез n-(4-фторбензил)-n-(1-метилпиперидин-4-ил)-n'-(4-(2-метилпропилокси)фенилметил)карбамида, а также его тартрата и кристаллических форм
PL2134330T3 (pl) 2007-03-19 2013-10-31 Acadia Pharm Inc Kombinacje odwrotnych agonistów i antagonistów 5-HT2A z antypsychotykami
WO2017015272A1 (en) 2015-07-20 2017-01-26 Acadia Pharmaceuticals Inc. Methods for preparing n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and polymorphic form c
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
WO2018200977A1 (en) 2017-04-28 2018-11-01 Acadia Pharmaceuticals Inc. Pimavanserin for treating impulse control disorder
WO2019046167A1 (en) 2017-08-30 2019-03-07 Acadia Pharmaceuticals Inc. PIMAVANSERIN FORMULATIONS

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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
GR64907B (en) 1980-06-07
NO842563L (no) 1979-10-04
JPH0240666B2 (enExample) 1990-09-12
SU1056902A3 (ru) 1983-11-23
CS256358B2 (en) 1988-04-15
EP0005318B1 (en) 1982-01-06
YU42484B (en) 1988-10-31
NZ189978A (en) 1984-05-31
ZA791557B (en) 1980-11-26
CY1250A (en) 1984-08-31
HU182965B (en) 1984-03-28
NO791097L (no) 1979-10-04
MY8500046A (en) 1985-12-31
IL56992A (en) 1983-03-31
CA1140119A (en) 1983-01-25
YU78479A (en) 1983-10-31
EG13913A (en) 1982-09-30
JPS54151982A (en) 1979-11-29
NO154058B (no) 1986-04-01
ATA242579A (de) 1983-07-15
AU4529679A (en) 1979-10-18
YU43158B (en) 1989-04-30
AU523352B2 (en) 1982-07-22
DK169325B1 (da) 1994-10-10
PL123380B1 (en) 1982-10-30
FI791084A7 (fi) 1979-10-04
CS222779A2 (en) 1987-03-12
AT373887B (de) 1984-02-27
JPS641477B2 (enExample) 1989-01-11
ES479206A1 (es) 1979-12-16
DE2961740D1 (en) 1982-02-25
EP0005318A1 (en) 1979-11-14
PL214648A1 (enExample) 1980-03-24
IL56992A0 (en) 1979-07-25
IE790676L (en) 1979-10-03
NO154090C (no) 1986-07-16
RO79320A (ro) 1982-08-17
PH15877A (en) 1983-04-13
FI64801B (fi) 1983-09-30
NO154058C (no) 1986-07-09
SG29883G (en) 1984-04-19
BG38164A3 (bg) 1985-10-15
PT69429A (pt) 1979-05-01
HK3184A (en) 1984-01-20
FI64801C (fi) 1984-01-10
JPH01117880A (ja) 1989-05-10
NO154090B (no) 1986-04-07
YU50283A (en) 1983-12-31
DK129879A (da) 1979-10-04

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