CS256358B2 - Method of n-heterocyclyl-4-piperidinamines preparation - Google Patents

Method of n-heterocyclyl-4-piperidinamines preparation Download PDF

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Publication number
CS256358B2
CS256358B2 CS792227A CS222779A CS256358B2 CS 256358 B2 CS256358 B2 CS 256358B2 CS 792227 A CS792227 A CS 792227A CS 222779 A CS222779 A CS 222779A CS 256358 B2 CS256358 B2 CS 256358B2
Authority
CS
Czechoslovakia
Prior art keywords
group
benzimidazol
alkyl
piperidinyl
carbon atoms
Prior art date
Application number
CS792227A
Other languages
Czech (cs)
English (en)
Other versions
CS222779A2 (en
Inventor
Frans Janssens
Raymond Stokbroekx
Joseph Torremans
Marcel Luyckx
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=CS256358(B2) "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 CS222779A2 publication Critical patent/CS222779A2/cs
Publication of CS256358B2 publication Critical patent/CS256358B2/cs

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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)
CS792227A 1978-04-03 1979-04-02 Method of n-heterocyclyl-4-piperidinamines preparation CS256358B2 (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
CS222779A2 CS222779A2 (en) 1987-03-12
CS256358B2 true CS256358B2 (en) 1988-04-15

Family

ID=26670178

Family Applications (1)

Application Number Title Priority Date Filing Date
CS792227A CS256358B2 (en) 1978-04-03 1979-04-02 Method of n-heterocyclyl-4-piperidinamines preparation

Country Status (29)

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

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA19091A1 (fr) * 1980-03-10 1981-10-01 Janssen Pharmaceutica Nv Nouveaux derives de i-(4-aryl-cyclohexyl)piperidine .
IN156065B (fr) * 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.
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
DE3781173T2 (de) * 1986-02-03 1992-12-17 Janssen Pharmaceutica Nv N-heterozyklische-4-piperidinamine enthaltende anti-histaminische zusammensetzungen.
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
FI955523A0 (fi) * 1993-05-20 1995-11-16 Kissei Pharmaceutical 1-(2-bentsimidatsolyyli)-1,5-diatsasyklo-oksataaniyhdisteet
US5547966A (en) * 1993-10-07 1996-08-20 Bristol-Myers Squibb Company Aryl urea and related compounds
KR20010032968A (ko) * 1998-03-06 2001-04-25 디르크 반테 글리신 수송 저해제
EP1196410B1 (fr) 1999-06-28 2004-02-18 Janssen Pharmaceutica N.V. Inhibiteurs de replication de virus syncytiaux respiratoires
EE04590B1 (et) 1999-06-28 2006-02-15 Janssen Pharmaceutica N.V. Respiratoorse süntsütiaalviiruse replikatsiooni inhibiitorid, nende kasutamine ja valmistamismeetod, farmatseutiline kompositsioon ja selle valmistamismeetod ning produkt
WO2001000612A2 (fr) 1999-06-28 2001-01-04 Janssen Pharmaceutica N.V. Inhibiteurs de replication du virus respiratoire syncytial
CA2397981C (fr) 2000-03-06 2010-12-21 Acadia Pharmaceuticals, Inc. Composes azacycliques utilises dans le traitement de maladies liees a la serotonine
JP2004524303A (ja) 2001-02-02 2004-08-12 テバ ファーマシューティカル インダストリーズ リミティド 置換された２−（２−ピリジルメチル）スルフィニル−１ｈ−ベンゾイミダゾール類の製造方法
EP1461339B1 (fr) 2001-12-28 2010-04-28 Acadia Pharmaceuticals Inc. Composes spiroazacycliques utilises comme modulateurs du recepteur de monoamine
CA2477088A1 (fr) 2002-02-22 2003-10-02 New River Pharmaceuticals Inc. Systemes de distribution d'agents actifs et methodes de protection et d'administration d'agents actifs
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
IL165907A0 (en) 2002-06-24 2006-01-15 Acadia Pharm Inc N-substituted piperidine derivatives as serotonin receptor agents
CN1816524B (zh) 2003-01-16 2012-06-27 阿卡蒂亚药品公司 用于神经退行性疾病的治疗的选择性五羟色胺2a/2c受体反向激动剂
ES2328700T3 (es) 2003-12-18 2009-11-17 Tibotec Pharmaceuticals Ltd. Aminobenzimidazoles y benzimidazoles como inhibidores de la replicacion del virus respiratorio sincital.
BRPI0417668A (pt) * 2003-12-18 2007-04-03 Tibotec Pharm Ltd derivados de piperidina-amino-benzimidazol como inibidores de replicação do vìrus sincicial respiratório
AU2004298459B2 (en) 2003-12-18 2011-03-17 Tibotec Pharmaceuticals Ltd. 5- or 6-substituted benzimidazole derivatives as inhibitors of respiratory syncytial virus replication
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
CN102153505B (zh) 2004-09-27 2014-10-22 阿卡蒂亚药品公司 N-(4-氟苄基)-n-(1-甲基哌啶-4-基)-n’-(4-(2-甲基丙氧基)苯基甲基)脲及其酒石酸盐的合成和晶形
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
US20090053329A1 (en) 2007-03-19 2009-02-26 Acadia Pharmaceuticals, Inc. Combinations of 5-ht2a inverse agonists and antagonists with antipsychotics
SI3325444T1 (sl) 2015-07-20 2021-11-30 Acadia Pharmaceuticals Inc. Postopki za pripravo N-(4-fluorobenzil)-N-(1-metilpiperidin-4-il)-N'- (4-(2-metilpropiloksi)fenilmetil)karbamida in njegove tartratne soli in polimorfne oblike C
WO2017165635A1 (fr) 2016-03-25 2017-09-28 Acadia Pharmaceuticals Inc. Association de pimavansérine et de modulateurs du cytochrome p450
US10953000B2 (en) 2016-03-25 2021-03-23 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome P450 modulators
WO2018118626A1 (fr) 2016-12-20 2018-06-28 Acadia Pharmaceuticals Inc. Pimavansérine seule ou en association pour une utilisation dans le traitement de la psychose liée à la maladie d'alzheimer
US11135211B2 (en) 2017-04-28 2021-10-05 Acadia Pharmaceuticals Inc. Pimavanserin for treating impulse control disorder
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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
JPS641477B2 (fr) 1989-01-11
JPH01117880A (ja) 1989-05-10
HK3184A (en) 1984-01-20
NO154090B (no) 1986-04-07
YU50283A (en) 1983-12-31
NO791097L (no) 1979-10-04
ZA791557B (en) 1980-11-26
MY8500046A (en) 1985-12-31
YU43158B (en) 1989-04-30
ES479206A1 (es) 1979-12-16
PL214648A1 (fr) 1980-03-24
NZ189978A (en) 1984-05-31
NO154058C (no) 1986-07-09
IE790676L (en) 1979-10-03
NO842563L (no) 1979-10-04
DK169325B1 (da) 1994-10-10
HU182965B (en) 1984-03-28
IE47818B1 (en) 1984-06-27
JPH0240666B2 (fr) 1990-09-12
EG13913A (en) 1982-09-30
SG29883G (en) 1984-04-19
NO154058B (no) 1986-04-01
EP0005318B1 (fr) 1982-01-06
AU4529679A (en) 1979-10-18
DK129879A (da) 1979-10-04
SU1056902A3 (ru) 1983-11-23
ATA242579A (de) 1983-07-15
BG38164A3 (bg) 1985-10-15
FI64801C (fi) 1984-01-10
NO154090C (no) 1986-07-16
CA1140119A (fr) 1983-01-25
YU78479A (en) 1983-10-31
AU523352B2 (en) 1982-07-22
PL123380B1 (en) 1982-10-30
PT69429A (pt) 1979-05-01
AT373887B (de) 1984-02-27
CS222779A2 (en) 1987-03-12
PH15877A (en) 1983-04-13
IL56992A0 (en) 1979-07-25
RO79320A (fr) 1982-08-17
YU42484B (en) 1988-10-31
DE2961740D1 (en) 1982-02-25
EP0005318A1 (fr) 1979-11-14
JPS54151982A (en) 1979-11-29
CY1250A (en) 1984-08-31
FI64801B (fi) 1983-09-30
IL56992A (en) 1983-03-31
FI791084A7 (fi) 1979-10-04

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