FI62667C - Foerfarande foer framstaellning av antiemetiska 1-(benzazolylalkyl)piperidinderivat - Google Patents

Foerfarande foer framstaellning av antiemetiska 1-(benzazolylalkyl)piperidinderivat Download PDF

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Publication number
FI62667C
FI62667C FI762086A FI762086A FI62667C FI 62667 C FI62667 C FI 62667C FI 762086 A FI762086 A FI 762086A FI 762086 A FI762086 A FI 762086A FI 62667 C FI62667 C FI 62667C
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FI
Finland
Prior art keywords
dihydro
benzimidazol
parts
formula
piperidinyl
Prior art date
Application number
FI762086A
Other languages
English (en)
Finnish (fi)
Other versions
FI62667B (fi
FI762086A (sv
Inventor
Jan Vanderberk
Ludo E J Kennis
Der Aa Marcel J M C Van
Heertum Albert H M Th Van
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
Priority claimed from US05/687,139 external-priority patent/US4066772A/en
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of FI762086A publication Critical patent/FI762086A/fi
Priority to FI813935A priority Critical patent/FI65249C/fi
Application granted granted Critical
Publication of FI62667B publication Critical patent/FI62667B/fi
Publication of FI62667C publication Critical patent/FI62667C/fi

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    • 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
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • 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
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Otolaryngology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (2)

1. Förfarande för framställning av antiemetiska 1-(bensazo-lylalkyDpiperidin-derivat med formeln I och farmaceutiskt godtag-bara syraadditionssalter därav, Y II E(CH,) -Ah-ICH.) -l/ N//C'\-M (I) 2
" 2" Y_yV/ 2 r7A=Ar8 1 2 i vilken formel R och R betecknar väte, halogen, lägre alkyl eller trifluormetyl, B är en tvävärd -N<L)-CO- eller -N=CH-radi- kal, som är bunden till besinningen via heteroatomen, varvid L är väte, lägre alkyl, lägre alkylkarbonyl eller lägre alkenyl, R3 är väte eller metyl, m och n betecknar ett heltal 1 eller 2, 7 8 R och R betecknar väte, halogen, lägre alkyl eller trifluormetyl, Y är 0 eller S, M är väte, lägre alkyl eller lägre alkylkarbonyl och den streckade linjen är en eventuell bindning mellan kolato-merna 3 och 4 i piperidinringen, förutsatt att, dä Y är S, har piperidinringen en enkelbindning mellan kolatomerna 3 och 4 och M är väte, kännetecknat därav, att man a) omsätter en förening med formeln /Ά r3 B N-(CH_) -CH-(CH0) -x (II) v f 2 m 2 n 12 3 där R , R , R , B, m och n betecknar samma som ovan och X är en reaktiv estergrupp, som är härledd frän motsvarande alkohol, med en förening med formeln 6 2 6 6 7 41 Υ It / \ /\ ΗΝ f—KL Ν-Μ (III) 7 8 där R , R , Υ och M betecknar samma som ovan, i ett lämpligt organiskt lösningsmedel, eller b) avlägsnar skyddsgruppen P pä i och för sig känt sätt frän en förening med formeln
0 Y Il O tl /\ I f~\ /C\ ^-(CH2)m-CH-(CH2)n-N^ ^~M (IV) 1 2 3 7 8 där R,R,R,R,R,m,n, Y och M betecknar samma sora ovan, eller c) cykliserar en förening med formeln R3 " ΐ n_/\ H,li .,ΝΗ-(ΟΗ,) -CH-(CH,) -N ,)-if N-M (V) 1 2 3 7 8 där R, R , R , R , R , m, nY och M betecknar samma som ovan, medelst ett lämpligt cykliseringsmedel pä i och för sig känt sätt, eller d) cykliserar en förening med formeln
FI762086A 1975-07-21 1976-07-20 Foerfarande foer framstaellning av antiemetiska 1-(benzazolylalkyl)piperidinderivat FI62667C (fi)

Priority Applications (1)

Application Number Priority Date Filing Date Title
FI813935A FI65249C (fi) 1975-07-21 1981-12-08 Foerfarande foer framstaellning av terapeutiskt anvaendbara 1-enyl-8-bensimidazol-1-ylpropyl-1,3,8-triazaspiro(4,5)deka n--onderivat

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US59779375A 1975-07-21 1975-07-21
US59779375 1975-07-21
US05/687,139 US4066772A (en) 1975-07-21 1976-05-17 1,3-Dihydro-1-[3-(1-piperidinyl)propyl]-2H-benzimidazol-2-ones and related compounds
US68713976 1976-05-17
KR760001697 1976-07-12
KR7601697A KR810000334B1 (ko) 1975-07-21 1976-07-12 1-(벤즈 아조릴알킬) 피페리딘 유도체의 제조방법

Publications (3)

Publication Number Publication Date
FI762086A FI762086A (sv) 1977-01-22
FI62667B FI62667B (fi) 1982-10-29
FI62667C true FI62667C (fi) 1983-02-10

Family

ID=27348142

Family Applications (1)

Application Number Title Priority Date Filing Date
FI762086A FI62667C (fi) 1975-07-21 1976-07-20 Foerfarande foer framstaellning av antiemetiska 1-(benzazolylalkyl)piperidinderivat

Country Status (25)

Country Link
JP (1) JPS5217475A (sv)
AT (1) AT364358B (sv)
AU (1) AU511027B2 (sv)
BG (1) BG26526A3 (sv)
CA (1) CA1085852A (sv)
CH (1) CH623820A5 (sv)
CS (1) CS202550B2 (sv)
DE (1) DE2632870A1 (sv)
DK (1) DK154950C (sv)
ES (3) ES449740A1 (sv)
FI (1) FI62667C (sv)
GB (1) GB1542514A (sv)
HK (1) HK14180A (sv)
IE (1) IE43496B1 (sv)
IT (1) IT1062614B (sv)
KE (1) KE3215A (sv)
LU (1) LU75354A1 (sv)
MY (1) MY8100017A (sv)
NL (1) NL187442C (sv)
NZ (1) NZ181256A (sv)
PH (1) PH13710A (sv)
PT (1) PT65387B (sv)
RO (1) RO70566A (sv)
SE (2) SE426490B (sv)
YU (1) YU39969B (sv)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4501749A (en) * 1983-10-31 1985-02-26 Merck & Co., Inc. Peripherally selective dopamine antagonists in the treatment of ocular hypertension
JPS6248684A (ja) * 1985-08-26 1987-03-03 Sumitomo Chem Co Ltd 新規なヨ−ドブチロフエノン誘導体およびその製造法
JPS62251313A (ja) * 1986-04-25 1987-11-02 信越ポリマー株式会社 結束装置
US6355659B1 (en) 1994-07-29 2002-03-12 Laboratorios Del Dr. Esteve, S.A. 4-(4-Chlorophenyl)-1236-tetrahydro-1(1H-124-triazol-1-yl)butty)pyrideine and salts thereof; pharmaceutical compositions and method of treating psychoses utilizing same
FR2723091B1 (fr) * 1994-07-29 1996-11-08 Esteve Labor Dr Tetrahydropyridine-(6,4-hydroxypiperidine) alkylazoles
PA8603801A1 (es) * 2003-05-27 2004-12-16 Janssen Pharmaceutica Nv Derivados de la quinazolina
MXPA06007017A (es) 2003-12-18 2006-08-31 Janssen Pharmaceutica Nv Derivados de pirido y pirimidopirimidina como agentes antiproliferativos.
NI200700147A (es) 2004-12-08 2019-05-10 Janssen Pharmaceutica Nv Derivados de quinazolina inhibidores de cinasas dirigidos a multip
WO2008006884A2 (en) 2006-07-13 2008-01-17 Janssen Pharmaceutica N.V. Mtki quinazoline derivatives
EP1997805A1 (en) * 2007-06-01 2008-12-03 Commissariat à l'Energie Atomique Compounds with antiparasitic activity, applications thereof to the treatment of infectious diseases caused by apicomplexans
DK2185562T3 (en) 2007-07-27 2016-02-22 Janssen Pharmaceutica Nv PYRROLOPYRIMIDINES SUITABLE FOR TREATING PROLIFERATIVE DISEASES
EP3564240B1 (en) 2007-08-31 2022-04-06 Purdue Pharma L.P. Piperidine intermediates
US9090618B2 (en) 2012-12-27 2015-07-28 Purdue Pharma L.P. Substituted benzimidazole-type piperidine compounds and uses thereof
CN108697700B (zh) * 2016-02-04 2021-08-17 辛多美制药有限公司 氘代多潘立酮组合物和用于治疗病症的方法
US11364226B2 (en) 2017-06-30 2022-06-21 Cinrx Pharma, Llc Deuterated domperidone compositions, methods, and preparation

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE633495A (sv) * 1962-06-13
BE633914A (sv) * 1962-06-22
US3629267A (en) * 1968-10-28 1971-12-21 Smith Kline French Lab Benzoheterocyclicalkyl derivatives of 4-(2-keto -1-benzimidazolinyl)-piperidine 4-(2-keto - 1 - benzimidazolinyl) -1 2 3 6 tetrahydropyridine 1 - phenyl - 1 3 8-triazaspiro(4 5)decan - 4 - one and 2 4 9-triazaspiro(5 5)undecan-1 3 5-trione
AU4698672A (en) * 1972-09-22 1972-11-09 Ciba-Geigy Ag Azacycloaliphatic compounds, process for their manufacture and compositions containing them
FR2218100A1 (en) * 1973-02-20 1974-09-13 Janssen Pharmaceutica Nv Neuroleptic tricyclic derivs. - of benzimidazolinones and triazaspiro-4,5-decan-4-ones
US3989707A (en) * 1974-06-21 1976-11-02 Janssen Pharmaceutica N.V. Benzimidazolinone derivatives

Also Published As

Publication number Publication date
ES461630A1 (es) 1978-06-16
ES449740A1 (es) 1978-02-16
MY8100017A (en) 1981-12-31
KE3215A (en) 1982-07-09
SE7608265L (sv) 1977-01-22
NL187442B (nl) 1991-05-01
LU75354A1 (sv) 1977-02-28
AT364358B (de) 1981-10-12
JPS5217475A (en) 1977-02-09
JPS6131109B2 (sv) 1986-07-17
SE8008713L (sv) 1980-12-11
CA1085852A (en) 1980-09-16
BG26526A3 (sv) 1979-04-12
IE43496L (en) 1977-01-21
AU1596476A (en) 1978-01-19
ATA534776A (de) 1981-03-15
DK327576A (da) 1977-01-22
DK154950C (da) 1989-05-29
SE426490B (sv) 1983-01-24
PT65387A (en) 1976-08-01
FI62667B (fi) 1982-10-29
PT65387B (en) 1978-06-09
YU179476A (en) 1983-01-21
CS202550B2 (en) 1981-01-30
NL7608023A (nl) 1977-01-25
PH13710A (en) 1980-09-09
SE435621B (sv) 1984-10-08
YU39969B (en) 1985-06-30
FI762086A (sv) 1977-01-22
DE2632870C2 (sv) 1989-02-16
CH623820A5 (en) 1981-06-30
NL187442C (nl) 1991-10-01
RO70566A (ro) 1982-10-11
GB1542514A (en) 1979-03-21
HK14180A (en) 1980-03-28
DE2632870A1 (de) 1977-02-10
NZ181256A (en) 1978-04-28
ES461631A1 (es) 1978-12-01
IE43496B1 (en) 1981-03-11
IT1062614B (it) 1984-10-20
DK154950B (da) 1989-01-09
AU511027B2 (en) 1980-07-24

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Owner name: JANSSEN PHARMACEUTICA N.V.