SE8008713L - 1- (benzazolylalkyl) piperidines - Google Patents

1- (benzazolylalkyl) piperidines

Info

Publication number
SE8008713L
SE8008713L SE8008713A SE8008713A SE8008713L SE 8008713 L SE8008713 L SE 8008713L SE 8008713 A SE8008713 A SE 8008713A SE 8008713 A SE8008713 A SE 8008713A SE 8008713 L SE8008713 L SE 8008713L
Authority
SE
Sweden
Prior art keywords
formula
lower alkyl
compound
van
preparation
Prior art date
Application number
SE8008713A
Other languages
Swedish (sv)
Other versions
SE435621B (en
Inventor
J Vandenberk
L E J Kennis
Der Aa M J M C Van
Heertum A 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 SE8008713L publication Critical patent/SE8008713L/en
Publication of SE435621B publication Critical patent/SE435621B/en

Links

Classifications

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

Abstract

1-(Benzazolylalkyl)piperidine derivatives of formula I and their salts are prepared by subjecting an amine of formula to N-alkylation to introduce the corresponding substituted alkyl radical. In the compounds of formula I, the substituents have the meanings given in Patent Claim 1. These compounds and their salts have a spasmolytic action and they are in particular used in agents to prevent vomiting.

Claims (2)

Pat entkrav. 1. Farfarande for framstallning av en kemisk fOrening corn gares av ett 1-(bensazolylalkyl)piperidinderivat med fox-main; (I-h) eller c) an Torening'med formeln R3 N7,1-(CHdin-C1-1-(CHz)n-N A (V ) ut- I2 R R• och farmaceutiskt godtagbara syraadditionssalter darav, Vari RI och R2 var far sig betecknar vate, halo, lagalkyl eller trifluorometyl; 9 o betecknar en tvavard grupp corn utgares an -N(L)-C-, -NH-C-, -S-C-, 9 -0-c-, -NN- eller -NCH-, .varvid L betecknar vEte, lagalkyl, lagalkylkarbonyl eller lagalkenyl, och de tvavarda grupperna Or bUndna till bensenkarnan via heteroatomen; R3 betecknar vate elleigyl; r m och n vardea beteck,tt tal fran11 2; ochPat entkrav. A process for the preparation of a chemical compound corn gares of a 1- (benzazolylalkyl) piperidine derivative with fox-main; (Ih) or c) an Torening 'of the formula R3 N7,1- (CHdin-C1-1- (CH2) nN A (V) out- I2 RR • and pharmaceutically acceptable acid addition salts thereof, wherein R1 and R2 each represent hydrogen, halo, lower alkyl or trifluoromethyl; wherein L represents hydrogen, lower alkyl, lower alkylcarbonyl or lower alkenyl, and the divalent radicals Or bonded to the benzene nucleus via the heteroatom; R3 denotes hydrogen or alkyl; rm and n denote denotes, a number from 11 2; and 1. (I-c) il van i B2 betecknar iiiiC(0)-, -NH-C ' l'- eller -NCH-, - 0th, on a Onskas,111,maceutiskt ggbara syraadditionssalt fram- stalles an produkterna fin stegen (1-a) till (I-c). ringslutes med ett lampligt cykliseringsmedel enligt kanda metoder for framstallning av en farening med formeln N3 -y—N N-(Cliz)m-LH-(C1-12.).-N\_.! gruppen -N A utgOres av en grupp med formeln 0 -R4 -N R R6 van i R4 betecknar vate eller lagalkyl; och och 6 var fbr sig betecknar vate, halo, lagalkyl eller trifluorometyl; kanneteckoat av att a) en fOrening med formeln 3 B van i 31 bar samma'betydelse eon B men ej -NH-C(S)-, och X Sr en lamp-hg reaktiv esterfunktion harledd fran motsvarande alkohol, bringas att reagera med en fOrening med formeln ett lampligt organiskt losningsmedel, rdrframstgllning av en fore-fling med formeln RI 3 BN -(C14 )NA1. (Ic) il van in B2 denotes iiiiC (0) -, -NH-C '1'- or -NCH-, - 0th, on a Onskas, 111, pharmaceutically acceptable acid addition salt is prepared from the products in fine steps (1 -a) to (Ic). cyclized with a suitable cyclizing agent according to known methods for the preparation of a compound of the formula N3 -γ-N N- (Cliz) m-LH- (C1-12.) .- N the group -N A consists of a group of the formula O -R 4 -N R R 6 van in R 4 represents vate or lower alkyl; and and 6 each represent hydrogen, halo, lower alkyl or trifluoromethyl; can be characterized in that a) a compound of formula 3 B van in 31 bar has the same meaning eon B but not -NH-C (S) -, and X Sr a lamp-hg reactive ester function derived from the corresponding alcohol, is reacted with a Compound of the formula a suitable organic solvent, for the preparation of a precursor of the formula RI 3 BN - (C14) NA 2. rn (1-a ) •2. rn (1-a) •
SE8008713A 1975-07-21 1980-12-11 Analogue process for the production of 1-(benzimidazolylalkyl)piperidines SE435621B (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US59779375A 1975-07-21 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
KR7601697A KR810000334B1 (en) 1975-07-21 1976-07-12 Process for preparation 1-(benzazolylalkyl)-piperidine derivatives

Publications (2)

Publication Number Publication Date
SE8008713L true SE8008713L (en) 1980-12-11
SE435621B SE435621B (en) 1984-10-08

Family

ID=27348142

Family Applications (2)

Application Number Title Priority Date Filing Date
SE7608265A SE426490B (en) 1975-07-21 1976-07-20 ANALOGY PROCEDURE FOR PREPARATION OF 1- (BENSAZOLYLALKYL) PIPERIDINES
SE8008713A SE435621B (en) 1975-07-21 1980-12-11 Analogue process for the production of 1-(benzimidazolylalkyl)piperidines

Family Applications Before (1)

Application Number Title Priority Date Filing Date
SE7608265A SE426490B (en) 1975-07-21 1976-07-20 ANALOGY PROCEDURE FOR PREPARATION OF 1- (BENSAZOLYLALKYL) PIPERIDINES

Country Status (25)

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

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 (en) * 1985-08-26 1987-03-03 Sumitomo Chem Co Ltd Novel iodobutyrophenone derivative and production thereof
JPS62251313A (en) * 1986-04-25 1987-11-02 信越ポリマー株式会社 Bundling device
FR2723091B1 (en) * 1994-07-29 1996-11-08 Esteve Labor Dr TETRAHYDROPYRIDINE- (6,4-HYDROXYPIPERIDINE) ALKYLAZOLES
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
JO2785B1 (en) 2003-05-27 2014-03-15 شركة جانسين فارماسوتيكا ان. في Quinazoline derivatives
EA013904B1 (en) 2003-12-18 2010-08-30 Янссен Фармацевтика Н.В. Pyrido- and pyrimidopyrimidine derivatives as anti- proliferative agents
NI200700147A (en) 2004-12-08 2019-05-10 Janssen Pharmaceutica Nv QUINAZOLINE DERIVATIVES KINE INHIBITORS TARGETING MULTIP
EP2044084B1 (en) 2006-07-13 2016-02-17 Janssen Pharmaceutica NV 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
JP5536647B2 (en) 2007-07-27 2014-07-02 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 Pyrrolopyrimidine
TWI448289B (en) 2007-08-31 2014-08-11 Purdue Pharma Lp Substituted-quinoxaline-type piperidine compounds and the uses thereof
US9090618B2 (en) 2012-12-27 2015-07-28 Purdue Pharma L.P. Substituted benzimidazole-type piperidine compounds and uses thereof
WO2017136617A1 (en) * 2016-02-04 2017-08-10 Cinrx Pharma, Llc Deuterated domperidone compositions and methods for therapy of disorders
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 (en) * 1962-06-13
BE633914A (en) * 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
GB1542514A (en) 1979-03-21
DK327576A (en) 1977-01-22
PT65387B (en) 1978-06-09
IT1062614B (en) 1984-10-20
JPS5217475A (en) 1977-02-09
SE435621B (en) 1984-10-08
RO70566A (en) 1982-10-11
DK154950C (en) 1989-05-29
JPS6131109B2 (en) 1986-07-17
NL187442C (en) 1991-10-01
IE43496B1 (en) 1981-03-11
AU511027B2 (en) 1980-07-24
DE2632870C2 (en) 1989-02-16
DE2632870A1 (en) 1977-02-10
KE3215A (en) 1982-07-09
LU75354A1 (en) 1977-02-28
NL187442B (en) 1991-05-01
MY8100017A (en) 1981-12-31
SE7608265L (en) 1977-01-22
YU179476A (en) 1983-01-21
FI62667C (en) 1983-02-10
PH13710A (en) 1980-09-09
FI62667B (en) 1982-10-29
PT65387A (en) 1976-08-01
ES449740A1 (en) 1978-02-16
DK154950B (en) 1989-01-09
FI762086A (en) 1977-01-22
HK14180A (en) 1980-03-28
ES461630A1 (en) 1978-06-16
YU39969B (en) 1985-06-30
CA1085852A (en) 1980-09-16
NL7608023A (en) 1977-01-25
BG26526A3 (en) 1979-04-12
CS202550B2 (en) 1981-01-30
CH623820A5 (en) 1981-06-30
NZ181256A (en) 1978-04-28
AT364358B (en) 1981-10-12
ATA534776A (en) 1981-03-15
ES461631A1 (en) 1978-12-01
SE426490B (en) 1983-01-24
AU1596476A (en) 1978-01-19
IE43496L (en) 1977-01-21

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