HUP9903948A2 - Tachikinin antagonista 1-(1,2-diszubsztituált piperidinil)-4-(kondenzált imidazolil)-piperidin-származékok, előállításuk és alkalmazásuk - Google Patents

Tachikinin antagonista 1-(1,2-diszubsztituált piperidinil)-4-(kondenzált imidazolil)-piperidin-származékok, előállításuk és alkalmazásuk

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Publication number
HUP9903948A2
HUP9903948A2 HU9903948A HUP9903948A HUP9903948A2 HU P9903948 A2 HUP9903948 A2 HU P9903948A2 HU 9903948 A HU9903948 A HU 9903948A HU P9903948 A HUP9903948 A HU P9903948A HU P9903948 A2 HUP9903948 A2 HU P9903948A2
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Hungary
Prior art keywords
alkyl
pipe powder
tachikinin
antagonists
preparation
Prior art date
Application number
HU9903948A
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English (en)
Inventor
Frans Eduard Janssens
Joseph Elisabeth Leenaerts
Yves Emiel Maria Van Roosbroeck
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Janssen Pharmaceutica N.V.
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Publication date
Application filed by Janssen Pharmaceutica N.V. filed Critical Janssen Pharmaceutica N.V.
Publication of HUP9903948A2 publication Critical patent/HUP9903948A2/hu
Publication of HUP9903948A3 publication Critical patent/HUP9903948A3/hu
Publication of HU229766B1 publication Critical patent/HU229766B1/hu

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14Ortho-condensed systems
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    • 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/20Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • 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
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00Anaesthetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • AHUMAN NECESSITIES
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
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  • Virology (AREA)
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  • Molecular Biology (AREA)
  • Immunology (AREA)
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  • Pain & Pain Management (AREA)
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  • Biomedical Technology (AREA)
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  • Anesthesiology (AREA)
  • Urology & Nephrology (AREA)
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  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Biotechnology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

A cím szerinti vegyületek (I) általánős képletében n értéke 0, 1 vagy, m értéke 1 vagy 2, azzal a megkötésel, hőgy ha m értéke 2, akkőr nértéke 1, =Q jelentése =Q vagy =NR3, X jelentése kővalens kötés, -O-, -S- vagy -NR3-, R1 jelentése Ar1-, Ar1-(1-6 szénatőmős alkil)- vagy di(Ar1)-(1-6szénatőmős alkil)-csőpőrt, ahől az 1-6 szénatőmős alkilcsőpőrtők adőttesetben szűbsztitűálva lehetnek, R2 jelentése Ar2-, Ar2-(1-6 szénatőmős alkil)-, Het- vagy Het-(1-6szénatőmős alkil)-csőpőrt, R3 jelentése hidrőgénatőm vagy 1-6 szénatőmős alkilcsőpőrt, L jelentése (a-1) vagy (a-2) általánős képletű csőpőrt, és Ar1 jelentése adőtt esetben szűbsztitűált fenilcsőpőrt, Ar2 jelentése naftilcsőpőrt vagy adőtt esetben szűbsztitűáltfenilcsőpőrt, és Het jelentése adőtt esetben szűbsztitűált, egy- vagy kétgyűrűsheterőciklűsős csőpőrt. A vegyületek közelebbről gyógyszerkészítményeknem peptid jellegű P-anyag antagőnista hatóanyagaként alkalmazhatók. ŕ
HU9903948 1995-12-27 1996-12-20 1-(1,2-diszubsztituált piperidinil)-4-(kondenzált imidazolil)-piperidin-származékok HU229766B1 (hu)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP95203652 1995-12-27
PCT/EP1996/005885 WO1997024356A1 (en) 1995-12-27 1996-12-20 1-(1,2-disubstituted piperidinyl)-4-(fused imidazole)-piperidine derivatives

Publications (3)

Publication Number Publication Date
HUP9903948A2 true HUP9903948A2 (hu) 2000-03-28
HUP9903948A3 HUP9903948A3 (hu) 2000-04-28
HU229766B1 HU229766B1 (hu) 2014-06-30

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HU9903948 HU229766B1 (hu) 1995-12-27 1996-12-20 1-(1,2-diszubsztituált piperidinil)-4-(kondenzált imidazolil)-piperidin-származékok

Country Status (30)

Country Link
US (1) US6251894B1 (hu)
EP (1) EP0843679B1 (hu)
JP (1) JP4097043B2 (hu)
KR (1) KR100485147B1 (hu)
CN (1) CN1066733C (hu)
AR (2) AR005278A1 (hu)
AT (1) ATE208392T1 (hu)
AU (1) AU716071B2 (hu)
BR (1) BR9612307A (hu)
CA (1) CA2238817C (hu)
CY (1) CY2271B1 (hu)
CZ (1) CZ295861B6 (hu)
DE (1) DE69616802T2 (hu)
DK (1) DK0843679T3 (hu)
EA (1) EA001374B1 (hu)
ES (1) ES2167619T3 (hu)
HK (1) HK1011206A1 (hu)
HU (1) HU229766B1 (hu)
IL (2) IL124642A (hu)
MY (1) MY117680A (hu)
NO (1) NO310916B1 (hu)
NZ (1) NZ325845A (hu)
PL (1) PL183767B1 (hu)
PT (1) PT843679E (hu)
SI (1) SI0843679T1 (hu)
SK (1) SK283540B6 (hu)
TR (1) TR199801210T2 (hu)
TW (1) TW382017B (hu)
WO (1) WO1997024356A1 (hu)
ZA (1) ZA9610889B (hu)

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TW527186B (en) 1996-03-19 2003-04-11 Janssen Pharmaceutica Nv Fused imidazole derivatives as multidrug resistance modulators
AU1146099A (en) * 1997-09-18 1999-04-05 Janssen Pharmaceutica N.V. Fused imidazole derivatives for improving oral bioavailability of pharmaceuticalagents
SI1144411T1 (en) * 1998-12-19 2005-10-31 Janssen Pharmaceutica N.V. Antihistaminic spiro compounds
WO2001030348A1 (en) * 1999-10-25 2001-05-03 Janssen Pharmaceutica N.V. Use of substance p antagonists for influencing the circadian timing system
EP1401838B1 (en) 2001-06-12 2014-03-26 Janssen Pharmaceutica NV Novel substituted tetracyclic imidazole derivatives, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine
US20030083345A1 (en) * 2001-07-10 2003-05-01 Torsten Hoffmann Method of treatment and/or prevention of brain, spinal or nerve injury
CN100379744C (zh) * 2001-11-23 2008-04-09 詹森药业有限公司 抗组胺药快速降低高颅内压的用途
AU2002354104A1 (en) 2001-12-10 2003-06-23 Kyorin Pharmaceutical Co., Ltd. Fused bicyclic pyridine derivatives as tachykinin receptor antagonists
RU2301806C2 (ru) * 2002-01-16 2007-06-27 Янссен Фармацевтика Н.В. Прукалоприд-n-оксид
EP1473295B1 (en) * 2002-01-18 2009-04-01 Kyorin Pharmaceutical Co., Ltd. Fused bicyclic pyrimidine derivatives
US7026309B2 (en) 2002-03-26 2006-04-11 Kyorin Pharmaceutical Co., Ltd. Fused bicyclic pyridine derivative as tachykinin receptor antagonist
JO2696B1 (en) 2002-12-23 2013-03-03 شركة جانسين فارماسوتيكا ان. في Derivatives of 1-piperdine-4-yl-4-biprolidine-3-yl-piperazine substituted and used as quinine antagonists
ES2310260T3 (es) * 2002-12-23 2009-01-01 Janssen Pharmaceutica Nv Derivados sustituidos de 4-(4-piperidin-4-il-piperazin-1-il)-azepan y su uso como antagonistas de la neuroquinina.
JO2676B1 (en) 2004-04-06 2012-06-17 جانسين فارماسوتيكا ان. في Derivatives of second-aza-spiro- (5,4) -dikan and their use as antihistamines
JO2525B1 (en) * 2004-04-08 2010-03-17 شركة جانسين فارماسوتيكا ان. في Derived 4-alkyl-and-4-canoelperidine derivatives and their use as anti-neroquin
BRPI0608074A2 (pt) 2005-03-03 2009-11-03 Janssen Pharmaceutica Nv derivados de oxa-diaza-espiro-[5.5]-undecanona substituìdos e uso como antagonistas da neurocinina do mesmo
ATE478075T1 (de) 2005-03-08 2010-09-15 Janssen Pharmaceutica Nv Diazaspiro-ä4,4ü-nonanderivate als neurokinin- (nk1)-antagonisten
AU2008278273A1 (en) * 2007-07-19 2009-01-22 Adelaide Research & Innovation Pty Ltd Method for reducing intracranial pressure
UA105182C2 (ru) 2008-07-03 2014-04-25 Ньюрексон, Інк. Бензоксазины, бензотиазины и родственные соединения, которые имеют ингибирующую nos активность
US9782397B2 (en) 2011-07-04 2017-10-10 Irbm Science Park S.P.A. Treatment of corneal neovascularization
CN111918647A (zh) 2018-02-26 2020-11-10 圣拉斐尔医院有限公司 用于治疗眼痛的nk-1拮抗剂
US20230134843A1 (en) 2020-03-11 2023-05-04 Ospedale San Raffaele S.R.L. Treatment of stem cell deficiency

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US4329353A (en) 1980-10-22 1982-05-11 Janssen Pharmaceutica, N.V. 1-(4-Aryl-cyclohexyl)piperidine derivatives, method of use thereof and pharmaceutical compositions thereof
EP0552292B1 (en) * 1990-10-10 1995-06-21 Schering Corporation Substituted imidazobenzazepines and imidazopyridoazepines
IL101851A (en) * 1991-06-13 1996-05-14 Janssen Pharmaceutica Nv History 01 -) 4 - Pipridinyl - and Pipridinylidene (- Imidazo] A-1,2 [Pirolo, Thiano or Purano (] 3,2 [Azpin, their preparation and pharmaceutical preparations containing them and composition
IL101850A (en) * 1991-06-13 1996-01-31 Janssen Pharmaceutica Nv History 11-) 4-Pipridinyl (-Imidazo] B-1, 2 [] 3 [Benzazepine, their preparation and pharmaceutical preparations containing them
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NZ321575A (en) 1995-10-30 1999-05-28 Janssen Pharmaceutica Nv 1-(1,2-disubstituted piperidinyl)-4- substituted piperazine derivatives

Also Published As

Publication number Publication date
EA001374B1 (ru) 2001-02-26
DK0843679T3 (da) 2002-02-25
HUP9903948A3 (hu) 2000-04-28
IL124641A (en) 2001-11-25
NO982405L (no) 1998-08-19
DE69616802T2 (de) 2002-07-04
CZ295861B6 (cs) 2005-11-16
CN1206417A (zh) 1999-01-27
US6251894B1 (en) 2001-06-26
AR005278A1 (es) 1999-04-28
EP0843679B1 (en) 2001-11-07
DE69616802D1 (de) 2001-12-13
CA2238817C (en) 2006-10-17
EP0843679A1 (en) 1998-05-27
AU1308697A (en) 1997-07-28
PL327136A1 (en) 1998-11-23
AU716071B2 (en) 2000-02-17
ES2167619T3 (es) 2002-05-16
CZ186598A3 (cs) 1998-11-11
MY117680A (en) 2004-07-31
JP2000506503A (ja) 2000-05-30
ZA9610889B (en) 1998-06-23
PL183767B1 (pl) 2002-07-31
IL124642A0 (en) 1998-12-06
TW382017B (en) 2000-02-11
IL124642A (en) 2002-08-14
KR19990076715A (ko) 1999-10-15
HK1011206A1 (en) 1999-07-09
ATE208392T1 (de) 2001-11-15
CA2238817A1 (en) 1997-07-10
JP4097043B2 (ja) 2008-06-04
CY2271B1 (en) 2003-07-04
SK283540B6 (sk) 2003-09-11
NZ325845A (en) 1999-06-29
AR051817A2 (es) 2007-02-14
SK83098A3 (en) 1999-01-11
TR199801210T2 (xx) 1999-10-21
KR100485147B1 (ko) 2005-09-13
BR9612307A (pt) 1999-07-13
NO982405D0 (no) 1998-05-27
PT843679E (pt) 2002-04-29
SI0843679T1 (en) 2002-06-30
NO310916B1 (no) 2001-09-17
EA199800603A1 (ru) 1998-12-24
IL124641A0 (en) 1998-12-06
HU229766B1 (hu) 2014-06-30
WO1997024356A1 (en) 1997-07-10
CN1066733C (zh) 2001-06-06

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