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AR005278A1 - Derivados de 1- (piperidinil 1,2 - disustituido) -4- (imidazol fusionado) -piperidina, proceso para la preparación de los mismos, composición farmacéutica que los contiene y proceso para la preparación de dicha composición. - Google Patents

Derivados de 1- (piperidinil 1,2 - disustituido) -4- (imidazol fusionado) -piperidina, proceso para la preparación de los mismos, composición farmacéutica que los contiene y proceso para la preparación de dicha composición.

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Publication number
AR005278A1
AR005278A1 ARP960105895A ARP960105895A AR005278A1 AR 005278 A1 AR005278 A1 AR 005278A1 AR P960105895 A ARP960105895 A AR P960105895A AR P960105895 A ARP960105895 A AR P960105895A AR 005278 A1 AR005278 A1 AR 005278A1
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AR
Argentina
Prior art keywords
formula
alkyl
radical
preparation
hydrogen
Prior art date
Application number
ARP960105895A
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English (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
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR005278A1 publication Critical patent/AR005278A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic 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
    • C07D487/14—Ortho-condensed systems
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/20—Spiro-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • 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
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
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    • A61P37/08—Antiallergic agents
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    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic 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
    • C07D495/14—Ortho-condensed systems

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  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Se describen derivados 1-(piperidinil 1,2-disustituido)-4- (imidazolfusionado)-piperidina, que comprende un compuesto de la fórmula (I),en forma N-óxido, una sal de adición farmacéuticamente aceptable o una forma estereoquímicamen te isomérica delmismo, donde n es 0,1o 2; m es 1 o 2, siempreque si m es 2, n sea 1; =Q es =O o =NR3; X es un enlace covalente o un radical bivalente de la fórmula -O-, -S-, NR3-; R1 es Ar1.Ar1 alquilo C1-6 o di(Ar1)alquilo C1-6, donde cada grupo a lquilo C1-C6está optaitvamentte sustituido con hidroxi, alquilox C1-C4, oxo o un sustituyente oxo cetalizado de lafórmula -O-CH2-CH2-O o -O-CH2-CH2-CH2-O-; R2 es Ar2, Ar2 alquilo C1-6, Het o Het alquilo C1-6; R3 es hidrógeno o alquilo C1-C6; L es un radicalde lafórmula (a-1) o (a2),en la cual la línea de puntos es un enlace optativo; cada -A-B es, independientemente, un radical bivalente de la fórmula: Y-CR7=CH-(b-1); -CH=CR7-Y (b-2); -CH=CH-CH=CH- (b-3); -CH=CR7-CH=CH- (b-4); -CH=CH-CR7=CH- (b-5); o-CH=CH-CH=CR7 (b-6) en el cual cada Y esindependientemente , alquilo C1-6, halo, etenilo sustituido con carboxilo o alquiloxicarbonilo C1-C6, hidroxialquilo C1-C6; o R7 es hidrógeno en el casoque -A-B- es un radical de fórmula (b-1)o (b-2); R8 eshidrógeno, alquilo C1-C6 o alquilcarbonilo C1-C6; cada Z es, independientemente, Z1 o Z2; dondeZ1 es un radical bivalente de la fórmula -CH2-, -CH2-CH2-,o -CH=Ch-, siempre que cuando L es un radical de la fórmu la (a-1) y la línea de puntos esunenlace adicional, Z1 no sea -CH2-; Z2 es un radical bivalente de la fórmula -CH2-CHOH, -CH2-O-, -CH2C(=O)- o -CH2-C(=NOH)-, siempre que la porción -CH2- dedichos radicales bivalentes esté conectada al nitrógeno del anillo de imidazol; cada R4 es,independientemente, hidrógeno, alquilo C1-C6, halo, etenilo
ARP960105895A 1995-12-27 1996-12-26 Derivados de 1- (piperidinil 1,2 - disustituido) -4- (imidazol fusionado) -piperidina, proceso para la preparación de los mismos, composición farmacéutica que los contiene y proceso para la preparación de dicha composición. AR005278A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP95203652 1995-12-27

Publications (1)

Publication Number Publication Date
AR005278A1 true AR005278A1 (es) 1999-04-28

Family

ID=8221024

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP960105895A AR005278A1 (es) 1995-12-27 1996-12-26 Derivados de 1- (piperidinil 1,2 - disustituido) -4- (imidazol fusionado) -piperidina, proceso para la preparación de los mismos, composición farmacéutica que los contiene y proceso para la preparación de dicha composición.
ARP050105316A AR051817A2 (es) 1995-12-27 2005-12-16 Derivados de piperidina-1-(1,2-piperidinil disustituidos)-4-(imidazol condensados)

Family Applications After (1)

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ARP050105316A AR051817A2 (es) 1995-12-27 2005-12-16 Derivados de piperidina-1-(1,2-piperidinil disustituidos)-4-(imidazol condensados)

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

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JP3775780B2 (ja) 1997-09-18 2006-05-17 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 薬剤の経口的バイオアベイラビリテイを向上させるための縮合イミダゾール誘導体
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JP4452496B2 (ja) 2001-06-12 2010-04-21 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 新規な置換四環式イミダゾール誘導体、それらの製造法、それらを含む製薬学的組成物及び薬剤としてのそれらの使用
US20030083345A1 (en) * 2001-07-10 2003-05-01 Torsten Hoffmann Method of treatment and/or prevention of brain, spinal or nerve injury
AU2002356715B2 (en) * 2001-11-23 2008-05-15 Janssen Pharmaceutica N.V. The use of anti-histaminics for acute reduction of elevated intracranial pressure
US7030107B2 (en) 2001-12-10 2006-04-18 Kyorin Pharmaceutical.Co., Ltd. Fused bicyclic pyridine derivatives as tachykinin receptor antagonists
CA2471729C (en) 2002-01-16 2010-03-23 Janssen Pharmaceutica N.V. Prucalopride-n-oxide
KR100887471B1 (ko) * 2002-01-18 2009-03-10 교린 세이야꾸 가부시키 가이샤 축합 바이사이클릭 피리미딘 유도체
CN1310922C (zh) * 2002-03-26 2007-04-18 杏林制药株式会社 作为速激肽受体拮抗剂的稠合双环吡啶衍生物
AU2003298369B2 (en) * 2002-12-23 2009-08-27 Janssen Pharmaceutica N.V. Substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives and their use as neurokinin antagonists
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
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
ATE469159T1 (de) 2005-03-03 2010-06-15 Janssen Pharmaceutica Nv Substituierte oxadiazaspiro-ä5.5ü- undecanonderivate und ihre verwendung als neurokininantagonisten
ES2350647T3 (es) 2005-03-08 2011-01-25 Janssen Pharmaceutica Nv Derivados de diaza-espiro-[4.4]-nonano como antagonistas de neuroquininas (nk1).
WO2009009829A1 (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
EP2729147B1 (en) 2011-07-04 2017-09-06 IRBM - Science Park S.p.A. Nk-1 receptor antagonists for treating corneal neovascularisation
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
WO2021180885A1 (en) 2020-03-11 2021-09-16 Ospedale San Raffaele S.R.L. Treatment of stem cell deficiency

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AU1308697A (en) 1997-07-28
JP2000506503A (ja) 2000-05-30
CA2238817C (en) 2006-10-17
CN1206417A (zh) 1999-01-27
HUP9903948A3 (hu) 2000-04-28
NO982405D0 (no) 1998-05-27
NO982405L (no) 1998-08-19
TW382017B (en) 2000-02-11
TR199801210T2 (xx) 1999-10-21
HU229766B1 (hu) 2014-06-30
IL124641A (en) 2001-11-25
CY2271B1 (en) 2003-07-04
BR9612307A (pt) 1999-07-13
ZA9610889B (en) 1998-06-23
SI0843679T1 (en) 2002-06-30
MY117680A (en) 2004-07-31
NZ325845A (en) 1999-06-29
PL327136A1 (en) 1998-11-23
CN1066733C (zh) 2001-06-06
IL124642A (en) 2002-08-14
IL124641A0 (en) 1998-12-06
HK1011206A1 (en) 1999-07-09
SK83098A3 (en) 1999-01-11
EA199800603A1 (ru) 1998-12-24
PL183767B1 (pl) 2002-07-31
DK0843679T3 (da) 2002-02-25
NO310916B1 (no) 2001-09-17
EP0843679A1 (en) 1998-05-27
ES2167619T3 (es) 2002-05-16
KR100485147B1 (ko) 2005-09-13
EA001374B1 (ru) 2001-02-26
PT843679E (pt) 2002-04-29
DE69616802T2 (de) 2002-07-04
CZ186598A3 (cs) 1998-11-11
DE69616802D1 (de) 2001-12-13
CZ295861B6 (cs) 2005-11-16
HUP9903948A2 (hu) 2000-03-28
US6251894B1 (en) 2001-06-26
AU716071B2 (en) 2000-02-17
KR19990076715A (ko) 1999-10-15
EP0843679B1 (en) 2001-11-07
SK283540B6 (sk) 2003-09-11
IL124642A0 (en) 1998-12-06
JP4097043B2 (ja) 2008-06-04
AR051817A2 (es) 2007-02-14
ATE208392T1 (de) 2001-11-15
CA2238817A1 (en) 1997-07-10
WO1997024356A1 (en) 1997-07-10

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