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AR060840A1 - Moduladores bencimidazolicos de vr1 - Google Patents

Moduladores bencimidazolicos de vr1

Info

Publication number
AR060840A1
AR060840A1 ARP070101901A ARP070101901A AR060840A1 AR 060840 A1 AR060840 A1 AR 060840A1 AR P070101901 A ARP070101901 A AR P070101901A AR P070101901 A ARP070101901 A AR P070101901A AR 060840 A1 AR060840 A1 AR 060840A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
cycloalkyl
amino
aminocarbonylamino
Prior art date
Application number
ARP070101901A
Other languages
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 AR060840A1 publication Critical patent/AR060840A1/es

Links

Classifications

    • 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
    • C07D235/08Radicals containing only hydrogen and carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

La invencion se refiere a compuestos de bencimidazol moduladores del VR1 a composiciones farmacéuticas que contienen tales compuestos y a un proceso de preparacion del compuesto. Estos compuestos son utiles para el tratamiento de la ansiedad, trastornos de pánico, respuestas de no adaptacion al estrés y dolor cronico. Reivindicacion 1: Un compuesto de formula (1) y una forma del mismo donde: las líneas punteadas entre las posiciones 1, 2 y 3 de la Formula (1) indican las posiciones de un doble enlace tautomerico, donde cuando se forma un doble enlace entre las posiciones 1 y 2, entonces R3b está presente y donde, cuando se forma un doble enlace entre las posiciones 2 y 3, entonces R3a está presente; p es 1 o 2; q es 0 o 1; r es 0, 1, 2 o 3; L es alquilo C1-3, alquenilo C2-3, alquinilo C2-3 o ciclopropilo; A1 se selecciona del grupo que consiste en fenilo, bifenilo, naftilo, piridinilo, quinolinil e indol; cada R1 se selecciona del grupo que consiste en hidroxi, ciano, halogeno, formilo, carboxi, alquilo, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, alquilcarbonilo C1-6, alcoxicarbonilo C1-6, alquiltio C1-6, alquilsulfonilo C1-6, cicloalquilo C3-8, cicloalquil C3-8-alquilo C1-4, cicloalquil C3-8-alcoxi C1-4, cicloalquilC3-8-oxígeno, amino, (alquil C1-6)1-2amino, (cicloalquil C3-8)1-2amino, (cicloalquil C3-8-alquil C1-4)1-2amino, aminocarbonilo, (alquil C1-6)1-2 aminocarbonilo, alquilcarbonilamino C1-6, alcoxicarbonilamino C1-6, aminocarbonilamino, (alquil C1-6)1-2 aminocarbonilamino, alquilsulfonilamino C1-6, alquilsulfinilamino C1-6, aminosulfonilo, (alquil C1-4)1-2 aminosulfonilo, aminosulfonilamino y (alquil C1-6)1-2 aminosulfonilamino, donde el alquilo está opcionalmente sustituido con alcoxi C1-8, amino, (alquil C1-4)1-2amino, alquilcarbonilamino C1-6, alcoxicarbonilamino C1-6, aminocarbonilamino, (alquil C1-6)1-2 aminocarbonilamino, alquilsulfonilamino C1-6, aminosulfonilamino, (alquil C1-6)1-2aminosulfonilamino, hidroxi y fenilo, donde el fenilo está opcionalmente sustituido con uno, dos o tres sustituyentes independientemente seleccionados del grupo que consiste en halogeno, ciano, nitro, alquilo C1-6, alcoxi C1-6, alquiltio C1-6 y alquilsulfonilo C1-6 y donde, cada caso de alquilo y alcoxi está opcionalmente perfluorado; R2 se selecciona del grupo que consiste en halogeno, alquilo C1-4, alcoxi C1-4, alquilsulfonilo C1-4, nitro, amino, (alquil C1-4)1-2 amino y ciano, donde, cada caso de alquilo y alcoxi está opcionalmente perfluorado; cada R3a y R3b se selecciona del grupo que consiste en hidrogeno y alquilo C1-4 opcionalmente perfluorado; y cada R4 se selecciona del grupo que consiste en halogeno, nitro, ciano, carboxi, alquilo C1-6, alcoxi C1-6, haloalquilo C1-6, haloalcoxi C1-6, alcoxi C1-6 -alquilo C1-6, alquilcarbonilo C1-6, alquiltio C1-6, haloalquiltio C1-6, alquilsulfonilo C1-6, haloalquilsulfonilo C1-6, cicloalquilo C3-8, cicloalquil C3-8-alquilo C1-4, cicloalquil C3-8-alcoxi C1-4, cicloalquil C3-8-oxígeno, amino, (alquil C1-6)1-2amino, (cicloalquil C3-8)1-2amino, (cicloalquil-C3-8-alquil C3-8)1-2 amino, aminocarbonilo, (alquil C1-6)1-2 aminocarbonilo, alquilcarbonilamino C1-6, alcoxicarbonilamino C1-6, aminocarbonilamino, (alquil C1-6)1-2 aminocarbonilamino, alquilsulfonilamino C1-6, haloalquilsulfonilamino C1-6, alquilsulfinilamino C1-6, aminosulfonilo y (alquil C1-4)1-2 aminosulfonilo, donde cada caso de alquilo está opcionalmente sustituido con uno, dos o tres sustituyentes independientemente seleccionados del grupo que consiste en alcoxi C1-8, amino, (alquil C1-4)1-2 amino, alquilcarbonilamino C1-6, alcoxicarbonilamino C1-6, aminocarbonilamino, (alquil C1-6)1-2 aminocarbonilamino, alquilsulfonilamino C1- 6, oxo e hidroxi y donde, cada caso de alquilo y alcoxi está opcionalmente perfluorado.
ARP070101901A 2006-05-03 2007-05-02 Moduladores bencimidazolicos de vr1 AR060840A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US79750406P 2006-05-03 2006-05-03

Publications (1)

Publication Number Publication Date
AR060840A1 true AR060840A1 (es) 2008-07-16

Family

ID=38566108

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070101901A AR060840A1 (es) 2006-05-03 2007-05-02 Moduladores bencimidazolicos de vr1

Country Status (36)

Country Link
US (3) US7951829B2 (es)
EP (1) EP2021330B1 (es)
JP (1) JP5302884B2 (es)
KR (1) KR101434883B1 (es)
CN (1) CN101511797B (es)
AR (1) AR060840A1 (es)
AT (1) ATE482201T1 (es)
AU (1) AU2007248341C1 (es)
BR (1) BRPI0709803B8 (es)
CA (1) CA2651128C (es)
CO (1) CO6160329A2 (es)
CR (1) CR10479A (es)
CY (1) CY1111269T1 (es)
DE (1) DE602007009378D1 (es)
DK (1) DK2021330T3 (es)
EA (1) EA019386B1 (es)
EC (1) ECSP088854A (es)
ES (1) ES2350959T3 (es)
HR (1) HRP20100700T1 (es)
IL (1) IL194916A (es)
JO (1) JO3602B1 (es)
MX (1) MX2008014108A (es)
MY (1) MY154595A (es)
NI (1) NI200800290A (es)
NO (1) NO341965B1 (es)
NZ (1) NZ572251A (es)
PE (1) PE20080065A1 (es)
PL (1) PL2021330T3 (es)
PT (1) PT2021330E (es)
RS (1) RS51473B (es)
SI (1) SI2021330T1 (es)
TW (1) TWI419882B (es)
UA (1) UA94749C2 (es)
UY (1) UY30322A1 (es)
WO (1) WO2007130780A2 (es)
ZA (1) ZA200810234B (es)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2551709T3 (es) * 2006-12-15 2015-11-23 Janssen Pharmaceutica, N.V. Inhibidores Bencimidazola TRPV1
US20090092574A1 (en) 2006-12-29 2009-04-09 Scott Richard W Ophthalmic And Otic Compositions Of Facially Amphiphilic Polymers And Oligomers And Uses Thereof
US20090156598A1 (en) * 2007-12-17 2009-06-18 Lebsack Alec D Imidazolopyrimidine modulators of TRPV1
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KR101252334B1 (ko) * 2008-04-18 2013-04-08 주식회사 대웅제약 신규 벤조옥사진 벤즈이미다졸 유도체, 이를 포함하는 약학 조성물 및 이의 용도
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US8217060B2 (en) 2009-05-15 2012-07-10 Janssen Pharmaceutica, Nv Benzimidazole derivatives useful as TRP M8 receptor modulators
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CN102002010A (zh) * 2009-08-31 2011-04-06 住友化学株式会社 双噁唑啉基烷烃化合物的精制方法
MX2013013330A (es) * 2011-05-16 2014-07-09 Cellceutix Corp Compuestos para utilizar en el tratamiento de mucositis.
US9056874B2 (en) 2012-05-04 2015-06-16 Novartis Ag Complement pathway modulators and uses thereof
CN105229003B (zh) 2013-03-14 2017-03-15 诺华股份有限公司 作为补体因子b抑制剂用于治疗眼科疾病的2‑(1h‑吲哚‑4‑基甲基)‑3h‑咪唑并[4,5‑b]吡啶‑6‑甲腈衍生物
CA2917964A1 (en) * 2013-07-11 2015-01-15 Bristol-Myers Squibb Company Ido inhibitors
US9676728B2 (en) 2013-10-30 2017-06-13 Novartis Ag 2-benzyl-benzimidazole complement factor B inhibitors and uses thereof
JP6705458B2 (ja) * 2015-09-08 2020-06-03 住友化学株式会社 トリアゾール化合物の製造方法
US10870630B2 (en) 2016-11-01 2020-12-22 Merck Sharp & Dohme Corp. Substituted bicyclic heteroaryl allosteric modulators of nicotinic acetylcholine receptors
AU2019262169B2 (en) * 2018-05-03 2024-05-02 Jiangsu Hengrui Medicine Co., Ltd. Benzimidazole derivatives as modulators of retinoid-related orphan receptor gamma (RORy) and pharmaceutical uses thereof
CN108997398B (zh) * 2018-07-23 2020-12-15 被忽略疾病药物研发组织 一种3,3-二甲基苯并[c][1,2]氧杂戊硼烷-1(3h)-醇的制备方法
CN112745268B (zh) * 2019-10-31 2022-09-16 江苏恒瑞医药股份有限公司 苯并咪唑衍生物的晶型及制备方法
US20220411380A1 (en) * 2019-10-31 2022-12-29 Jiangsu Hengrui Medicine Co., Ltd. ACID ADDITION SALT OF RORy REGULATOR
WO2021248008A1 (en) 2020-06-05 2021-12-09 Innovation Pharmaceuticals Inc. Arylamide compounds for treatment and prevention of viral infections

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US5612360A (en) * 1992-06-03 1997-03-18 Eli Lilly And Company Angiotensin II antagonists
US6299796B1 (en) 1997-12-18 2001-10-09 Fuji Photo Film Co., Ltd. Styryl compound, method for the preparation thereof and electroluminescent element employing the same
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SI1660492T1 (sl) * 2003-07-28 2009-02-28 Janssen Pharmaceutica Nv Benzimidazolni, benztiazolni in benzoksazolni derivati in njihova uporaba kot modulatorji LTA4H
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BRPI0714199A2 (pt) * 2006-07-04 2012-12-25 Janssen Pharmaceutica Nv agonistas de canabinàide de benzimidazol que transportam um grupo heterocÍclico substituÍdo
ES2551709T3 (es) * 2006-12-15 2015-11-23 Janssen Pharmaceutica, N.V. Inhibidores Bencimidazola TRPV1

Also Published As

Publication number Publication date
NI200800290A (es) 2012-01-30
JP2009535414A (ja) 2009-10-01
HK1131971A1 (en) 2010-02-12
EP2021330A2 (en) 2009-02-11
RS51473B (sr) 2011-04-30
CA2651128C (en) 2014-09-02
AU2007248341B2 (en) 2011-12-08
PT2021330E (pt) 2010-12-03
US20110190344A1 (en) 2011-08-04
NZ572251A (en) 2010-08-27
NO341965B1 (no) 2018-03-05
UY30322A1 (es) 2007-08-31
BRPI0709803B1 (pt) 2019-12-10
NO20085031L (no) 2009-01-06
UA94749C2 (en) 2011-06-10
SI2021330T1 (sl) 2011-01-31
JP5302884B2 (ja) 2013-10-02
IL194916A (en) 2013-01-31
PL2021330T3 (pl) 2011-03-31
US20110190364A1 (en) 2011-08-04
JO3602B1 (ar) 2020-07-05
KR101434883B1 (ko) 2014-08-27
BRPI0709803A2 (pt) 2011-07-26
CY1111269T1 (el) 2015-08-05
HRP20100700T1 (hr) 2011-02-28
ATE482201T1 (de) 2010-10-15
PE20080065A1 (es) 2008-02-25
CA2651128A1 (en) 2007-11-15
ZA200810234B (en) 2010-02-24
DK2021330T3 (da) 2010-12-06
MX2008014108A (es) 2008-11-14
CN101511797B (zh) 2013-01-02
KR20090008428A (ko) 2009-01-21
TWI419882B (zh) 2013-12-21
AU2007248341C1 (en) 2013-01-17
ECSP088854A (es) 2008-11-27
US20070259936A1 (en) 2007-11-08
EP2021330B1 (en) 2010-09-22
WO2007130780A3 (en) 2008-02-14
CO6160329A2 (es) 2010-05-20
AU2007248341A1 (en) 2007-11-15
EA019386B1 (ru) 2014-03-31
DE602007009378D1 (de) 2010-11-04
CR10479A (es) 2009-03-31
IL194916A0 (en) 2009-08-03
TW200808738A (en) 2008-02-16
BRPI0709803B8 (pt) 2021-05-25
MY154595A (en) 2015-06-30
WO2007130780A2 (en) 2007-11-15
CN101511797A (zh) 2009-08-19
EA200870497A1 (ru) 2009-06-30
US7951829B2 (en) 2011-05-31
ES2350959T3 (es) 2011-01-28

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