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AR077055A1 - Derivados de benzimidazol como moduladores del canal trpm8 - Google Patents

Derivados de benzimidazol como moduladores del canal trpm8

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Publication number
AR077055A1
AR077055A1 ARP100102053A ARP100102053A AR077055A1 AR 077055 A1 AR077055 A1 AR 077055A1 AR P100102053 A ARP100102053 A AR P100102053A AR P100102053 A ARP100102053 A AR P100102053A AR 077055 A1 AR077055 A1 AR 077055A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
group
heterocycloalkyl
heteroaryl
cycloalkyl
Prior art date
Application number
ARP100102053A
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 AR077055A1 publication Critical patent/AR077055A1/es

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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
    • C07D235/24Benzimidazoles; 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
    • C07D235/30Nitrogen atoms not forming part of a nitro radical
    • 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
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • 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
    • A61P21/00Drugs for disorders of the muscular or neuromuscular 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/06Antimigraine agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • 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
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/06Peri-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Otolaryngology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Se describen los compuestos, composiciones y métodos para tratar diferentes enfermedades, síndromes, afecciones y trastornos que incluyen el dolor. Reivindicacion 1: Un compuesto de la formula (1) en donde a es un numero entero de 0 a 3; cada R0 se selecciona independientemente del grupo que consiste de halogeno, hidroxi, ciano, alquilo inferior, alquilo inferior fluorado, alcoxi inferior y alcoxi inferior fluorado; R2 se selecciona del grupo que consiste de hidrogeno, halogeno, hidroxi, ciano, alquilo inferior, alquilo inferior fluorado, alcoxi inferior y alcoxi inferior fluorado; R1 se selecciona del grupo que consiste de alquilo, alquilo inferior sustituido con hidroxi, alquilo inferior halogenado, cicloalquilo-(alquilo inferior) y fenilo-(alquilo inferior); alternativamente, R2 y R1 se toman juntos como en restos (2) o (3); R3 se selecciona del grupo que consiste de alquilo inferior, cicloalquilo, arilo, heteroarilo, heterocicloalquilo, cicloalquilo-(alquilo inferior), arilo-(alquilo inferior), heteroarilo-(alquilo inferior) y heterocicloalquilo-(alquilo inferior); en donde el cicloalquilo, arilo, heteroarilo o heterocicloalquilo, ya sea solo o como parte de un grupo sustituyente se sustituye opcionalmente con uno o más sustituyentes independientemente seleccionados del grupo que consiste de halogeno, alquilo inferior, alquilo inferior halogenado, alcoxi inferior, alcoxi inferior halogenado, -C(O)OH, -C(O)O-(alquilo inferior) y -C(O)NRARB; en donde RA y RB se seleccionan independientemente del grupo que consiste de hidrogeno y alquilo inferior; alternativamente RA y RB se toman juntos con el átomo de nitrogeno al cual están unidos para formar una estructura de anillo que contiene nitrogeno saturado de 5 a 6 miembros; R4 se selecciona del grupo que consiste de alquilo inferior, cicloalquilo, arilo, heteroarilo, heterocicloalquilo, cicloalquilo-(alquilo inferior), arilo-(alquilo inferior), heteroarilo-(alquilo inferior) y heterocicloalquilo-(alquilo inferior); en donde el cicloalquilo, arilo, heteroarilo o heterocicloalquilo, ya sea solo o como parte de un grupo sustituyente se sustituye opcionalmente con uno o más sustituyentes independientemente seleccionados del grupo que consiste de halogeno, alquilo inferior, alquilo inferior halogenado, alcoxi inferior, alcoxi inferior halogenado y -S-CF3; siempre y cuando R4 sea heteroarilo o heterocicloalquilo, entonces el grupo R4 está unido al N del compuesto de la formula (1) a través de un átomo de carbono; o una sal farmacéuticamente aceptable de éstos.
ARP100102053A 2009-06-10 2010-06-10 Derivados de benzimidazol como moduladores del canal trpm8 AR077055A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US18568609P 2009-06-10 2009-06-10

Publications (1)

Publication Number Publication Date
AR077055A1 true AR077055A1 (es) 2011-07-27

Family

ID=42670634

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100102053A AR077055A1 (es) 2009-06-10 2010-06-10 Derivados de benzimidazol como moduladores del canal trpm8

Country Status (10)

Country Link
US (1) US8242157B2 (es)
EP (1) EP2440294B1 (es)
JP (1) JP2012530053A (es)
CN (1) CN102802731A (es)
AR (1) AR077055A1 (es)
AU (1) AU2010258714B2 (es)
CA (1) CA2764567A1 (es)
RU (1) RU2011153431A (es)
TW (1) TW201103941A (es)
WO (1) WO2010144680A1 (es)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001098344A2 (en) * 2000-06-16 2001-12-27 Curis, Inc. Angiogenesis-modulating compositions and uses
CN103354812A (zh) 2010-12-09 2013-10-16 詹森药业有限公司 作为trpm8调节剂的咪唑并[1,2-a]吡啶磺酰胺
WO2012098281A2 (es) 2011-01-19 2012-07-26 Universidad Miguel Hernández De Elche Péptidos moduladores de receptores trp y sus usos
CN103443080B (zh) 2011-03-16 2016-10-12 田边三菱制药株式会社 具有trpm8拮抗活性的磺酰胺化合物
MY157429A (en) * 2011-06-24 2016-06-15 Amgen Inc Trpm8 antagonists and their use in treatments
EP2896613B1 (en) * 2012-09-14 2018-03-21 Mitsubishi Tanabe Pharma Corporation Sulfonamide compound
JP5985453B2 (ja) * 2012-09-14 2016-09-06 田辺三菱製薬株式会社 医薬組成物
WO2014143768A1 (en) 2013-03-15 2014-09-18 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
ES2635560T3 (es) 2013-07-08 2017-10-04 Incyte Holdings Corporation Heterociclos tricíclicos como inhibidores de la proteína NET
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
ES2942723T3 (es) 2014-04-23 2023-06-06 Incyte Holdings Corp 1H-pirrolo[2,3-C]piridin-7(6H)-onas y pirazolo[3,4-C]piridin-7(6H)-onas como inhibidores de proteínas BET
ES2855225T3 (es) 2014-09-15 2021-09-23 Incyte Corp Heterociclos tricíclicos para su uso como inhibidores de proteínas BET
WO2017075377A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
CN114748624A (zh) 2016-06-13 2022-07-15 田边三菱制药株式会社 用于治疗或预防血管舒缩症状的组合物
KR20250163425A (ko) 2016-06-20 2025-11-20 인사이트 코포레이션 Bet 저해제의 결정질 고체 형태
WO2020038387A1 (zh) * 2018-08-24 2020-02-27 杭州阿诺生物医药科技有限公司 高活性sting蛋白激动剂
CA3110474C (en) * 2018-08-29 2024-04-23 Adlai Nortye Biopharma Co., Ltd. Highly active sting protein agonist compound
WO2020132566A1 (en) * 2018-12-21 2020-06-25 Nimbus Titan, Inc. Sting pyrazole agonists and uses thereof
WO2020151682A1 (zh) * 2019-01-23 2020-07-30 成都先导药物开发股份有限公司 一种大环类免疫调节剂
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007134107A2 (en) * 2006-05-10 2007-11-22 Janssen Pharmaceutica N.V. Cold menthol receptor-1 antagonists
US20080287398A1 (en) * 2007-05-02 2008-11-20 Colburn Raymond W Cold menthol receptor-1 antagonists
PA8790401A1 (es) 2007-07-18 2009-03-31 Janssen Pharmaceutica Nv Sulfonamidas como moduladores de trpm8

Also Published As

Publication number Publication date
EP2440294B1 (en) 2013-07-24
US8242157B2 (en) 2012-08-14
WO2010144680A1 (en) 2010-12-16
TW201103941A (en) 2011-02-01
AU2010258714B2 (en) 2014-09-11
EP2440294A1 (en) 2012-04-18
US20110003801A1 (en) 2011-01-06
AU2010258714A1 (en) 2012-01-12
RU2011153431A (ru) 2013-07-20
JP2012530053A (ja) 2012-11-29
HK1169070A1 (en) 2013-01-18
CA2764567A1 (en) 2010-12-16
CN102802731A (zh) 2012-11-28

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