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AR088701A1 - CARBOXAMIDE AND UREA DERIVATIVES BASED ON PIRAZOLILO, SUBSTITUTED, CONTAINING A FENILE PORTION REPLACED WITH A GROUP CONTAINING N AS LIGANDOS OF THE VANILLOIDE RECEIVER - Google Patents

CARBOXAMIDE AND UREA DERIVATIVES BASED ON PIRAZOLILO, SUBSTITUTED, CONTAINING A FENILE PORTION REPLACED WITH A GROUP CONTAINING N AS LIGANDOS OF THE VANILLOIDE RECEIVER

Info

Publication number
AR088701A1
AR088701A1 ARP120104203A ARP120104203A AR088701A1 AR 088701 A1 AR088701 A1 AR 088701A1 AR P120104203 A ARP120104203 A AR P120104203A AR P120104203 A ARP120104203 A AR P120104203A AR 088701 A1 AR088701 A1 AR 088701A1
Authority
AR
Argentina
Prior art keywords
alkyl
substituted
group
vanilloide
pirazolilo
Prior art date
Application number
ARP120104203A
Other languages
Spanish (es)
Inventor
Kim Myeong
Seop-Prof Dr Lee Jeewoo
Stockhausen Hannelore
Kim Yong
Soo-Dr Damann Nils
Dr Bahrenberg Gregor
Dr Lesch Bernhard
Dr Frank Robert
John Dr Saunders Derek
Dr Christoph Thomas
Original Assignee
Gruenenthal Gmbh
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 Gruenenthal Gmbh filed Critical Gruenenthal Gmbh
Publication of AR088701A1 publication Critical patent/AR088701A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A61P1/04—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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • A61P23/02—Local anaesthetics
    • 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
    • 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
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Psychology (AREA)
  • Anesthesiology (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Otolaryngology (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)

Abstract

Composiciones farmacéuticas que contienen esos compuestos y también con esos compuestos para usarse en el tratamiento y/o profilaxis del dolor y enfermedades y/o trastornos adicionales. Reivindicación 1: Un compuesto de fórmula general (1), caracterizado porque R¹⁰¹, R¹⁰² y R¹⁰³ son, independientemente uno del otro, seleccionados del grupo que consiste de H, F, Cl, Br, CFH₂, CF₂H, CF₃, CN, CH₂-OH, CH₂CH₂-OH, CH₂-OCH₃, CH₂CH₂-OCH₃, OCFH₂, OCF₂H, OCF₃, OH, NH₂ , un alquilo C₁₋₄, un O-alquilo C₁₋₄, un NH-alquilo C₁₋₄, y un N(alquilo C₁₋₄)₂, donde el alquilo C₁₋₄ está en cada caso no sustituido; R² representa CF₃, un alquilo no sustituido C₁₋₄ ₐ ᵘₙ ᶜⁱᶜₗₒₐₗqᵘⁱₗₒ C₃₋₆ no sustituido; R⁷ y R⁹ son, independientemente uno del otro, seleccionados del grupo que consiste de H, F, Cl, Br, CFH₂, CF₂H, CF₃, CN, OH, OCF₃, un alquilo C₁₋₄, y un O-alquilo C₁₋₄, donde el alquilo C₁₋₄ está en cada caso no sustituido; A denota N, CH o C(CH₃); q denota 0, 1 ó 2; R¹¹² representa un H o un alquilo C₁₋₄, el cual no está sustituido o mono-, di- o trisustituido con 1, 2 ó 3 sustituyentes seleccionados del grupo que consiste de F, Cl, Br, OH, =O y OCH₃; R¹¹³ representa un H, S(=O)₂-NH₂, un alquilo C₁₋₄ o un S(=O)₂-alquilo C₁₋₄, donde el alquilo C₁₋₄ está en cada caso no sustituido o mono-, di- o trisustituido con 1, 2 ó 3 sustituyentes seleccionados del grupo que consiste de F, Cl, Br, OH, =O y OCH₃, o -con la condición de que q es &Pharmaceutical compositions containing those compounds and also with those compounds for use in the treatment and / or prophylaxis of pain and diseases and / or additional disorders. Claim 1: A compound of the general formula (1), characterized in that R¹⁰¹, R¹⁰² and R¹⁰³ are, independently of each other, selected from the group consisting of H, F, Cl, Br, CFH₂, CF₂H, CF₃, CN, CH₂- OH, CH₂CH₂-OH, CH₂-OCH₃, CH₂CH₂-OCH₃, OCFH₂, OCF₂H, OCF₃, OH, NH₂, a C₁₋₄ alkyl, an O-C₁₋₄ alkyl, an NH-C₁₋₄ alkyl, and an N ( C₁₋₄) ₂ alkyl, where the C₁₋₄ alkyl is in each case unsubstituted; R² represents CF₃, an unsubstituted C₁₋₄ ₐ ᵘₙ ᶜⁱᶜₗₒₐₗqᵘⁱₗₒ C₃₋₆ alkyl; R⁷ and R⁹ are, independently of each other, selected from the group consisting of H, F, Cl, Br, CFH₂, CF₂H, CF₃, CN, OH, OCF₃, a C₁₋₄ alkyl, and a C₁₋₄ O-alkyl , where the C₁₋₄ alkyl is in each case unsubstituted; A denotes N, CH or C (CH₃); q denotes 0, 1 or 2; R¹¹² represents an H or a C₁₋₄ alkyl, which is not substituted or mono-, di- or trisubstituted with 1, 2 or 3 substituents selected from the group consisting of F, Cl, Br, OH, = O and OCH₃; R¹¹³ represents an H, S (= O) ₂-NH₂, a C₁₋₄ alkyl or an S (= O) ₂-C alquilo alkyl, where the C₁₋₄ alkyl is in each case unsubstituted or mono-, di - or trisubstituted with 1, 2 or 3 substituents selected from the group consisting of F, Cl, Br, OH, = O and OCH₃, or - with the proviso that q is &

ARP120104203A 2011-11-09 2012-11-08 CARBOXAMIDE AND UREA DERIVATIVES BASED ON PIRAZOLILO, SUBSTITUTED, CONTAINING A FENILE PORTION REPLACED WITH A GROUP CONTAINING N AS LIGANDOS OF THE VANILLOIDE RECEIVER AR088701A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP11008913 2011-11-09

Publications (1)

Publication Number Publication Date
AR088701A1 true AR088701A1 (en) 2014-06-25

Family

ID=47143123

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120104203A AR088701A1 (en) 2011-11-09 2012-11-08 CARBOXAMIDE AND UREA DERIVATIVES BASED ON PIRAZOLILO, SUBSTITUTED, CONTAINING A FENILE PORTION REPLACED WITH A GROUP CONTAINING N AS LIGANDOS OF THE VANILLOIDE RECEIVER

Country Status (13)

Country Link
EP (1) EP2776399A1 (en)
JP (1) JP2014532742A (en)
KR (1) KR20140096351A (en)
CN (1) CN103906736A (en)
AR (1) AR088701A1 (en)
AU (1) AU2012334066A1 (en)
BR (1) BR112014010957A2 (en)
CA (1) CA2854935A1 (en)
HK (1) HK1202116A1 (en)
IN (1) IN2014KN00847A (en)
MX (1) MX2014005611A (en)
TW (1) TW201326134A (en)
WO (1) WO2013068462A1 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3224252B1 (en) 2014-11-24 2019-01-09 Medifron Dbt Inc. Substituted oxazole- and thiazole-based carboxamide and urea derivatives as vanilloid receptor ligands ii
CN114920697A (en) * 2022-05-16 2022-08-19 河南应用技术职业学院 Heterocyclic group substituted indan propionamide compound and application thereof

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1020447A4 (en) * 1997-09-11 2000-11-15 Nissan Chemical Ind Ltd Pyrazole compounds and plant disease control agent
EP1940821B1 (en) * 2005-10-19 2013-03-20 Grünenthal GmbH Novel vanilloid receptor ligands and their use for producing medicaments
WO2008073825A1 (en) * 2006-12-08 2008-06-19 Exelixis, Inc. Lxr and fxr modulators
DE102007018151A1 (en) * 2007-04-16 2008-10-23 Günenthal GmbH Novel vanilloid receptor ligands and their use in the preparation of medicines
CA2683461A1 (en) * 2007-04-16 2008-10-23 Gruenenthal Gmbh Novel vanilloid receptor ligands and the use thereof for the production of pharmaceuticals
ES2640257T3 (en) 2009-05-07 2017-11-02 Medifron Dbt Inc. Phenylureas and substituted phenylamides as vanilloid receptor ligands
US8334315B2 (en) 2009-05-07 2012-12-18 Gruenenthal Gmbh Substituted aromatic carboxamide and urea derivatives as vanilloid receptor ligands
EP2776424A1 (en) * 2011-11-09 2014-09-17 Grünenthal GmbH Substituted pyrazolyl-based carboxamide and urea derivatives bearing a phenyl moiety substituted with an n-cyclic group as vanilloid receptor ligands

Also Published As

Publication number Publication date
KR20140096351A (en) 2014-08-05
AU2012334066A1 (en) 2014-05-22
HK1202116A1 (en) 2015-09-18
WO2013068462A1 (en) 2013-05-16
CN103906736A (en) 2014-07-02
BR112014010957A2 (en) 2017-06-06
EP2776399A1 (en) 2014-09-17
CA2854935A1 (en) 2013-05-16
MX2014005611A (en) 2014-07-30
JP2014532742A (en) 2014-12-08
IN2014KN00847A (en) 2015-10-02
TW201326134A (en) 2013-07-01

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