BR112012022369A2 - Derivados azabicíclicos de imidazol substituídos úteis como moduladores do receptor trpm8 - Google Patents

Derivados azabicíclicos de imidazol substituídos úteis como moduladores do receptor trpm8

Info

Publication number
BR112012022369A2
BR112012022369A2 BR112012022369A BR112012022369A BR112012022369A2 BR 112012022369 A2 BR112012022369 A2 BR 112012022369A2 BR 112012022369 A BR112012022369 A BR 112012022369A BR 112012022369 A BR112012022369 A BR 112012022369A BR 112012022369 A2 BR112012022369 A2 BR 112012022369A2
Authority
BR
Brazil
Prior art keywords
inflammatory
imidazole derivatives
receptor modulators
derivatives useful
substituted azabicyclic
Prior art date
Application number
BR112012022369A
Other languages
English (en)
Inventor
Branum Shawn
Calvo Raul
Parks Daniel
Ballentine Scott
Meegalla Sanath
R Player Mark
Chen Jinsheng
Parsons William
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 BR112012022369A2 publication Critical patent/BR112012022369A2/pt

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    • 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
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/15—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing halogen
    • C07C53/16—Halogenated acetic acids
    • C07C53/18—Halogenated acetic acids containing fluorine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

DERIVADOS AZABICÍCLICOS DE IMIDAZOL SUBSTITUÍDOS ÚTEIS COMO MODULADORES DO RECEPTOR TRPM8. A presente invenção refere-se a um derivados azabicíclicos de imidazol substituídos, composições farmacêuticas contendo os mesmos e seu uso no tratamento de distúrbios e condições modulados por TRP M8, incluindo por exemplo, dor inflamatória, hiperalgesia inflamatória, condição de hipersensibilidade inflamatória, dor neuropática, alodinia neuropática ao frio, hiperalgesia inflamatória somática, hiperalgesia visceral inflamatório, doença cardiovascular agravada pelo frio e doença pulmonar agravada pelo frio.
BR112012022369A 2010-03-05 2011-03-03 Derivados azabicíclicos de imidazol substituídos úteis como moduladores do receptor trpm8 BR112012022369A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US31087010P 2010-03-05 2010-03-05
PCT/US2011/026974 WO2011109587A1 (en) 2010-03-05 2011-03-03 Substituted aza-bicyclic imidazole derivatives useful as trpm8 receptor modulators

Publications (1)

Publication Number Publication Date
BR112012022369A2 true BR112012022369A2 (pt) 2017-08-29

Family

ID=43875233

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012022369A BR112012022369A2 (pt) 2010-03-05 2011-03-03 Derivados azabicíclicos de imidazol substituídos úteis como moduladores do receptor trpm8

Country Status (16)

Country Link
US (4) US8680098B2 (pt)
EP (1) EP2542552B1 (pt)
JP (1) JP5782054B2 (pt)
KR (1) KR101667277B1 (pt)
CN (1) CN102884063B (pt)
AR (1) AR080388A1 (pt)
AU (1) AU2011223566B2 (pt)
BR (1) BR112012022369A2 (pt)
CA (1) CA2791715C (pt)
DK (1) DK2542552T3 (pt)
ES (1) ES2654399T3 (pt)
MX (3) MX336354B (pt)
NZ (1) NZ601998A (pt)
TW (1) TWI567071B (pt)
UY (1) UY33264A (pt)
WO (1) WO2011109587A1 (pt)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8680098B2 (en) * 2010-03-05 2014-03-25 Janssen Pharmaceutica, Nv Substituted aza-bicyclic imidazole derivatives useful as TRPM8 receptor modulators
GB2581032B (en) 2015-06-22 2020-11-04 Time Machine Capital Ltd System and method for onset detection in a digital signal
MY195177A (en) * 2015-06-23 2023-01-11 Kissei Pharmaceutical Pyrazole Derivative or Pharmaceutically Acceptable Salt Thereof
CN111253390B (zh) * 2018-11-30 2023-10-03 四川科伦博泰生物医药股份有限公司 并环化合物、其制备方法及用途
CN110638807A (zh) * 2019-08-23 2020-01-03 陈明英 局部镇痛用药物组合物、其制备方法及其应用

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS60260579A (ja) * 1984-01-13 1985-12-23 Yoshitomi Pharmaceut Ind Ltd プリン誘導体
DE60115092T2 (de) * 2000-12-12 2006-03-30 Neurogen Corp., Brandford Spiro[isobenzofuran-1,4'-piperidin]-3-one und 3h-spiroisobenzofuran-1,4'-piperidine
WO2003045929A1 (fr) * 2001-11-26 2003-06-05 Takeda Chemical Industries, Ltd. Derive bicyclique, procede de production de ce derive et utilisation correspondante
MXPA05003948A (es) 2002-10-17 2005-06-17 Amgen Inc Derivados de bencimidazol y su uso como ligandos de receptor vaniloide.
WO2005054188A1 (en) 2003-12-02 2005-06-16 Ucb, S.A. Imidazole derivatives, processes for preparing them and their uses
AR050630A1 (es) * 2004-09-09 2006-11-08 Solvay Pharm Bv DERIVADOS DE 6- TRIFLUOROMETIL PURINA 2- SUSTITUIDA CON ACTIVIDAD ANTAGONISTA DE ADENOSINA-A3. PROCESOS DE OBTENCIoN Y COMPOSICIONES FARMACÉUTICAS.
GB0508472D0 (en) 2005-04-26 2005-06-01 Glaxo Group Ltd Compounds
WO2006134318A1 (en) 2005-06-11 2006-12-21 Vernalis R & D Limited Pyrazole-substituted benzimidazole derivatives for use in the treatment of cancer and autoimmune disorders
RU2470016C2 (ru) 2006-03-22 2012-12-20 Ф.Хоффманн-Ля Рош Аг Производное бипиразола
US20080139608A1 (en) 2006-12-06 2008-06-12 Universiteit Leiden 2,6,8, Trisubstituted 1-deazapurines and their different uses
US8796253B2 (en) 2007-05-18 2014-08-05 Bayer Intellectual Property Gmbh Heteroaryl substituted pyrazole derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis
ME01532B (me) 2008-02-06 2014-04-20 Astrazeneca Ab Jedinjenja
SI2294066T1 (sl) 2008-04-28 2014-12-31 Janssen Pharmaceutica N.V. Benzoimidazoli kot inhibitorji prolil-hidroksilaze
US8680098B2 (en) * 2010-03-05 2014-03-25 Janssen Pharmaceutica, Nv Substituted aza-bicyclic imidazole derivatives useful as TRPM8 receptor modulators

Also Published As

Publication number Publication date
DK2542552T3 (en) 2017-12-11
CA2791715C (en) 2018-05-15
WO2011109587A1 (en) 2011-09-09
ES2654399T3 (es) 2018-02-13
MX2012010270A (es) 2013-04-24
AU2011223566A1 (en) 2012-09-20
US8680098B2 (en) 2014-03-25
TWI567071B (zh) 2017-01-21
TW201144309A (en) 2011-12-16
CA2791715A1 (en) 2011-09-09
MX336354B (es) 2016-01-14
US20140155395A1 (en) 2014-06-05
JP5782054B2 (ja) 2015-09-24
UY33264A (es) 2011-09-30
CN102884063A (zh) 2013-01-16
JP2013521306A (ja) 2013-06-10
MX348957B (es) 2017-07-04
US20110218197A1 (en) 2011-09-08
KR101667277B1 (ko) 2016-10-18
US9718820B2 (en) 2017-08-01
US9023846B2 (en) 2015-05-05
EP2542552A1 (en) 2013-01-09
NZ601998A (en) 2014-03-28
US9409915B2 (en) 2016-08-09
CN102884063B (zh) 2015-11-25
EP2542552B1 (en) 2017-11-15
AU2011223566B2 (en) 2015-05-21
AR080388A1 (es) 2012-04-04
US20160304518A1 (en) 2016-10-20
US20150158875A1 (en) 2015-06-11
KR20130018750A (ko) 2013-02-25

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]

Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI

B06T Formal requirements before examination [chapter 6.20 patent gazette]
B11E Dismissal acc. art. 34 of ipl - requirements for examination incomplete
B11T Dismissal of application maintained [chapter 11.20 patent gazette]