PE20120774A1 - COMPUESTOS DERIVADOS DE PIRAZOLO[3,4-d]PIRIMIDINDIONA COMO MODULADORES DE TRPA1 - Google Patents

COMPUESTOS DERIVADOS DE PIRAZOLO[3,4-d]PIRIMIDINDIONA COMO MODULADORES DE TRPA1

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Publication number
PE20120774A1
PE20120774A1 PE2011001707A PE2011001707A PE20120774A1 PE 20120774 A1 PE20120774 A1 PE 20120774A1 PE 2011001707 A PE2011001707 A PE 2011001707A PE 2011001707 A PE2011001707 A PE 2011001707A PE 20120774 A1 PE20120774 A1 PE 20120774A1
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PE
Peru
Prior art keywords
thiazol
dioxo
pyrimidin
acetamide
hydroxyl
Prior art date
Application number
PE2011001707A
Other languages
English (en)
Inventor
Sukeerthi Kumar
Abraham Thomas
Sachin Vasantrao Dhone
Neelima Khairatkar-Joshi
Indranil Mukhopadhyay
Nisha Parag Patil
Ashok Bhausaheb Kadam
Vishal Govindrao Deshmukh
Rajendra Prakash Chikhale
Sachin Sundarlal Chaudhari
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Glenmark Pharmaceuticals Sa
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Publication date
Application filed by Glenmark Pharmaceuticals Sa filed Critical Glenmark Pharmaceuticals Sa
Publication of PE20120774A1 publication Critical patent/PE20120774A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/525Isoalloxazines, e.g. riboflavins, vitamin B2
    • 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
    • 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
    • A61P1/06Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/14Antitussive agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00Drugs for skeletal disorders
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    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
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    • A61P25/28Drugs 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
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • A61P7/12Antidiuretics, e.g. drugs for diabetes insipidus
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Otolaryngology (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA (I) DONDE: R1 Y R2 SON CADA UNO H, HIDROXILO, ALQUILO, HALOALQUILO, ENTRE OTROS; Rb ES H, HIDROXILO, CIANO, HALOGENO, HALOALQUILO, ENTRE OTROS; U ES ARILO OPCIONALMENTE SUSTITUIDO, HETEROCICLOS C5 TALES COMO TIAZOL, IMIDAZOL, ISOXAZOL, PIRAZOL, TIADIAZOL, PIRIMIDINA O BENZOTIAZOL; V ES H, CIANO, NITRO, -NRXRY, HALOGENO, ENTRE OTROS; RX Y RY SON H, HIDROXILO, HALOGENO, ALQUILO, ALQUENILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-[4-(2,4-DIFLUOROFENIL)-1,3-TIAZOL-2-IL]-2-(1,3-DIMETIL-2,4-DIOXO-1,2,3,4-TETRA HIDRO-5H-PIRROLO[3,2-d]PIRIMIDIN-5-IL)ACETAMIDA; 2-(1,3-DIMETIL-2,4-DIOXO-1,2,3,4-TETRAHIDRO-5H-PIRROLO[3,2-d]PIRIMIDIN-5-IL)-N-{4-[4-FLUORO-3-(TRIFLUOROMETIL)FENIL]-1,3-TIAZOL-2-IL} ACETAMIDA; 2-(4,6-DIMETIL-5,7-DIOXO-4,5,6,7-TETRAHIDRO-1H-PIRAZOLO [4,3-d]PIRIMIDIN-1-IL)-N-{4-[3-FLUORO-4-(TRIFLUOROMETIL)FENIL]-1,3-TIAZOL-2-IL} ACETAMIDA; ENTRE OTROS. DICHO COMPUESTO ES UN DERIVADO DE PIRIMIDINDIONA FUSIONADO MODULADOR DEL RECEPTOR DE POTENCIAL TRANSITORIO DE LA SUBFAMILIA A, MIEMBRO 1 (TRPA1) UTILES PARA TRATAR O PREVENIR UNA ENFERMEDAD RELACIONADA CON TRPA1
PE2011001707A 2009-03-23 2010-03-17 COMPUESTOS DERIVADOS DE PIRAZOLO[3,4-d]PIRIMIDINDIONA COMO MODULADORES DE TRPA1 PE20120774A1 (es)

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
IN665MU2009 2009-03-23
US17135509P 2009-04-21 2009-04-21
IN2212MU2009 2009-09-23
IN2211MU2009 2009-09-23
US25194409P 2009-10-15 2009-10-15
US25326309P 2009-10-20 2009-10-20
IN2892MU2009 2009-12-15
IN2891MU2009 2009-12-15
US29446310P 2010-01-12 2010-01-12
US30024110P 2010-02-01 2010-02-01

Publications (1)

Publication Number Publication Date
PE20120774A1 true PE20120774A1 (es) 2012-06-27

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PE2011001707A PE20120774A1 (es) 2009-03-23 2010-03-17 COMPUESTOS DERIVADOS DE PIRAZOLO[3,4-d]PIRIMIDINDIONA COMO MODULADORES DE TRPA1

Country Status (24)

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US (1) US9000159B2 (es)
EP (2) EP2708538B1 (es)
JP (1) JP5657638B2 (es)
KR (1) KR20110132575A (es)
CN (1) CN102361873B (es)
AP (1) AP3280A (es)
AU (1) AU2010227245B2 (es)
BR (1) BRPI1013559A2 (es)
CA (1) CA2756518A1 (es)
CL (2) CL2011002315A1 (es)
DK (1) DK2411393T3 (es)
EA (1) EA023857B1 (es)
ES (2) ES2456515T3 (es)
HK (2) HK1166075A1 (es)
IL (1) IL215178A (es)
MX (1) MX2011009824A (es)
PE (1) PE20120774A1 (es)
PL (1) PL2411393T3 (es)
PT (1) PT2411393E (es)
SG (1) SG174402A1 (es)
SI (1) SI2411393T1 (es)
UA (1) UA108069C2 (es)
WO (1) WO2010109287A1 (es)
ZA (1) ZA201107648B (es)

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