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PE20130576A1 - Compuestos heterociclicos de nitrogeno utiles como inhibidores de pde10 - Google Patents

Compuestos heterociclicos de nitrogeno utiles como inhibidores de pde10

Info

Publication number
PE20130576A1
PE20130576A1 PE2012002159A PE2012002159A PE20130576A1 PE 20130576 A1 PE20130576 A1 PE 20130576A1 PE 2012002159 A PE2012002159 A PE 2012002159A PE 2012002159 A PE2012002159 A PE 2012002159A PE 20130576 A1 PE20130576 A1 PE 20130576A1
Authority
PE
Peru
Prior art keywords
alkyl
halo
phenyl
helpful
nitrogen compounds
Prior art date
Application number
PE2012002159A
Other languages
English (en)
Inventor
Jennifer R Allen
Jian J Chen
Michael J Frohn
Essa Hu Harrington
Qingyian Liu
Alexander J Pickerell
Shannon Rumfelt
Robert M Rzasa
Wenge Zhong
Original Assignee
Amgen Inc
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Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44278966&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20130576(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Amgen Inc filed Critical Amgen Inc
Publication of PE20130576A1 publication Critical patent/PE20130576A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P25/14—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
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P25/00—Drugs for disorders of the nervous system
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    • A61P25/36—Opioid-abuse
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
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    • 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
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
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    • 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
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
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    • 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
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    • 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
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    • 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
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    • 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
    • C07D487/08—Bridged systems
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    • C07—ORGANIC CHEMISTRY
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    • 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
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    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems

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Abstract

SE REFIERE A COMPUESTOS HETEROCICLICOS DE FORMULA (I) DONDE X1 Y X4 SON CADA UNO N O CR6; X2 ES N O CR2; X3 ES N O CR3, EN DONDE R2 Y R3 SON CADA UNO H, HALO, CN, OH, ENTRE OTROS; R6 ES R1, HALO, CN, ALQUILO(C1-C4), ENTRE OTROS; R1 -ORc O ALQUILO(C0-C4)-L1, EN DONDE Rc ES ALQUILO(C0-C4)-L2; L1 ES UN ANILLO MONOCICLICO DE 3 A 7 MIENBROS, ENTRE OTROS; L2 ES UN ANILLO BICICLICO DE 6 A 12 MIEMBROS, ENTRE OTROS; R4a ES H, OH, F, Cl O METILO; R4b ES HALO, CN, OH, O-ALQUILO(C1-C4), ENTRE OTROS; Y ES ALQUILO(C0-C4), -C=O, SO O SO2; R5 ES PIRIDINA, PIRIMIDINA, BENZIMIDAZOL, ENTRE OTROS; m ES DE 0 A 4; p Y q SON CADA UNO DE 0 A 6 DONDE LA SUMA DE p Y q ES DE 2 HASTA 6. SON COMPUESTOS PREFERIDOS: (1H-BENZOIMIDAZOL-2-IL)-[3-(3-FENIL-PIRIDIN-2-IL)-AZETIDIN-1-IL]-METANONA; [3-(3-FENIL-PIRAZIN-2-IL)-AZETIDIN-1-IL]-[1-(2,2,2-TRIFLUORO-ETIL)-1H-BENZOIMIDAZOL-2-IL]-METANONA; 1-(3-{3-[1-(1H-BENZOIMIDAZOL-2-CARBONIL)-AZETIDIN-3-IL]-PIRAZIN-2-IL}-FENIL)-ETANONA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA FOSFODIESTERASA 10 SIENDO UTILES EN EL TRATAMIENTO DE OBESIDAD, ENFERMEDAD DE HUNTINGTON, ESQUIZOFRENIA, TRASTORNO BIPOLAR
PE2012002159A 2010-05-13 2011-05-11 Compuestos heterociclicos de nitrogeno utiles como inhibidores de pde10 PE20130576A1 (es)

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US33452510P 2010-05-13 2010-05-13

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US (3) US8957073B2 (es)
EP (1) EP2569300A1 (es)
JP (1) JP5702855B2 (es)
KR (1) KR101564806B1 (es)
CN (1) CN103221404B (es)
AR (1) AR081627A1 (es)
AU (1) AU2011253057B2 (es)
BR (1) BR112012029026A2 (es)
CA (1) CA2798490A1 (es)
CL (1) CL2012003178A1 (es)
CO (1) CO6630189A2 (es)
CR (1) CR20120635A (es)
EA (1) EA201291236A1 (es)
IL (1) IL222898A (es)
MA (1) MA34300B1 (es)
MX (1) MX2012013130A (es)
NZ (1) NZ603876A (es)
PE (1) PE20130576A1 (es)
PH (1) PH12012502212A1 (es)
SG (1) SG185515A1 (es)
TN (1) TN2012000530A1 (es)
TW (1) TW201206902A (es)
UA (1) UA109438C2 (es)
UY (1) UY33382A (es)
WO (1) WO2011143365A1 (es)
ZA (1) ZA201208510B (es)

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