PE14202000A1 - Modulators of CCR5 - Google Patents

Modulators of CCR5

Info

Publication number
PE14202000A1
PE14202000A1 PE00119099A PE00119099A PE14202000A1 PE 14202000 A1 PE14202000 A1 PE 14202000A1 PE 00119099 A PE00119099 A PE 00119099A PE 00119099 A PE00119099 A PE 00119099A PE 14202000 A1 PE14202000 A1 PE 14202000A1
Authority
PE
Peru
Prior art keywords
c2
c1
oh
region
ch2
Prior art date
Application number
PE00119099A
Other languages
Spanish (es)
Inventor
Duncan Robert Armour
Martin Paul Edwards
Anthony Wood
David Anthony Price
Blanda Luzia Christa Stammen
Manoussos Perros
Original Assignee
Pfizer
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
Priority to GBGB9828420.1A priority Critical patent/GB9828420D0/en
Priority to GBGB9921375.3A priority patent/GB9921375D0/en
Application filed by Pfizer filed Critical Pfizer
Publication of PE14202000A1 publication Critical patent/PE14202000A1/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/14Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
    • C07D211/56Nitrogen atoms
    • C07D211/58Nitrogen atoms attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • 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
    • C07D513/08Bridged systems

Abstract

SE REFIERE A UN COMPUESTO QUE COMPRENDE REGIONES; It REFERS TO A compound comprising regions; LA REGION PUEDE SER RESTOS HETEROFENILMETILENO DE FORMULA 1; THE REGION MAY BE HETEROFENILMETILENO REMAINS OF FORMULA 1; DONDE R5 ES UN ENLACE, O, CO, NR4, S(=O)p; Wherein R5 is a bond, O, CO, NR4, S (= O) p; R4 ES H, ALQUILO C1-C2; R4 is H, alkyl C1-C2; R6 ES H, ALQUILO C1-C2, ALCOXI C1-C2, CN, OH, C=ONH2; R6 is H, alkyl C1-C2, C1-C2, CN, OH, C = ONH2; j, m, p SON 0-2; j, m, p are 0-2; R7 Y R8 SON F, Cl, OH, CN, CONR4aR4b, ENTRE OTROS; R7 and R8 are F, Cl, OH, CN, CONR4aR4b, among others; R4a Y R4b SON H, ALQUILO C1-C2; R4a and R4b are H, C1-C2; EL RESTO 1.0.1 ES UN HETEROCICLO MONOCICLICO, BICICLO BENZOCONDENSADO; 1.0.1 THE REST IS A monocyclic, BICICLO benzofused; R12a ES F, Cl, CO2R4, OXO, ENTRE OTROS; R12a is F, Cl, CO2R4, OXO, among others; R9 ES F, Cl, CO2R4, OH, CN, ENTRE OTROS; R9 is F, Cl, CO2R4, OH, CN, among others; R12b ES H, ALQUILO C1-C4, ALQUENILO C2-C4, ENTRE OTROS; R12b is H, alkyl C1-C4, alkenyl C2-C4, among others; LA REGION ES -C(R40)-C(R41)-; The region is -C (R40) -C (R41) -; R40 Y R41 SON H, ALQUILO, OH, ALCOXI C1-C3; R40 and R41 are H, alkyl, OH, C1-C3; LA REGION ES UN AZABICICLO (4.2.0, W4 ES UN ENLACE, CH2, CH2-O-CH2, ENTRE OTROS; LA REGION ES UN HETEROCICLO DE 5 MIEMBROS CON 2 N, AMIDA, CARBAMATO, UREA, ENTRE OTROS; UN COMPUESTO PREFERIDO ES N-{3-[3-EXO-(2-METIL-1H-BENZOIMIDAZOL-1-IL)-ß-AZABICICLO[3.2.1.]OCT-8-IL]-1-FENILPROPIL}-CICLOBUTANOCARBOXAMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION QUE COMPRENDE ADEMAS INDINAVIR, SAQUINAVIR, NELFINAVIR, AMPRENAVIR, NEVIRAPINA, DELAVIRDINA, EFAVIRENZ, ZIDOVUDINA, DIDANOSINA, ZALCITABINA, ESTAVUDINA, LAMIVUDINA, ABACAVIR, ADEFOVIR DIPIVOXIL, ENTRE OTROS. EL COMPUESTO MODULA LA ACTIVIDAD DEL RECEPTOR DE QUIMIOCINA CCR5 Y PUEDE SER UTIL PARA EL TRATAMIENTO DE UNA INFECCION POR EL VIRUS DE LA INMUDEFICIENCIA HUMANA The region is a azabicyclo (4.2.0, W4 is a bond, CH2, CH2-O-CH2, among others, the region is a 5-membered heterocycle with 2 N, amide, carbamate, urea, among others, a preferred compound It is N- {3- [3-exo- (2-methyl-1H-benzimidazol-1-yl) -ß-azabicyclo [3.2.1.] oct-8-yl] -1-phenylpropyl} -cyclobutanecarboxamide, LIMITED . also relates to a composition further comprising indinavir, saquinavir, nelfinavir, amprenavir, nevirapine, delavirdine, efavirenz, zidovudine, didanosine, zalcitabine, stavudine, lamivudine, abacavir, adefovir dipivoxil, among others. COMPOUND MODULATES receptor activity chemokine CCR5 AND BE SUITABLE FOR THE TREATMENT OF iNFECTION OF HUMAN Immunodeficiency
PE00119099A 1998-12-23 1999-11-29 Modulators of CCR5 PE14202000A1 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
GBGB9828420.1A GB9828420D0 (en) 1998-12-23 1998-12-23 CCR5 antagonists useful as anti-hiv agents
GBGB9921375.3A GB9921375D0 (en) 1999-09-10 1999-09-10 CCR5 Modulators

Publications (1)

Publication Number Publication Date
PE14202000A1 true PE14202000A1 (en) 2000-12-18

Family

ID=26314899

Family Applications (1)

Application Number Title Priority Date Filing Date
PE00119099A PE14202000A1 (en) 1998-12-23 1999-11-29 Modulators of CCR5

Country Status (45)

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US (1) US6586430B1 (en)
EP (1) EP1140085B1 (en)
JP (1) JP3602795B2 (en)
KR (1) KR100425612B1 (en)
CN (1) CN1331591A (en)
AP (1) AP1697A (en)
AR (1) AR024233A1 (en)
AT (1) AT505190T (en)
AU (1) AU763644B2 (en)
BG (1) BG65448B1 (en)
BR (1) BRPI9917007B1 (en)
CA (1) CA2350073C (en)
CO (1) CO5300387A1 (en)
CR (2) CR6392A (en)
CU (1) CU23344A3 (en)
CY (1) CY1111504T1 (en)
CZ (1) CZ300926B6 (en)
DE (1) DE69943352D1 (en)
DK (1) DK1140085T3 (en)
DZ (2) DZ2979A1 (en)
EA (1) EA004988B1 (en)
EE (1) EE05170B1 (en)
EG (1) EG24400A (en)
GC (1) GC0000117A (en)
GE (1) GEP20033131B (en)
HR (2) HRP20010468B1 (en)
HU (1) HU228754B1 (en)
ID (1) ID28965A (en)
IL (2) IL143512D0 (en)
IS (1) IS5944A (en)
MA (1) MA26714A1 (en)
ME (1) ME00513B (en)
NO (1) NO330677B1 (en)
NZ (1) NZ511794A (en)
OA (1) OA11735A (en)
PA (1) PA8487201A1 (en)
PE (1) PE14202000A1 (en)
PL (1) PL201875B1 (en)
PT (1) PT1140085E (en)
RS (1) RS51701B (en)
SK (1) SK287020B6 (en)
TN (1) TNSN99252A1 (en)
TR (1) TR200101793T2 (en)
TW (1) TW577888B (en)
WO (1) WO2000038680A1 (en)

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