BRPI0813695B8 - compostos de heteroaril piridil e fenil benzenossulfonamidas fundidas, composição, método de modular a função de ccr2, usos dos compostos e forma cristalina - Google Patents

compostos de heteroaril piridil e fenil benzenossulfonamidas fundidas, composição, método de modular a função de ccr2, usos dos compostos e forma cristalina

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Publication number
BRPI0813695B8
BRPI0813695B8 BRPI0813695A BRPI0813695A BRPI0813695B8 BR PI0813695 B8 BRPI0813695 B8 BR PI0813695B8 BR PI0813695 A BRPI0813695 A BR PI0813695A BR PI0813695 A BRPI0813695 A BR PI0813695A BR PI0813695 B8 BRPI0813695 B8 BR PI0813695B8
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BR
Brazil
Prior art keywords
compounds
composition
crystalline form
fused heteroaryl
ccr2 function
Prior art date
Application number
BRPI0813695A
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English (en)
Inventor
Krasinski Antoni
Wang Qiang
Ungashe Solomon
Punna Sreenivas
Zeng Yibin
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Chemocentryx Inc
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Application filed by Chemocentryx Inc filed Critical Chemocentryx Inc
Publication of BRPI0813695A2 publication Critical patent/BRPI0813695A2/pt
Publication of BRPI0813695B1 publication Critical patent/BRPI0813695B1/pt
Publication of BRPI0813695B8 publication Critical patent/BRPI0813695B8/pt

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    • 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
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • 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
    • 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
    • C07D471/12—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 three hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring 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)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Communicable Diseases (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

compostos de heteroaril piridil e fenil benzenossulfonamidas fundidas, composição, método de modular a função de ccr2, usos dos referidos compostos e forma cristalina. são fornecidos compostos que agem como potentes antagonistas do receptor ccr2. os compostos são geralmente derivados de aril sulfonamida e são úteis em composições farmacêuticas, métodos para o tratamento de doenças mediadas por ccr2 e como controles em ensaios para a identificação de antagonistas de ccr2. um composto da fórmula (i) ou um sal do mesmo: em que r1 e r2 são cada um independentemente hidrogênio, c1-8 alquila, -cn, ou c1-8 haloalquila, contanto que pelo menos um de r1 ou r2 é diferente do hidrogênio cada r3 é independentemente, r4 é hidrogênio; r5 é halogênio ou c1-8 alquila; r6 é hidrogênio; x1 é cr7 , n ou no; x2 e x4 são n ou no; x3 é cr7; x6 e x7 são cada um independentemente selecionado a partir de cr7 , n e no; cada r7 é independentemente selecionado a partir do grupo consistindo em hidrogênio, halogênio, c2-8 alquila substituída ou não-substituída, c2-8 alquenila substituída ou não-substituída, c2-8 alquinila substituída ou não-substituída, -cn, =o, -no2 , -or6, -oc(o)r8, -co2r8, -c(o)r8, -c(o)nr0r8, -oc(o)nr9r8, -nr10c(o)r8, -nr10c(o)nr9r8, -nr9r8, -nr10co2r8, -sr8, -s(o)r8, -s(o)2r8, -s(o)2nr9r8, -nr10s(o)2r8, c5-10 arila substituída ou não-substituída, heteroarila de 5 a 10 membros substituída ou não-substituída e heterociclila de 3 a 10 membros substituída ou não-substituída.
BRPI0813695A 2007-07-12 2008-07-11 compostos de heteroaril piridil e fenil benzenossulfonamidas fundidas, composição, método de modular a função de ccr2, usos dos compostos e forma cristalina BRPI0813695B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US94932807P 2007-07-12 2007-07-12
US60/949,328 2007-07-12
PCT/US2008/069813 WO2009009740A1 (en) 2007-07-12 2008-07-11 Fused heteroaryl pyridyl and phenyl benzenesuflonamides as ccr2 modulators for the treament of inflammation

Publications (3)

Publication Number Publication Date
BRPI0813695A2 BRPI0813695A2 (pt) 2014-12-30
BRPI0813695B1 BRPI0813695B1 (pt) 2019-02-12
BRPI0813695B8 true BRPI0813695B8 (pt) 2021-05-25

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BRPI0813695A BRPI0813695B8 (pt) 2007-07-12 2008-07-11 compostos de heteroaril piridil e fenil benzenossulfonamidas fundidas, composição, método de modular a função de ccr2, usos dos compostos e forma cristalina

Country Status (17)

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US (6) US7884110B2 (pt)
EP (1) EP2175859B1 (pt)
JP (1) JP5306344B2 (pt)
KR (4) KR101969689B1 (pt)
CN (1) CN101820881B (pt)
AT (1) ATE548039T1 (pt)
AU (1) AU2008275000B2 (pt)
BR (1) BRPI0813695B8 (pt)
CA (1) CA2692761C (pt)
DK (1) DK2175859T3 (pt)
ES (1) ES2383568T3 (pt)
HK (1) HK1142547A1 (pt)
IL (1) IL203258A (pt)
PL (1) PL2175859T3 (pt)
PT (1) PT2175859E (pt)
WO (1) WO2009009740A1 (pt)
ZA (1) ZA201000212B (pt)

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US20090233946A1 (en) 2009-09-17
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