BRPI0417605A - derivados de 3-cicloalquilaminopirrolidina como moduladores de receptores de quimiocina - Google Patents

derivados de 3-cicloalquilaminopirrolidina como moduladores de receptores de quimiocina

Info

Publication number
BRPI0417605A
BRPI0417605A BRPI0417605-7A BRPI0417605A BRPI0417605A BR PI0417605 A BRPI0417605 A BR PI0417605A BR PI0417605 A BRPI0417605 A BR PI0417605A BR PI0417605 A BRPI0417605 A BR PI0417605A
Authority
BR
Brazil
Prior art keywords
receptor modulators
chemokine receptor
chemokine
ccr2
useful
Prior art date
Application number
BRPI0417605-7A
Other languages
English (en)
Inventor
Chu-Biao Xue
Brian Metcalf
Amy Qi Han
Darius J Robinson
Changsheng Zheng
Anlai Wang
Yingxin Zhang
Original Assignee
Incyte Corp
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 Incyte Corp filed Critical Incyte Corp
Publication of BRPI0417605A publication Critical patent/BRPI0417605A/pt
Publication of BRPI0417605B1 publication Critical patent/BRPI0417605B1/pt
Publication of BRPI0417605B8 publication Critical patent/BRPI0417605B8/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/24Radicals substituted by oxygen atoms
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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 bond 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
    • 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
    • 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
    • C07D401/14Heterocyclic 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
    • 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Abstract

"DERIVADOS DE 3-CICLOALQUILAMINOPIRROLIDINA COMO MODULADORES DE RECEPTORES DE QUIMIOCINA". A presente invenção está relacionada com derivados de 3-cicloalquilaminopirrolidina de fórmula 1: (na qual R¬ 1¬, R¬ 2¬, R¬ 3¬, R¬ 4¬, R¬ 5¬, R¬ 6¬, R¬ 7¬, X, Y, e Z são como definido nesta) que são úteis como moduladores da atividade dos receptores de quimiocina. Em particular, esses compostos são úteis como moduladores de receptores de quimiocinas e mais especificamente como moduladores dos receptores CCR2 e/ou CCRS. os compostos e composições da invenção podem se ligar aos receptores de quimiocina, por exemplo, os receptores CCR2 e/ou CCR5, e são úteis para o tratamento de doenças associadas a quimiocina, por exemplo, atividade de CCR2 e/ou CCR5, tais como arteriosclerose, restenose, lúpus, rejeição ao transplante de órgãos e artrite reumatóide.
BRPI0417605A 2003-12-18 2004-12-16 “n-[2-((3s)-3-{[4-hidróxi-4-(5-pirimidin-2- ilpiridin-2-il)ciclohexil]amino}-pirrolidin-1-il)-2- oxoetil]-3-(trifluor-metil)benzamida, ou um sal farmaceuticamente aceitável do mesmo e composição que o compreende”. BRPI0417605B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US53127003P 2003-12-18 2003-12-18
US60/531.270 2003-12-18
PCT/US2004/042321 WO2005060665A2 (en) 2003-12-18 2004-12-16 3-cycloalkylaminopyrrolidine derivatives as modulators of chemokine receptors

Publications (3)

Publication Number Publication Date
BRPI0417605A true BRPI0417605A (pt) 2007-03-27
BRPI0417605B1 BRPI0417605B1 (pt) 2020-05-12
BRPI0417605B8 BRPI0417605B8 (pt) 2021-05-25

Family

ID=34710216

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0417605A BRPI0417605B8 (pt) 2003-12-18 2004-12-16 “n-[2-((3s)-3-{[4-hidróxi-4-(5-pirimidin-2- ilpiridin-2-il)ciclohexil]amino}-pirrolidin-1-il)-2- oxoetil]-3-(trifluor-metil)benzamida, ou um sal farmaceuticamente aceitável do mesmo e composição que o compreende”.

Country Status (28)

Country Link
US (5) US7576089B2 (pt)
EP (1) EP1696919B1 (pt)
JP (1) JP4740151B2 (pt)
KR (2) KR100859027B1 (pt)
CN (2) CN1893945A (pt)
AP (1) AP2439A (pt)
AU (1) AU2004305079B2 (pt)
BR (1) BRPI0417605B8 (pt)
CA (1) CA2550596C (pt)
CR (1) CR8455A (pt)
DK (1) DK1696919T3 (pt)
EA (1) EA013631B1 (pt)
EC (1) ECSP066615A (pt)
ES (1) ES2439894T3 (pt)
GE (1) GEP20084505B (pt)
HK (1) HK1166321A1 (pt)
IL (1) IL175953A (pt)
IS (1) IS2956B (pt)
MA (1) MA28391B1 (pt)
MX (1) MXPA06007000A (pt)
NI (1) NI200600136A (pt)
NO (1) NO336486B1 (pt)
NZ (1) NZ547316A (pt)
OA (1) OA13338A (pt)
TN (1) TNSN06188A1 (pt)
UA (1) UA82917C2 (pt)
WO (1) WO2005060665A2 (pt)
ZA (1) ZA200604875B (pt)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004050024A2 (en) 2002-11-27 2004-06-17 Incyte Corporation 3-aminopyrrolidine derivatives as modulators of chemokine receptors
JP4948395B2 (ja) * 2004-04-13 2012-06-06 インサイト・コーポレイション ケモカインレセプターアンタゴニストとしてのピペラジニルピペリジン誘導体
GEP20084519B (en) 2004-05-11 2008-10-27 Incyte Corp 3-(4-heteroarylcyclo-hexylamino) cyclopenta-necarboxamides as modulators of chemokine receptors
AU2005259983B2 (en) 2004-06-28 2011-07-28 Incyte Corporation 3-aminocyclopentanecarboxamides as modulators of chemokine receptors
JP4116670B2 (ja) 2004-06-28 2008-07-09 インサイト コーポレイション ケモカイン受容体の調節剤としての3−アミノシクロペンタンカルボキサミド
BRPI0513953A (pt) * 2004-07-30 2008-05-20 Pfizer Prod Inc métodos para tratamento de doenças ou distúrbios mediados pela ccr2
JP2008512463A (ja) * 2004-09-08 2008-04-24 ボーイズ タウン ナショナル リサーチ ホスピタル マトリックスメタロプロテイナーゼ−12に関連する糸球体基底膜疾患の治療
EP2316458A1 (en) 2004-09-20 2011-05-04 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-coa-desaturase
EP2289510A1 (en) 2004-09-20 2011-03-02 Xenon Pharmaceuticals Inc. Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-coa desaturase enzymes
WO2006034440A2 (en) * 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
CN101084212A (zh) 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其作为硬脂酰CoA去饱和酶介导剂的用途
CN101084207A (zh) 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其作为硬脂酰CoA去饱和酶抑制剂的用途
US7592343B2 (en) 2004-09-20 2009-09-22 Xenon Pharmaceuticals Inc. Pyridazine-piperazine compounds and their use as stearoyl-CoA desaturase inhibitors
MX2007003321A (es) 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como agentes terapeuticos.
US8937184B2 (en) * 2005-02-16 2015-01-20 Abbvie B.V. 1H-imidazole derivatives as cannabinoid CB2 receptor modulators
CN101208089A (zh) 2005-06-03 2008-06-25 泽农医药公司 氨基噻唑衍生物作为人硬酯酰-CoA去饱和酶抑制剂
US8067415B2 (en) 2005-11-01 2011-11-29 Millennium Pharmaceuticals, Inc. Compounds useful as antagonists of CCR2
US8067457B2 (en) 2005-11-01 2011-11-29 Millennium Pharmaceuticals, Inc. Compounds useful as antagonists of CCR2
WO2007143600A2 (en) 2006-06-05 2007-12-13 Incyte Corporation Sheddase inhibitors combined with cd30-binding immunotherapeutics for the treatment of cd30 positive diseases
US20100210633A1 (en) * 2006-10-12 2010-08-19 Epix Delaware, Inc. Carboxamide compounds and their use
US8754107B2 (en) * 2006-11-17 2014-06-17 Abbvie Inc. Aminopyrrolidines as chemokine receptor antagonists
AR065369A1 (es) * 2007-02-19 2009-06-03 Novartis Ag Derivados de ciclohexil - amida del acido aril- carboxilico
CA2687931C (en) * 2007-05-31 2016-05-24 Boehringer Ingelheim International Gmbh Ccr2 receptor antagonists and uses thereof
US7977358B2 (en) * 2007-07-26 2011-07-12 Hoffmann-La Roche Inc. Pyrazol derivatives
KR20100087291A (ko) * 2007-09-25 2010-08-04 아보트 러보러터리즈 케모카인 수용체 길항제로서의 옥타하이드로펜탈렌 화합물
EP2297137A1 (en) * 2008-06-18 2011-03-23 F. Hoffmann-La Roche AG Novel heteroaryl carboxamide derivatives
WO2010003240A1 (en) 2008-07-08 2010-01-14 The Royal Institution For The Advancement Of Learning/Mcgill University Gmcsf and truncated ccl2 conjugates and methods and uses thereof
SI2370442T1 (sl) * 2008-11-26 2013-06-28 Pfizer Inc. 3-aminociklopentankarboksiamidi kot modulatorji kemokinskega receptorja
ES2555004T3 (es) 2008-12-10 2015-12-28 Janssen Pharmaceutica N.V. Antagonistas 4-azetidinil-1-heteroaril ciclohexanol de CCR2
PE20120061A1 (es) 2008-12-19 2012-02-19 Boehringer Ingelheim Int Derivados de pirimidina como antagonistas del receptor ccr2
CN102459227B (zh) 2009-04-17 2014-08-20 詹森药业有限公司 Ccr2的4-氮杂环丁烷基-1-苯基-环己烷拮抗剂
KR101151415B1 (ko) * 2009-07-10 2012-06-01 양지화학 주식회사 Ccr2 길항제로서의 피페라지닐에틸 3-아미노피롤리딘 유도체
PT3091012T (pt) 2009-12-17 2018-06-27 Centrexion Therapeutics Corp Antagonistas do receptor ccr2 e suas utilizações
JP2013526507A (ja) 2010-05-12 2013-06-24 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規ccr2受容体アンタゴニスト、その製造方法及び薬物としてのその使用
US8946218B2 (en) 2010-05-12 2015-02-03 Boehringer Ingelheim International Gmbh CCR2 receptor antagonists, method for producing the same, and use thereof as medicaments
US8841313B2 (en) 2010-05-17 2014-09-23 Boehringer Ingelheim International Gmbh CCR2 antagonists and uses thereof
JP5636094B2 (ja) 2010-05-25 2014-12-03 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ccr2受容体アンタゴニスト
EP2576538B1 (en) 2010-06-01 2015-10-28 Boehringer Ingelheim International GmbH New CCR2 antagonists
KR101743280B1 (ko) 2010-06-17 2017-06-02 얀센 파마슈티카 엔.브이. Ccr2의 사이클로헥실-아제티디닐 길항제
WO2012007500A2 (de) 2010-07-15 2012-01-19 Bayer Cropscience Ag Neue heterocyclische verbindungen als schädlingsbekämpfungsmittel
JP5868418B2 (ja) * 2010-12-01 2016-02-24 ヤンセン ファーマシューティカ エヌ.ベー. Ccr2の4−置換シクロヘキシルアミノ−4−ピペリジニル−アセトアミドアンタゴニスト
WO2012114223A1 (en) * 2011-02-25 2012-08-30 Pfizer Limited A method of treating liver fibrosis
JP5786258B2 (ja) 2011-07-15 2015-09-30 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規かつ選択的なccr2拮抗薬
MX2017017177A (es) 2015-07-02 2018-11-09 Centrexion Therapeutics Corp Citrato de (4-((3r,4r)-3-metoxitetrahidro-piran-4-ilamino)piperidi n-1-il)(5-metil-6-(((2r,6s)-6-(p-tolil)tetrahidro-2h-piran-2-il)m etilamino)pirimidin-4il) metanona.
EP3490873A1 (en) * 2016-08-01 2019-06-05 All Day Designs Ltd Transportation apparatus
US11198699B2 (en) 2019-04-02 2021-12-14 Aligos Therapeutics, Inc. Compounds targeting PRMT5

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3882145A (en) * 1972-12-22 1975-05-06 Ppg Industries Inc Halogenated N-substituted thiocarboxy maleimides
HU175454B (hu) * 1977-07-25 1980-08-28 Chinoin Gyogyszer Es Vegyeszet Sposob poluchenija novykh predel'nykh i chastichno predel'nykh n-acil-pirrol-2,5-dionov
DE4029054A1 (de) * 1990-09-13 1992-03-19 Bayer Ag N-acylpyrrolidin-derivate
US5770573A (en) * 1993-12-06 1998-06-23 Cytel Corporation CS-1 peptidomimetics, compositions and methods of using the same
EP0914319B1 (en) 1996-05-20 2001-11-21 Teijin Limited Diarylalkyl cyclic diamine derivatives as chemokine receptor antagonists
US6166037A (en) * 1997-08-28 2000-12-26 Merck & Co., Inc. Pyrrolidine and piperidine modulators of chemokine receptor activity
KR100622613B1 (ko) 1997-11-18 2006-09-11 데이진 화-마 가부시키가이샤 시클릭 아민 유도체 및 그 약제로서의 용도
US6288083B1 (en) * 1998-09-04 2001-09-11 Millennium Pharmaceuticals, Inc. Chemokine receptor antagonists and methods of use therefor
AU3389300A (en) * 1999-03-02 2000-09-21 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
AU3386700A (en) * 1999-03-02 2000-09-21 Merck & Co., Inc. 3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity
AU4796700A (en) 1999-05-13 2000-12-05 Dupont Pharmaceuticals Research Laboratories, Inc. Ureido-substituted cyclic amine derivatives and their use as drug
WO2000069432A1 (fr) 1999-05-18 2000-11-23 Teijin Limited Moyens de traitement et de prevention contre les maladies associees a des chimiokines
AU5600100A (en) * 1999-06-11 2001-01-02 Merck & Co., Inc. Cyclopentyl modulators of chemokine receptor activity
US7576117B1 (en) 1999-08-04 2009-08-18 Teijin Limited Cyclic amine CCR3 antagonist
US6410566B1 (en) * 2000-05-16 2002-06-25 Teijin Limited Cyclic amine derivatives and their use as drugs
JP4029960B2 (ja) * 2001-10-05 2008-01-09 独立行政法人理化学研究所 アブシジン酸生合成阻害剤
TWI262077B (en) 2002-04-29 2006-09-21 Merck & Co Inc Tetrahydropyranyl cyclopentyl tetrahydropyridopyridine modulators of chemokine receptor activity
AU2003223755B2 (en) * 2002-04-29 2008-08-21 Merck Sharp & Dohme Corp. Tetrahydropyranyl cyclopentyl tetrahydroisoquinoline modulators of chemokine receptor activity
NZ536477A (en) 2002-04-29 2005-05-27 Merck & Co Inc Tetrahydropyranyl cyclopentyl tetrahydropyridopyridine modulators of chemokine receptor activity
WO2004042351A2 (en) 2002-10-30 2004-05-21 Merck & Co., Inc. Piperidinyl-alpha-aminoamide modulators of chemokine receptor activity
AU2003284984B2 (en) 2002-10-30 2008-10-23 Merck Sharp & Dohme Corp. Gamma-aminoamide modulators of chemokine receptor activity
EP1558243A4 (en) 2002-10-30 2006-11-02 Merck & Co Inc MODULATORS OF ACTIVITY OF TETRAHYDROPYRANYL-CYCLOPENTYL-BENZYLAMIDE-BASED CHEMOKINE RECEPTORS
WO2004041163A2 (en) 2002-10-30 2004-05-21 Merck & Co., Inc. Piperidinyl cyclopentyl aryl benzylamide modulators of chemokine receptor activity
JP2006508948A (ja) 2002-10-30 2006-03-16 メルク エンド カムパニー インコーポレーテッド ケモカイン受容体活性のヘテロアリールピペリジンモジュレーター
WO2004050024A2 (en) * 2002-11-27 2004-06-17 Incyte Corporation 3-aminopyrrolidine derivatives as modulators of chemokine receptors
AR045875A1 (es) 2003-10-27 2005-11-16 Merck & Co Inc Procedimiento para la preparacion del antagonista ccr-2
RU2317295C1 (ru) 2003-10-27 2008-02-20 Мерк Энд Ко., Инк. Соль антагониста ccr-2
TWI341835B (en) * 2003-11-12 2011-05-11 Lg Life Sciences Ltd Melanocortin receptor agonists
EP1701724A4 (en) 2004-01-02 2007-11-14 Merck & Co Inc CYCLOPENTYL AMIDE MODULATORS OF ALKYLAMINO, ARYLAMINO AND SULFONAMIDO OF CHEMOKINE RECEPTOR ACTIVITY
AU2005206791A1 (en) 2004-01-20 2005-08-04 Merck Sharp & Dohme Corp. 2,6-disubstituted piperidines as modulators of chemokine receptor activity
WO2005072361A2 (en) 2004-01-28 2005-08-11 Merck & Co., Inc. Aminocyclopentyl pyridopyrazinone modulators of chemokine receptor activity
WO2005110409A2 (en) 2004-04-26 2005-11-24 Merck & Co., Inc. Tetrahydropyranyl cyclopentyl 1-substituted and 1,1-disubstituted tetrahydroisoquinoline modulators of chemokine receptor activity
UY29219A1 (es) * 2004-11-22 2006-04-28 Incyte Corp Sales de la n-(2- (((3r)-1-(trans-4-hidroxi-4-(6-metoxipiridin-3-il)-cilohexil) pirrolidin-3-il)amino)-2-oxoetil)-3- (trifluorometil) benzamida

Also Published As

Publication number Publication date
IL175953A (en) 2015-09-24
EP1696919B1 (en) 2013-10-02
US20050192302A1 (en) 2005-09-01
US20090286792A1 (en) 2009-11-19
EP1696919A4 (en) 2009-07-01
IL175953A0 (en) 2006-10-05
CN1893945A (zh) 2007-01-10
BRPI0417605B8 (pt) 2021-05-25
KR100859027B1 (ko) 2008-09-17
TNSN06188A1 (fr) 2007-11-15
US8697870B2 (en) 2014-04-15
AP2006003629A0 (en) 2006-06-30
AP2439A (en) 2012-08-31
EP1696919A2 (en) 2006-09-06
WO2005060665A3 (en) 2005-12-15
MA28391B1 (fr) 2007-01-02
MXPA06007000A (es) 2006-08-31
CN102344398B (zh) 2015-02-25
JP4740151B2 (ja) 2011-08-03
CA2550596C (en) 2011-03-15
AU2004305079A1 (en) 2005-07-07
NO336486B1 (no) 2015-09-07
NI200600136A (es) 2008-04-24
UA82917C2 (en) 2008-05-26
DK1696919T3 (da) 2013-12-09
WO2005060665A2 (en) 2005-07-07
ECSP066615A (es) 2006-10-25
HK1166321A1 (en) 2012-10-26
CA2550596A1 (en) 2005-07-07
ES2439894T3 (es) 2014-01-27
IS2956B (is) 2016-12-15
ZA200604875B (en) 2007-11-28
KR20080052683A (ko) 2008-06-11
GEP20084505B (en) 2008-10-10
US20170050942A1 (en) 2017-02-23
US7576089B2 (en) 2009-08-18
US20140155377A1 (en) 2014-06-05
EA200600991A1 (ru) 2006-10-27
BRPI0417605B1 (pt) 2020-05-12
KR20070008536A (ko) 2007-01-17
WO2005060665A8 (en) 2006-05-04
CR8455A (es) 2007-03-02
EA013631B1 (ru) 2010-06-30
US20150231114A1 (en) 2015-08-20
JP2007514751A (ja) 2007-06-07
CN102344398A (zh) 2012-02-08
NO20063255L (no) 2006-09-14
IS8466A (is) 2006-05-15
NZ547316A (en) 2011-01-28
AU2004305079B2 (en) 2011-05-12
OA13338A (en) 2007-04-13

Similar Documents

Publication Publication Date Title
BRPI0417605A (pt) derivados de 3-cicloalquilaminopirrolidina como moduladores de receptores de quimiocina
BR0316732A (pt) Derivados de 3-aminopirrolidina como moduladores de receptores de quimiocina
BR0312695A (pt) Derivados de 1h-pirrolidina-2,4-diona espirocìclicos substituìdos por cis-alcóxi
BRPI0510409A (pt) heterociclos bicìclicos contendo nitrogênio como inibidores da aromatase
BRPI0510410A (pt) compostos orgánicos
BRPI0413860A (pt) [1,8]naftiridin-2-onas e compostos relacionados para o tratamento de esquizofrenia
ECSP055621A (es) Aza-biciclo-alquil-éteres y su uso como agonistas de alfa7-nachr
BRPI0510665A (pt) 3-(4-heteroarilcicloexilamino) ciclopentano-carboxiamidas como moduladores de receptores de quimiocinas
BR0214666A (pt) Derivados de acetileno tendo atividade antagonìstica de mglur5
BR0010304A (pt) Derivados de piperazina úteis como antagonistas do ccr5
MA29369B1 (fr) Dosage fixe d'anticorps anti-her
BRPI0513405A (pt) tienopirimidinas úteis como inibidores de aurora quinase
BRPI0517945A (pt) derivados de quinuclidina e seu uso como antagonistas de receptor muscarìnico m3
BRPI0508644A (pt) catalisador ácido sólido e método de utilizar o mesmo
ATE509920T1 (de) Quadratsäurederivate als inhibitoren von histondeacetylase
BR0214884A (pt) Derivados de 7-amino-benzotiazol como ligantes do receptor de adenosina
ATE485261T1 (de) Salicylsäurederivate
BR0317222A (pt) Compostos de 2-aminocarbonil-quinolina como antagonistas dos receptores de difosfato de adenisina de plaquetas
BR0308592A (pt) Derivados de piperidina ou 8-azabiciclo [3.2.1] oct-3-il-piperidina, de utilidade como moduladores da atividade do receptor de quimocina (especialmente ccr5)
BR0317459A (pt) Novos derivados de piperidina como moduladores do receptor ccr5 quimiocina
BRPI0411738A (pt) compostos orgánicos
EA200501593A1 (ru) Азабициклические производные в качестве антагонистов мускаринового рецептора
BRPI0412910A (pt) derivados de nicotinamida úteis como inibidores de pde4
BRPI0108990B8 (pt) processo para preparação de derivados de pirimidona com atividade antifungos
BRPI0412862A (pt) derivados da nicotinamida úteis como inibidores de pde4

Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B15K Others concerning applications: alteration of classification

Free format text: "PARA: INT. CL. A61K 31/44

Ipc: A61K 31/44 (2011.01), C07D 401/12 (2011.01), C07D

Free format text: PARA: INT. CL. A61K 31/44; C07D 401/12, 401/14; A61P 37/00

Ipc: A61K 31/44 (2011.01), C07D 401/12 (2011.01), C07D

B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B25G Requested change of headquarter approved

Owner name: INCYTE CORPORATION (US)

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]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 12/05/2020, OBSERVADAS AS CONDICOES LEGAIS.

B16C Correction of notification of the grant [chapter 16.3 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 16/12/2004 OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF

B21F Lapse acc. art. 78, item iv - on non-payment of the annual fees in time

Free format text: REFERENTE A 18A ANUIDADE.

B24J Lapse because of non-payment of annual fees (definitively: art 78 iv lpi, resolution 113/2013 art. 12)

Free format text: EM VIRTUDE DA EXTINCAO PUBLICADA NA RPI 2701 DE 11-10-2022 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDA A EXTINCAO DA PATENTE E SEUS CERTIFICADOS, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.