NO20090190L - Modulatorer av kjemokin reseptor aktivitet, krystallinske former og fremgangsmate - Google Patents

Modulatorer av kjemokin reseptor aktivitet, krystallinske former og fremgangsmate

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Publication number
NO20090190L
NO20090190L NO20090190A NO20090190A NO20090190L NO 20090190 L NO20090190 L NO 20090190L NO 20090190 A NO20090190 A NO 20090190A NO 20090190 A NO20090190 A NO 20090190A NO 20090190 L NO20090190 L NO 20090190L
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Norway
Prior art keywords
diseases
present
crystalline forms
receptor activity
modulators
Prior art date
Application number
NO20090190A
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English (en)
Inventor
Percy H Carter
John V Duncia
Boguslaw M Mudryk
Michael E Randazzo
Zili Xiao
Michael G Yang
Rulin Zhao
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Bristol Myers Squibb Co
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Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of NO20090190L publication Critical patent/NO20090190L/no

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • 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
    • A61K31/40—Heterocyclic 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
    • A61K31/4025—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/18—Heterocyclic 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 one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic 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 one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/72—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 spiro-condensed with carbocyclic rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Transplantation (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)

Abstract

Foreliggende oppfinnelse tilveiebringer en ny antagonist eller partielle agonister/antagonist av MCP-1 reseptor aktivitet: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-okso-3-(6-(trifluormetyl)kinazolin-4-ylamino)pyrrolidin-1-yl)cykloheksyl)acetamid eller et farmasøytisk akseptabelt salt, solvat eller prodroge, derav, som har en uventet kombinasjon av ønskelige farmakologiske karakteristika. Krystallinske former ifølge foreliggende oppfinnelse er også gitt. Farmasøytiske preparater inneholdende disse og metoder for anvendelse av disse som midler for behandling av inflammatoriske sykdommer, allergiske sykdommer, autoimmune sykdommer, metabolske sykdommer, kreft og/eller kardiovaskulære sykdommer er også en hensikt ifølge foreliggende oppfinnelse. Foreliggende beskrivelse tilveiebringer også en fremgangsmåte for fremstilling av forbindelser med formel (I), omfattende N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-okso-3-(6-(trifluormetyl)kinazolin-4-ylamino)pyrrolidin-1-yl)cykloheksyl)acetamid: hvor R1, R8, R9, R10 og er som beskrevet her. Forbindelser som er anvendelige mellomprodukter av fremgangsmåten er også gitt her. 1
NO20090190A 2006-07-28 2009-01-13 Modulatorer av kjemokin reseptor aktivitet, krystallinske former og fremgangsmate NO20090190L (no)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US83423506P 2006-07-28 2006-07-28
US89602607P 2007-03-21 2007-03-21
US11/782,742 US7629351B2 (en) 2006-07-28 2007-07-25 N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino) pyrrolidin-1-yl)cyclohexyl)acetamide and other modulators of chemokine receptor activity, crystalline forms and process
PCT/US2007/074377 WO2008014360A2 (en) 2006-07-28 2007-07-26 Modulators of chemokine receptor activity, crystalline forms and process

Publications (1)

Publication Number Publication Date
NO20090190L true NO20090190L (no) 2009-01-29

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ID=38829183

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20090190A NO20090190L (no) 2006-07-28 2009-01-13 Modulatorer av kjemokin reseptor aktivitet, krystallinske former og fremgangsmate

Country Status (26)

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US (2) US7629351B2 (no)
EP (2) EP2046779B1 (no)
JP (1) JP5236643B2 (no)
KR (1) KR20090033915A (no)
CN (1) CN101535301B (no)
AR (1) AR062124A1 (no)
AT (2) ATE522522T1 (no)
AU (1) AU2007279333B2 (no)
BR (1) BRPI0715415A2 (no)
CA (2) CA2659253A1 (no)
CY (1) CY1111744T1 (no)
DK (1) DK2046779T3 (no)
EA (1) EA016563B1 (no)
ES (1) ES2365264T3 (no)
HR (1) HRP20110465T1 (no)
IL (2) IL196427A (no)
MX (1) MX2009000808A (no)
NO (1) NO20090190L (no)
NZ (1) NZ574425A (no)
PE (1) PE20080732A1 (no)
PL (1) PL2046779T3 (no)
PT (1) PT2046779E (no)
SG (1) SG158924A1 (no)
SI (1) SI2046779T1 (no)
TW (2) TWI421249B (no)
WO (1) WO2008014360A2 (no)

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WO2008014360A2 (en) 2008-01-31
US7629351B2 (en) 2009-12-08
ES2365264T3 (es) 2011-09-27
JP5236643B2 (ja) 2013-07-17
EP2046779A2 (en) 2009-04-15
SI2046779T1 (sl) 2011-09-30
PT2046779E (pt) 2011-07-25
IL196427A0 (en) 2009-09-22
AU2007279333A1 (en) 2008-01-31
PL2046779T3 (pl) 2011-09-30
EP2194051A1 (en) 2010-06-09
US20100113489A1 (en) 2010-05-06
HRP20110465T1 (hr) 2011-07-31
EA016563B1 (ru) 2012-05-30
EP2194051B1 (en) 2011-08-31
AR062124A1 (es) 2008-10-15
EP2046779B1 (en) 2011-05-18
HK1130476A1 (en) 2009-12-31
MX2009000808A (es) 2009-01-29
TW200821301A (en) 2008-05-16
CN101535301A (zh) 2009-09-16
CA2831219A1 (en) 2008-01-31
NZ574425A (en) 2011-11-25
CN101535301B (zh) 2014-06-18
WO2008014360A3 (en) 2008-12-31
ATE509926T1 (de) 2011-06-15
KR20090033915A (ko) 2009-04-06
TW201414729A (zh) 2014-04-16
PE20080732A1 (es) 2008-06-13
DK2046779T3 (da) 2011-09-05
BRPI0715415A2 (pt) 2014-01-21
US20080027084A1 (en) 2008-01-31
CA2659253A1 (en) 2008-01-31
TWI421249B (zh) 2014-01-01
AU2007279333B2 (en) 2012-07-26
SG158924A1 (en) 2010-02-26
ATE522522T1 (de) 2011-09-15
IL196427A (en) 2013-02-28
IL206679A0 (en) 2010-12-30
JP2009544756A (ja) 2009-12-17
CY1111744T1 (el) 2015-10-07
US8049019B2 (en) 2011-11-01
EA200900245A1 (ru) 2009-08-28

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