PE20021084A1 - Ciclobuten-1,2-dionas 3,4-di-substituidas como ligandos del receptor de cxc-quimiocina - Google Patents

Ciclobuten-1,2-dionas 3,4-di-substituidas como ligandos del receptor de cxc-quimiocina

Info

Publication number
PE20021084A1
PE20021084A1 PE2002000318A PE2002000318A PE20021084A1 PE 20021084 A1 PE20021084 A1 PE 20021084A1 PE 2002000318 A PE2002000318 A PE 2002000318A PE 2002000318 A PE2002000318 A PE 2002000318A PE 20021084 A1 PE20021084 A1 PE 20021084A1
Authority
PE
Peru
Prior art keywords
cyclobuten
cxc
substituted
dionas
ligands
Prior art date
Application number
PE2002000318A
Other languages
English (en)
Inventor
Richard W Bond
Michael Dwyer
Johan A Ferreira
Jianhua Chao
Cynthia J Aki
Younong Yu
Ge Li
Nelson
J Robert Merrit
Bernd Kaiser
Laura Rokosz
Arthur G Taveras
John J Baldwin
Jianping Chao
Original Assignee
Schering Corp
Pharmacopeia Drug Discovery
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 Schering Corp, Pharmacopeia Drug Discovery filed Critical Schering Corp
Publication of PE20021084A1 publication Critical patent/PE20021084A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
    • C07D231/38—Nitrogen atoms
    • 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
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C225/00—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
    • C07C225/20—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/30—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C07C255/59—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
    • 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/52—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/30—Hetero atoms other than halogen
    • C07D333/36—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/04—Systems containing only non-condensed rings with a four-membered ring

Landscapes

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

Abstract

SE FERIERE A CICLOBUTEN-1,2-DIONAS 3,4-DI-SUBSTITUIDAS DE FORMULA I DONDE A ES EL GRUPO a, b, ENTRE OTROS; R7 Y R8 SON H, ALQUILO, ARILO, HETEROARILO, HETEROARILALQUILO, ENTRE OTROS; R9 ES R7, R8, HALOGENO, CF3, -COR7, -OR7, ENTRE OTROS; B ES EL GRUPO a, ENTRE OTROS; R2 ES H, OH, C(O)OH, SH, ENTRE OTROS; R3 Y R4 SON H, HALOGENO, ALQUILO, ALCOXI, ENTRE OTROS; R5 Y R6 SON H, HALOGENO, ALQUILO, ALCOXI, ENTRE OTROS. LOS COMPUESTOS DE FORMULA I SON LIGANDOS DEL RECEPTOR DE CXC-QUIMIOCINA Y SON UTILES PARA EL TRATAMIENTO DE ENFERMEDADES INFLAMATORIAS
PE2002000318A 2001-04-16 2002-04-16 Ciclobuten-1,2-dionas 3,4-di-substituidas como ligandos del receptor de cxc-quimiocina PE20021084A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US28402601P 2001-04-16 2001-04-16

Publications (1)

Publication Number Publication Date
PE20021084A1 true PE20021084A1 (es) 2002-12-20

Family

ID=23088576

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2002000318A PE20021084A1 (es) 2001-04-16 2002-04-16 Ciclobuten-1,2-dionas 3,4-di-substituidas como ligandos del receptor de cxc-quimiocina

Country Status (30)

Country Link
EP (2) EP1381590B1 (es)
JP (3) JP4499993B2 (es)
KR (2) KR100952531B1 (es)
CN (2) CN1990457A (es)
AR (1) AR035825A1 (es)
AT (2) ATE458715T1 (es)
AU (3) AU2002311841B2 (es)
BR (1) BRPI0208957B8 (es)
CA (1) CA2444031C (es)
CY (2) CY1109908T1 (es)
CZ (1) CZ20032831A3 (es)
DE (2) DE60235507D1 (es)
DK (2) DK1381590T3 (es)
EC (1) ECSP034809A (es)
ES (2) ES2287284T3 (es)
HU (1) HUP0401783A3 (es)
IL (3) IL158262A0 (es)
MX (1) MXPA03009441A (es)
MY (2) MY138202A (es)
NO (2) NO330790B1 (es)
NZ (3) NZ543869A (es)
PE (1) PE20021084A1 (es)
PL (2) PL208928B1 (es)
PT (2) PT1818325E (es)
RU (1) RU2344123C9 (es)
SI (2) SI1818325T1 (es)
SK (1) SK287598B6 (es)
TW (2) TWI316930B (es)
WO (1) WO2002083624A1 (es)
ZA (1) ZA200307905B (es)

Families Citing this family (75)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040106794A1 (en) 2001-04-16 2004-06-03 Schering Corporation 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
US7132445B2 (en) 2001-04-16 2006-11-07 Schering Corporation 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
CN1599734A (zh) 2001-10-12 2005-03-23 先灵公司 作为cxc趋化因子受体拮抗剂的3,4－二取代的马来酰亚胺化合物
US8246969B2 (en) 2001-11-16 2012-08-21 Skinmedica, Inc. Compositions containing aromatic aldehydes and their use in treatments
US6878709B2 (en) 2002-01-04 2005-04-12 Schering Corporation 3,4-di-substituted pyridazinediones as CXC chemokine receptor antagonists
WO2003080053A1 (en) 2002-03-18 2003-10-02 Schering Corporation Combination treatments for chemokine-mediated diseases
GB0218326D0 (en) * 2002-08-07 2002-09-11 Glaxo Group Ltd Compounds
EP1551818B1 (en) 2002-10-09 2009-02-04 Schering Corporation Thiadiazoledioxides and thiadiazoleoxides as cxc- and cc-chemokine receptor ligands
GB0302094D0 (en) 2003-01-29 2003-02-26 Pharmagene Lab Ltd EP4 receptor antagonists
EP2258365B1 (en) 2003-03-28 2013-05-29 Novartis Vaccines and Diagnostics, Inc. Use of organic compounds for immunopotentiation
DE502004009440D1 (de) * 2003-04-03 2009-06-10 Merck Patent Gmbh Pyrrolidin-1,2-dicarbonsäure-1-(phenylamid)-2-(4-(3-oxo-morpholin-4-yl)-phenylamid) derivate und verwandte verbindungen als inhibitoren des koagulationsfaktors xa zur behandlung von thromboembolischen erkrankungen
CN100448860C (zh) * 2003-04-18 2009-01-07 先灵公司 合成2－羟基－n,n－二甲基－3－[[2－[[1(r)－(5－甲基－2－呋喃基)丙基]氨基]－3,4－二氧代－1－环丁烯－1－基]氨基]苯甲酰胺
BRPI0412259B1 (pt) 2003-07-22 2019-08-20 Astex Therapeutics Limited Compostos de 1H-pirazol 3,4-dissubstituídos como moduladores de quinases dependentes de ciclina (CDK), seus usos, processo para a preparação dos mesmos e composição farmacêutica
GB0320983D0 (en) * 2003-09-08 2003-10-08 Biofocus Plc Compound libraries
ATE452882T1 (de) 2003-09-23 2010-01-15 Fermion Oy Herstellung von quetiapin
GB0324269D0 (en) 2003-10-16 2003-11-19 Pharmagene Lab Ltd EP4 receptor antagonists
DE602004016211D1 (en) 2003-12-19 2008-10-09 Schering Corp Thiadiazole als cxc- und cc-chemokinrezeptorliganden
WO2005068460A1 (en) 2003-12-22 2005-07-28 Schering Corporation Isothiazole dioxides as cxc- and cc- chemokine receptor ligands
MXPA06008599A (es) * 2004-01-30 2006-08-28 Schering Corp Polimorfos cristalinos de un ligando receptor de cxc-quimiocina.
CN1946690A (zh) * 2004-02-27 2007-04-11 先灵公司 用作丙型肝炎病毒ns3丝氨酸蛋白酶抑制剂的含环丁烯二酮基团化合物
CN101039652A (zh) 2004-08-16 2007-09-19 宝洁公司 2－(氨基或取代的氨基)－5,6－取代的苯酚化合物，包含该化合物的染料组合物以及它们的应用
EP1634573A1 (en) * 2004-08-16 2006-03-15 The Procter and Gamble Company 2-(Amino or substituted Amino)-5,6-substituted Phenol compounds, dyeing compositions containing them, and use thereof
TW200626138A (en) 2004-09-20 2006-08-01 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as therapeutic agents
CA2580855A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
CA2580857A1 (en) 2004-09-20 2006-09-28 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
MX2007003318A (es) 2004-09-20 2007-05-18 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como agentes terapeuticos.
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
MX2007003319A (es) 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como agentes terapeuticos.
US8071603B2 (en) 2004-09-20 2011-12-06 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
ES2327840T3 (es) 2004-12-23 2009-11-04 Gpc Biotech Ag Derivados de acido escuarico con actividad antiproliferativa.
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
EP2029138A1 (en) 2005-06-03 2009-03-04 Xenon Pharmaceuticals Inc. Aminothiazole derivatives as human stearoyl-coa desaturase inhibitors
US7718678B2 (en) 2005-06-29 2010-05-18 Schering Corporation Di-substituted oxadiazoles as CXC-chemokine receptor ligands
DE602006017849D1 (de) * 2005-06-29 2010-12-09 Schering Corp 5,6-disubstituierte oxadiazolopyrazine und thiadiazolopyrazine als liganden des cxc-chemokinrezeptors
DE102005035742A1 (de) * 2005-07-29 2007-02-01 Merck Patent Gmbh Quadratsäurederivate II
PL1951663T3 (pl) * 2005-11-24 2017-01-31 Dompé Farmaceutici S.P.A. Pochodne (R)-aryloalkiloaminowe i zawierające je kompozycje farmaceutyczne
CN101448778A (zh) * 2006-05-26 2009-06-03 艾博特公司 Polo样激酶的抑制剂
JP2009539990A (ja) * 2006-06-12 2009-11-19 シェーリング コーポレイション Ｃｘｃｒ２またはｃｘｃｒ１とｃｘｃｒ２との両方のいずれかの選択的アンタゴニストの薬学的処方物および組成物ならびに炎症性障害を治療するためにそれらを使用する方法
TW200813033A (en) * 2006-07-07 2008-03-16 Schering Corp 3, 4-di-substituted cyclobutene-1, 2-diones as CXC-chemokine receptor ligands
US8450348B2 (en) 2007-02-21 2013-05-28 Forma Tm, Llc Derivatives of squaric acid with anti-proliferative activity
BRPI0812222A2 (pt) * 2007-06-06 2014-12-16 Novartis Ag Compostos ciclobutenodiona substituídos anti-inflamatórios.
CA2692269A1 (en) * 2007-07-03 2009-01-08 Schering Corporation Process and intermediates for the synthesis of 1,2-substituted 3,4-dioxo-1-cyclobutene compounds
CN102123988B (zh) * 2008-06-24 2013-08-14 顶标公司 作为烟酰胺抑制剂的方酸衍生物
UA103198C2 (en) 2008-08-04 2013-09-25 Новартис Аг Squaramide derivatives as cxcr2 antagonists
WO2010063802A1 (en) * 2008-12-05 2010-06-10 Novartis Ag 3, 4-di-substituted cyclobutene- 1, 2 -diones as cxcr2 receptor antagonists
CA2799154A1 (en) 2010-05-12 2011-11-17 Abbvie Inc. Indazole inhibitors of kinase
FR2961695B1 (fr) * 2010-06-29 2012-07-06 Galderma Res & Dev Utilisation de composes dans le traitement ou la prevention de troubles cutanes
SG10202009963PA (en) 2011-01-07 2020-11-27 Allergan Inc Melanin modification compositions and methods of use
EP2760821B1 (en) 2011-09-02 2017-10-11 Novartis AG Choline salt of an anti-inflammatory substituted cyclobutenedione compound
FR2981934B1 (fr) 2011-10-28 2013-12-20 Galderma Res & Dev Nouveaux composes di-substitues de la diamino-3,4-cyclobutene-3-dione-1,2 utiles dans le traitement de pathologies mediees par des chimiokines.
FR2981935B1 (fr) * 2011-10-28 2015-08-07 Galderma Res & Dev Nouveaux composes di-substitues de la diamino-3,4-cyclobutene-3-dione-1,2 utiles dans le traitement de pathologies mediees par des chimiokines.
FR2981936B1 (fr) 2011-10-28 2013-12-20 Galderma Res & Dev Nouveaux composes di-substitues de la diamino-3,4-cyclobutene-3-dione-1,2 utiles dans le traitement de pathologies mediees par des chimiokines.
CN103242210B (zh) * 2012-02-09 2014-09-24 北京艾百诺科技有限公司 含有取代方酸的乙酸妙林酯及其应用
MX2014011115A (es) 2012-03-16 2015-03-13 Axikin Pharmaceuticals Inc Inhibidores de 3,5-diaminopirazol cinasa.
US8889730B2 (en) 2012-04-10 2014-11-18 Pfizer Inc. Indole and indazole compounds that activate AMPK
CN103382192A (zh) * 2012-05-04 2013-11-06 同创医药(苏州)有限公司 N-单取代哌嗪衍生物的制备
CA2905242C (en) 2013-03-15 2016-11-29 Pfizer Inc. Indole compounds that activate ampk
CN103214327A (zh) * 2013-03-22 2013-07-24 郑州泰基鸿诺药物科技有限公司 一种芳香环或芳杂环三氟甲基酮化合物及其制备方法
US10046002B2 (en) 2013-08-02 2018-08-14 Syntrix Biosystems Inc. Method for treating cancer using chemokine antagonists
US10561676B2 (en) * 2013-08-02 2020-02-18 Syntrix Biosystems Inc. Method for treating cancer using dual antagonists of CXCR1 and CXCR2
NZ631142A (en) 2013-09-18 2016-03-31 Axikin Pharmaceuticals Inc Pharmaceutically acceptable salts of 3,5-diaminopyrazole kinase inhibitors
MY191736A (en) 2014-12-23 2022-07-13 Axikin Pharmaceuticals Inc 3,5-diaminopyrazole kinase inhibitors
FR3030515B1 (fr) 2014-12-23 2017-01-20 Galderma Res & Dev Nouveaux composes antagonistes des recepteurs cxcr1 et cxcr2 aux chimiokines, et leur utilisation dans le traitement de pathologies mediees par des chimiokines
TWI724056B (zh) 2015-11-19 2021-04-11 美商卡默森屈有限公司 Ｃｘｃｒ２抑制劑
TWI734715B (zh) * 2015-11-19 2021-08-01 美商卡默森屈有限公司 趨化因子受體調節劑
WO2018073248A1 (en) 2016-10-17 2018-04-26 Icm (Institut Du Cerveau Et De La Moelle Épinière) Prognosis of demyelinating diseases patients and treatment thereof
RU2020106383A (ru) * 2017-08-14 2021-09-16 Аллерган, Инк. 3,4-двузамещенные 3-циклобутен-1,2-дионы и их применение
US11052065B2 (en) 2017-09-27 2021-07-06 Merck Sharp & Dohme Corp. Compositions and methods for treating cancer with a combination of programmed death receptor (PD-1) antibodies and a CXCR2 antagonist
IL275839B2 (en) 2018-01-08 2024-02-01 Chemocentryx Inc Methods for the treatment of generalized abscess psoriasis using a CCR6 or CXCR2 antagonist
UA128700C2 (uk) 2018-09-21 2024-10-02 Пфайзер Інк. N-заміщені діоксоциклобутеніламіно-3-гідроксипіколінаміди, прийнятні як інгібітори ccr6
CN110041309B (zh) * 2019-04-04 2022-01-28 广东工业大学 一种2-羧基哌嗪连接的他克林-8-氨基(羟基)喹啉衍生物及制备与应用
MX2022004145A (es) * 2019-10-07 2022-06-14 De Shaw Res Llc Compuestos heterociclicos de arilmetileno como bloqueadores del canal de potasio tipo shaker kv1.3.
KR102710925B1 (ko) * 2021-06-01 2024-09-27 부산대학교 산학협력단 신규 스퀘어아마이드 유도체 및 이의 용도
CN118339161B (zh) * 2021-12-10 2025-12-09 正大天晴药业集团股份有限公司 一种异噻唑并[5,4-d]嘧啶类IRAK4抑制剂的制备方法

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0692915A (ja) * 1992-07-28 1994-04-05 Sumitomo Metal Ind Ltd １，２−ジアミノシクロブテン−３，４−ジオン誘導体及びその用途
GB9312210D0 (en) * 1993-06-14 1993-07-28 Smithkline Beecham Plc Chemical compounds
GB9316111D0 (en) * 1993-08-04 1993-09-22 Pfizer Ltd Benzopyrans
US5354763A (en) * 1993-11-17 1994-10-11 American Home Products Corporation Substituted N-heteroaryl and N-aryl-1,2-diaminocyclobutene-3,4-diones
US5466712A (en) * 1994-11-04 1995-11-14 American Home Products Corporation Substituted n-aryl-1,2-diaminocyclobutene-3,4-diones
DK0796243T3 (da) * 1994-11-16 1999-09-13 American Home Prod Diaminocyclobuten-3,4-dioner
KR20000022273A (ko) * 1996-06-27 2000-04-25 스튜어트 알. 수터, 스티븐 베네티아너, 피터 존 기딩스 Il-8 수용체 길항제
US5840764A (en) * 1997-01-30 1998-11-24 American Home Products Corporation Substituted hydroxy-anilino derivatives of cyclobutene-3,4-diones
AU6250298A (en) * 1997-01-30 1998-08-25 American Home Products Corporation Substituted hydroxy-anilino derivatives of cyclobutene-3,4-diones
US6211220B1 (en) * 1998-11-23 2001-04-03 Cell Pathways, Inc. Method for treating neoplasia with amino or pyridylamino cyclobutene derivatives
AU2357600A (en) * 1998-12-14 2000-07-03 American Home Products Corporation 3,4-diamino-3-cyclobutene-1,2-dione derivatives which inhibit leukocyte adhesionmediated by vla-4
ID30235A (id) * 1998-12-16 2001-11-15 Bayer Ag Senyawa bifenil dan analognya sebagai antagonis-antagonis integrin
US6518283B1 (en) * 1999-05-28 2003-02-11 Celltech R&D Limited Squaric acid derivatives
AR033803A1 (es) * 2000-03-01 2004-01-07 Smithkline Beecham Corp Compuestos de dianilino escuarano, composiciones farmaceuticas que los comprenden, y el uso de los mismos en la fabricacion de medicamentos para tratar enfermedades mediadas por quimioquinas
CN1454204A (zh) * 2000-05-30 2003-11-05 史密丝克莱恩比彻姆公司 Il－8受体拮抗剂
ATE346043T1 (de) * 2001-01-16 2006-12-15 Smithkline Beecham Corp Il-8-rezeptorantagonisten
HUP0500644A3 (en) * 2001-03-30 2005-11-28 Smithkline Beecham Corp Method of synthesizing phenol-containing compounds
WO2003080053A1 (en) * 2002-03-18 2003-10-02 Schering Corporation Combination treatments for chemokine-mediated diseases

Also Published As

Publication number Publication date
PL208928B1 (pl) 2011-06-30
AR035825A1 (es) 2004-07-14
NZ560453A (en) 2009-03-31
WO2002083624A1 (en) 2002-10-24
MY138202A (en) 2009-05-29
SI1381590T1 (sl) 2007-10-31
EP1818325B1 (en) 2010-02-24
HK1057538A1 (en) 2004-04-08
TWI316930B (en) 2009-11-11
ECSP034809A (es) 2004-02-26
AU2006203679A1 (en) 2006-09-14
CA2444031A1 (en) 2002-10-24
KR100952531B1 (ko) 2010-04-12
ATE458715T1 (de) 2010-03-15
DE60220778T2 (de) 2008-03-06
EP1381590A1 (en) 2004-01-21
PL367129A1 (en) 2005-02-21
JP2009179641A (ja) 2009-08-13
DK1818325T3 (da) 2010-05-31
JP5294418B2 (ja) 2013-09-18
CN1289471C (zh) 2006-12-13
EP1818325A3 (en) 2008-02-13
CN1990457A (zh) 2007-07-04
NO20110050L (no) 2003-12-08
NO330790B1 (no) 2011-07-18
AU2010212484B2 (en) 2012-04-12
MY149050A (en) 2013-07-15
BRPI0208957B1 (pt) 2018-10-09
JP2004532846A (ja) 2004-10-28
NZ543869A (en) 2007-09-28
EP1381590B1 (en) 2007-06-20
TW200736196A (en) 2007-10-01
NO20034612D0 (no) 2003-10-15
PT1381590E (pt) 2007-08-06
IL201754A0 (en) 2010-06-16
AU2002311841B2 (en) 2006-09-14
SK12882003A3 (sk) 2004-06-08
SI1818325T1 (sl) 2010-06-30
DE60235507D1 (de) 2010-04-08
CA2444031C (en) 2012-02-21
SK287598B6 (sk) 2011-03-04
JP2010053151A (ja) 2010-03-11
PL207255B1 (pl) 2010-11-30
KR20030092074A (ko) 2003-12-03
BRPI0208957B8 (pt) 2021-05-25
DK1381590T3 (da) 2007-10-22
KR20100008794A (ko) 2010-01-26
CN1516687A (zh) 2004-07-28
CY1109908T1 (el) 2014-09-10
RU2344123C2 (ru) 2009-01-20
ATE365154T1 (de) 2007-07-15
IL158262A (en) 2012-05-31
NO20034612L (no) 2003-12-08
MXPA03009441A (es) 2004-02-12
HUP0401783A2 (hu) 2005-01-28
RU2344123C9 (ru) 2009-05-20
BR0208957A (pt) 2004-06-22
HUP0401783A3 (en) 2005-06-28
HK1107818A1 (en) 2008-04-18
JP4499993B2 (ja) 2010-07-14
RU2003133448A (ru) 2005-06-10
ZA200307905B (en) 2005-03-30
ES2287284T3 (es) 2007-12-16
DE60220778D1 (en) 2007-08-02
PT1818325E (pt) 2010-05-12
ES2340207T3 (es) 2010-05-31
CZ20032831A3 (cs) 2004-03-17
IL158262A0 (en) 2004-05-12
EP1818325A2 (en) 2007-08-15
CY1109989T1 (el) 2014-09-10
NZ529551A (en) 2006-02-24
AU2010212484A1 (en) 2010-09-09

Similar Documents

Publication Publication Date Title
PE20021084A1 (es) Ciclobuten-1,2-dionas 3,4-di-substituidas como ligandos del receptor de cxc-quimiocina
PE20030703A1 (es) Inhibidores de la 17b-hidroxiesteroide deshidrogenasa tipo 3
AR035234A1 (es) Aril y biaril-piperidinas con actividad moduladora mch, metodo para preparar dichos compuestos, composiciones farmaceuticas, metodo para preparar las composiciones farmaceuticas y el uso de dichos compuestos para la manufactura de un medicamento
PE20050767A1 (es) Amino-benzazoles como inhibidores del receptor p2y1
ECSP056105A (es) Acidos carboxilicos alfa sustituidos como moduladores ppar
PE20001467A1 (es) Derivados de 4-fenilpiridina como antagonistas del receptor de neuroquinina
AR029301A1 (es) Compuestos derivados de biarilo, metodos para su preparacion composiciones que los contienen, su uso como agonistas en receptores beta-adreno-receptores atipicos
PE20110588A1 (es) Derivados de benzotiazol como agentes anticancerigenos
NI200700157A (es) Análogos de rapamicina y los usos de los mismos en el tratamiento de trastornos neurológicos
AR054799A1 (es) Derivados de oxindol
CR11620A (es) Derivados de Imadazo-[1,2,b]-Piridazina para el Tratamiento de Enfermedad Mediada por Cinosa de Tirosina C-Met
PE20020657A1 (es) Derivados de amida de piperidinas 1,4-disustituidas de formula (i)
AR052866A1 (es) Fenil-metanonas monociclicas sustituidas
PE20011186A1 (es) Acidos malonamicos y derivados de los mismos como ligandos de receptor tiroideo
PE20021011A1 (es) Derivados quinazolinicos como inhibidores de la rho-quinasa
AR054024A1 (es) Derivados de piridina -3- carboxamida como agonistas inversos de cb1
CY1110025T1 (el) Παραγωγα ισοξαζολινης και η χρηση αυτων ως ζιζανιοκτονα
MA28729B1 (fr) Composés et procédés destinés à traiter la dyslipidémie
AR066421A1 (es) Compuestos derivados de piridona
CY1119787T1 (el) Υποκατεστημενα παραγωγα 2-[2-(φαινυλ)αιθυλαμινο] αλκαναμιδιου και η χρηση αυτων ως τροποποιητων του διαυλου νατριου και/ή ασβεστιου
AR040278A1 (es) Ligandos del receptor de glucocorticoides para el tratamiento de trastornos metabolicos
PE20060483A1 (es) Compuestos heterociclicos como antagonistas de nk1
PA8576101A1 (es) Difenilazetidinonas sustituidas en grupo acido, procedimiento para su preparacion, medicamentos que comprenden estos compuestos y su uso
PE20080136A1 (es) Arilsulfonamidas sustituidas como agentes antivirales
PE20030705A1 (es) Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3 para el tratamiento de enfermedades androgeno-dependientes

Legal Events

Date Code Title Description
FG Grant, registration
FD Application declared void or lapsed