CN1454086A - 高亲和性小分子C5a受体调节物 - Google Patents

高亲和性小分子C5a受体调节物 Download PDF

Info

Publication number
CN1454086A
CN1454086A CN00819935A CN00819935A CN1454086A CN 1454086 A CN1454086 A CN 1454086A CN 00819935 A CN00819935 A CN 00819935A CN 00819935 A CN00819935 A CN 00819935A CN 1454086 A CN1454086 A CN 1454086A
Authority
CN
China
Prior art keywords
alkyl
base
group
substituted
alkynyl
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN00819935A
Other languages
English (en)
Chinese (zh)
Inventor
A·瑟考夫
张小燕
何夏树
赵何
J·彼得森
G·梅南德
R·奥利格
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Neurogen Corp
Original Assignee
Neurogen 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 Neurogen Corp filed Critical Neurogen Corp
Publication of CN1454086A publication Critical patent/CN1454086A/zh
Pending legal-status Critical Current

Links

Classifications

    • 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
    • C07D207/30—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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—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 two 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
    • C07D207/325—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 two 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 with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • C07D207/327—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82B—NANOSTRUCTURES FORMED BY MANIPULATION OF INDIVIDUAL ATOMS, MOLECULES, OR LIMITED COLLECTIONS OF ATOMS OR MOLECULES AS DISCRETE UNITS; MANUFACTURE OR TREATMENT THEREOF
    • B82B3/00—Manufacture or treatment of nanostructures by manipulation of individual atoms or molecules, or limited collections of atoms or molecules as discrete units
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • 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
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61P11/06—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
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • 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
    • 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
    • A61P31/04—Antibacterial 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • A61P7/06—Antianaemics
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/04—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • 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
    • C07D231/12—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • C07D333/06—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • H—ELECTRICITY
    • H01—ELECTRIC ELEMENTS
    • H01J—ELECTRIC DISCHARGE TUBES OR DISCHARGE LAMPS
    • H01J1/00—Details of electrodes, of magnetic control means, of screens, or of the mounting or spacing thereof, common to two or more basic types of discharge tubes or lamps
    • H01J1/02—Main electrodes
    • H01J1/30—Cold cathodes, e.g. field-emissive cathode

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Nanotechnology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Manufacturing & Machinery (AREA)
CN00819935A 2000-09-29 2000-09-29 高亲和性小分子C5a受体调节物 Pending CN1454086A (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US2000/026816 WO2002049993A2 (en) 2000-09-29 2000-09-29 High affinity small molecule c5a receptor modulators

Publications (1)

Publication Number Publication Date
CN1454086A true CN1454086A (zh) 2003-11-05

Family

ID=21741822

Family Applications (1)

Application Number Title Priority Date Filing Date
CN00819935A Pending CN1454086A (zh) 2000-09-29 2000-09-29 高亲和性小分子C5a受体调节物

Country Status (13)

Country Link
EP (1) EP1322309B1 (https=)
JP (1) JP5260818B2 (https=)
KR (1) KR20030060887A (https=)
CN (1) CN1454086A (https=)
AT (1) ATE404553T1 (https=)
AU (1) AU7622500A (https=)
BR (1) BR0017338A (https=)
DE (1) DE60039921D1 (https=)
IL (1) IL154993A0 (https=)
MX (1) MXPA03002788A (https=)
NO (1) NO20031370L (https=)
WO (1) WO2002049993A2 (https=)
YU (1) YU23503A (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114957165A (zh) * 2021-02-26 2022-08-30 清华大学 一种抗病毒化合物及其制备方法和应用

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PA8535601A1 (es) 2000-12-21 2002-11-28 Pfizer Derivados benzimidazol y piridilimidazol como ligandos para gabaa
US6858637B2 (en) 2002-03-28 2005-02-22 Neurogen Corporation Substituted biaryl amides as C5a receptor modulators
AU2003218374A1 (en) 2002-03-28 2003-10-13 Neurogen Corporation Substituted tetrahydroisoquinolines as c5a receptor modulators
EP1487796A4 (en) * 2002-03-28 2005-11-16 Neurogen Corp SUBSTITUTED BIARYLAMIDES AS MODULATORS OF THE C5A RECEPTOR
CA2480888A1 (en) * 2002-03-29 2003-10-09 Neurogen Corporation New aryl imidazoles and related compounds as c5a receptor modulators
GB0214139D0 (en) * 2002-06-19 2002-07-31 Glaxo Group Ltd Chemical compounds
WO2004018460A1 (en) * 2002-08-21 2004-03-04 Neurogen Corporation Amino methyl imidazoles as c5a receptor modulators
CN100528846C (zh) * 2002-09-11 2009-08-19 株式会社吴羽 胺化合物及其用途
ATE552253T1 (de) 2002-11-08 2012-04-15 Novartis Int Pharm Ltd 3-substituierte-6-aryl- pyridin derivate als liganden für c5a-rezeptoren
US8329169B2 (en) 2003-05-15 2012-12-11 Genentech, Inc. Methods and compositions for the prevention and treatment of sepsis
US7932281B2 (en) 2004-03-10 2011-04-26 Kureha Corporation Amine-based compound and use thereof
WO2006012373A2 (en) * 2004-07-20 2006-02-02 Critical Therapeutics, Inc. Combination therapies of hmgb and complement inhibitors against inflammation
JP2007284352A (ja) * 2004-08-05 2007-11-01 Dai Ichi Seiyaku Co Ltd ピラゾール誘導体
AR055287A1 (es) 2004-12-01 2007-08-15 Kalypsys Inc Inhibidores de la dimerizacion de la sintasa inducible por oxido nitrico ,composiciones farmaceuticas
EP1856126A2 (en) 2005-02-17 2007-11-21 Wyeth a Corporation of the State of Delaware Cycloalkylfused indole, benzothiophene, benzofuran and indene derivatives
EP1739078A1 (de) 2005-05-30 2007-01-03 Jerini AG C5a-Rezeptor-Antagonisten
CA2965223C (en) 2008-12-22 2019-09-24 Chemocentryx, Inc. C5ar antagonists
PT2585064T (pt) 2010-06-24 2017-08-08 Chemocentryx Inc Antagonistas do c5ar
AU2014257164B2 (en) * 2013-04-22 2018-10-11 Abbvie Inc. Thiazoles and uses thereof
NZ730123A (en) 2014-09-29 2023-05-26 Chemocentryx Inc Processes and intermediates in the preparation of c5ar antagonists
EP3072891A1 (en) * 2015-03-24 2016-09-28 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. New Toll-Like Receptor 9 Antagonists
CN108601790B (zh) 2016-01-14 2026-01-27 凯莫森特里克斯股份有限公司 C3肾小球病的治疗方法
AU2017246228B2 (en) 2016-04-04 2021-04-15 Chemocentryx, Inc. Soluble C5aR antagonists
WO2018222601A1 (en) 2017-05-31 2018-12-06 Chemocentryx, Inc. 5-5 FUSED RINGS AS C5a INHIBITORS
CN110997674B (zh) 2017-05-31 2022-12-20 凯莫森特里克斯股份有限公司 作为C5a抑制剂的6-5稠合环类
KR20200109298A (ko) 2017-10-30 2020-09-22 케모센트릭스, 인크. 면역조절제로서의 중수소화된 화합물
MX2020006460A (es) 2017-12-22 2020-11-06 Chemocentryx Inc Compuestos de anillo 5,5 fusionado sustituido con diarilo como inhibidores de c5ar.
ES2980175T3 (es) 2017-12-22 2024-09-30 Chemocentryx Inc Compuestos anulares fusionados en 6,5 sustituidos con diarilo como inhibidores de C5aR
WO2019195159A1 (en) 2018-04-02 2019-10-10 Chemocentryx, Inc. PRODRUGS OF FUSED-BICYCLIC C5aR ANTAGONISTS

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6157590A (ja) * 1984-08-29 1986-03-24 Asahi Shiyueebell Kk シラン化合物およびその製造法
US5681956A (en) * 1990-12-28 1997-10-28 Neurogen Corporation 4-aryl substituted piperazinylmethyl phenylimidazole derivatives; a new class of dopamine receptor subtype specific ligands
US5159083A (en) * 1990-12-28 1992-10-27 Neurogen Corporation Certain aminomethyl phenylimidazole derivatives; a class of dopamine receptor subtype specific ligands
MX9308025A (es) * 1992-12-22 1994-08-31 Lilly Co Eli Compuestos inhibidores de la proteasa del virus dela inmunodeficiencia humana, procedimiento para supreparacion y formulacion farmaceutica que los contiene.
US5652237A (en) * 1994-09-09 1997-07-29 Warner-Lambert Company 2-substituted-4H-3, 1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease for the treatment of inflammatory processes
AU4368996A (en) * 1994-11-23 1996-06-17 Neurogen Corporation Certain 4-aminomethyl-2-substituted imidazole derivatives and 2-aminomethyl-4-substituted imidazole derivatives; new classes of dopamine receptor subtype specific ligands
GB9426103D0 (en) * 1994-12-23 1995-02-22 Merck Sharp & Dohme Therapeutic agents
ID19609A (id) * 1996-07-13 1998-07-23 Glaxo Group Ltd Senyawa-senyawa heterosiklik
EP1017382B1 (en) * 1997-05-29 2006-03-01 Merck & Co., Inc. (a New Jersey corp.) Biarylalkanoic acids as cell adhesion inhibitors
MY153569A (en) * 1998-01-20 2015-02-27 Mitsubishi Tanabe Pharma Corp Inhibitors of ?4 mediated cell adhesion
ES2255251T3 (es) * 1998-03-20 2006-06-16 Daiichi Asubio Pharma Co., Ltd. Inhibidores de nf-kb que contienen derivados de benzoquinona.
ATE316961T1 (de) * 1998-05-22 2006-02-15 Scios Inc Heterozyclische derivate für die behandlung von herzversagen und andere erkrankungen
CN1309638A (zh) * 1998-07-10 2001-08-22 阿斯特拉曾尼卡有限公司 作为神经激肽受体拮抗剂的n－取代的萘甲酰胺
US6423519B1 (en) * 1998-07-15 2002-07-23 Gpc Biotech Inc. Compositions and methods for inhibiting fungal growth
ID27787A (id) * 1998-08-21 2001-04-26 Viro Pharma Inc Senyawa, komposisi dan metode untuk pengobatan atau pencegahan infeksi yang disebabkan oleh virus dan penyakit-penyakit yang berkaitan
US6437146B1 (en) * 1998-09-25 2002-08-20 Fujisawa Pharmaceutical Co., Ltd. Oxazole compounds as prostaglandin e2 agonists or antagonists
WO2000025780A1 (en) * 1998-10-29 2000-05-11 Bristol-Myers Squibb Company Compounds derived from an amine nucleus that are inhibitors of impdh enzyme
US6503905B1 (en) * 1998-12-29 2003-01-07 Pfizer Inc 3,3-biarylpiperidine and 2,2-biarylmorpholine derivatives
BR0010655A (pt) * 1999-03-24 2002-02-13 Anormed Inc Compostos heterocìclicos para ligação ao receptor de quimiocina
US6369226B1 (en) * 1999-06-21 2002-04-09 Agouron Pharmaceuticals, Inc. Substituted benzamide inhibitors of rhinovirus 3C protease
EP1218358B1 (en) * 1999-09-23 2006-09-13 AstraZeneca AB Therapeutic quinazoline compounds
PT1317451E (pt) * 2000-09-15 2006-12-29 Anormed Inc Compostos heterocíclicos que se ligam a receptores de quimioquinas

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114957165A (zh) * 2021-02-26 2022-08-30 清华大学 一种抗病毒化合物及其制备方法和应用

Also Published As

Publication number Publication date
NO20031370L (no) 2003-05-30
MXPA03002788A (es) 2004-12-13
WO2002049993A2 (en) 2002-06-27
WO2002049993A3 (en) 2003-02-20
DE60039921D1 (de) 2008-09-25
NO20031370D0 (no) 2003-03-26
EP1322309A4 (en) 2004-10-13
JP5260818B2 (ja) 2013-08-14
EP1322309A2 (en) 2003-07-02
BR0017338A (pt) 2004-04-27
ATE404553T1 (de) 2008-08-15
KR20030060887A (ko) 2003-07-16
AU7622500A (en) 2002-07-01
IL154993A0 (en) 2003-10-31
YU23503A (sh) 2006-03-03
EP1322309B1 (en) 2008-08-13
JP2004525873A (ja) 2004-08-26

Similar Documents

Publication Publication Date Title
CN1454086A (zh) 高亲和性小分子C5a受体调节物
CN1158256C (zh) 吡咯烷衍生物-ccr-3受体拮抗剂
CN1192773C (zh) 环胺ccr3拮抗剂
CN1049654C (zh) 哌嗪衍生物及含其的药物组合物和用途
CN1660815A (zh) 环胺衍生物及其作为药物的用途
CN1443170A (zh) 辣椒素受体配体
CN1443167A (zh) 用于治疗5－羟色胺相关性疾病的氮杂环化合物
CN1615300A (zh) 苯并咪唑衍生物以及它们作为gnrh拮抗剂的用途
CN1246856A (zh) 芳基和杂芳基取代的稠合吡咯抗炎药
CN1143848C (zh) 用作毒蕈碱性受体拮抗剂的2-芳基乙基-(哌啶-4-基甲基)胺衍生物
CN1756746A (zh) 作为阿片样物质受体拮抗剂的6－取代的烟酰胺衍生物
CN1184425A (zh) 5－取代－3－(1,2,3,6－四氢吡啶－4－基)－和3－(哌啶－4－基)－1h－吲哚:新型5－ht1f激动剂
CN1173867A (zh) 吲哚基神经肽y受体拮抗剂
CN1708476A (zh) 具有mch－拮抗作用的新颖酰胺化合物及包括这些化合物的药物
CN1732154A (zh) 具有mch拮抗作用的新颖炔类化合物及包括这些化合物的药物
CN1671386A (zh) 作为mch选择性拮抗剂的取代苯胺基哌啶
CN1633290A (zh) 抑制配体与高级糖化终产物受体相互作用的单和双环吡咯衍生物
CN1498211A (zh) 用作磷酸二酯酶4抑制剂的苯胺衍生物
CN1777584A (zh) 作为5－ht1f激动剂的(哌啶氧基)苯基、(哌啶氧基)吡啶基、(哌啶硫基)苯基和(哌啶硫基)吡啶基化合物
CN1608050A (zh) 哌嗪衍生物
CN1933830A (zh) 吲哚衍生物和其作为激酶抑制剂特别是ikk2抑制剂的用途
CN101048405A (zh) 芳基取代的哌嗪衍生物
CN1610664A (zh) 3－氮杂二环[3.1.0]己烷衍生物作为类阿片受体拮抗剂
CN1098264C (zh) 用于治疗变态反应疾病的取代的4－(1h－苯并咪唑－2－基－氨基)哌啶
CN1735595A (zh) 取代的烷基酰氨基哌啶

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1059899

Country of ref document: HK

C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication
REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 1059899

Country of ref document: HK