CN100369898C - 用作p38抑制剂的烟酰胺衍生物 - Google Patents

用作p38抑制剂的烟酰胺衍生物 Download PDF

Info

Publication number
CN100369898C
CN100369898C CNB038038064A CN03803806A CN100369898C CN 100369898 C CN100369898 C CN 100369898C CN B038038064 A CNB038038064 A CN B038038064A CN 03803806 A CN03803806 A CN 03803806A CN 100369898 C CN100369898 C CN 100369898C
Authority
CN
China
Prior art keywords
methyl
niacinamide
fluoro
phenyl
cyclopropyl
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.)
Expired - Lifetime
Application number
CNB038038064A
Other languages
English (en)
Chinese (zh)
Other versions
CN1633416A (zh
Inventor
N·M·阿斯顿
P·巴姆博罗格
A·L·沃克尔
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.)
SmithKline Beecham Corp
Original Assignee
SmithKline Beecham 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
Priority claimed from GBGB0203301.7A external-priority patent/GB0203301D0/en
Priority claimed from GB0225385A external-priority patent/GB0225385D0/en
Application filed by SmithKline Beecham Corp filed Critical SmithKline Beecham Corp
Publication of CN1633416A publication Critical patent/CN1633416A/zh
Application granted granted Critical
Publication of CN100369898C publication Critical patent/CN100369898C/zh
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/04Drugs for disorders of the respiratory system for throat disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/14Drugs for genital or sexual disorders; Contraceptives for lactation disorders, e.g. galactorrhoea
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/08Antiseborrheics
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/14Decongestants or antiallergics
    • 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
    • A61P3/08Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • A61P31/06Antibacterial agents for tuberculosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • A61P31/08Antibacterial agents for leprosy
    • 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
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06Antimalarials
    • 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
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • A61P39/02Antidotes
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • 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
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Virology (AREA)
  • Obesity (AREA)
CNB038038064A 2002-02-12 2003-02-10 用作p38抑制剂的烟酰胺衍生物 Expired - Lifetime CN100369898C (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB0203301.7 2002-02-12
GBGB0203301.7A GB0203301D0 (en) 2002-02-12 2002-02-12 Novel compounds
GB0225385A GB0225385D0 (en) 2002-10-31 2002-10-31 Novel compounds
GB0225385.4 2002-10-31

Publications (2)

Publication Number Publication Date
CN1633416A CN1633416A (zh) 2005-06-29
CN100369898C true CN100369898C (zh) 2008-02-20

Family

ID=27736200

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB038038064A Expired - Lifetime CN100369898C (zh) 2002-02-12 2003-02-10 用作p38抑制剂的烟酰胺衍生物

Country Status (25)

Country Link
US (5) US7125898B2 (https=)
EP (3) EP2258687B1 (https=)
JP (2) JP4472349B2 (https=)
KR (1) KR101058292B1 (https=)
CN (1) CN100369898C (https=)
AT (2) ATE485275T1 (https=)
AU (1) AU2003207298B2 (https=)
BR (1) BRPI0307351B8 (https=)
CA (1) CA2474192C (https=)
CO (1) CO5611147A2 (https=)
CY (2) CY1107117T1 (https=)
DE (2) DE60316913T2 (https=)
DK (2) DK1474395T3 (https=)
ES (2) ES2400486T3 (https=)
IL (1) IL163090A (https=)
IS (1) IS2520B (https=)
MX (1) MXPA04007838A (https=)
NO (1) NO327418B1 (https=)
NZ (1) NZ533865A (https=)
PL (1) PL212910B1 (https=)
PT (2) PT1864975E (https=)
RU (1) RU2309951C2 (https=)
SI (2) SI1864975T1 (https=)
WO (1) WO2003068747A1 (https=)
ZA (1) ZA200405602B (https=)

Families Citing this family (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20020506A1 (es) 2000-08-22 2002-07-09 Glaxo Group Ltd Derivados de pirazol fusionados como inhibidores de la proteina cinasa
GB0124936D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124939D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124938D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124934D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124931D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124933D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124941D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
EP2258687B1 (en) * 2002-02-12 2012-12-26 Glaxosmithkline LLC Nicotinamide derivates useful as P38 inhibitors
GB0209891D0 (en) 2002-04-30 2002-06-05 Glaxo Group Ltd Novel compounds
GB0217757D0 (en) 2002-07-31 2002-09-11 Glaxo Group Ltd Novel compounds
GB0308186D0 (en) 2003-04-09 2003-05-14 Smithkline Beecham Corp Novel compounds
GB0308201D0 (en) 2003-04-09 2003-05-14 Smithkline Beecham Corp Novel compounds
GB0308185D0 (en) * 2003-04-09 2003-05-14 Smithkline Beecham Corp Novel compounds
ATE482205T1 (de) * 2003-07-25 2010-10-15 Novartis Ag P-38-kinasehemmer
GB0318814D0 (en) * 2003-08-11 2003-09-10 Smithkline Beecham Corp Novel compounds
WO2005033079A1 (ja) 2003-09-30 2005-04-14 Eisai Co., Ltd. ヘテロ環化合物を含有する新規な抗真菌剤
GB0324790D0 (en) * 2003-10-24 2003-11-26 Astrazeneca Ab Amide derivatives
GB0402138D0 (en) * 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
GB0402140D0 (en) * 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
GB0402143D0 (en) * 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
GB0402137D0 (en) * 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
WO2006016548A1 (ja) * 2004-08-09 2006-02-16 Eisai R & D Management Co., Ltd. ヘテロ環化合物を含有する新規な抗マラリア剤
DK1789390T3 (da) 2004-09-02 2012-02-27 Genentech Inc Pyridyl-inhibitorer af hedgehog-signalering
US20080051416A1 (en) * 2004-10-05 2008-02-28 Smithkline Beecham Corporation Novel Compounds
JP4874958B2 (ja) 2005-03-30 2012-02-15 エーザイ・アール・アンド・ディー・マネジメント株式会社 ピリジン誘導体を含有する抗真菌剤
GB0512429D0 (en) * 2005-06-17 2005-07-27 Smithkline Beecham Corp Novel compound
WO2007031791A1 (en) 2005-09-16 2007-03-22 Arrow Therapeutics Limited Biphenyl derivatives and their use in treating hepatitis c
TWI385169B (zh) 2005-10-31 2013-02-11 Eisai R&D Man Co Ltd 經雜環取代之吡啶衍生物及含有彼之抗真菌劑
US20070254926A1 (en) * 2006-01-31 2007-11-01 Jun Jiang Pyridylphenyl compounds for inflammation and immune-related uses
JP2009528344A (ja) * 2006-02-28 2009-08-06 アストラゼネカ・アクチエボラーグ インドール誘導体の新規な塩及び医薬におけるその使用
GB0612026D0 (en) * 2006-06-16 2006-07-26 Smithkline Beecham Corp New use
RU2315040C1 (ru) * 2006-07-07 2008-01-20 Государственное образовательное учреждение высшего профессионального образования "Пермская государственная фармацевтическая академия Федерального агентства по здравоохранению и социальному развитию" (ГОУ ВПО ПГФА Росздрава) 3-гидроксипропиламид 4,6-диметил-1н-2-оксоникотиновой кислоты, проявляющий антикоагулянтную, противовоспалительную и анальгетическую активность
EP2065377B1 (en) 2006-09-21 2011-11-23 Eisai R&D Management Co., Ltd. Pyridine derivative substituted by heteroaryl ring, and antifungal agent comprising the same
WO2008071665A1 (en) * 2006-12-12 2008-06-19 Smithkline Beecham Corporation A nicotinamide derivative useful as p38 kinase inhibitor
WO2008136279A1 (ja) 2007-04-27 2008-11-13 Eisai R & D Management Co., Ltd. ヘテロ環置換ピリジン誘導体の塩またはその結晶
TW200841879A (en) 2007-04-27 2008-11-01 Eisai R&D Man Co Ltd Pyridine derivatives substituted by heterocyclic ring and phosphonoamino group, and anti-fungal agent containing same
GEP20125379B (en) 2007-05-03 2012-01-10 Pfizer Ltd 2 -pyridine carboxamide derivatives as sodium channel modulators
US20090099242A1 (en) 2007-08-15 2009-04-16 Cuny Gregory D Heterocyclic inhibitors of necroptosis
UY31322A1 (es) * 2007-09-05 2009-04-30 Amidas heterocíclicas y sus métodos de uso-975
WO2009034390A1 (en) * 2007-09-14 2009-03-19 Arrow Therapeutics Limited Heterocyclic derivatives and their use in treating hepatitis c
US8513287B2 (en) 2007-12-27 2013-08-20 Eisai R&D Management Co., Ltd. Heterocyclic ring and phosphonoxymethyl group substituted pyridine derivatives and antifungal agent containing same
US20090281089A1 (en) * 2008-04-11 2009-11-12 Genentech, Inc. Pyridyl inhibitors of hedgehog signalling
US8188119B2 (en) 2008-10-24 2012-05-29 Eisai R&D Management Co., Ltd Pyridine derivatives substituted with heterocyclic ring and γ-glutamylamino group, and antifungal agents containing same
US8713459B2 (en) 2009-05-29 2014-04-29 Jason Philip Yanchar Graphical planner
CN102633715B (zh) * 2012-03-23 2014-03-26 无锡爱内特营养保健品科技有限公司 一种丝裂原蛋白激酶p38的抑制剂及其制备方法
CA2879222A1 (en) 2012-07-17 2014-01-23 Glaxosmithkline Llc Nicotinamide derivate in the treatment of acute coronary syndrome
HUE046132T2 (hu) 2012-10-17 2020-02-28 Macrophage Pharma Ltd N-[2-{4-[6-amino-5-(2,4-difluor-benzoil)-2-oxopiridin-1(2H)-il]-3,5-difluor-fenil}etil]-l-alanin és annak tercbutil-észtere
US9725452B2 (en) 2013-03-15 2017-08-08 Presidents And Fellows Of Harvard College Substituted indoles and pyrroles as RIP kinase inhibitors
KR20160030206A (ko) * 2013-07-10 2016-03-16 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 사구체 질환을 치료하는데 사용하기 위한 로스마피모드
CN106029639B (zh) * 2014-02-19 2019-01-08 H.隆德贝克有限公司 治疗阿尔茨海默病的bace1抑制剂的2-氨基-3,5,5-三氟-3,4,5,6-四氢吡啶
WO2015170218A1 (en) 2014-05-07 2015-11-12 Pfizer Inc. Tropomyosin-related kinase inhibitors
CR20170187A (es) 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer
MA40941A (fr) 2014-11-10 2017-09-19 H Lundbeck As 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
JO3458B1 (ar) 2014-11-10 2020-07-05 H Lundbeck As 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1
TW201717948A (zh) 2015-08-10 2017-06-01 H 朗德貝克公司 包括給予2-胺基-3,5,5-三氟-3,4,5,6-四氫吡啶的聯合治療
AU2016305275A1 (en) 2015-08-12 2018-02-08 H. Lundbeck A/S 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridins as bace1 inhibitors
CN106554314B (zh) * 2015-09-30 2021-07-27 石药集团中奇制药技术(石家庄)有限公司 苯甲酰胺类衍生物
DE102015120397A1 (de) 2015-11-25 2017-01-05 Miele & Cie. Kg Kochfeld, insbesondere Induktionskochfeld
DE102015120409A1 (de) 2015-11-25 2017-01-12 Miele & Cie. Kg Kochfeld, insbesondere Induktionskochfeld
WO2017151409A1 (en) 2016-02-29 2017-09-08 University Of Florida Research Foundation, Incorporated Chemotherapeutic methods
JP7204640B2 (ja) 2016-09-12 2023-01-16 ニューラルステム・インコーポレーテッド 糖尿病に関連する神経障害の改善
GB201713975D0 (en) 2017-08-31 2017-10-18 Macrophage Pharma Ltd Medical use
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
WO2019071147A1 (en) * 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. INHIBITORS OF KINASE P38 REDUCING EXPRESSION OF DUX4 GENE AND DOWNSTREAM GENES FOR THE TREATMENT OF FSHD
EP3697755B1 (en) * 2017-10-20 2021-09-15 SABIC Global Technologies B.V. Novel synthesis method for the preparation of dibenzoate compounds, such as 4-[benzoyl(methyl)amino]pentane-2-yl dibenzoate
EP3727315B1 (en) 2017-12-18 2021-10-13 Unilever Global IP Limited A topical composition comprising n-cyclopropyl nicotinamide
EP3773579A4 (en) 2018-03-26 2022-03-09 Clear Creek Bio, Inc. COMPOSITIONS AND METHODS FOR INHIBITING DIHYDROOROTATE DEHYDROGENASE
TW202112368A (zh) 2019-06-13 2021-04-01 荷蘭商法西歐知識產權股份有限公司 用於治療有關dux4表現之疾病的抑制劑組合
US12351556B2 (en) * 2019-10-04 2025-07-08 Inserm (Institut National De La Sante Et De La Recherche Medicale) Pyridin-2(1H)one derivatives, their preparation and their use for the treatment of pain
US20210300873A1 (en) 2020-03-20 2021-09-30 Clear Creek Bio, Inc. Stable polymorphic compositions of brequinar sodium and methods of use and manufacture thereof
KR102298450B1 (ko) * 2021-01-29 2021-09-08 (주)프레이저테라퓨틱스 p38 MAP 키나아제 억제제로 항염증 활성을 나타내는 신규 화합물
US20240342148A1 (en) 2021-07-27 2024-10-17 Fulcrum Therapeutics, Inc. Methods of treating facioscapulohumeral muscular dystrophy with losmapimod

Family Cites Families (132)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3822277A (en) * 1967-11-13 1974-07-02 C Dufour Certain pyridyl cyclopropylamides
US4200750A (en) * 1977-01-07 1980-04-29 Westwood Pharmaceuticals Inc. 4-Substituted imidazo [1,2-a]quinoxalines
JPS5651488A (en) 1979-10-02 1981-05-09 Meiji Seika Kaisha Ltd Penicillin derivative and its preparation
DE3332272A1 (de) 1983-09-07 1985-03-21 Bayer Ag, 5090 Leverkusen Herbizide mittel enthaltend metribuzin in kombination mit pyridincarbonsaeureamiden
US4863940A (en) * 1984-07-26 1989-09-05 Rohm And Haas N-acetonyl-substituted amides and phytopathogenic fungicidal use thereof
EP0187284A3 (de) 1984-12-20 1987-04-15 Bayer Ag Verfahren zur Herstellung von Pyridin-carbonsäure-N-tert.-alkylamiden
DE3600288A1 (de) 1986-01-08 1987-07-16 Bayer Ag Verwendung von amiden zur verbesserung der kulturpflanzen-vertraeglichkeit von herbizid wirksamen sulfonylharnstoff-derivaten
DE3605423A1 (de) 1986-02-20 1987-08-27 Bayer Ag Verfahren zur herstellung von pyridin-carbonsaeure-n-tert.-alkylamiden
DE3618004A1 (de) 1986-05-28 1987-12-03 Bayer Ag Verwendung von amiden zur verbesserung der kulturpflanzen-vertraeglichkeit von herbizid wirksamen sulfonyliso(thio)-harnstoff-derivaten
JPH01102064A (ja) 1987-10-16 1989-04-19 Ishihara Sangyo Kaisha Ltd ハロゲノピリジンカルボン酸アミド類の製造方法
EP0346841A3 (de) 1988-06-16 1991-01-09 Ciba-Geigy Ag 1-Aryl-naphthoesäureamide und diese enthaltende mikrobizide Mittel
MX16687A (es) * 1988-07-07 1994-01-31 Ciba Geigy Ag Compuestos de biarilo y procedimiento para su preparacion.
JP2768721B2 (ja) * 1989-03-01 1998-06-25 株式会社東芝 真空バルブ用接点材料
EP0430033A3 (en) 1989-11-24 1991-09-11 Ciba-Geigy Ag Microbicidal agents
US5166352A (en) 1991-09-12 1992-11-24 Dowelanco Pyridinecarboxylic acid chlorides from (trichloromethyl)pyridines
PT533268E (pt) 1991-09-18 2002-02-28 Glaxo Group Ltd Derivados de benzanilida como antagonistas de 5-ht1d
GB9119920D0 (en) 1991-09-18 1991-10-30 Glaxo Group Ltd Chemical compounds
GB9816837D0 (en) 1998-08-04 1998-09-30 Zeneca Ltd Amide derivatives
US5502194A (en) 1992-02-19 1996-03-26 Bayer Aktiengesellschaft Process for the preparation of 2-halogeno-pyridine derivatives
US5246943A (en) * 1992-05-19 1993-09-21 Warner-Lambert Company Substituted 1,2,3,4-tetahydroisoquinolines with angiotensin II receptor antagonist properties
US5236934A (en) * 1992-08-26 1993-08-17 E. I. Du Pont De Nemours And Company 1,2,3,4-tetrahydroisoquinolines useful in the treatment of CNS disorders
TW240217B (https=) 1992-12-30 1995-02-11 Glaxo Group Ltd
GB2273930A (en) 1992-12-30 1994-07-06 Glaxo Group Ltd Benzanilide derivatives
IL108630A0 (en) * 1993-02-18 1994-05-30 Fmc Corp Insecticidal substituted 2,4-diaminoquinazolines
GB2276161A (en) 1993-03-17 1994-09-21 Glaxo Group Ltd Aniline and benzanilide derivatives
GB2276162A (en) 1993-03-17 1994-09-21 Glaxo Group Ltd Aniline and benazilide derivatives
DK0716649T3 (da) 1993-08-31 1999-02-08 Pfizer 5-Arylindolderivater
EP0716656A1 (en) 1993-09-03 1996-06-19 Smithkline Beecham Plc Amide derivatives as 5ht1d receptor antagonists
WO1995011243A1 (en) 1993-10-19 1995-04-27 Smithkline Beecham Plc Benzanilide derivatives as 5ht-1d receptor antagonists
EP0733048A1 (en) 1993-12-07 1996-09-25 Smithkline Beecham Plc Heterocyclic biphenylylamides useful as 5ht1d antagonists
GB9326008D0 (en) 1993-12-21 1994-02-23 Smithkline Beecham Plc Novel compounds
GB9408577D0 (en) 1994-04-29 1994-06-22 Fujisawa Pharmaceutical Co New compound
EP0758330A1 (en) 1994-05-06 1997-02-19 Smithkline Beecham Plc Biphenylcarboxamides useful as 5-ht1d antagonists
US5521213A (en) * 1994-08-29 1996-05-28 Merck Frosst Canada, Inc. Diaryl bicyclic heterocycles as inhibitors of cyclooxygenase-2
TW397825B (en) * 1994-10-14 2000-07-11 Novartis Ag Aroyl-piperidine derivatives
GB2295387A (en) 1994-11-23 1996-05-29 Glaxo Inc Quinazoline antagonists of alpha 1c adrenergic receptors
EA199700209A1 (ru) 1995-04-04 1998-04-30 Глаксо Груп Лимитед ПРОИЗВОДНЫЕ ИМИДАЗО[1,2-a]ПИРИДИНА
GB9507203D0 (en) 1995-04-07 1995-05-31 Smithkline Beecham Plc Novel compounds
IL118544A (en) * 1995-06-07 2001-08-08 Smithkline Beecham Corp History of imidazole, the process for their preparation and the pharmaceutical preparations containing them
WO1997003034A2 (en) 1995-07-10 1997-01-30 The Dow Chemical Company Polynitrile oxides
DE69634822T2 (de) 1995-08-22 2006-04-27 Japan Tobacco Inc. Amid-verbindungen und ihre anwendung
US6323227B1 (en) * 1996-01-02 2001-11-27 Aventis Pharmaceuticals Products Inc. Substituted N-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides
US6080767A (en) * 1996-01-02 2000-06-27 Aventis Pharmaceuticals Products Inc. Substituted n-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides
PL187516B1 (pl) * 1996-01-11 2004-07-30 Smithkline Beecham Corp Nowe podstawione pochodne imidazolu, sposób ich wytwarzania oraz kompozycja farmaceutyczna zawierająca te związki
DE19608791A1 (de) 1996-03-07 1997-09-11 Hoechst Ag Verfahren zur Herstellung von fluorierten Aromaten und fluorierten stickstoffhaltigen Heteroaromaten
FR2754260B1 (fr) * 1996-10-04 1998-10-30 Adir Nouveaux derives substitues de biphenyle ou de phenylpyridine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
GB9614236D0 (en) * 1996-07-06 1996-09-04 Zeneca Ltd Chemical compounds
US5945418A (en) * 1996-12-18 1999-08-31 Vertex Pharmaceuticals Incorporated Inhibitors of p38
US6147080A (en) * 1996-12-18 2000-11-14 Vertex Pharmaceuticals Incorporated Inhibitors of p38
EP0983260A2 (en) * 1997-05-22 2000-03-08 G.D. Searle & Co. 3(5)-HETEROARYL SUBSTITUTED PYRAZOLES AS p38 KINASE INHIBITORS
US6087496A (en) * 1998-05-22 2000-07-11 G. D. Searle & Co. Substituted pyrazoles suitable as p38 kinase inhibitors
CA2294057A1 (en) * 1997-06-13 1998-12-17 Smithkline Beecham Corporation Novel pyrazole and pyrazoline substituted compounds
WO1998057934A1 (en) 1997-06-19 1998-12-23 The Du Pont Merck Pharmaceutical Company (AMIDINO)6-MEMBERED AROMATICS AS FACTOR Xa INHIBITORS
US6060491A (en) * 1997-06-19 2000-05-09 Dupont Pharmaceuticals 6-membered aromatics as factor Xa inhibitors
WO1999001452A1 (en) * 1997-07-02 1999-01-14 Smithkline Beecham Corporation Novel cycloalkyl substituted imidazoles
ES2256817T3 (es) * 1997-09-05 2006-07-16 Glaxo Group Limited Composiciones farmaceuticas que comprenden derivados de 2,3-diaril-pirazolo(1,5-b)piridazina.
JP3887769B2 (ja) 1997-12-22 2007-02-28 バイエル コーポレイション 対称および非対称ジフェニル尿素を用いるp38キナーゼの阻害
JPH11218884A (ja) 1998-02-03 1999-08-10 Konica Corp ハロゲン化銀写真感光材料
DE19817461A1 (de) * 1998-04-20 1999-10-21 Basf Ag Neue substituierte Benzamide, deren Herstellung und Anwendung
IL129596A (en) 1998-05-08 2003-10-31 Dow Agrosciences Llc Preparation of 2-substituted pyridines
MY132496A (en) * 1998-05-11 2007-10-31 Vertex Pharma Inhibitors of p38
CA2328927C (en) * 1998-05-15 2008-02-19 Astrazeneca Ab Benzamide derivatives for the treatment of diseases mediated by cytokines
US6130235A (en) * 1998-05-22 2000-10-10 Scios Inc. Compounds and methods to treat cardiac failure and other disorders
US6448257B1 (en) * 1998-05-22 2002-09-10 Scios, Inc. Compounds and methods to treat cardiac failure and other disorders
US6867209B1 (en) * 1998-05-22 2005-03-15 Scios, Inc. Indole-type derivatives as inhibitors of p38 kinase
CA2342251A1 (en) 1998-08-28 2000-03-09 Scios Inc. Use of piperidines and/or piperazines as inhibitors of p38-alpha kinase
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
WO2000017175A1 (en) * 1998-09-18 2000-03-30 Vertex Pharmaceuticals Incorporated INHIBITORS OF p38
HUP0104204A3 (en) 1998-11-03 2002-06-28 Glaxo Group Ltd Pyrazolopyridine derivatives as cox-2 inhibitors, process for their preparation and pharmaceutical compositions thereof
WO2000042012A1 (en) * 1999-01-13 2000-07-20 Bayer Corporation φ-CARBOXYARYL SUBSTITUTED DIPHENYL UREAS AS RAF KINASE INHIBITORS
CA2361428A1 (en) * 1999-02-11 2000-08-17 Cor Therapeutics, Inc. Inhibitors of factor xa
US6498166B1 (en) * 1999-02-27 2002-12-24 Smithkline Beecham Corporation Pyrazolopyridines
GB9906566D0 (en) 1999-03-23 1999-05-19 Zeneca Ltd Chemical compounds
US6509361B1 (en) * 1999-05-12 2003-01-21 Pharmacia Corporation 1,5-Diaryl substituted pyrazoles as p38 kinase inhibitors
JP2003500382A (ja) 1999-05-24 2003-01-07 シーオーアール セラピューティクス インコーポレイテッド Xa因子の阻害剤
EP1185509A2 (en) 1999-05-24 2002-03-13 Cor Therapeutics, Inc. INHIBITORS OF FACTOR Xa
AU5158100A (en) 1999-05-24 2000-12-12 Cor Therapeutics, Inc. Inhibitors of factor xa
DE19932571A1 (de) * 1999-07-13 2001-01-18 Clariant Gmbh Verfahren zur Herstellung von Biarylen unter Palladophosphacyclobutan-Katalyse
GB9919778D0 (en) * 1999-08-21 1999-10-27 Zeneca Ltd Chemical compounds
US6576632B1 (en) * 1999-08-27 2003-06-10 Pfizer Inc Biaryl compounds useful as anticancer agents
GB9924092D0 (en) 1999-10-13 1999-12-15 Zeneca Ltd Pyrimidine derivatives
DE60018037T2 (de) 1999-11-10 2006-01-12 Ortho-Mcneil Pharmaceutical, Inc. Substituierte 2-aryl-3-(heteroaryl)-imidazo[1,2-alpha]pyrimidine und ihren verwandten arzneimittel und verfahren
US6303790B1 (en) * 1999-11-29 2001-10-16 Hoffman-La Roche Inc. Process for the preparation of pyridine derivatives
SE9904652D0 (sv) * 1999-12-17 1999-12-17 Astra Pharma Prod Novel Compounds
MY141144A (en) 2000-03-02 2010-03-15 Smithkline Beecham Corp 1, 5-disubstituted-3,4-dihydro-1h-pyrimido 4,5-dipyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
US7235551B2 (en) * 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
CA2403828A1 (en) 2000-03-22 2001-09-27 Vertex Pharmaceuticals Incorporated Inhibitors of p38
CA2409096A1 (en) 2000-05-18 2002-11-15 Junji Nakamura Novel benzofuran derivatives
PE20020506A1 (es) * 2000-08-22 2002-07-09 Glaxo Group Ltd Derivados de pirazol fusionados como inhibidores de la proteina cinasa
ATE521353T1 (de) 2000-10-23 2011-09-15 Glaxosmithkline Llc Neues trisubstitutiertes 8h-pyridoä2,3- düpyrimidin-7-onderivat zur behandlung von durch csbp/p38kinase vermittelten krankheiten
YU37903A (sh) 2000-11-17 2006-05-25 Bristol-Myers Squibb Company POSTUPCI LEČENJA STANJA POVEZANIH SA p38 KINAZOM I JEDINJENJA PIROLOTRIAZINA KOJA SE KORISTE KAO INHIBITORI KINAZE
DE10059418A1 (de) * 2000-11-30 2002-06-20 Aventis Pharma Gmbh Ortho, meta-substituierte Bisarylverbindungen, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament sowie sie enthaltende pharmazeutische Zubereitungen
DE10060807A1 (de) 2000-12-07 2002-06-20 Aventis Pharma Gmbh Ortho, ortho-substituierte stickstoffhaltige Bisarylverbindungen, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament sowie sie enthaltende pharmazeutische Zubereitungen
DE10063008A1 (de) * 2000-12-16 2002-06-20 Merck Patent Gmbh Carbonsäureamidderivate
DE10110749A1 (de) * 2001-03-07 2002-09-12 Bayer Ag Substituierte Aminodicarbonsäurederivate
EE200300437A (et) 2001-03-09 2004-02-16 Pfizer Products Inc. Triasolopüridiinid kui põletikuvastased ained
AUPR399301A0 (en) * 2001-03-27 2001-04-26 Silverbrook Research Pty. Ltd. An apparatus and method(ART106)
US20020152397A1 (en) * 2001-04-06 2002-10-17 Mckay Drew Virtual investigator
RU2003132706A (ru) 2001-04-06 2005-04-20 Байокрист Фармасьютикалз, Инк. (Us) Диариловые соединения в качестве ингибиторов сериновых протеаз
FR2824827B1 (fr) 2001-05-17 2004-02-13 Fournier Lab Sa Nouveaux derives de 5-phenyl-1h-indole antagoniste des recepteurs de l'interleukine-8
AR037233A1 (es) * 2001-09-07 2004-11-03 Euro Celtique Sa Piridinas aril sustituidas, composiciones farmaceuticas y el uso de dichos compuestos para la elaboracion de un medicamento
GB0124848D0 (en) * 2001-10-16 2001-12-05 Celltech R&D Ltd Chemical compounds
GB0124938D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124934D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124928D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124932D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124941D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124939D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124936D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124933D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124931D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
EP2258687B1 (en) 2002-02-12 2012-12-26 Glaxosmithkline LLC Nicotinamide derivates useful as P38 inhibitors
US20030225089A1 (en) * 2002-04-10 2003-12-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmaceutical compositions based on anticholinergics and p38 kinase inhibitors
GB0209891D0 (en) 2002-04-30 2002-06-05 Glaxo Group Ltd Novel compounds
EP1535609A4 (en) 2002-06-10 2009-01-07 Inst Med Molecular Design Inc Nf-kb activation inhibitors
GB0217757D0 (en) 2002-07-31 2002-09-11 Glaxo Group Ltd Novel compounds
US20040038014A1 (en) * 2002-08-20 2004-02-26 Donaldson Company, Inc. Fiber containing filter media
US20040116479A1 (en) * 2002-10-04 2004-06-17 Fortuna Haviv Method of inhibiting angiogenesis
DE10256052B4 (de) * 2002-11-30 2006-04-06 A. Raymond & Cie Abdeckvorrichtung für Montageaussparungen in den Abdeckleisten eines Fahrzeugdaches
US7136850B2 (en) * 2002-12-20 2006-11-14 International Business Machines Corporation Self tuning database retrieval optimization using regression functions
GB0308186D0 (en) 2003-04-09 2003-05-14 Smithkline Beecham Corp Novel compounds
GB0308201D0 (en) * 2003-04-09 2003-05-14 Smithkline Beecham Corp Novel compounds
GB0308185D0 (en) 2003-04-09 2003-05-14 Smithkline Beecham Corp Novel compounds
ATE482205T1 (de) * 2003-07-25 2010-10-15 Novartis Ag P-38-kinasehemmer
GB0318814D0 (en) 2003-08-11 2003-09-10 Smithkline Beecham Corp Novel compounds
GB0402140D0 (en) * 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
GB0402137D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
GB0402143D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
GB0402138D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
UA90864C2 (en) * 2004-09-09 2010-06-10 Ромарк Лебораториз, Л.К. Halogenated benzamide derivatives
UY29439A1 (es) 2005-03-25 2006-10-02 Glaxo Group Ltd Nuevos compuestos
GB0612026D0 (en) * 2006-06-16 2006-07-26 Smithkline Beecham Corp New use

Also Published As

Publication number Publication date
US8575204B2 (en) 2013-11-05
BRPI0307351B8 (pt) 2021-05-25
JP2005519932A (ja) 2005-07-07
US7514456B2 (en) 2009-04-07
US20100215661A1 (en) 2010-08-26
IS2520B (is) 2009-07-15
KR20040082425A (ko) 2004-09-24
CY1111083T1 (el) 2015-06-11
AU2003207298B2 (en) 2009-09-03
IL163090A (en) 2010-06-16
JP4472349B2 (ja) 2010-06-02
DK1474395T3 (da) 2008-02-11
EP1864975B1 (en) 2010-10-20
CN1633416A (zh) 2005-06-29
US20060276516A1 (en) 2006-12-07
CA2474192A1 (en) 2003-08-21
EP1474395B1 (en) 2007-10-17
ES2295553T3 (es) 2008-04-16
EP1864975A3 (en) 2008-01-23
EP2258687B1 (en) 2012-12-26
ES2400486T3 (es) 2013-04-10
DE60316913D1 (de) 2007-11-29
CA2474192C (en) 2011-06-21
KR101058292B1 (ko) 2011-08-22
US7125898B2 (en) 2006-10-24
ATE485275T1 (de) 2010-11-15
CY1107117T1 (el) 2012-01-25
US7709506B2 (en) 2010-05-04
EP1864975A2 (en) 2007-12-12
DK1864975T3 (da) 2011-01-24
SI1474395T1 (sl) 2008-02-29
HK1070896A1 (en) 2005-06-30
DE60316913T2 (de) 2008-11-20
US20060264479A1 (en) 2006-11-23
US20100215652A1 (en) 2010-08-26
JP2010111699A (ja) 2010-05-20
MXPA04007838A (es) 2004-10-15
HK1113056A1 (en) 2008-09-19
NO20043176L (no) 2004-07-26
BRPI0307351B1 (pt) 2018-09-04
NO327418B1 (no) 2009-06-22
SI1864975T1 (sl) 2011-01-31
NZ533865A (en) 2006-02-24
WO2003068747A1 (en) 2003-08-21
IS7337A (is) 2004-06-28
RU2309951C2 (ru) 2007-11-10
DE60334651D1 (de) 2010-12-02
RU2004120553A (ru) 2005-05-27
PT1864975E (pt) 2010-12-27
ATE375980T1 (de) 2007-11-15
PT1474395E (pt) 2008-01-02
US8252818B2 (en) 2012-08-28
EP2258687A1 (en) 2010-12-08
AU2003207298A1 (en) 2003-09-04
ZA200405602B (en) 2005-09-28
PL212910B1 (pl) 2012-12-31
US20050176964A1 (en) 2005-08-11
PL372628A1 (en) 2005-07-25
BR0307351A (pt) 2004-12-14
CO5611147A2 (es) 2006-02-28
EP1474395A1 (en) 2004-11-10

Similar Documents

Publication Publication Date Title
CN100369898C (zh) 用作p38抑制剂的烟酰胺衍生物
JP4845733B2 (ja) P38キナーゼ阻害剤としての3−アミノカルボニル、6−フェニル置換ピリジン−1−オキシド
DE60314639T2 (de) Fusionierte heteroaryl-derivate zur verwendung als p38 kinase inhibitoren zur behandlung von u.a rheumatischer arthritis
JP2005511531A (ja) 5’−アシルアミノ−1,1’−ビフェニル−4−カルボキサミド誘導体およびp38キナーゼ阻害剤としてのそれらの使用
CN101765593A (zh) 用作大麻素受体配体的2-亚氨基异噻唑衍生物
TW200403223A (en) Novel compounds
RS56331B1 (sr) Derivati piridazinon-amida
EP1264820A1 (en) Novel amide compounds
KR20110031318A (ko) Ia 심부전 및 암 치료에 유용한 단백질 키나제 d 억제제로서의 2,4'-비피리디닐 화합물
CN101605783A (zh) 作为药物、药物组合物尤其作为ikk抑制剂的新型n,n’-2,4-二苯胺基嘧啶衍生物及其制备
CN101511828A (zh) 作为蛋白激酶抑制剂的杂芳基衍生物
CA2187214C (en) Aminostilbazole derivative and medicine
JP4932720B2 (ja) ベンズアミド誘導体
CN103992311B (zh) Hedgehog信号通路抑制剂
JPWO2008029912A1 (ja) シクロオキシゲナーゼ1(cox−1)選択的阻害活性を有するベンズアミドを骨格とする化合物
WO2026075117A1 (en) Bridged bicyclic compounds
HK1151527A (en) Nicotinamide derivates useful as p38 inhibitors
HK1070896B (en) Nicotinamide derivates useful as p38 inhibitors
TW200404539A (en) Acetamides and benzamides that are useful in treating sexual dysfunction
JPH08245621A (ja) チエニルチアゾール誘導体
JPWO2001068585A1 (ja) 新規アミド化合物

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
CX01 Expiry of patent term
CX01 Expiry of patent term

Granted publication date: 20080220