DE60103976D1 - Pyrimidinylcarboxamiden als inhibitoren der pde4 isoenzyme - Google Patents

Pyrimidinylcarboxamiden als inhibitoren der pde4 isoenzyme

Info

Publication number
DE60103976D1
DE60103976D1 DE60103976T DE60103976T DE60103976D1 DE 60103976 D1 DE60103976 D1 DE 60103976D1 DE 60103976 T DE60103976 T DE 60103976T DE 60103976 T DE60103976 T DE 60103976T DE 60103976 D1 DE60103976 D1 DE 60103976D1
Authority
DE
Germany
Prior art keywords
carboxamides
pyrimidinyl
inhibitors
pde4 isoenzyme
isoenzyme
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 - Fee Related
Application number
DE60103976T
Other languages
English (en)
Other versions
DE60103976T2 (de
Inventor
Robert James Chambers
Thomas Victor Magee
Anthony Marfat
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.)
Pfizer Products Inc
Original Assignee
Pfizer Products Inc
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 Pfizer Products Inc filed Critical Pfizer Products Inc
Application granted granted Critical
Publication of DE60103976D1 publication Critical patent/DE60103976D1/de
Publication of DE60103976T2 publication Critical patent/DE60103976T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P1/04—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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • 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
    • A61P31/10—Antimycotics
    • 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
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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
    • 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
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Biotechnology (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
DE60103976T 2000-01-31 2001-01-30 Pyrimidinylcarboxamiden als inhibitoren der pde4 isoenzyme Expired - Fee Related DE60103976T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US17928200P 2000-01-31 2000-01-31
US179282P 2000-01-31
PCT/IB2001/000125 WO2001057025A1 (en) 2000-01-31 2001-01-30 Pyrimidine carboxamides useful as inhibitors of pde4 isozymes

Publications (2)

Publication Number Publication Date
DE60103976D1 true DE60103976D1 (de) 2004-07-29
DE60103976T2 DE60103976T2 (de) 2005-07-21

Family

ID=22655926

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60103976T Expired - Fee Related DE60103976T2 (de) 2000-01-31 2001-01-30 Pyrimidinylcarboxamiden als inhibitoren der pde4 isoenzyme

Country Status (44)

Country Link
US (1) US6740655B2 (de)
EP (1) EP1252157B1 (de)
JP (1) JP2003522165A (de)
KR (1) KR20020071029A (de)
CN (1) CN1404480A (de)
AP (1) AP2002002590A0 (de)
AR (1) AR027336A1 (de)
AT (1) ATE269860T1 (de)
AU (1) AU2700301A (de)
BG (1) BG106868A (de)
BR (1) BR0107934A (de)
CA (1) CA2396458C (de)
CO (1) CO5271669A1 (de)
CR (1) CR6714A (de)
CZ (1) CZ20022413A3 (de)
DE (1) DE60103976T2 (de)
DK (1) DK1252157T3 (de)
DZ (1) DZ3406A1 (de)
EA (1) EA005028B1 (de)
EE (1) EE200200426A (de)
ES (1) ES2223772T3 (de)
GE (1) GEP20043385B (de)
GT (1) GT200100023A (de)
HK (1) HK1054232A1 (de)
HN (1) HN2001000018A (de)
HU (1) HUP0204271A3 (de)
IL (1) IL150486A0 (de)
IS (1) IS6444A (de)
MA (1) MA26871A1 (de)
MX (1) MXPA02007465A (de)
NO (1) NO20023614L (de)
NZ (1) NZ519726A (de)
OA (1) OA12170A (de)
PA (1) PA8511301A1 (de)
PE (1) PE20011059A1 (de)
PL (1) PL357555A1 (de)
PT (1) PT1252157E (de)
SK (1) SK10342002A3 (de)
SV (1) SV2001000298A (de)
TN (1) TNSN01019A1 (de)
TR (1) TR200402292T4 (de)
UY (1) UY26570A1 (de)
WO (1) WO2001057025A1 (de)
ZA (1) ZA200206034B (de)

Families Citing this family (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
ES2238334T3 (es) * 1999-12-24 2005-09-01 Glaxo Group Limited Formulacion farmaceutica en aerosol de salmeterol y propionato de fluticasona.
DE10110772A1 (de) * 2001-03-07 2002-09-12 Boehringer Ingelheim Pharma Neue Arzneimittelkompositionen auf der Basis von Anticholinergika und PDE-IV-Inhibitoren
US7776315B2 (en) 2000-10-31 2010-08-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmaceutical compositions based on anticholinergics and additional active ingredients
YU39503A (sh) * 2000-11-22 2006-05-25 F. Hoffmann-La Roche Ag. Derivati pirimidina
ATE293109T1 (de) * 2001-01-31 2005-04-15 Pfizer Prod Inc Nikotinsäureamid-derivate und ihre mimetika als inhibitoren von pde4-isozyms
HUP0401305A2 (hu) 2001-01-31 2004-10-28 Pfizer Products Inc. Tiazolil-, oxazolil-, pirrolil- és imidazolil-savamid-származékok, mint PDE4 izozimek inhibitorai és az ezeket tartalmazó gyógyszerkészítmények
PL364910A1 (en) 2001-01-31 2004-12-27 Pfizer Products Inc. Ether derivatives useful as inhibitors of pde4 isozymes
US7250518B2 (en) 2001-01-31 2007-07-31 Pfizer Inc. Nicotinamide acids, amides, and their mimetics active as inhibitors of PDE4 isozymes
JP2004520386A (ja) 2001-01-31 2004-07-08 ファイザー・プロダクツ・インク Ｐｄｅ４アイソザイムの阻害剤として有用なニコチンアミドビアリール誘導体
JP4510383B2 (ja) * 2001-05-23 2010-07-21 田辺三菱製薬株式会社 軟骨疾患修復治療用組成物
US20040146561A1 (en) * 2001-05-23 2004-07-29 Naoki Sakurai Compositions for promoting healing of bone fracture
DE10142176A1 (de) * 2001-08-29 2003-03-27 Eucro Europe Contract Res Gmbh Verwendung einer Kombination aus ß-adrenergen Agonisten und NDMA-Antagonisten
DE10163991A1 (de) * 2001-12-24 2003-07-03 Merck Patent Gmbh Pyrrolo-pyrimidine
MY140561A (en) 2002-02-20 2009-12-31 Nycomed Gmbh Dosage form containing pde 4 inhibitor as active ingredient
US6951869B2 (en) * 2002-02-26 2005-10-04 Schlesinger Stephen L Use of leukotriene receptor antagonist for treatment of scarring
SI1511516T1 (sl) * 2002-05-28 2009-06-30 Nycomed Gmbh Topično uporaben farmacevtski pripravek
DE10224888A1 (de) * 2002-06-05 2003-12-24 Merck Patent Gmbh Pyridazinderivate
GB2389530B (en) 2002-06-14 2007-01-10 Cipla Ltd Pharmaceutical compositions
US20040001895A1 (en) * 2002-06-17 2004-01-01 Pfizer Inc. Combination treatment for depression and anxiety
RU2327450C2 (ru) * 2002-08-29 2008-06-27 Сипла Лимитед Фармацевтические продукты и композиции, содержащие специфические антихолинергические средства, агонисты бета-2 и кортикостероиды
US9415102B2 (en) 2002-09-06 2016-08-16 Alexion Pharmaceuticals, Inc. High concentration formulations of anti-C5 antibodies
WO2004022096A1 (en) * 2002-09-06 2004-03-18 Alexion Pharmaceuticals, Inc. Method of treatment of asthma using antibodies to complement component c5
US20050271660A1 (en) 2002-09-06 2005-12-08 Alexion Pharmaceuticals, Inc. Nebulization of monoclonal antibodies for treating pulmonary diseases
US7507531B2 (en) 2002-10-17 2009-03-24 Decode Genetics Chf. Use of 5-lipoxygenase activating protein (FLAP) gene to assess susceptibility for myocardial infarction
US7851486B2 (en) 2002-10-17 2010-12-14 Decode Genetics Ehf. Susceptibility gene for myocardial infarction, stroke, and PAOD; methods of treatment
CA2511521C (en) 2002-12-30 2012-02-07 Angiotech International Ag Drug delivery from rapid gelling polymer composition
CA2523267C (en) 2003-04-23 2013-09-03 Biovalve Technologies, Inc. Hydraulically actuated pump for long duration medicament administration
US7439241B2 (en) * 2003-05-27 2008-10-21 Galderma Laboratories, Inc. Compounds, formulations, and methods for treating or preventing rosacea
US7132435B2 (en) * 2003-07-25 2006-11-07 Pfizer Inc. Compounds
US7153870B2 (en) 2003-07-25 2006-12-26 Pfizer Inc. Nicotinamide derivatives useful as PDE4 inhibitors
GB0317482D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as pde4 inhibitors
GB0317498D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Compounds
GB0317516D0 (en) 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as PDE4 inhibitors
US20050020587A1 (en) * 2003-07-25 2005-01-27 Pfizer Inc Nicotinamide derivatives useful as PDE4 inhibitors
GB0317484D0 (en) 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as pde4 inhibitors
US20050059643A1 (en) * 2003-08-05 2005-03-17 Boehringer Ingelheim International Gmbh Medicaments for inhalation comprising a steroid and a betamimetic
EP1660661A2 (de) * 2003-08-08 2006-05-31 Arriva Pharmaceuticals, Inc. Verfahren zur proteinproduktion in hefe
US20050142104A1 (en) * 2003-11-06 2005-06-30 Zeldis Jerome B. Methods of using and compositions comprising PDE4 modulators for the treatment and management of asbestos-related diseases and disorders
WO2005048985A2 (en) * 2003-11-14 2005-06-02 Baxter International Inc. Alpha 1-antitrypsin compositions and treatment methods using such compositions
WO2006073413A1 (en) * 2004-02-20 2006-07-13 The Board Of Trustees Of The University Of Illinois Blood pressure reduction in salt-sensitive
EP1737499A4 (de) * 2004-03-09 2009-07-22 Arriva Pharmaceuticals Inc Behandlung von chronisch obstruktiver lungenerkrankung durch inhalation von niedrigen dosen eines proteasehemmers
CN101163489A (zh) * 2004-04-23 2008-04-16 细胞基因公司 用于治疗和控制肺高血压的包含免疫调节化合物的组合物及其使用方法
PE20060272A1 (es) * 2004-05-24 2006-05-22 Glaxo Group Ltd (2r,3r,4s,5r,2'r,3'r,4's,5's)-2,2'-{trans-1,4-ciclohexanodiilbis-[imino(2-{[2-(1-metil-1h-imidazol-4-il)etil]amino}-9h-purin-6,9-diil)]}bis[5-(2-etil-2h-tetrazol-5-il)tetrahidro-3,4-furanodiol] como agonista a2a
US9089636B2 (en) 2004-07-02 2015-07-28 Valeritas, Inc. Methods and devices for delivering GLP-1 and uses thereof
LT3056492T (lt) 2004-10-08 2022-01-25 Abbvie Inc. Meglumino druska ir atitinkamos vaisto (delafloksacino) kristalinės formos
US20070105768A1 (en) * 2004-11-10 2007-05-10 Rajiv Nayar Dry recombinant human alpha 1-antitrypsin formulation
BRPI0520129A2 (pt) * 2005-03-17 2009-04-28 Proyecto Biomedicina Cima Sl uso de 5'-metiltioadenosina (mta) na prevenÇço e/ou no tratamento de doenÇas auto-imunes e/ou rejeiÇço de transplante
GB0514809D0 (en) 2005-07-19 2005-08-24 Glaxo Group Ltd Compounds
CA2620333A1 (en) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
EP2258358A3 (de) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenese mit Acetylcholinesterasehemmer
EP1940389A2 (de) 2005-10-21 2008-07-09 Braincells, Inc. Modulation von neurogenese durch pde-hemmung
CA2625210A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
RU2008122978A (ru) 2005-11-09 2009-12-20 Комбинаторкс, Инкорпорейтед (Us) Способы, композиции и наборы для лечения медицинских состояний
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
KR101361376B1 (ko) 2006-03-30 2014-02-10 발레리타스 인코포레이티드 복합-카트리지 유체 전달 장치
MX2008014320A (es) 2006-05-09 2009-03-25 Braincells Inc Neurogenesis mediada por el receptor de 5-hidroxitriptamina.
AU2007249399A1 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
MX2009002496A (es) 2006-09-08 2009-07-10 Braincells Inc Combinaciones que contienen un derivado de 4-acilaminopiridina.
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
WO2008088727A2 (en) * 2007-01-12 2008-07-24 Concert Pharmaceuticals, Inc. Endothelin receptor antagonists
US8080549B2 (en) * 2007-01-12 2011-12-20 Concert Pharmaceuticals, Inc. Endothelin receptor antagonists
GB0706398D0 (en) * 2007-04-02 2007-05-09 Univ Hospital Of North Staford Improvements in and relating to copd determination
CA2682730A1 (en) * 2007-04-11 2008-10-23 Alcon Research, Ltd. Use of an inhibitor of tnf.alpha. plus an antihistamine to treat allergic rhinitis and allergic conjunctivitis
CA2920996A1 (en) * 2007-10-19 2009-04-23 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
US7989465B2 (en) * 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
EP2100599A1 (de) 2008-03-13 2009-09-16 Laboratorios Almirall, S.A. Inhalationszusammensetzung enthaltend Aclidinium zur Behandlung von Asthma sowie chronisch-obstruktiver Lungenerkrankung
EP2100598A1 (de) 2008-03-13 2009-09-16 Laboratorios Almirall, S.A. Inhalationszusammensetzung enthaltend Aclidinium zur Behandlung von Asthma sowie chronisch-obstruktiver Lungenerkrankung
BRPI0910921B1 (pt) 2008-04-16 2022-06-21 Portola Pharmaceuticals, Inc Inibidores de proteína syk quinase, composição farmacêutica, kit e usos dos referidos inibidores
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
AU2008359989A1 (en) * 2008-07-30 2010-02-04 Nitto Denko Corporation Drug carriers
EP2196465A1 (de) 2008-12-15 2010-06-16 Almirall, S.A. (3-oxo)pyridazin-4-ylurea-Derivate als PDE4 Hemmern
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
EP2226323A1 (de) 2009-02-27 2010-09-08 Almirall, S.A. Neuartige Tetrahydropyrazol[3,4-c]isochinolin-5-amin-Derivate
EP2380890A1 (de) 2010-04-23 2011-10-26 Almirall, S.A. Neue 7,8-Dihydro-1,6-Naphthyridin-5(6H)-on-Derivate als PDE4 Inhibitoren
EP2394998A1 (de) 2010-05-31 2011-12-14 Almirall, S.A. 3-(5-Amino-6-oxo-1,6-dihydropyridazin-3-yl)-biphenyl Derivate als PDE4 Inhibitoren
JP5898676B2 (ja) * 2011-03-31 2016-04-06 マルホ株式会社 製剤安定性に優れた軟膏剤
EP2510928A1 (de) 2011-04-15 2012-10-17 Almirall, S.A. Aclidinium zur Verbesserung der Schlafqualität bei atemwegserkrankten Patienten
CN102850321A (zh) * 2011-06-28 2013-01-02 中国科学院上海药物研究所 芳香氧基嘧啶甲酰胺或芳香氧基吡啶甲酰胺类化合物及其制备方法、药物组合物和用途
CA2856301C (en) 2011-11-23 2020-10-06 Portola Pharmaceuticals, Inc. Pyrazine kinase inhibitors
EP2804603A1 (de) 2012-01-10 2014-11-26 President and Fellows of Harvard College Betazellen-replikation für promoterverbindungen und verwendungsverfahren dafür
KR102006547B1 (ko) * 2017-11-16 2019-08-01 서울대학교산학협력단 벤즈아미드 유도체 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 염증질환의 치료 또는 예방용 약학적 조성물
EP3737364A1 (de) * 2018-01-11 2020-11-18 Emphysema Solutions BV Zusammensetzungen und verfahren zur behandlung von lungenemphysem und anderen formen von copd
KR102200032B1 (ko) * 2019-03-13 2021-01-08 전남대학교산학협력단 호흡기 질환의 예방 또는 치료용 조성물
US11116737B1 (en) 2020-04-10 2021-09-14 University Of Georgia Research Foundation, Inc. Methods of using probenecid for treatment of coronavirus infections

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4861891A (en) * 1988-08-31 1989-08-29 Pfizer Inc. Antidepressant N-substituted nicotinamide compounds
TW429148B (en) * 1995-10-27 2001-04-11 Pfizer Pharmaceutical agents for the treatment of acute and chronic inflammatory diseases
YU49899A (sh) 1997-04-04 2002-09-19 Pfizer Products Inc. Nikotinamidni derivati
YU39503A (sh) * 2000-11-22 2006-05-25 F. Hoffmann-La Roche Ag. Derivati pirimidina

Also Published As

Publication number Publication date
PT1252157E (pt) 2004-10-29
AR027336A1 (es) 2003-03-26
CN1404480A (zh) 2003-03-19
TNSN01019A1 (fr) 2005-11-10
BR0107934A (pt) 2003-03-25
HUP0204271A3 (en) 2003-07-28
TR200402292T4 (tr) 2004-12-21
CO5271669A1 (es) 2003-04-30
DK1252157T3 (da) 2004-10-25
CA2396458A1 (en) 2001-08-09
DE60103976T2 (de) 2005-07-21
SV2001000298A (es) 2001-07-03
CR6714A (es) 2004-01-14
AP2002002590A0 (en) 2002-09-30
EA005028B1 (ru) 2004-10-28
ATE269860T1 (de) 2004-07-15
BG106868A (en) 2003-01-31
HUP0204271A2 (en) 2003-05-28
AU2700301A (en) 2001-08-14
NO20023614D0 (no) 2002-07-30
ES2223772T3 (es) 2005-03-01
OA12170A (en) 2006-05-08
NO20023614L (no) 2002-09-30
DZ3406A1 (de) 2001-08-09
CA2396458C (en) 2006-12-05
HK1054232A1 (zh) 2003-11-21
GT200100023A (es) 2001-12-19
KR20020071029A (ko) 2002-09-11
EP1252157B1 (de) 2004-06-23
GEP20043385B (en) 2004-04-13
PA8511301A1 (es) 2002-12-11
IS6444A (is) 2002-06-25
PL357555A1 (en) 2004-07-26
MXPA02007465A (es) 2002-12-13
CZ20022413A3 (cs) 2003-08-13
NZ519726A (en) 2004-05-28
SK10342002A3 (sk) 2003-12-02
US6740655B2 (en) 2004-05-25
IL150486A0 (en) 2002-12-01
PE20011059A1 (es) 2001-10-19
UY26570A1 (es) 2001-08-27
EA200200739A1 (ru) 2002-12-26
ZA200206034B (en) 2003-07-29
EE200200426A (et) 2003-12-15
WO2001057025A1 (en) 2001-08-09
EP1252157A1 (de) 2002-10-30
US20030144300A1 (en) 2003-07-31
JP2003522165A (ja) 2003-07-22
HN2001000018A (es) 2001-09-11
MA26871A1 (fr) 2004-12-20

Similar Documents

Publication Publication Date Title
DE60103976D1 (de) Pyrimidinylcarboxamiden als inhibitoren der pde4 isoenzyme
EE200300360A (et) PDE4 isosüümide inhibiitoritena kasutatavad nikotiinamiidi biarüülderivaadid
ATE305467T1 (de) Als inhibitoren von pde4-isozymen geeignete etherderivate
ATE323072T1 (de) Pyrimidin-derivate als selective inhibitoren von cox-2
ATE370938T1 (de) Pro-pharmakon von cox-2-inhibitoren
ATE269327T1 (de) Imidazol-5-yl-2-anilino-pyrimidine als inhibitoren der zellproliferation
ATE293624T1 (de) Nicotinamide benzoanellierte-heterocyclische derivate als selektive inhibitoren der pde4 isoenzyme
DE60020100D1 (de) Dimerverbindungen und als inhibitoren der neuramidinase
ATE256127T1 (de) Betacarbolinderivate als phosphodiesterase- inhibitoren
ATE378049T1 (de) Nicotinamid-derivate als pde4-hemmer
DE60321324D1 (de) Sulfonylaminoderivate als neue inhibitoren von histondeacetylase
DE602004008303D1 (de) Triazolopyrimidinderivate als inhibitoren von glycogensynthasekinase-3
ATE333446T1 (de) Pyrimidin-4-onderivat als ldl-pla2 inhibitor
DE60106252D1 (de) Substituierte pyprolopyridinonderivate als phosphodiesterase-inhibitoren
DE60324805D1 (de) Inhibitoren von tyrosinkinasen
ATE370137T1 (de) 4-(6-gliedriger)-heteroaryl-acyl-pyrrolidin derivate als hcv-inhibitoren
ATE435211T1 (de) Imidazolidinone als ns3-serin protease inhibitoren von hepatitis c virus
DE60135087D1 (de) Dipeptidnitrile als inhibitoren von cathepsin k
DE60110232D1 (de) Neue verwendung von lipase-inhibitoren
ATE323081T1 (de) N-formylhydroxylamin verbindungen als inhibitoren von pdf
ATE357432T1 (de) Substituierte 2-amino-zykloalkankarboxamide und ihre verwendung als zysteinprotease-inhibitoren
PT1272488E (pt) Inibidores de pde4 etanos tri-aril-substituidos
DE602004004794D1 (de) Nicotinamid-derivate verwendbar als pde4 inhibitoren
ATE429431T1 (de) 2-amino-benzoxazol-suphonamide als breitspektrum- hiv-protease-inhibitoren
DE60119076D1 (de) Gebrauch von Pyrometerdaten um Oxydation festzustellen

Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee