TNSN03050A1 - Derives d'amides de thiazolyl -, oxazolyl - pyrrolyl - et imidazolyl - acides utiles comme inhibiteurs d' isozymes pde4. - Google Patents

Derives d'amides de thiazolyl -, oxazolyl - pyrrolyl - et imidazolyl - acides utiles comme inhibiteurs d' isozymes pde4.

Info

Publication number
TNSN03050A1
TNSN03050A1 TNPCT/IB2001/002728A TNSN03050A TNSN03050A1 TN SN03050 A1 TNSN03050 A1 TN SN03050A1 TN SN03050 A TNSN03050 A TN SN03050A TN SN03050 A1 TNSN03050 A1 TN SN03050A1
Authority
TN
Tunisia
Prior art keywords
equal
group
represent
alkyle
pde4 inhibitors
Prior art date
Application number
TNPCT/IB2001/002728A
Other languages
English (en)
Inventor
Anthony Marfat
Michael William Mickechney
Original Assignee
Pfizer Prod 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 Prod Inc filed Critical Pfizer Prod Inc
Publication of TNSN03050A1 publication Critical patent/TNSN03050A1/fr

Links

Classifications

    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P25/14—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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P37/04—Immunostimulants
    • 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
    • A61P7/06—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen

Abstract

COMPOSES UTILES EN TANT QU* INHIBITEURS DE PDE4 DANS LE TRAITEMENT DE MALADIES, REGULEES PAR L* ACTIVATION ET LA DEGRANULATION DES CELLULES EOSINOPHILES, NOTAMMENT L “ASTHME, LA BRONCHITE CHRONIQUE, ET UNE MALADIE PULMONAIRE OBSTRUCTIVE CHRONIQUE, DE FORMULE (1) DANS LAQUELLE J EST EGAL A 0 OU I ; K EST EGAL A 0 OU I ; m EST EGAL A 0, I, 2 OU 3 ; n EST EGAL A I OU 2 W1 REPRESENTE UN GROUPE -O- ; OU C S (=0) t-, DANS LEQUEL t EGAL A 0,1, 2 ; OU CN(R3)-; W2 REPRESENTE UN GROUPE -O-CRa Rb- OU EST ABSENT ; Y REPRESENTE UN GROUPE =C(Rla) OU -[N (*(0)k|-, DANS LEQUEL k EST EGAL A 0 OU I; Ra ET Rb REPRESENTENT DES GROUPES *CH ; -F: -CF3;- (ALKYLE EN Cl A C4); CYCLOALKYLE EN C3 A Cl); PHENYLE; OU BENZYLE SUBSTITUE AVEC 0 A 3 SUBSTITUANTS RIO ; OU BIEN Ra ET Rb SONT PRIS CONJOINTEMENT, MAIS SEULEMENT DANS LE CAS OU m EST EGAL A 1, POUR FORMER UN GROUPEMENT S?\RO ; RC ET RD REPONDENT AUX DEFINITIONS DE Ra ET Rb, SAUF QU’UN D- ENTRE EUX DOIT REPRESENTER -II, RI ET R2 REPRESENTENT DES GROUPES "CH ; -F; -CI;- CN; -N02 ; -(ALKYLE EN CI-C4) ; -(ALCYNYLE EN C2 A C4); - (FLUORALKYLE EN Cl A C3) ; -ORI6 ; OU TC (=0)NR22a R22b ; R3 REPRESENTE -H; UN GROUPE C (ALKYLE EN CI-C3); PnENYLE; BENZYLE ; OU -ORI6 : OU C C(= O) NR 22a R22b ; R3 REPRESENTE CH ; UN GROUPE- (ALKYLE EN Cl A C3) ; PHENYLE ; BENZYLE ; OU C OR16 ; R4, R5 ET R6 EN PLUS D AUTRES DEFINITIONS, PEUVENT ETRE PRIS CONJOINTEMENT POUR FORMER LE COMPOSE (II);Gl REPRESENTE UN SYSTEME DE NOYAU CARBONE SATURE OU INSATURE DANS LEQUEL FACULTATIVEMENT, UN ATOME DE CARBONE PEUT ETRE REMPLACE PAR UN HETEROATOME CHOISI ENTRE N, O ET S ; G2 REPRESENTE UN SYSTEME DE NOYAU CARBONE SATURE OU INSATURE ; DANS LEQUEL UN ATOME DE CARBONE PEUT ETRE REMPLACE PAR UN HETEROATOME SELECTIONNE PARMI N, O ET S ; ET E EST CHOISI PARMI LES GROUPES DE FORMULE (III).
TNPCT/IB2001/002728A 2001-01-31 2003-07-08 Derives d'amides de thiazolyl -, oxazolyl - pyrrolyl - et imidazolyl - acides utiles comme inhibiteurs d' isozymes pde4. TNSN03050A1 (fr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US26548601P 2001-01-31 2001-01-31

Publications (1)

Publication Number Publication Date
TNSN03050A1 true TNSN03050A1 (fr) 2005-12-23

Family

ID=23010641

Family Applications (1)

Application Number Title Priority Date Filing Date
TNPCT/IB2001/002728A TNSN03050A1 (fr) 2001-01-31 2003-07-08 Derives d'amides de thiazolyl -, oxazolyl - pyrrolyl - et imidazolyl - acides utiles comme inhibiteurs d' isozymes pde4.

Country Status (24)

Country Link
US (3) US6559168B2 (fr)
EP (1) EP1355907A1 (fr)
JP (1) JP2004518691A (fr)
KR (1) KR20030072614A (fr)
CN (1) CN1489588A (fr)
BG (1) BG108039A (fr)
BR (1) BR0116850A (fr)
CA (1) CA2436551A1 (fr)
CR (1) CR7038A (fr)
CZ (1) CZ20031903A3 (fr)
EA (1) EA200300622A1 (fr)
EC (1) ECSP034683A (fr)
EE (1) EE200300362A (fr)
HU (1) HUP0401305A2 (fr)
IL (1) IL156412A0 (fr)
IS (1) IS6844A (fr)
MA (1) MA26985A1 (fr)
MX (1) MXPA03006886A (fr)
NO (1) NO20033398L (fr)
OA (1) OA12542A (fr)
PL (1) PL365443A1 (fr)
TN (1) TNSN03050A1 (fr)
WO (1) WO2002060898A1 (fr)
ZA (1) ZA200305769B (fr)

Families Citing this family (75)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1371650A4 (fr) * 2001-03-23 2005-05-04 Nippon Chemiphar Co Activateur de recepteur active par les proliferateurs du peroxysome
US20030055026A1 (en) 2001-04-17 2003-03-20 Dey L.P. Formoterol/steroid bronchodilating compositions and methods of use thereof
MXPA03010679A (es) * 2001-05-23 2004-03-02 Tanabe Seiyaku Co Una composicion para acelerar la cicatrizacion de fractura osea.
US20040180900A1 (en) * 2001-05-23 2004-09-16 Masaharu Takigawa Therapeutic composition for repairing chondropathy
EP1424078A4 (fr) * 2001-09-04 2009-03-25 Ono Pharmaceutical Co Medicaments contre les maladies respiratoires renfermant un agent de regulation du recepteur de la sphingosine-1-phosphate
CZ2004747A3 (cs) * 2001-12-21 2004-11-10 Novo Nordisk A/S Deriváty amidů jako GK aktivátory
EP1465882B1 (fr) * 2001-12-21 2011-08-24 X-Ceptor Therapeutics, Inc. Modulateurs heterocycliques de recepteurs nucleaires
GB0201677D0 (en) 2002-01-25 2002-03-13 Glaxo Group Ltd Medicament dispenser
WO2003063911A1 (fr) * 2002-02-01 2003-08-07 Anges Mg, Inc. Compositions pharmaceutiques contenant un leurre et procede d'utilisation
US20050158371A1 (en) * 2002-02-12 2005-07-21 Sumitomo Pharmaceuticals Co., Ltd. Novel external agent
KR101116627B1 (ko) * 2002-06-27 2012-10-09 노보 노르디스크 에이/에스 치료제로서 아릴 카르보닐 유도체
GB0217196D0 (en) * 2002-07-25 2002-09-04 Glaxo Group Ltd Medicament dispenser
FI114917B (fi) * 2002-08-29 2005-01-31 Hormos Nutraceutical Oy Ltd Lignaanikomplekseja
WO2004047817A1 (fr) * 2002-11-27 2004-06-10 Altana Pharma Ag Inhibiteurs de pde4 et pde3/4 que l'on utilise dans le traitement de la cachexie
EP1424101A3 (fr) * 2002-11-29 2004-08-18 NOZAKI, Masako Utilisation d'un antagoniste du leucotriène c4/d4 pour la préparation d'un médicament pour le traitement ou la prévention d'une inflammation ou septicémie du cerveau
US7148248B2 (en) * 2002-11-29 2006-12-12 Masako Nozaki Method of treating or inhibiting the development of brain inflammation and sepsis
JP2006516548A (ja) 2002-12-30 2006-07-06 アンジオテック インターナショナル アクツィエン ゲゼルシャフト 迅速ゲル化ポリマー組成物からの薬物送達法
GB0302094D0 (en) 2003-01-29 2003-02-26 Pharmagene Lab Ltd EP4 receptor antagonists
US20050079548A1 (en) * 2003-07-07 2005-04-14 Plexxikon, Inc. Ligand development using PDE4B crystal structures
GB0317482D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as pde4 inhibitors
GB0317516D0 (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
GB0317484D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as pde4 inhibitors
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
US20050020587A1 (en) * 2003-07-25 2005-01-27 Pfizer Inc Nicotinamide derivatives useful as PDE4 inhibitors
US20050187278A1 (en) * 2003-08-28 2005-08-25 Pharmacia Corporation Treatment or prevention of vascular disorders with Cox-2 inhibitors in combination with cyclic AMP-specific phosphodiesterase inhibitors
MXPA06002521A (es) * 2003-09-05 2006-06-20 Altana Pharma Ag Uso de inhibidores de pde4 para el tratamiento de diabetes mellitus.
US7534894B2 (en) * 2003-09-25 2009-05-19 Wyeth Biphenyloxy-acids
GB0324269D0 (en) 2003-10-16 2003-11-19 Pharmagene Lab Ltd EP4 receptor antagonists
AU2005203930C1 (en) 2004-01-06 2012-02-23 Vtv Therapeutics Llc Heteroaryl-ureas and their use as glucokinase activators
US20090042951A1 (en) * 2004-02-20 2009-02-12 Robert Danziger Blood Pressure Reduction in Salt-Sensitive Hypertension
WO2005102388A1 (fr) * 2004-04-26 2005-11-03 Ono Pharmaceutical Co., Ltd. Nouvelle maladie médiée par blt2, et agent et composé de liaison à blt2
CN101031293A (zh) * 2004-05-06 2007-09-05 普莱希科公司 Pde4b抑制剂及其应用
US7655680B2 (en) * 2004-05-17 2010-02-02 Otsuka Pharmaceutical Co., Ltd. Thiazole compound and use thereof
US20060004185A1 (en) * 2004-07-01 2006-01-05 Leese Richard A Peptide antibiotics and peptide intermediates for their prepartion
CA2583428A1 (fr) * 2004-09-03 2006-03-09 Plexxikon, Inc. Inhibiteurs de la phosphodiesterase 4b (pde4b)
US7704522B2 (en) 2004-09-08 2010-04-27 Clyde Morgan Topical medicament
NZ560269A (en) * 2005-03-08 2010-12-24 Nycomed Gmbh Roflumilast for the treatment of diabetes mellitus
WO2006094942A1 (fr) * 2005-03-08 2006-09-14 Nycomed Gmbh Roflumilast pour le traitement du diabète sucré
PL2366393T3 (pl) * 2005-04-19 2014-01-31 Takeda Gmbh Roflumilast do leczenia nadciśnienia płucnego
US7999114B2 (en) * 2005-07-08 2011-08-16 Novo Nordisk A/S Dicycloalkylcarbamoyl ureas as glucokinase activators
EP2377856A1 (fr) * 2005-07-14 2011-10-19 Novo Nordisk A/S Activateurs de la glucokinase d'urée
US7678363B2 (en) 2005-08-26 2010-03-16 Braincells Inc Methods of treating psychiatric conditions comprising administration of muscarinic agents in combination with SSRIs
EP2258358A3 (fr) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenèse avec un inhibiteur de l'acetylcholinestérase
CN1954882A (zh) 2005-10-14 2007-05-02 李海 长效人重组可溶性肿瘤坏死因子α受体在制备防治肝衰竭药物中的用途
JP2009512711A (ja) 2005-10-21 2009-03-26 ブレインセルス，インコーポレイティド Ｐｄｅ阻害による神経新生の調節
AU2006308889A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. GABA receptor mediated modulation of neurogenesis
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
NZ568694A (en) 2005-11-09 2011-09-30 Zalicus Inc Method, compositions, and kits for the treatment of medical conditions
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
EP2377531A2 (fr) 2006-05-09 2011-10-19 Braincells, Inc. Neurogénèse par modulation de l'angiotensine
EP2026813A2 (fr) 2006-05-09 2009-02-25 Braincells, Inc. Neurogenèse induite par le récepteur 5ht
AU2007283404B2 (en) * 2006-08-11 2013-04-18 Merck Canada Inc. Thiophenecarboxamide derivatives as EP4 receptor ligands
AU2007292848A1 (en) 2006-09-08 2008-03-13 Braincells, Inc. Combinations containing a 4-acylaminopyridine derivative
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
US8138185B2 (en) * 2007-01-09 2012-03-20 Novo Nordisk A/S Urea glucokinase activators
JP5226008B2 (ja) 2007-01-11 2013-07-03 ノボ・ノルデイスク・エー／エス ウレアグルコキナーゼアクチベーター
MX2009007916A (es) 2007-01-24 2009-07-31 Glaxo Group Ltd Composiciones farmaceuticas que comprenden 3,5-diamino-6-(2,3-dicl orofenil)-l,2,4,-triazina; o r(-)-2,4-diamino-5-(2,3-diclorofenil) -6-fluorometil pirimidina y un receptor neuroquinina 1.
AU2008326385B2 (en) * 2007-11-21 2013-12-05 Decode Genetics Ehf Substituted benzoazole PDE4 inhibitors for treating inflammatory, cardiovascular and CNS disorders
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
US20090269354A1 (en) * 2008-03-28 2009-10-29 Concert Pharmaceuticals, Inc. Quinazoline derivatives and methods of treatment
US10517839B2 (en) * 2008-06-09 2019-12-31 Cornell University Mast cell inhibition in diseases of the retina and vitreous
NZ593892A (en) 2008-12-23 2013-11-29 Biosource Pharm Inc Antibiotic compositions for the treatment of gram negative infections
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
ES2568629T3 (es) * 2009-06-18 2016-05-03 Concert Pharmaceuticals Inc. Derivados deuterados de isoindolin-1,3-diona como inhibidores de PDE4 y TNF-alfa
US8415307B1 (en) 2010-06-23 2013-04-09 Biosource Pharm, Inc. Antibiotic compositions for the treatment of gram negative infections
US20150119399A1 (en) 2012-01-10 2015-04-30 President And Fellows Of Harvard College Beta-cell replication promoting compounds and methods of their use
JO3264B1 (ar) * 2013-03-13 2018-09-16 Lilly Co Eli مركبات ازيتيدينيل أوكسي فينيل بيروليدين
RU2662806C2 (ru) * 2013-06-12 2018-07-31 Какен Фармасьютикал Ко., Лтд. 4-алкинилимидазольное производное и лекарственное средство, включающее такое производное в качестве активного ингредиента
TW201625591A (zh) * 2014-09-12 2016-07-16 美國禮來大藥廠 吖丁啶基氧苯基吡咯啶化合物
CN108794620A (zh) * 2017-05-04 2018-11-13 南开大学 茶碱的偶联物及其制备方法与应用
WO2019157144A1 (fr) 2018-02-07 2019-08-15 Duke University Système et procédé de phosphorylation du gpcr homogène et d'identification de modulateurs allostériques positifs des récepteurs bêta-2 adrénergique
AU2019287437A1 (en) 2018-06-12 2020-09-10 Vtv Therapeutics Llc Therapeutic uses of glucokinase activators in combination with insulin or insulin analogs
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 (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2140772A5 (en) 1971-06-07 1973-01-19 Aries Robert Phenoxynicotinoylaminophenols - analgesics tranquillisers antipyretics, anti-inflammatories and antirheumatics
US4270946A (en) * 1979-10-01 1981-06-02 Stauffer Chemical Company N-Aryl,2-phenoxy nicotinamide compounds and the herbicidal use thereof
US4692185A (en) * 1986-01-13 1987-09-08 Stauffer Chemical Company N-(ortho-substituted) benzyl, 3-trifluoromethylphenoxy nicotinamides as herbicides
US4861891A (en) 1988-08-31 1989-08-29 Pfizer Inc. Antidepressant N-substituted nicotinamide compounds
EP0500989B1 (fr) 1991-02-27 1998-12-09 Lacer, S.A. Agents antihypertensifs dipeptidiques N-(pyridyl-alpha-substituée) carbonyle
DE4200323A1 (de) 1992-01-09 1993-07-15 Bayer Ag Herbizide und pflanzennematizide mittel auf basis von mercaptonicotinsaeurederivaten
MX9301943A (es) 1992-04-02 1994-08-31 Smithkline Beecham Corp Compuestos.
JPH08511805A (ja) 1993-06-18 1996-12-10 スミスクライン・ビーチャム・コーポレイション 化合物
JP3406689B2 (ja) 1994-03-15 2003-05-12 株式会社大塚製薬工場 ナフチリジン及びピリドピラジン誘導体
US5618027A (en) * 1994-07-20 1997-04-08 Nevrekar; Venkatesh R. Gate valve
WO1996019990A1 (fr) 1994-12-23 1996-07-04 Smithkline Beecham Corporation Monomeres 4,4-(disubstitues)cyclohexan-1-carboxylate et composes correspondants
TW429148B (en) * 1995-10-27 2001-04-11 Pfizer Pharmaceutical agents for the treatment of acute and chronic inflammatory diseases
GB9622386D0 (en) 1996-10-28 1997-01-08 Sandoz Ltd Organic compounds
US5922557A (en) 1997-01-09 1999-07-13 Merck & Co., Inc. System for stably expressing a high-affinity camp phosphodiesterase and use thereof
TR199902432T2 (xx) 1997-04-04 2000-01-21 Prizer Products Inc. Nikotinamid t�revleri.
GB9715584D0 (en) * 1997-07-23 1997-10-01 Eisai Co Ltd Compounds
UA67753C2 (uk) 1997-10-10 2004-07-15 Смітклайн Бічам Корпорейшн Спосіб отримання заміщених 4-феніл-4-ціанциклогексанових кислот
AR015966A1 (es) 1997-10-17 2001-05-30 Smithkline Beecham Corp Uso de un compuesto inhibidor de pde4 para la preparacion de un medicamento util para el tratamiento de prurito
AR015190A1 (es) 1997-10-23 2001-04-18 Smithkline Beecham Corp Un polimorfo cristalino de 1,3-diciclopropilmetil-8-aminoxantina, procedimiento para su preparacion, composiciones farmaceuticas que lo contienen y su usopara la manufactura de un medicamento
OA12170A (en) * 2000-01-31 2006-05-08 Pfizer Prod Inc Pyrimidine carboxamides useful as inhibitors of PDE4 isozymes.
EA004885B1 (ru) * 2000-01-31 2004-08-26 Пфайзер Продактс Инк. Никотинамидные бензоконденсированные гетероциклические производные, полезные в качестве селективных ингибиторов pde4-изозимов

Also Published As

Publication number Publication date
BG108039A (en) 2004-07-30
CN1489588A (zh) 2004-04-14
US20030186974A1 (en) 2003-10-02
US6559168B2 (en) 2003-05-06
BR0116850A (pt) 2004-02-25
AU2002222429A2 (fr) 2002-08-12
US6894041B2 (en) 2005-05-17
EE200300362A (et) 2003-12-15
IL156412A0 (en) 2004-01-04
NO20033398L (no) 2003-09-29
ZA200305769B (en) 2004-10-25
EA200300622A1 (ru) 2003-12-25
OA12542A (en) 2006-06-05
US20030130254A1 (en) 2003-07-10
EP1355907A1 (fr) 2003-10-29
NO20033398D0 (no) 2003-07-30
US6869945B2 (en) 2005-03-22
CR7038A (es) 2004-04-22
JP2004518691A (ja) 2004-06-24
CZ20031903A3 (cs) 2004-07-14
CA2436551A1 (fr) 2002-08-08
PL365443A1 (en) 2005-01-10
MXPA03006886A (es) 2003-11-13
MA26985A1 (fr) 2004-12-20
IS6844A (is) 2003-06-16
ECSP034683A (es) 2003-08-29
HUP0401305A2 (hu) 2004-10-28
US20020123520A1 (en) 2002-09-05
WO2002060898A1 (fr) 2002-08-08
KR20030072614A (ko) 2003-09-15

Similar Documents

Publication Publication Date Title
TNSN03050A1 (fr) Derives d'amides de thiazolyl -, oxazolyl - pyrrolyl - et imidazolyl - acides utiles comme inhibiteurs d' isozymes pde4.
AU2018200368B2 (en) Compositions and methods of modulating 15-pgdh activity
AU2009282480B2 (en) Halofuginone analogs for inhibition of tRNA synthetases and uses thereof
CN100402492C (zh) 前列腺癌、脱发和其他雄激素过多综合征的治疗和诊断中的雄激素受体抑制剂
JP5643233B2 (ja) プロリルヒドロキシラーゼ阻害物質としてのキナゾリノン
CN103030597B (zh) 肾脏型谷氨酰胺酶抑制剂及其制备方法和用途
CN112839940B (zh) 氨基脲敏感性胺氧化酶抑制剂制备及其应用
JP2021527088A (ja) Ｈｅｒ２阻害剤としてのシアノキノリンアミド化合物及び使用方法
JP2021501123A (ja) Ｅｇｆｒおよび／またはｈｅｒ２の阻害剤ならびに使用方法
KR20160045925A (ko) 퀴나졸린 유도체
EP0469984B1 (fr) Dérivés de la N-sulfonyl indoline, leur préparation, les compositions pharmaceutiques en contenant
CA2447305A1 (fr) Nouveaux derives de 5-phenyl-1h-indole antagonistes des recepteurs de l'interleukine-8
US4761404A (en) Phospholipid analogs useful as PAF synthesis inhibitors
EP0600832A1 (fr) Dérivés de diamino acid benzoique et diamino acid phthalique et leur application à titre des inhibiteurs de protéine kinase
EP1493739A1 (fr) Dérivés thiophényliques d'aminoacides, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent
TW201739452A (zh) 含有青蒿琥酯的組合物
JPH06228108A (ja) フタラジノン誘導体
EP0303871B1 (fr) Oxadiazolo pyrimidinones, leur préparation et leur utilisation en cosmétique et dermopharmacie
JPH06199786A (ja) ジアミドフタリミドの置換誘導体
JP7425925B2 (ja) 二官能性化合物及び使用方法
DE69908756T2 (de) Matrix-metalloproteinase-inhibitoren
US5726311A (en) 7-disubstituted-methyl-4-oxo-3H,5H-pyrrolo 3,2-d!pyrimidine and pharmaceutical uses and compositions containing the same
CA2447184A1 (fr) Derives de 5-cyano-1h-indole antagonistes des recepteurs de l'interleukine-8
EP4198017A1 (fr) Dérivé de benzylamine, son procédé de préparation et son utilisation
WO2023224128A1 (fr) Composition pharmaceutique pour le traitement ou la prévention d'une fibrose