AR032676A1 - Quinazolinas como inhibidores de mmp-13 - Google Patents

Quinazolinas como inhibidores de mmp-13

Info

Publication number
AR032676A1
AR032676A1 ARP020100470A ARP020100470A AR032676A1 AR 032676 A1 AR032676 A1 AR 032676A1 AR P020100470 A ARP020100470 A AR P020100470A AR P020100470 A ARP020100470 A AR P020100470A AR 032676 A1 AR032676 A1 AR 032676A1
Authority
AR
Argentina
Prior art keywords
alkyl
oxygen
nitrogen
sulfur
nr10r11
Prior art date
Application number
ARP020100470A
Other languages
English (en)
Inventor
Bernard Gaudilliere
Henry Jacobelli
Daniel Fred Ortwine
William Chester Patt
Catherine Rose Kostlan
Charles Andrianjara
Barvian Nicole Chantel
Michael William Wilson
Ly Phan
Original Assignee
Warner Lambert Co
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 Warner Lambert Co filed Critical Warner Lambert Co
Publication of AR032676A1 publication Critical patent/AR032676A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P35/00—Antineoplastic 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C07D239/96—Two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Indole Compounds (AREA)

Abstract

Compuesto de quinazolinas substituidas de formula (1), donde R1 es hidrogeno, amino, C1-6alquilo , C3-6alquenilo, alquinilo C3-6, mono C1-6 alquilamino C1-6 alquilo, di C1-6 alquilamino C1-6 alquilo, arilo, aril C1-6 alquilo, heterociclo y cicloalquil C1-6 alquil de 3 a 6 miembros, insustituidos o sustituidos con uno o más grupos amino, C1-6 alquilo, ciano, halo C1-6 alquilo, C(=O)OR4, OR4 y SR4; R4 representa hidrogeno o C1-6 alquilo, en donde R4 es tal como se define en la memoria; W es oxígeno, azufre, o =N-R'; R' representa C1-6 alquilo, hidroxilo o ciano; X1, X2 y X3 representan, nitrogeno o -C-R6 y R6 es tal como se define en la memoria; Y representan oxígeno, azufre, -NH y -N C1-6 alquilo; Z es oxígeno, azufre o -NR7, y R7 es tal como se define en la memoria; n es de 1 a 8 inclusive; Z1 representa -CR8R9, y R8 y R9 son tal como se definen en la memoria; A representa un monociclo de 5 o 6 miembros, aromático o no aromático, con 0 a 4 heteroátomos nitrogeno, oxígeno y azufre, y un biciclo, de dos anillos de 5 o 6 miembros, aromáticos o no aromáticos, idénticos o diferentes, con 0 a 4 heteroátomos nitrogeno, oxígeno y azufre; m es 0 a 7 inclusive; R2 es C1-6 alquilo, halogeno, -CN, NO2, SCF3, -CF3, -OCF3, -NR10R11, -OR10, -SR10, SOR10, -SO2R10, (CH2)kSO2NR10R11, -X5(CH2)kC(=O)OR10, -(CH2)kC(=O)OR10, -X5(CH2)kC(=O)NR10R11, -(CH2)kC(=O)NR10R11, y -X4-R12, en los cuales X5, k, R10, R11, X4 y R12 son tal como se definen en la memoria; R3 representa hidrogeno, C1-6 alquilo, C3-6 alquenilo, C3-6 alquinilo, insustituidos o sustituidos con amino, ciano , halo C1-6 alquilo, cicloalquilo, -C(=O)NR10R11, -C(=O)OR10, OR10, y S10, donde R10 y R11, son como se definen en la memoria; y, cuando el anillo es heterocíclico, comprende de 1 a 4 heteroátomos nitrogeno, oxígeno y azufre, con la condicion de que cuando X1 representa un nitrogeno, X2 no puede representar un carbono sustituido por un grupo metilo o por NH-CH3, las formas racémicas, isomeros, N-oxido, y sales farmacéuticamente aceptables. Se incluyen compuestos intermediarios, los procesos de fabricacion y el uso de esos compuestos para preparar un producto medicinal para una terapia de inhibicion de la metaloproteasa de matriz de tipo 13 (MMP-13), como ser para tratar artritis, artritis reumatoide, osteoartritis, osteoporosis, afecciones periodontales, afeccion por inflamacion intestinal, psoriasis, esclerosis multiple, insuficiencia cardíaca, ateroesclerosis, asma, enfermedad de obstruccion pulmonar cronica (COPD), deterioro macular relacionado con la edad (ARMD) y cánceres.
ARP020100470A 2001-02-14 2002-02-13 Quinazolinas como inhibidores de mmp-13 AR032676A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US26866101P 2001-02-14 2001-02-14

Publications (1)

Publication Number Publication Date
AR032676A1 true AR032676A1 (es) 2003-11-19

Family

ID=23023949

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP020100470A AR032676A1 (es) 2001-02-14 2002-02-13 Quinazolinas como inhibidores de mmp-13

Country Status (30)

Country Link
US (1) US20020193377A1 (es)
EP (1) EP1368324A1 (es)
JP (1) JP2004523546A (es)
KR (1) KR20030074827A (es)
CN (1) CN1537105A (es)
AP (1) AP2003002841A0 (es)
AR (1) AR032676A1 (es)
BG (1) BG108091A (es)
BR (1) BR0207268A (es)
CA (1) CA2437122A1 (es)
CZ (1) CZ20032142A3 (es)
EA (1) EA200300792A1 (es)
EC (1) ECSP034730A (es)
EE (1) EE200300384A (es)
HU (1) HUP0303164A2 (es)
IL (1) IL157109A0 (es)
IS (1) IS6886A (es)
MA (1) MA26994A1 (es)
MX (1) MXPA03007248A (es)
NO (1) NO20033593D0 (es)
OA (1) OA12550A (es)
PA (1) PA8539401A1 (es)
PE (1) PE20021005A1 (es)
PL (1) PL367396A1 (es)
SK (1) SK10012003A3 (es)
SV (1) SV2003000876A (es)
TN (1) TNSN03045A1 (es)
UY (1) UY27173A1 (es)
WO (1) WO2002064572A1 (es)
ZA (1) ZA200306008B (es)

Families Citing this family (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PA8539501A1 (es) 2001-02-14 2002-09-30 Warner Lambert Co Compuestos triazolo como inhibidores de mmp
DOP2002000334A (es) * 2001-02-14 2002-08-30 Warner Lambert Co Pirimidinas biciclicas como inhibidores de metaloproteinasas de matriz
US6924276B2 (en) 2001-09-10 2005-08-02 Warner-Lambert Company Diacid-substituted heteroaryl derivatives as matrix metalloproteinase inhibitors
JP4164028B2 (ja) 2001-10-12 2008-10-08 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー アルキンマトリックスメタロプロテイナーゼ阻害剤
US6962922B2 (en) 2001-10-12 2005-11-08 Warner-Lambert Company Llc Alkynylated quinazoline compounds
US6894057B2 (en) 2002-03-08 2005-05-17 Warner-Lambert Company Oxo-azabicyclic compounds
US6747147B2 (en) 2002-03-08 2004-06-08 Warner-Lambert Company Oxo-azabicyclic compounds
AU2002249275A1 (en) * 2002-03-08 2003-09-22 Warner-Lambert Company Llc Oxo azabicyclic compounds
US20040006077A1 (en) * 2002-06-25 2004-01-08 Bernard Gaudilliere Thiazine and oxazine derivatives as MMP-13 inhibitors
BR0312943A (pt) * 2002-07-17 2005-07-12 Warner Lambert Co Combinação de um inibidor alostérico de matriz metaloproteinase-13 com um inibidor seletivo de ciclooxigenase-2 que não é celecoxib ou valdecoxib
CA2492379A1 (en) * 2002-07-17 2004-01-22 Warner-Lambert Company Llc Combination of an allosteric inhibitor of matrix metalloproteinase-13 with celecoxib or valdecoxib
EP1530467A2 (en) * 2002-07-17 2005-05-18 Warner-Lambert Company LLC Combination of an allosteric carboxylic inhibitor of matrix metalloproteinase-13 with celecoxib or valdecoxib
EP1530475A2 (en) * 2002-07-17 2005-05-18 Warner-Lambert Company LLC Pharmaceutical compositions comprising an allosteric carboxylic inhibitor of matrix metalloproteinase-13 and a selective inhibitor of cyclooxygenase-2
CA2497658A1 (en) 2002-08-13 2004-02-19 Warner-Lambert Company Llc Chromone derivatives as matrix metalloproteinase inhibitors
AU2003250466A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc 3-isoquinolinone derivatives as matrix metalloproteinase inhiitors
MXPA05001786A (es) 2002-08-13 2005-04-25 Warner Lambert Co Derivados de azaisoquinolina como inhibidores de la metaloproteinasa de matriz.
WO2004014908A1 (en) * 2002-08-13 2004-02-19 Warner-Lambert Company Llc Heterobicylcic metalloproteinase inhibitors
EP1530472A1 (en) * 2002-08-13 2005-05-18 Warner-Lambert Company LLC Isoquinoline derivatives as matrix metalloproteinase inhibitors
AU2003249539A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc Cyclic compounds containing zinc binding groups as matrix metalloproteinase inhibitors
EP1537098A1 (en) 2002-08-13 2005-06-08 Warner-Lambert Company LLC Monocyclic derivatives as matrix metalloproteinase inhibitors
AU2003253186A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc Fused tetrahydropyridine derivatives as matrix metalloproteinase inhibitors
JP2006500351A (ja) 2002-08-13 2006-01-05 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー マトリックスメタロプロテアーゼ−１３阻害剤としてのピリミジン−２，４−ジオン誘導体
AU2003249535A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc 1,6-fused uracil derivatives as matrix metalloproteinase inhibitors
AU2003250482A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc Phthalimide derivatives as matrix metalloproteinase inhibitors
WO2004014923A1 (en) 2002-08-13 2004-02-19 Warner-Lambert Company Llc Pyrimidinone fused bicyclic metalloproteinase inhibitors
PA8578101A1 (es) 2002-08-13 2004-05-07 Warner Lambert Co Derivados de heterobiarilo como inhibidores de metaloproteinasa de la matriz
AU2003249540A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc Fused bicyclic metalloproteinase inhibitors
AU2003250465A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc 5,6-fused uracil derivatives as matrix metalloproteinase inhibitors
AU2003250475A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc 5,6-fused 3,4-dihydropyrimidine-2-one derivatives as matrix metalloproteinase inhibitors
US7790709B2 (en) * 2002-12-06 2010-09-07 Affinium Pharmaceuticals, Inc. Heterocyclic compounds, methods of making them and their use in therapy
EP1583747A2 (en) * 2002-12-31 2005-10-12 Vertex Pharmaceuticals Incorporated Inhibitors of phosphatases
US20040142950A1 (en) * 2003-01-17 2004-07-22 Bunker Amy Mae Amide and ester matrix metalloproteinase inhibitors
CA2572324A1 (en) * 2003-07-02 2005-01-13 Warner-Lambert Company Llc Combination of an allosteric inhibitor of matrix metalloproteinase-13 and a ligand to an alpha-2-delta receptor
WO2005016926A1 (en) * 2003-08-19 2005-02-24 Warner-Lambert Company Llc Pyrido [3,4-d] pyrimidine derivatives as matrix metalloproteinase-13 inhibitors
EP1657238A4 (en) * 2003-08-22 2008-12-03 Takeda Pharmaceutical MERGED PYRIMIDINE DERIVATIVE AND USE THEREOF
US20060247231A1 (en) * 2003-12-18 2006-11-02 Warner-Lambert Company Llc Amide and ester matrix metalloproteinase inhibitors
DE10360835A1 (de) * 2003-12-23 2005-07-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyclische Imidazolverbindungen, deren Herstellung und deren Verwendung als Arzneimittel
JP4205757B2 (ja) 2004-05-06 2009-01-07 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー ４−フェニルアミノ−キナゾリン−６−イル−アミド
US8327467B2 (en) 2005-03-16 2012-12-11 Toyama Chemical Co., Ltd. Anthranilic acid derivative or salt thereof
EP2687533B1 (en) 2006-07-20 2017-07-19 Debiopharm International SA Acrylamide derivatives as FAB I inhibitors
EP2125802A4 (en) 2007-02-16 2014-08-20 Debiopharm Int Sa SALTS, PRODRUGS AND POLYMORPHES OF FAB I INHIBITORS
KR20090115953A (ko) * 2007-03-06 2009-11-10 노파르티스 아게 염증성 또는 알레르기성 상태의 치료에 적합한 바이시클릭 유기 화합물
CN104926815B (zh) 2008-01-04 2017-11-03 英特利凯恩有限责任公司 某些化学实体、组合物和方法
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
AU2009260503B2 (en) 2008-05-27 2014-03-27 The Board Of Regents Of The University Of Texas System Wnt protein signalling inhibitors
US9187406B2 (en) 2009-05-15 2015-11-17 The Research Foundation Of State University Of New York Curcumin analogues as zinc chelators and their uses
EP2266984A1 (en) * 2009-06-26 2010-12-29 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts Pyrido[2,3-d]pyrimidines as Wnt antagonists for treatment of cancer and arthritis
US8912184B1 (en) 2010-03-01 2014-12-16 Alzheimer's Institute Of America, Inc. Therapeutic and diagnostic methods
BR112013017670B1 (pt) 2011-01-10 2022-07-19 Infinity Pharmaceuticals, Inc Processos de preparação de isoquinolinonas e formas sólidas de isoquinolinonas
WO2013019682A1 (en) * 2011-07-29 2013-02-07 Tempero Pharmaceuticals, Inc. Compounds and methods
FR2991578B1 (fr) * 2012-06-06 2019-12-27 L'oreal Composes pour application anti-age et peau seche
RS58898B1 (sr) 2012-06-19 2019-08-30 Debiopharm Int Sa Prolek derivati (e)-n-metil-n-((3-metilbenzofuran-2-il)metil)-3-(7-okso-5,6,7,8-tetrahidro-1,8-naftiridin-3-il)akrilamida
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
ITMI20130646A1 (it) * 2013-04-19 2014-10-20 Univ Bologna Alma Mater Composti chinazolindionici con attività inibente sulle sirtuine
CN103664767A (zh) * 2013-12-06 2014-03-26 常熟市联创化学有限公司 一种2,6-吡啶二甲酸的制备方法
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
WO2016023830A1 (en) * 2014-08-11 2016-02-18 Hydra Biosciences, Inc. Pyrido[2,3-d]pyrimidine-2,4(1h,3h)-dione derivatives
WO2016023825A1 (en) * 2014-08-11 2016-02-18 Hydra Biosciences, Inc. Pyrido[3,4-d]pyrimidine-2,4(1h,3h)-dione derivatives
EP3180342B1 (en) * 2014-08-11 2019-06-26 Hydra Biosciences, Inc. Pyrrolo[3,2-d]pyrimidine-2,4(3h,5h)-dione derivatives
WO2016023832A1 (en) * 2014-08-11 2016-02-18 Hydra Biosciences, Inc. Thieno- and furo[2,3-d]pyrimidine-2,4[1h,3h]-dione derivatives as trpc5 modulators for the treatment of neuropsychiatric disorders
WO2016039408A1 (ja) * 2014-09-11 2016-03-17 武田薬品工業株式会社 複素環化合物
LT3419628T (lt) 2016-02-26 2021-01-25 Debiopharm International Sa Medikamentas diabetinėms pėdų infekcijoms gydyti
MX2018016227A (es) 2016-06-24 2019-07-08 Infinity Pharmaceuticals Inc Terapias de combinacion.
CN111116494B (zh) * 2019-12-31 2022-08-16 江苏中旗科技股份有限公司 一类含喹唑啉二酮结构的酰胺类化合物、其制备方法与应用

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SU119879A1 (ru) * 1958-10-21 1958-11-30 В.М. Нестеров Способ получени 1,3-диметил-4-имино-5,-изонитрозоурацила
CA762455A (en) * 1962-03-22 1967-07-04 Dr. Karl Thomae Gesellschaft Mit Beschrankter Haftung Pyrido-pyrimidines
CA764962A (en) * 1962-03-22 1967-08-08 Ohnacker Gerhard Pyrido-pyrimidines
DK408574A (es) * 1973-09-06 1975-05-05 Ciba Geigy Ag
DE3502590A1 (de) * 1985-01-26 1986-07-31 Gödecke AG, 1000 Berlin 5-alkoxy-pyrido(4,3-d)pyrimidin-derivate, verfahren zu deren herstellung und deren verwendung
DE3502742A1 (de) * 1985-01-28 1986-07-31 Gödecke AG, 1000 Berlin 5-oxo-pyrido(4,3-d)pyrimidin-derivate, verfahren zu deren herstellung und deren verwendung
GB9214053D0 (en) * 1992-07-02 1992-08-12 Ici Plc Heterocyclic amides
EP0621037B1 (de) * 1993-04-23 1999-07-07 Hoechst Aktiengesellschaft Pyrido-pyrimidindione, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US5281602A (en) * 1993-04-23 1994-01-25 American Cyanamid Company Angiotensin II receptor blocking 2,3,6-substituted 5,6,7,8-tetrahydro-pyrido[4,3-D]pyrimidin-4(3H)-ones
DE69611512T2 (de) * 1995-08-02 2001-05-31 J. Uriach & Cia. S.A., Barcelona Pyrimidonderivate mit antifungaler wirkung
HRP970244B1 (en) * 1996-05-15 2005-06-30 Bayer Corporation Inhibition of matrix metalloproteases by 2-substit
US6008243A (en) * 1996-10-24 1999-12-28 Agouron Pharmaceuticals, Inc. Metalloproteinase inhibitors, pharmaceutical compositions containing them, and their use
IL128545A0 (en) * 1996-12-09 2000-01-31 Warner Lambert Co Method for treating and preventing heart failure and ventricular dilatation
EP1086085A1 (en) * 1998-06-12 2001-03-28 Vertex Pharmaceuticals Incorporated INHIBITORS OF p38
PA8539301A1 (es) * 2001-02-14 2002-09-30 Warner Lambert Co Inhibidores de la metaloproteinasa de la matriz
US20030114666A1 (en) * 2001-06-19 2003-06-19 Ellsworth Edmund Lee Antibacterial agents
US7038048B2 (en) * 2002-05-23 2006-05-02 Cytokinetics, Inc. 3H-pyridopyrimidin-4-one compounds, compositions, and methods of their use
AU2003249505A1 (en) * 2002-07-17 2004-02-02 Warner-Lambert Company Llc Combination of an allosteric alkyne inhibitor of matrix metalloproteinase-13 with celecoxib or valdecoxib
AU2003281168A1 (en) * 2002-07-17 2004-02-02 Warner-Lambert Company Llc Combination of an allosteric alkyne inhibitor of matrix metalloproteinase-13 with a selective inhibitor of cyclooxygenase-2 that is not celecoxib or valdecoxib
EP1530467A2 (en) * 2002-07-17 2005-05-18 Warner-Lambert Company LLC Combination of an allosteric carboxylic inhibitor of matrix metalloproteinase-13 with celecoxib or valdecoxib
EP1530475A2 (en) * 2002-07-17 2005-05-18 Warner-Lambert Company LLC Pharmaceutical compositions comprising an allosteric carboxylic inhibitor of matrix metalloproteinase-13 and a selective inhibitor of cyclooxygenase-2
EP1539163A1 (en) * 2002-08-13 2005-06-15 Warner-Lambert Company LLC 4-hydroxyquinoline derivatives as matrix metalloproteinase inhibitors
AU2003249535A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc 1,6-fused uracil derivatives as matrix metalloproteinase inhibitors
EP1530472A1 (en) * 2002-08-13 2005-05-18 Warner-Lambert Company LLC Isoquinoline derivatives as matrix metalloproteinase inhibitors
WO2004014388A1 (en) * 2002-08-13 2004-02-19 Warner-Lambert Company Llc 6,6-fused heteroaryl derivatives as matrix metalloproteinase inhibitors
AU2003250475A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc 5,6-fused 3,4-dihydropyrimidine-2-one derivatives as matrix metalloproteinase inhibitors
AU2003250466A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc 3-isoquinolinone derivatives as matrix metalloproteinase inhiitors
WO2004014389A1 (en) * 2002-08-13 2004-02-19 Warner-Lambert Company Llc 3,4-dihydroquinolin-2-one, 5,6-fused oxazin-3-one, and 5,6-fused thiazin-3-one derivatives as matrix metalloproteinase inhibitors
AU2003250465A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc 5,6-fused uracil derivatives as matrix metalloproteinase inhibitors
CA2497658A1 (en) * 2002-08-13 2004-02-19 Warner-Lambert Company Llc Chromone derivatives as matrix metalloproteinase inhibitors
US7439249B2 (en) * 2002-12-31 2008-10-21 Vertex Pharmaceuticals Incorporated Inhibitors of phosphatases
AU2004249120B2 (en) * 2003-05-23 2008-07-24 Glaxosmithkline Guanidino-substituted quinazolinone compounds as MC4-R agonists
ATE433974T1 (de) * 2003-09-19 2009-07-15 Gilead Sciences Inc Azachinolinolphosphonatverbindungen als integraseinhibitoren

Also Published As

Publication number Publication date
TNSN03045A1 (en) 2005-12-23
CZ20032142A3 (cs) 2004-12-15
PL367396A1 (en) 2005-02-21
KR20030074827A (ko) 2003-09-19
CA2437122A1 (en) 2002-08-22
PA8539401A1 (es) 2002-10-28
MA26994A1 (fr) 2004-12-20
EE200300384A (et) 2003-12-15
UY27173A1 (es) 2002-09-30
ECSP034730A (es) 2003-12-01
WO2002064572A1 (en) 2002-08-22
IS6886A (is) 2003-07-24
IL157109A0 (en) 2004-02-08
CN1537105A (zh) 2004-10-13
SV2003000876A (es) 2003-08-19
PE20021005A1 (es) 2002-11-27
BG108091A (en) 2004-12-30
AP2003002841A0 (en) 2003-09-30
ZA200306008B (en) 2005-01-26
MXPA03007248A (es) 2005-02-14
OA12550A (en) 2006-06-05
NO20033593L (no) 2003-08-13
EP1368324A1 (en) 2003-12-10
SK10012003A3 (sk) 2004-09-08
HUP0303164A2 (hu) 2004-01-28
NO20033593D0 (no) 2003-08-13
EA200300792A1 (ru) 2004-02-26
US20020193377A1 (en) 2002-12-19
BR0207268A (pt) 2005-03-15
JP2004523546A (ja) 2004-08-05

Similar Documents

Publication Publication Date Title
AR032676A1 (es) Quinazolinas como inhibidores de mmp-13
AR011101A1 (es) Compuesto derivado de acidos arilsulfonilaminohidroxiamicos y composicion farmaceutica que lo contiene
CY1108313T1 (el) Παραγωγα της κινολινης και η χρηση τους ως προσδεματων 5-ht6
AR006360A1 (es) Derivados de 1,2,3,4-tetrahidronaftaleno substituidos, uso de los mismos para la preparacion de medicamentos y procedimiento para su preparacion.
HUP0402313A2 (hu) Szerotonin újrafelvételt gátló fenilpiperazin-származékok, az ezeket tartalmazó gyógyászati készítmények és alkalmazásuk
AR048934A1 (es) Morfolinas
PE20030703A1 (es) Inhibidores de la 17b-hidroxiesteroide deshidrogenasa tipo 3
ES522199A0 (es) Un procedimiento para preparar un derivado de dihidropiridina.
CO5150227A1 (es) Compuestos de triazol y su utilizacion
RU95108387A (ru) Дикетопиперазин, способ его получения, фармацевтическая композиция, применение дикетопиперазина
AR038881A1 (es) Compuestos que modulan la actividad de ppar, composicion farmaceutica que los contiene y un procedimiento para la preparcion de aquellos
AR013184A1 (es) Aminas heterociclicas espiroazobiciclicas, composicion farmaceutica, uso de dichas aminas para preparar medicamentos y metodo de tratamiento o profilaxis
AR046938A1 (es) Procedimiento para preparar hexahidropirimido[1,2-a]azepin-2-carboxilatos y compuetos similares
HRP20050830A2 (en) Non-nucleoside reverse transcriptase inhibitors i for treating hiv mediated diseases
AR053340A1 (es) Derivados de trifluormetilbenzamida y sus usos terapeuticos
AR048567A1 (es) Derivados de benzoxazinona, su preparacion y composiciones farmaceuticas.
EA200500822A1 (ru) Замещённый индолпиридиний в качестве противоинфекционных соединений
MXPA04004593A (es) Triazoles fenilo-sustituidos y su uso como inhibidores selectivos de cinasa de tipo activina-5.
AR016644A1 (es) Compuestos de 2-aminopiridinas con sustituyentes alcoxi ramificados, composicion farmaceutica y uso para la manufactura de medicamentos
DK1717229T3 (da) Ny cyklisk forbindelse med 4-pyridylalkylthiogruppe med deri indført (u)substitueret amino
DOP2002000399A (es) Nuevos derivados de acido sulfonico
CO4930276A1 (es) Nuevos derivados de aminofosfohato y proceso de prepara cion
UY28528A1 (es) Nuevos compuestos
DE69220133D1 (de) N-Cyclohexyl Benzamide Derivate, ihre Herstellungen und therapeutischen Anwendungen
AR036812A1 (es) Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3, composiciones farmaceuticas y el uso de dichos compuestos para la fabricacion de medicamentos para el tratamiento de enfermedades androgeno-dependientes

Legal Events

Date Code Title Description
FA Abandonment or withdrawal