AR053346A1 - Compuesto derivado de 8h -pirido (2,3-d) pirimidin -7 ona 2,4,8- trisustituida composicion farmaceutica y uso para preparar una composicion para tratamiento y profilxis de una enfermedad mediada por la quinasa csbp/ rk/p38 - Google Patents

Compuesto derivado de 8h -pirido (2,3-d) pirimidin -7 ona 2,4,8- trisustituida composicion farmaceutica y uso para preparar una composicion para tratamiento y profilxis de una enfermedad mediada por la quinasa csbp/ rk/p38

Info

Publication number
AR053346A1
AR053346A1 ARP060101147A ARP060101147A AR053346A1 AR 053346 A1 AR053346 A1 AR 053346A1 AR P060101147 A ARP060101147 A AR P060101147A AR P060101147 A ARP060101147 A AR P060101147A AR 053346 A1 AR053346 A1 AR 053346A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
optionally substituted
heteroaryl
heterocyclyl
Prior art date
Application number
ARP060101147A
Other languages
English (en)
Original Assignee
Glaxo Group Ltd
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 Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of AR053346A1 publication Critical patent/AR053346A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • 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
    • 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
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/16—Emollients or protectives, e.g. against radiation
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • 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
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • 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
    • 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
    • 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
    • A61P9/10—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

Abstract

Compuesto derivado de 8H-pirido[2,3-d]pirimidin-7-ona 2,4,8-trisustituida, caracterizado porque es de formula (1) o (2) donde G1 y G2 son independientemente N; G3 es CH2; G4 es CH; R1 es C(Z)N(R10')(CR10R20)vRb, C(Z)O(CR10R20)vRb, N(R10')C(Z)(CR10R20)vRb, N(R10')C(Z)N(R10')(CR!0R20)vRb o N(R10')OC(Z)(CR10R20)vRb; R1' se selecciona independientemente en cada caso entre halogeno, alquilo C1-4, halo-alquilo C1-4 sustituido, ciano, nitro, (CR10R20)v'NRdRd', (CR10R20)v'C(O)R12, SR5, S(O)R5, S(O)2R5 o (CR10R20)v'OR13; X es R2', OR2', S(O)mR2', (CH2)n'N(R10')S(O)mR2', (CH2)n'N(R10')C(O)R2', (CH2)n'NR4R14, (CH2)n'N(R2')(R2ö) o N(R10')RhNH-C(=N-CN)NRqRq'; X1 es N(R11), O, S(O)m o CR10R20; Rb es un resto H, alquilo C1-10, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-10, arilo, aril-alquilo C1-10, heteroarilo, heteroaril-alquilo C1-10, heterociclilo o heterociclil-alquilo C1-10, donde todos estos resto, excluyendo el H, pueden estar opcionalmente sustituidos; Rh se selecciona entre un alquilo C1-10 opcionalmente sustituido -CH2-C(O)-CH2-, -CH2-O-CH2-, -CH2-C(O)N(R10')CH2-CH2-, -CH2-N(R10')C(O)CH2-, -CH2-CH(OR10')-CH2-, -CH2-C(O)O-CH2-CH2- o -CH2-CH2-O-C(O)CH2-; Rq y Rq' se seleccionan independientemente en cada caso entre un resto H, alquilo C1-10, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-10, cicloalquenilo C5-7, cicloalquenil C5-7-alquilo C1-10, arilo, aril-alquilo C1-10, heteroarilo, heteroaril-alquilo C1-10, heterociclilo o heterociclil- alquilo C1-10 donde todos los restos excepto el resto H, están opcionalmente sustituidos, o Rq y Rq' junto con el N al que están unidos forman un anillo heterocíclico opcionalmente sustituido de 5 a 7 miembros, donde dicho anillo puede contener un heteroátomo adicional seleccionado entre O, N o S; R2 es un resto H, alquilo C1-10, cicloalquilo C3-7, cicloalquilalquilo C3-7, arilo, aril-alquilo C1-10, heteroarilo, heteroaril-alquilo C1-10, heterociclilo o heterociclil-alquilo C1-10, y donde cada uno de estos restos, excluyendo el H, pueden estar opcionalmente sustituido; o R2 es el resto (CR10R20)q'X1(CR10R20)qC(A1)(A2)(A3) o (CR10R20)q'C(A1)(A2)(A3); R2' es un resto H, alquilo C1-10, cicloalquilo C3-7, cicloalquilalquilo C3-7, arilo, aril-alquilo C1-10, heteroarilo, heteroaril-alquilo C1-10, heterociclilo o heterociclil-alquilo C1-10, y donde cada uno de estos restos, excluyendo el H, pueden estar opcionalmente sustituido; o R2ö es un resto H, alquilo C1-10, cicloalquilo C3-7, cicloalquilalquilo C3-7, arilo, aril-alquilo C1-10, heteroarilo, heteroaril-alquilo C1-10, heterociclilo o heterociclil-alquilo C1-10, y donde cada uno de estos restos, excluyendo el H, pueden estar opcionalmente sustituido; o donde R2ö es el resto (CR10R20)tX1(CR10R20)qC(A1)(A2)(A3); A1 es un alquilo C1-10 opcionalmente sustituido; A2 es un alquilo C1-10 opcionalmente sustituido, A3 es H o es un alquilo C1-10 opcionalmente sustituido; R3 es un resto alquilo C1-10, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-10, arilo, aril-alquilo C1-10, heteroarilo, heteroaril-alquilo C1-10, heterociclilo o heterociclil-alquilo C1-10, y donde cada uno de estos restos pueden estar opcionalmente sustituido; cada uno de R4 y R14 se selecciona independientemente en cada caso entre H, alquilo C1-4, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, arilo, aril-alquilo C1-4, heterociclilo, alquilo C1-4 heterocíclico, heteroarilo, heteroaril-alquilo C1-4, y donde cada uno de estos restos, excluyendo el H, pueden estar opcionalmente sustituido; o R4 y R14 junto con el N al que están unidos forman un anillo heterocíclico opcionalmente sustituido de 4 a 7 miembros, donde dicho anillo contiene opcionalmente un heteroátomo adicional seleccionado entre O, S o NR9; cada uno de R4' y R14' se selecciona independientemente en cada caso entre H o alquilo C1-4, o R4' y R14' junto con el N al que están unidos forman un anillo heterocíclico de 5 a 7 miembros, donde dicho anillo contiene opcionalmente un heteroátomo adicional seleccionado entre NR9'; R5 se selecciona independientemente en cada caso entre H, alquilo C1-4, alquenilo C2-4, alquinilo C2-4 o NR4'R14', excluyendo los restos SR5 que son SNR4'R14'; S(O)2R5 que son SO2H y S(O)R5 que son SOH; R6 se selecciona independientemente en cada caso entre un resto H, alquilo C1-10, cicloalquilo C3-7, heterociclilo, heterociclil-alquilo C1-10, arilo, aril-alquilo C1-10, heteroarilo o heteroaril-alquilo C1-10, y donde cada uno de estos restos, excluyendo el H, puede estar opcionalmente sustituido; R9 se selecciona independientemente en cada caso entre H, C(Z)R6, alquilo C1-10 opcionalmente sustituido, arilo opcionalmente sustituido o un aril-alquilo C1-14 opcionalmente sustituido; R9' se selecciona independientemente en cada caso entre H o alquilo C1-4; R10 y R20 se seleccionan independientemente en cada caso entre H o alquilo C1-4; R10' se selecciona independientemente en cada caso con H o alquilo C1-4; R11 se selecciona independientemente en cada caso entre H o alquilo C1-4; R12 se selecciona independientemente en cada caso entre un resto H, alquilo C1-4, halo-alquilo C1-4 sustituido, alquenilo C2-4, alquinilo C2-4, cicloalquilo C3-7, cicloalquil C3-7- alquilo C1-4, cicloalquenilo C5-7, cicloalquenil C5-7-alquilo C1-4, arilo, aril-alquilo C1-4, heteroarilo, heteroaril-alquilo C1-4, heterociclilo o heterociclil-alquilo C1-4, y donde cada uno de estos restos, excluyendo al H, puede estar opcionalmente sustituido; R13 se selecciona independientemente en cada caso entre un resto H, alquilo C1-4, halo-alquilo C1-4 sustituido, alquenilo C2-4, alquinilo C2-4, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, cicloalquenilo C5-7, cicloalquenil C5-7-alquilo C1-4, arilo, aril-alquilo C1-4, heteroarilo, heteroaril-alquilo C1-4, heterociclilo o heterociclil-alquilo C1-4, y donde cada uno de estos restos, excluyendo al H, puede estar opcionalmente sustituido; cada uno de Rd y Rd' se selecciona independientemente en cada caso entre un resto H, alquilo C1-4, cicloalquilo C3-6, cicloalquil C3-6-alquilo C1-4 y donde cada uno de estos restos, excluyendo al H, puede estar opcionalmente sustituido; o Rd y Rd' junto con el N al que están unidos forman un anillo heterocíclico opcionalmente sustituido de 5 a 6 miembros, donde dicho anillo contiene opcionalmente un heteroátomo adicional seleccionado entre O, S o NR9'; g es 0 o un numero entero que tiene el valor 1, 2, 3, o 4; n' es 0 o un numero entero que tiene un valor de 1 a 10; m es 0 o un numero entero que tiene el valor 1 o 2; q es 0 o un entero que tiene un valor de 1 a 10; q' es 0 o un numero entero que tiene un valor de 1 a 6; t es un numero entero que tiene un valor de 2 a 6; v es 0 o un numero entero que tiene el valor 1 o 2; v' es 0 o un numero entero que tiene el valor 1 o 2; Z se selecciona independientemente en cada caso entre O o S; y una sal farmacéuticamente aceptable, solvato o derivado fisiologicamente funcional del mismo. Composicion farmacéutica que lo comprende. Uso para preparar una composicion farmacéutica para el tratamiento, incluyendo profilaxis, de una enfermedad mediada por la quinasa CSBP/RK/p38.
ARP060101147A 2005-03-25 2006-03-23 Compuesto derivado de 8h -pirido (2,3-d) pirimidin -7 ona 2,4,8- trisustituida composicion farmaceutica y uso para preparar una composicion para tratamiento y profilxis de una enfermedad mediada por la quinasa csbp/ rk/p38 AR053346A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US66531505P 2005-03-25 2005-03-25

Publications (1)

Publication Number Publication Date
AR053346A1 true AR053346A1 (es) 2007-05-02

Family

ID=37053943

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060101147A AR053346A1 (es) 2005-03-25 2006-03-23 Compuesto derivado de 8h -pirido (2,3-d) pirimidin -7 ona 2,4,8- trisustituida composicion farmaceutica y uso para preparar una composicion para tratamiento y profilxis de una enfermedad mediada por la quinasa csbp/ rk/p38

Country Status (25)

Country Link
US (3) US8207176B2 (es)
EP (3) EP2447266B1 (es)
JP (1) JP5037487B2 (es)
KR (1) KR101235497B1 (es)
CN (4) CN101258148A (es)
AR (1) AR053346A1 (es)
AU (1) AU2006229993B2 (es)
BR (1) BRPI0609437A2 (es)
CA (1) CA2602553C (es)
EA (1) EA012875B1 (es)
ES (2) ES2398246T3 (es)
HK (1) HK1111422A1 (es)
IL (1) IL185870A (es)
MA (1) MA29341B1 (es)
MX (1) MX2007011856A (es)
MY (2) MY145343A (es)
NO (1) NO20075275L (es)
NZ (1) NZ561237A (es)
PE (2) PE20100737A1 (es)
SG (1) SG166771A1 (es)
TW (1) TWI389690B (es)
UA (1) UA95444C2 (es)
UY (1) UY29440A1 (es)
WO (1) WO2006104915A2 (es)
ZA (1) ZA200707564B (es)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7235551B2 (en) * 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
CZ20031125A3 (cs) * 2000-10-23 2003-10-15 Smithkline Beecham Corporation Nové sloučeniny
PL373339A1 (en) * 2002-04-19 2005-08-22 Smithkline Beecham Corporation Novel compounds
PE20100741A1 (es) * 2005-03-25 2010-11-25 Glaxo Group Ltd COMPUESTOS DERIVADOS DE 3,4-DIHIDROPIRIMIDO[4,5-d]PIRIMIDIN-2(1H)-ONA COMO INHIBIDORES DE QUINASA p38
EP1868612A4 (en) * 2005-03-25 2010-03-24 Glaxo Group Ltd NOVEL CONNECTIONS
WO2006104917A2 (en) * 2005-03-25 2006-10-05 Glaxo Group Limited Process for preparing pyrido[2,3-d]pyrimidin-7-one and 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1h)-one derivatives
TWI389690B (zh) 2005-03-25 2013-03-21 Glaxo Group Ltd 新穎化合物（一）
JP2009542816A (ja) * 2006-06-16 2009-12-03 グラクソ グループ リミテッド 新規化合物
EP2032142A4 (en) * 2006-06-16 2010-07-21 Glaxo Group Ltd NOVEL CONNECTIONS
GB0621830D0 (en) * 2006-11-02 2006-12-13 Chroma Therapeutics Ltd Inhibitors of p38 mitogen-activated protein kinase
EP1992344A1 (en) 2007-05-18 2008-11-19 Institut Curie P38 alpha as a therapeutic target in pathologies linked to FGFR3 mutation
WO2012158197A2 (en) * 2010-11-11 2012-11-22 Lyndor Biosciences L.L.C. Compounds useful as akt/pkb modulators and uses thereof
HUE034721T2 (hu) * 2011-08-25 2018-02-28 St Jude Childrens Res Hospital Szubsztituált 2-alkil-1-oxo-N-fenil-3-heteroaril-1,2,3,4-tetrahidroizokinolin-4-karboxamidok maláriaellenes terápiákhoz
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
WO2019071144A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. USE OF P38 INHIBITORS TO REDUCE DUX4 EXPRESSION

Family Cites Families (208)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US25386A (en) 1859-09-13 Fastening fob
US2833779A (en) 1956-10-29 1958-05-06 American Cyanamid Co Substituted pyrazoles
US2918408A (en) 1957-04-08 1959-12-22 Lakeside Lab Inc Anti-spasmodic compositions specific for treating spasm of the colon
US3631045A (en) 1969-11-04 1971-12-28 American Home Prod 4 5-diamino-7h-pyrrolo(2 3-d)pyrimidine derivatives
US3910913A (en) 1969-11-04 1975-10-07 American Home Prod 4,5-Diamino-7H-pyrrolo{8 2,3-d{9 pyrimidine derivatives
US3707475A (en) 1970-11-16 1972-12-26 Pfizer Antiinflammatory imidazoles
US3940486A (en) 1971-05-10 1976-02-24 Ciba-Geigy Corporation Imidazole derivatives in the treatment of pain
US3929807A (en) 1971-05-10 1975-12-30 Ciba Geigy Corp 2-Substituted-4(5)-(aryl)-5(4)-(2,3 or -4-pyridyl)-imidazoles
CA966134A (en) * 1972-05-05 1975-04-15 Haydn W.R. Williams 1,8-naphthyridine compounds
US4058614A (en) 1973-12-04 1977-11-15 Merck & Co., Inc. Substituted imidazole compounds and therapeutic compositions therewith
US4199592A (en) 1978-08-29 1980-04-22 E. I. Du Pont De Nemours And Company Antiinflammatory 4,5-diaryl-2-nitroimidazoles
JPS5618982A (en) * 1979-06-14 1981-02-23 Wellcome Found Pyrimidine derivatives and medicinal drug containing them
CY1308A (en) 1979-12-06 1985-12-06 Glaxo Group Ltd Device for dispensing medicaments
CA1175431A (en) 1980-07-25 1984-10-02 Alfred Sallmann Tri-substituted imidazole derivatives, processes for their manufacture, pharmaceutical preparations containing them, and their use
US4353656A (en) 1980-10-14 1982-10-12 Xerox Corporation Moving coil, multiple energy print hammer system including a closed loop servo
DE3274065D1 (de) 1981-07-08 1986-12-11 Draco Ab Powder inhalator
GB2123831B (en) 1981-07-20 1986-01-15 Ciba Geigy Ag Trisubstituted oxazo compounds
US4503065A (en) 1982-08-03 1985-03-05 E. I. Du Pont De Nemours And Company Antiinflammatory 4,5-diaryl 1-2-halo imidazoles
GB2169265B (en) 1982-10-08 1987-08-12 Glaxo Group Ltd Pack for medicament
CA1224992A (en) 1982-10-08 1987-08-04 Robert E. Newell Device for administering medicament to patients
US4778054A (en) 1982-10-08 1988-10-18 Glaxo Group Limited Pack for administering medicaments to patients
JPS60226882A (ja) 1984-04-24 1985-11-12 Nippon Zoki Pharmaceut Co Ltd 新規ピリミドピリミジン誘導体
US4565875A (en) 1984-06-27 1986-01-21 Fmc Corporation Imidazole plant growth regulators
US4560691A (en) * 1984-07-13 1985-12-24 Sterling Drug Inc. 5-(Phenyl)-1,6-naphthyridin-2(1H)-ones, their cardiotonic use and preparation
FR2585563B1 (fr) 1985-07-30 1993-11-12 Glaxo Group Ltd Dispositif pour administrer des medicaments a des patients
US4686231A (en) 1985-12-12 1987-08-11 Smithkline Beckman Corporation Inhibition of 5-lipoxygenase products
IL83467A0 (en) 1986-08-15 1988-01-31 Fujisawa Pharmaceutical Co Imidazole derivatives,processes for their preparation and pharmaceutical compositions containing the same
EP0278686A1 (en) 1987-02-07 1988-08-17 The Wellcome Foundation Limited Pyridopyrimidines methods for their preparation and pharmaceutical formulations thereof
JPH01261306A (ja) 1988-04-13 1989-10-18 Nippon Kayaku Co Ltd ２−アルキルチオ−４−アミノピリミジン誘導体を有効成分とする開花促進剤
GB9004781D0 (en) 1990-03-02 1990-04-25 Glaxo Group Ltd Device
EP0470600B1 (de) 1990-08-10 1997-05-07 Novartis AG Naphthylalkylaminopyrimidin-Derivate, Verfahren zu ihrer Herstellung und diese enthaltende Schädlingsbekämpfungsmittel
FR2665898B1 (fr) 1990-08-20 1994-03-11 Sanofi Derives d'amido-3 pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
IE913473A1 (en) 1990-10-15 1992-04-22 Fujisawa Pharmaceutical Co Quinazoline derivatives and their preparation
WO1992012154A1 (en) 1990-12-31 1992-07-23 Fujisawa Pharmaceutical Co., Ltd. Imidazotriazine derivatives
JP3375659B2 (ja) 1991-03-28 2003-02-10 テキサス インスツルメンツ インコーポレイテツド 静電放電保護回路の形成方法
EP0584222B1 (en) 1991-05-10 1997-10-08 Rhone-Poulenc Rorer International (Holdings) Inc. Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
FR2676734B1 (fr) 1991-05-23 1995-05-19 Roussel Uclaf Nouveaux derives de la pyrimidine, leur procede de preparation, les nouveaux intermediaires obtenus, leur application a titre de medicaments et les compositions pharmaceutiques les renfermant.
IL102764A0 (en) 1991-08-16 1993-01-31 Merck & Co Inc Quinazoline derivatives,and pharmaceutical compositions containing them
DE4131029A1 (de) * 1991-09-18 1993-07-29 Basf Ag Substituierte pyrido (2,3-d) pyrimidine als antidots
GB9127376D0 (en) 1991-12-24 1992-02-19 Wellcome Found Amidino derivatives
US5716972A (en) 1993-01-13 1998-02-10 Smithkline Beecham Corporation Pyridyl substituted imidazoles
US5916891A (en) 1992-01-13 1999-06-29 Smithkline Beecham Corporation Pyrimidinyl imidazoles
US5656644A (en) 1994-07-20 1997-08-12 Smithkline Beecham Corporation Pyridyl imidazoles
IL104369A0 (en) 1992-01-13 1993-05-13 Smithkline Beecham Corp Novel compounds and compositions
US6008235A (en) 1992-01-13 1999-12-28 Smithkline Beecham Corporation Pyridyl substituted imidazoles
CZ283425B6 (cs) 1992-04-02 1998-04-15 Smithkline Beecham Corporation Fenylové deriváty a farmaceutické prostředky s jejich obsahem
GB9303993D0 (en) 1993-02-26 1993-04-14 Fujisawa Pharmaceutical Co New heterocyclic derivatives
US5466692A (en) 1993-03-24 1995-11-14 American Home Products Corporation Substituted pyridopyrimidines and antihypertensives
US5593991A (en) 1993-07-16 1997-01-14 Adams; Jerry L. Imidazole compounds, use and process of making
US5670527A (en) 1993-07-16 1997-09-23 Smithkline Beecham Corporation Pyridyl imidazole compounds and compositions
US5593992A (en) 1993-07-16 1997-01-14 Smithkline Beecham Corporation Compounds
US5783664A (en) 1993-09-17 1998-07-21 Smithkline Beecham Corporation Cytokine suppressive anit-inflammatory drug binding proteins
US5869043A (en) 1993-09-17 1999-02-09 Smithkline Beecham Corporation Drug binding protein
CN1048731C (zh) 1993-09-17 2000-01-26 史密丝克莱恩比彻姆公司 编码细胞因子抑制性抗炎药物结合蛋白质的多核苷酸
US5426110A (en) * 1993-10-06 1995-06-20 Eli Lilly And Company Pyrimidinyl-glutamic acid derivatives
JPH09505055A (ja) 1993-11-08 1997-05-20 スミスクライン・ビーチャム・コーポレイション サイトカイン媒介疾患治療用オキサゾール
GB9325217D0 (en) 1993-12-09 1994-02-09 Zeneca Ltd Pyrimidine derivatives
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
US5559137A (en) 1994-05-16 1996-09-24 Smithkline Beecham Corp. Compounds
US5547954A (en) * 1994-05-26 1996-08-20 Fmc Corporation 2,4-Diamino-5,6-disubstituted-and 5,6,7-trisubstituted-5-deazapteridines as insecticides
US5545669A (en) 1994-06-02 1996-08-13 Adams; Jerry L. Anti-inflammatory compounds
TW574214B (en) 1994-06-08 2004-02-01 Pfizer Corticotropin releasing factor antagonists
ATE191470T1 (de) 1994-06-15 2000-04-15 Wellcome Found Enzymhemmer
US5998428A (en) 1995-05-31 1999-12-07 Smithkline Beecham Corporation Compounds and methods for treating PDE IV-related diseases
CN1043993C (zh) 1994-08-29 1999-07-07 山之内制药株式会社 萘啶衍生物及其医药组合物
IL115256A0 (en) 1994-11-14 1995-12-31 Warner Lambert Co 6-Aryl pyrido (2,3-d) pyrimidines and naphthyridines and their use
WO1996028367A2 (en) 1995-03-10 1996-09-19 Minnesota Mining And Manufacturing Company Aerosol valves
US5620981A (en) * 1995-05-03 1997-04-15 Warner-Lambert Company Pyrido [2,3-D]pyrimidines for inhibiting protein tyrosine kinase mediated cellular proliferation
IL118544A (en) 1995-06-07 2001-08-08 Smithkline Beecham Corp History of imidazole, the process for their preparation and the pharmaceutical preparations containing them
AU718553B2 (en) 1995-06-07 2000-04-13 Wyeth Process for preparation of biphenyl derivatives
US5739143A (en) 1995-06-07 1998-04-14 Smithkline Beecham Corporation Imidazole compounds and compositions
US5760220A (en) * 1995-06-07 1998-06-02 American Home Products Corporation Process for preparation of biphenyl derivatives
ZA9610687B (en) 1995-12-22 1997-09-29 Smithkline Beecham Corp Novel synthesis.
KR19990077164A (ko) 1996-01-11 1999-10-25 스티븐 베네티아너 신규 치환된 이미다졸 화합물
ZA97175B (en) 1996-01-11 1997-11-04 Smithkline Beecham Corp Novel substituted imidazole compounds.
US6150337A (en) 1996-01-23 2000-11-21 Icn Pharmaceuticals, Inc. Specific modulation of Th1/Th2 cytokine expression by Ribavirin in activated T-lymphocytes
US20020137696A1 (en) 1996-01-23 2002-09-26 Robert Tam Specific modulation of TH1/TH2 cytokine expression by ribavirin in activated T-lymphocytes
US5767097A (en) 1996-01-23 1998-06-16 Icn Pharmaceuticals, Inc. Specific modulation of Th1/Th2 cytokine expression by ribavirin in activated T-lymphocytes
EP1005343A4 (en) 1996-03-08 2000-06-07 Smithkline Beecham Corp USE OF CSAIDS AS ANGIOGENESIS INHIBITORS
EP0889888A4 (en) 1996-03-25 2003-01-08 Smithkline Beecham Corp NEW TREATMENT OF LESIONS IN THE CENTRAL NERVOUS SYSTEM
WO1997035855A1 (en) 1996-03-25 1997-10-02 Smithkline Beecham Corporation Novel treatment for cns injuries
ATE230740T1 (de) 1996-04-12 2003-01-15 Sumitomo Pharma Piperidinylpyrimidine derivate
US6875769B2 (en) * 1996-05-23 2005-04-05 Pfizer Inc. Substituted6,6-hetero-bicyclicderivatives
ZA973884B (en) * 1996-05-23 1998-11-06 Du Pont Merck Pharma Tetrahydropteridines and pyridylpiperazines for treatment of neurological disorders
DE69719193T2 (de) 1996-08-06 2003-09-25 Pfizer Substituierte pyrido- oder pyrimidogruppen enthaltende 6,6- oder 6,7-bicyclische derivate
TW477787B (en) 1996-08-27 2002-03-01 Pfizer Pyrido six-membered nitrogen-containing cyclic ring derivatives having corticotropin releasing factor antagonist activity and pharmaceutical composition containing same
US6455690B1 (en) 1996-10-16 2002-09-24 Robert Tam L-8-oxo-7-propyl-7,8-dihydro-(9H)-guanosine
US6509320B1 (en) 1996-10-16 2003-01-21 Icn Pharmaceuticals, Inc. Purine L-nucleosides, analogs and uses thereof
CZ126799A3 (cs) 1996-10-16 1999-07-14 Icn Pharmaceuticals Purinové L-nukleosidy a jejich analogy a farmaceutické prostředky, které je obsahují
US6147080A (en) 1996-12-18 2000-11-14 Vertex Pharmaceuticals Incorporated Inhibitors of p38
GB9700226D0 (en) 1997-01-08 1997-02-26 Glaxo Group Ltd Inhalation device
US5929076A (en) 1997-01-10 1999-07-27 Smithkline Beecham Corporation Cycloalkyl substituted imidazoles
MY117948A (en) 1997-01-13 2004-08-30 Glaxo Group Ltd Nitride oxide synthase inhibitors.
US6268310B1 (en) 1997-01-28 2001-07-31 Nippon Soda Co., Ltd. Oxazole derivative, process for producing the same, and herbicide
US6498163B1 (en) * 1997-02-05 2002-12-24 Warner-Lambert Company Pyrido[2,3-D]pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation
US5945422A (en) * 1997-02-05 1999-08-31 Warner-Lambert Company N-oxides of amino containing pyrido 2,3-D! pyrimidines
WO1998033798A2 (en) 1997-02-05 1998-08-06 Warner Lambert Company Pyrido[2,3-d]pyrimidines and 4-amino-pyrimidines as inhibitors of cell proliferation
DE19723722A1 (de) 1997-05-30 1998-12-10 Schering Ag Nichtsteroidale Gestagene
AU9281298A (en) 1997-10-01 1999-04-23 Kyowa Hakko Kogyo Co. Ltd. Benzodioxole derivatives
CA2306077A1 (en) 1997-10-08 1999-04-15 Smithkline Beecham Corporation Novel cycloalkenyl substituted compounds
JP2001526230A (ja) 1997-12-19 2001-12-18 スミスクライン・ビーチャム・コーポレイション ヘテロアリール置換イミダゾール化合物、その医薬組成物および使用
US6423695B1 (en) 1998-01-13 2002-07-23 Ribapharm, Inc. Cytokine related treatments of disease
US6506766B1 (en) 1998-02-13 2003-01-14 Abbott Laboratories Glucocortiocoid-selective antinflammatory agents
US6200977B1 (en) 1998-02-17 2001-03-13 Tularik Inc. Pyrimidine derivatives
US6306866B1 (en) 1998-03-06 2001-10-23 American Cyanamid Company Use of aryl-substituted pyrimidines as insecticidal and acaricidal agents
EP1070056B1 (en) 1998-03-14 2004-06-30 ALTANA Pharma AG Phthalazinone pde iii/iv inhibitors
JP2000038350A (ja) 1998-05-18 2000-02-08 Yoshitomi Pharmaceut Ind Ltd 糖尿病治療薬
ES2310039T3 (es) 1998-05-26 2008-12-16 Warner-Lambert Company Llc Pirimidinas biciclicas y 3,4-dihidropirimidinas biciclicas como inhibidores de la proliferacion celular.
US6248225B1 (en) 1998-05-26 2001-06-19 Ppg Industries Ohio, Inc. Process for forming a two-coat electrodeposited composite coating the composite coating and chip resistant electrodeposited coating composition
US20040044012A1 (en) 1998-05-26 2004-03-04 Dobrusin Ellen Myra Bicyclic pyrimidines and bicyclic 3,4-dihydropyrimidines as inhibitors of cellular proliferation
US6423425B1 (en) 1998-05-26 2002-07-23 Ppg Industries Ohio, Inc. Article having a chip-resistant electrodeposited coating and a process for forming an electrodeposited coating
GB9811599D0 (en) 1998-05-30 1998-07-29 Glaxo Group Ltd Nitric oxide synthase inhibitors
JP2002517486A (ja) 1998-06-12 2002-06-18 バーテックス ファーマシューティカルズ インコーポレイテッド ｐ３８のインヒビター
US5907465A (en) 1998-08-13 1999-05-25 Sensormatic Electronics Corporation Circuit for energizing EAS marker deactivation device with DC pulses of alternating polarity
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
AU762245B2 (en) 1998-09-18 2003-06-19 Vertex Pharmaceuticals Incorporated Inhibitors of p38
PT1117653E (pt) * 1998-10-01 2003-06-30 Astrazeneca Ab Derivados de quinolina e quinazolina e sua utilizacao como inibidores de doencas mediadas pela citosina
WO2000023444A1 (en) 1998-10-21 2000-04-27 Abbott Laboratories 5,7-disubstituted-4-aminopyrido[2,3-d]pyrimidine compounds
ID28276A (id) 1998-10-23 2001-05-10 Hoffmann La Roche Heterolingkar nitrogen bisiklik
US6358959B1 (en) 1999-01-26 2002-03-19 Merck & Co., Inc. Polyazanaphthalenone derivatives useful as alpha 1a adrenoceptor antagonists
AR035987A1 (es) 1999-03-01 2004-08-04 Smithkline Beecham Corp Uso de un compuesto inhibidor de la pde 4 para la manufactura de un medicamento y el medicamento para tratar asma inducida por ejercicio
EP1040831A3 (en) 1999-04-02 2003-05-02 Pfizer Products Inc. Use of corticotropin releasing factor (CRF) antagonists to prevent sudden death
CA2371273A1 (en) 1999-05-04 2000-11-09 Andrew Fensome Tetracyclic progesterone receptor modulator compounds and methods
ES2260033T3 (es) * 1999-07-02 2006-11-01 Stuart A. Lipton Uso de los inhibidores p38 mapk en efermadades oftalmicas.
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
US6263209B1 (en) 1999-07-28 2001-07-17 Motorola, Inc. Method and apparatus in a wireless communication system for creating a learning function
PL200923B1 (pl) 1999-08-21 2009-02-27 Nycomed Gmbh Lek zawierający inhibitor PDE w połączeniu z agonistą receptoraß₂ -adrenergicznego oraz zastosowanie połączenia roflumilastu i salmeterolu
CO5180649A1 (es) 1999-09-01 2002-07-30 Abbott Lab Antagonistas de los receptores de los glucocorticoides para el tratamiento de la diabetes para el tratamiento de la diabetes
EP1223924A4 (en) 1999-09-17 2004-07-14 Smithkline Beecham Corp USE OF CSAIDS AGAINST RHINOVIRUS INFECTION
CN1390220A (zh) 1999-09-17 2003-01-08 艾博特股份有限两合公司 作为治疗剂的激酶抑制剂
OA11558A (en) 1999-12-08 2004-06-03 Advanced Medicine Inc Beta 2-adrenergic receptor agonists.
WO2001042243A2 (en) 1999-12-08 2001-06-14 Advanced Medicine, Inc. Protein kinase inhibitors
US6632666B2 (en) 2000-01-14 2003-10-14 Biolife Solutions, Inc. Normothermic, hypothermic and cryopreservation maintenance and storage of cells, tissues and organs in gel-based media
PT1741447E (pt) 2000-01-21 2013-12-11 Novartis Ag Combinações que compreendem o inibidor da dipeptidilpeptidase-iv
CZ20022475A3 (cs) 2000-01-25 2003-03-12 Warner-Lambert Company Pyrido[2,3-d]pyrimidin-2,7-diaminové inhibitory kinázy
US20040224958A1 (en) * 2000-01-27 2004-11-11 Booth Richard John Pyridopyrimidinone derivatives for treatment of neurodegenerative disease
US7235551B2 (en) 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
SK12472002A3 (sk) 2000-03-06 2003-04-01 Warner-Lambert Company 5-Alkylpyrido[2,3-d]pyrimidínové inhibítory tyrosínových kináz
US7101882B2 (en) 2000-09-29 2006-09-05 Glaxo Group Limited Morpholin-acetamide derivatives for the treatment of inflammatory diseases
JP2004530648A (ja) 2000-10-19 2004-10-07 スミスクライン・ビーチャム・コーポレイション 炎症により促進される咳の治療のためのｐ３８阻害剤の使用
CZ20031125A3 (cs) 2000-10-23 2003-10-15 Smithkline Beecham Corporation Nové sloučeniny
US6945422B2 (en) * 2000-11-08 2005-09-20 Delphi Technologies, Inc. In-tank fuel line quick connector assembly
JP2002205986A (ja) 2000-11-08 2002-07-23 Takeda Chem Ind Ltd ピリミジン誘導体およびそれを含有する除草剤
AU2002246677B2 (en) * 2000-12-20 2006-11-16 Merck Sharp & Dohme Corp. (Halo-Benzo Carbonyl)Heterocyclo Fused Phenyl p38 Kinase Inhibiting Agents
GB0031179D0 (en) 2000-12-21 2001-01-31 Glaxo Group Ltd Nitric oxide synthase inhibitors
US6484903B2 (en) 2001-01-09 2002-11-26 Riverwood International Corporation Carton with an improved dispensing feature in combination with a unique handle
GB0103630D0 (en) 2001-02-14 2001-03-28 Glaxo Group Ltd Chemical compounds
US20030130264A1 (en) 2001-02-16 2003-07-10 Tularik Inc. Methods of using pyrimidine-based antiviral agents
DE10108481A1 (de) 2001-02-22 2002-10-24 Bayer Ag Pyridylpyrimidine
EP1366025B1 (en) 2001-03-08 2007-06-27 Glaxo Group Limited Agonists of beta-adrenoreceptors
ATE381537T1 (de) 2001-03-22 2008-01-15 Glaxo Group Ltd Formanilid-derivative als beta2-adrenorezeptor- agonisten
US7105667B2 (en) 2001-05-01 2006-09-12 Bristol-Myers Squibb Co. Fused heterocyclic compounds and use thereof
WO2002088079A2 (en) 2001-05-01 2002-11-07 Bristol-Myers Squibb Company Dual inhibitors of pde 7 and pde 4
PE20030008A1 (es) * 2001-06-19 2003-01-22 Bristol Myers Squibb Co Inhibidores duales de pde 7 y pde 4
US7087614B2 (en) 2001-06-19 2006-08-08 Bristol-Myers Squibb Co. Pyrimidine inhibitors of phosphodiesterase (PDE) 7
ATE417606T1 (de) 2001-09-14 2009-01-15 Glaxo Group Ltd Phenethanolamin-derivate zur behandlung von erkrankungen der atemwege
GB0124941D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
JP4178783B2 (ja) 2001-10-19 2008-11-12 三菱化学株式会社 光学記録媒体
WO2003042160A1 (en) 2001-11-13 2003-05-22 Theravance, Inc. Aryl aniline beta-2 adrenergic receptor agonists
US7019002B2 (en) * 2001-12-11 2006-03-28 Pharmacia & Upjohn, S.P.A. Pyridopyrimidinones derivatives as telomerase inhibitors
ATE346058T1 (de) 2002-01-14 2006-12-15 Boehringer Ingelheim Pharma Glucocorticoid mimetika, verfahren zu ihrer herstellung, pharmazeutische formulierungen sie enthaltend und verwendungen davon
IL162721A0 (en) * 2002-01-22 2005-11-20 Warner Lambert Co 2-(Pyridin-2-ylamino)-pyridoÄ2,3-dÜpyrimidin-7-ones
JP4745609B2 (ja) 2002-01-22 2011-08-10 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア グルココルチコイドレセプターのための非ステロイド性リガンド、その組成物および使用
GB0204719D0 (en) 2002-02-28 2002-04-17 Glaxo Group Ltd Medicinal compounds
EP1490317A1 (en) 2002-03-26 2004-12-29 Boehringer Ingelheim Pharmaceuticals Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
EA008830B1 (ru) 2002-03-26 2007-08-31 Бёрингер Ингельхайм Фармасьютиклз, Инк. Миметики глюкокортикоидов, способы их получения, фармацевтические композиции и их применение
DE10215316C1 (de) 2002-04-02 2003-12-18 Schering Ag Chinolin- und Isochinolin-Derivate, ein pharmazeutisches Mittel und ihre Verwendung als Entzündungshemmer
US7282591B2 (en) 2002-04-11 2007-10-16 Merck & Co., Inc. 1h-benzo{f}indazol-5-yl derivatives as selective glucocorticoid receptor modulators
JP2005523920A (ja) 2002-04-25 2005-08-11 グラクソ　グループ　リミテッド フェネタノールアミン誘導体
US20040063658A1 (en) * 2002-05-06 2004-04-01 Roberts Christopher Don Nucleoside derivatives for treating hepatitis C virus infection
ITBO20020304A1 (it) 2002-05-17 2003-11-17 Magneti Marelli Powertrain Spa Nuovi condotti in materiale polimerico
US7186864B2 (en) 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
AR040456A1 (es) * 2002-06-27 2005-04-06 Bristol Myers Squibb Co Piridina n-oxidos 2,4 -disubstituidos utiles como inhibidores de transcriptasa inversa del virus de inmunodeficiencia humana
ES2518940T3 (es) 2002-07-08 2014-11-06 Pfizer Products Inc. Moduladores del receptor de glucocorticoides
AU2003251969A1 (en) 2002-07-18 2004-02-09 Bristol-Myers Squibb Company Compositions and methods involving nuclear hormone receptor site ii
US6995181B2 (en) 2002-07-18 2006-02-07 Bristol-Myers Squibb Co. Modulators of the glucocorticoid receptor and method
GB0217225D0 (en) 2002-07-25 2002-09-04 Glaxo Group Ltd Medicinal compounds
CA2496175A1 (en) 2002-08-21 2004-03-04 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted hihydroquinolines as glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
JP4520309B2 (ja) 2002-09-20 2010-08-04 メルク・シャープ・エンド・ドーム・コーポレイション 選択的糖質コルチコイド受容体調節剤としてのオクタヒドロ−２−Ｈ−ナフト［１，２−ｆ］インドール−４−カルボキサミド誘導体
AU2003298094A1 (en) 2002-10-22 2004-05-13 Glaxo Group Limited Medicinal arylethanolamine compounds
AR041724A1 (es) 2002-10-28 2005-05-26 Glaxo Group Ltd Compuestos derivados de fenetanolamina y su utilizacion en composiciones farmaceuticas
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
GB0225535D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
GB0225540D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
TW200413381A (en) 2002-11-04 2004-08-01 Hoffmann La Roche Novel amino-substituted dihydropyrimido [4,5-d]pyrimidinone derivatives, their manufacture and use as pharmaceutical agents
WO2004043367A2 (en) 2002-11-06 2004-05-27 Bristol-Myers Squibb Company Fused heterocyclic compounds and use thereof
JP2004203751A (ja) 2002-12-24 2004-07-22 Pfizer Inc 置換６，６−ヘテロ二環式誘導体
JP2006516561A (ja) * 2003-01-17 2006-07-06 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 細胞増殖の阻害剤としての２−アミノピリジン置換ヘテロ環類
JP2006517976A (ja) 2003-02-14 2006-08-03 スミスクライン・ビーチャム・コーポレイション 新規化合物
US7138412B2 (en) * 2003-03-11 2006-11-21 Bristol-Myers Squibb Company Tetrahydroquinoline derivatives useful as serine protease inhibitors
WO2004106308A1 (en) 2003-05-27 2004-12-09 Pfizer Products Inc. Quinazolines and pyrido [3,4-d] pyrimidines as receptor tyrosine kinase inhibitors
AU2004263515A1 (en) 2003-08-05 2005-02-17 Vertex Pharmaceuticals Incorporated Condensed pyrimidine compounds as inhibitors of voltage-gated ion channels
DE102004020908A1 (de) 2004-04-28 2005-11-17 Grünenthal GmbH Substituierte 5,6,7,8,-Tetrahydro-pyrido[4,3-d]pyrimidin-2-yl- und 5,6,7,8,-Tetrahydro-chinazolin-2-yl-Verbindungen
US7098222B2 (en) * 2004-05-12 2006-08-29 Abbott Laboratories Bicyclic-substituted amines having cyclic-substituted monocyclic substituents
TWI389690B (zh) 2005-03-25 2013-03-21 Glaxo Group Ltd 新穎化合物（一）
EP1868612A4 (en) * 2005-03-25 2010-03-24 Glaxo Group Ltd NOVEL CONNECTIONS
PE20100741A1 (es) * 2005-03-25 2010-11-25 Glaxo Group Ltd COMPUESTOS DERIVADOS DE 3,4-DIHIDROPIRIMIDO[4,5-d]PIRIMIDIN-2(1H)-ONA COMO INHIBIDORES DE QUINASA p38
WO2006104917A2 (en) 2005-03-25 2006-10-05 Glaxo Group Limited Process for preparing pyrido[2,3-d]pyrimidin-7-one and 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1h)-one derivatives
WO2006127678A2 (en) 2005-05-23 2006-11-30 Smithkline Beecham Corporation Inhibition of p38 mark for treatment of obesity
EP1931667A1 (en) * 2005-09-28 2008-06-18 Ranbaxy Laboratories Limited Pyrido-pyridimidine derivatives useful as antiinflammatory agents
DK1940839T3 (da) * 2005-10-07 2013-10-14 Exelixis Inc Pyridopyrimidione Inhibitors of P13Ka
TW200738243A (en) 2005-11-15 2007-10-16 Glaxo Group Ltd Novel process and formulations
WO2007076085A2 (en) * 2005-12-22 2007-07-05 Prolexys Pharmaceuticals, Inc . Fused pyrimidones and thiopyrimidones, and uses thereof
TW200800997A (en) * 2006-03-22 2008-01-01 Astrazeneca Ab Chemical compounds
ES2382486T3 (es) * 2006-11-20 2012-06-08 Bristol-Myers Squibb Company 7,8-Dihidro-1,6-naftiridin-5(6H)-onas y compuestos bicíclicos relacionados como inhibidores de la dipeptidil peptidasa IV y procedimientos
CA2719868A1 (en) * 2008-04-29 2009-11-05 F. Hoffmann-La Roche Ag Pyrimidinyl pyridone inhibitors of jnk.

Also Published As

Publication number Publication date
CA2602553A1 (en) 2006-10-05
AU2006229993A1 (en) 2006-10-05
BRPI0609437A2 (pt) 2010-04-06
MX2007011856A (es) 2007-10-10
ZA200707564B (en) 2008-10-29
ES2426251T3 (es) 2013-10-22
EP2447266B1 (en) 2013-06-12
NZ561237A (en) 2011-02-25
US20090069318A1 (en) 2009-03-12
JP2008534513A (ja) 2008-08-28
WO2006104915A9 (en) 2008-01-03
CA2602553C (en) 2013-04-30
WO2006104915A3 (en) 2007-11-22
KR101235497B1 (ko) 2013-02-20
KR20070113255A (ko) 2007-11-28
IL185870A0 (en) 2008-01-06
EA012875B1 (ru) 2009-12-30
CN101258148A (zh) 2008-09-03
MY145281A (en) 2012-01-13
PE20100737A1 (es) 2010-11-27
SG166771A1 (en) 2010-12-29
TW200714281A (en) 2007-04-16
EP2436686A1 (en) 2012-04-04
EP1868611B1 (en) 2012-11-14
US20090156597A1 (en) 2009-06-18
US8354416B2 (en) 2013-01-15
EA200702071A1 (ru) 2008-02-28
NO20075275L (no) 2007-12-27
TWI389690B (zh) 2013-03-21
HK1111422A1 (es) 2008-08-08
EP2447266A1 (en) 2012-05-02
US8207176B2 (en) 2012-06-26
UY29440A1 (es) 2006-10-02
CN102746301A (zh) 2012-10-24
US7678801B2 (en) 2010-03-16
EP1868611A4 (en) 2009-05-27
UA95444C2 (ru) 2011-08-10
IL185870A (en) 2013-06-27
MA29341B1 (fr) 2008-03-03
AU2006229993B2 (en) 2011-05-19
ES2398246T3 (es) 2013-03-14
US20060235029A1 (en) 2006-10-19
CN102746299A (zh) 2012-10-24
PE20061351A1 (es) 2007-01-14
WO2006104915A2 (en) 2006-10-05
JP5037487B2 (ja) 2012-09-26
EP1868611A2 (en) 2007-12-26
MY145343A (en) 2012-01-31
CN102746300A (zh) 2012-10-24

Similar Documents

Publication Publication Date Title
AR053346A1 (es) Compuesto derivado de 8h -pirido (2,3-d) pirimidin -7 ona 2,4,8- trisustituida composicion farmaceutica y uso para preparar una composicion para tratamiento y profilxis de una enfermedad mediada por la quinasa csbp/ rk/p38
AR053450A1 (es) Derivados de 3,4-dihidro-pirimido(4,5-d)pirimidin-2-(1h)-ona 1,5,7 trisustituidos como inhibidores de la quinasa p38
AR056218A1 (es) Composicion farmaceutica de liberacion mantenida comprimido de liberacion inmediata y comprimido oralmente administrable que comprende una sla soluble en agua d 8-(2,6-difluorofenil)-4-(4-fluoro-2-metilfenil)-2-{[2- hidroxi-1-(hidroximetil)etil] amino}pirido (2,3-d)pirimidin-7(8h)-ona; dicho compues
AR049708A1 (es) Moduladores del receptor de progesterona que comprenden derivados de pirrol-oxindol y sus usos
AR049706A1 (es) Moduladores del receptor de progesterona que comprenden derivados de pirrol-oxindol y sus usos
AR030053A1 (es) 1h-pirimido [4,5-d] pirimidin-2-onas y sales, composiciones farmaceuticas, uso para la fabricacion de un medicamento y procedimiento para producirlas
CO5700754A2 (es) Derivados de piperazina y su uso en el tratamiento de enfermedades neurologicas y psiquiatricas
AR053202A1 (es) Pirazolpiridinas y analogos de las mismas como inmunomoduladores
AR073760A1 (es) Derivados heterociclicos y metodos de uso de los mismos
AR056556A1 (es) Imidazo(1,2-a)piridina con actividad antiproliferacion celular
RU2008116844A (ru) Ацилированные производные спиропиперидина как модуляторы рецептора меланокортина-4
RU2008129620A (ru) Пиразиноилгуанидиновые соединения, применяемые в лечении воспалительных или аллергических заболеваний
AR059937A1 (es) Compuesto de pirido (2,3-d) pirimidin -7-ona o compuesto que contiene 3,4- dihidropirimido (4,5-d) pirimidin -2 (1h) -ona y proceso para su preparacion
AR056875A1 (es) Ligandos del receptor vaniloide y su aplicacion para la fabricacion de medicamentos
CY1114241T1 (el) Ν-αρυλοσουλφονυλ-3-αμινοαλκοξυινδολια
ES2608152T3 (es) Aglomerante hidráulico o mortero de volumen estable
AR069494A1 (es) Derivados de acidos fosfonicos
AR056876A1 (es) Compuestos de pirazolo[1-5-a]pirimidina, antagonistas de receptores canabinoides cb1, composiciones farmaceuticas que los contienen y usos en el tratamiento de enfermedades del sistema nervioso central, tales como trastornos psicoticos, neurologicos y similares
AR044011A1 (es) Antagonistas de mchr1 heterociclicos
AR057769A1 (es) Pirazolo pirimidinas como inhibidores de map quinasa p38, metodos para utilizarlos y composiciones farmaceuticas
NO20073729L (no) Heterocykliske forbindelser som CCR2B-antagonister
ECSP034865A (es) Resolución óptica de (1-benzilo-4-metilopiperidina-3-il)-metilamina y su uso para la preparación de derivados de pirrolo 2,3-pirimidina como inhibidores de proteina quinasas
AR073079A1 (es) Compuestos triazolopiridina como inhibidores de pim cinasa
AR008327A1 (es) Aminoguanidinas y alcoxiguanidinas como inhibidores de proteasa, alcoxiaminas para su exclusivo uso en el procedimiento de obtencion de dichos compuestos, composicion farmaceutica, uso de dichos compuestos y composiciones para preparar medicamentos, dispositivo usado en la recolección, circulacion y almacenamiento de sangre y proceso para preparar dichos compuestos.
AR049443A1 (es) Derivados de pirrolpiridinas

Legal Events

Date Code Title Description
FA Abandonment or withdrawal