[go: up one dir, main page]

AR053011A1 - Compuestos de heteroarilo como inhibidores del receptor p2y1, composiciones farmaceuticas que los contienen y su uso en la manufactura de un medicamento para el tratamiento de un trastorno tromboembolico - Google Patents

Compuestos de heteroarilo como inhibidores del receptor p2y1, composiciones farmaceuticas que los contienen y su uso en la manufactura de un medicamento para el tratamiento de un trastorno tromboembolico

Info

Publication number
AR053011A1
AR053011A1 ARP060100185A ARP060100185A AR053011A1 AR 053011 A1 AR053011 A1 AR 053011A1 AR P060100185 A ARP060100185 A AR P060100185A AR P060100185 A ARP060100185 A AR P060100185A AR 053011 A1 AR053011 A1 AR 053011A1
Authority
AR
Argentina
Prior art keywords
substituted
alkyl
crfrf
heterocycle
carbon atoms
Prior art date
Application number
ARP060100185A
Other languages
English (en)
Inventor
James C Sutton
Zulan Pi
Rejean Ruel
Heureux Alexandre L
Carl Thibeault
Patrick Y S Lam
Original Assignee
Bristol Myers Squibb 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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR053011A1 publication Critical patent/AR053011A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • C07D213/80—Acids; Esters in position 3
    • 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
    • C07D277/38—Nitrogen atoms
    • C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D409/14—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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Compuestos de heteroarilo y análogos de los mismos, los cuales son inhibidores selectivos del receptor humano P2Y1. También diversas composiciones farmacéuticas de los mismos y uso en la fabricacion de medicamentos para el tratamiento de enfermedades en respuesta a la modulacion de la actividad del receptor P2Y1, tales como trastornos tromboembolicos. Reivindicacion 1: Un compuesto de la formula (1), o un estereoisomero, tautomero, sal farmacéuticamente aceptable, solvato, o fármaco del mismo, caracterizado porque: el anillo A es un heteroarilo de 5 a 6 miembros que comprende: átomos de carbono y 1-4 heteroátomos en el anillo seleccionados de N, NR11, S(O)p, y O, en donde el heteroarilo es sustituido con 0-4 R1; el anillo B es fenilo sustituido con 0-4 R7, piridilo sustituido con 0-3 R7, o tienilo sustituido con 0-2 R7; X es NH o NMe; Y es O u S; R1 es, independientemente cada vez que se presenta, F, Cl, Br, I, CF3, -CF2CF3, OCF3, -OCF2CF2H, -OCF2CF3, SiMe3, - (CRfRf)r-ORc, SRc, CN, NO2, -(CRfRf)r-NR12R13, -(CRfRf)r-C(O)Rc, -(CRfRf)r-CO2Rc, -(CRfRf)r-C(O)NR12R13, -C(O)NR14(CRfRf)tN12R13, -(CRfRf)r-OC(O)NR12R13, -(CRfRf)r-NR14C(O)NR12R13, -(CRfRf)r-NR14C(O)Rd, -(CRfRf)r-NR14C(O)ORh, -NR14(CRfRf)nC(O)Rd, - NR14CO(CRfRf)nORc, -(CH2)r-CR13(=NORc), -(CH2)r-C(NH2)(=NORc), -S(O)pNR12R13, -(CRfRf)r-NR14S(O)pNR12R13, -NR14SO2CF3, -NR14S(O)pRd, -S(O)2CF3, -S(O)Rd, -S(O)2Rd -OP(O)(OEt)2, -O(CH2)2OP(O)(OEt)2, 4,4,5,5-tetrametil-1,3,2-dioxaborolanilo, alquilo C1- 8 sustituido con 0-2 Ra, alquenilo C2-8 sustituido con 0-2 Ra, alquinilo C2-8 sustituido con 0-2 Ra, carbocicloC3-13-(CRfRf)r- substituido con 0-5 Rb, o (CRfRf)r-heterociclo de 5 a 10 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados de N, NR11, O, y S(O)p, en donde el heterociclo es sustituido con 0-5 Rb; alternativamente, dos R1 se combinan con los átomos de carbono a los cuales se enlazan, forman un carbociclo o heterociclo de 5 a 7 miembros que comprende: átomos de carbono y 0-3 heteroátomos adicionales seleccionados de N, NR11, O, y S(O)p, 0-2 carbonilos, y 0-2 enlaces dobles, en donde el carbociclo o heterociclo es sustituido con 0-4 Rb; R5 es un -(CRfRf)n-carbocicloC3-10 substituido con 1-4 R5a, o un -(CRfRf)n-heterociclo de 5 a 10 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados de N, NR11, O, y S(O)p, en donde el heterociclo es sustituido con 0-4 R5a; R5a es, independientemente cada vez que se presenta F, Cl, Br, I, -(CRiRi)r-ORc, SRc, CN, NO2, CF3, -CF2CF3, OCF3, -OCF2CF2H, -OCF2CF3, -NR12R13, -C(O)Rc, -C(O)ORc, -C(O)NR12R13, -NR14C(O)Rd, -S(O)pNR12R13, -S(O)Rd, -S(O)2Rd, -Si(Me)3, Si(alquilo C1-4)3, haloalquilo C1-4, haloalquiloxi C1-4, alquiloxi C1-4, alquiltio C1-4, alquiloC1-4-C(O), alquiloC1-4-O-C(O), alquiloC1-4-C(O)NH, alquilo C1-4 sustituido con 0-2 Ra, alquenilo C2-8 sustituido con 0-2 Ra, alquinilo C2-8 sustituido con 0-2 Ra, -(CRfRf)r-carbocicloC3-10 substituido con 0-3 Re, o -(CRfRf)r- heterociclo de 5 a 10 miembros que comprenden: átomos de carbono y 1-4 heteroátomos seleccionados de N, NR11, O, y S(O)p, en donde el heterociclo es sustituido con 0-3 Re; alternativamente, dos grupos R5a, junto con los átomos a los cuales se enlazan, forman un anillo carbocíclico o heterocíclico de 5 a 7 miembros que comprende: átomos de carbono y 0-2 heteroátomos seleccionados de N, NR11, O, y S(O)p, 0-1 carbonilo, y 0-3 enlaces dobles, en donde el anillo carbocíclico o heterocíclico es sustituido con 0-3 Re; R7 es, independientemente cada vez que se presenta, H, F, Cl, Br, I, OCF3, CF3, ORc, SRc, CN, NO2, -NR12R13, -C(O)Rc, -C(O)ORc, -C(O)NR12R13, -NR14C(O)Rd, -S(O)pNR12R13, -S(O)Rd, -S(O)2Rd, alquilo C1-8 substituido con 0-2 Ra, alquenilo C2.8 substituido con 0-2 Ra, alquinilo C2_8 substituido con 0-2 Ra, (CRfRf)r-carbocicloC3-10 sustituido con 0-3 Rb, o (CRfRf)r-heterociclo de 5 a 10 miembros que comprenden: átomos de carbono y 1-4 heteroátomos seleccionados de N, NR7b, O, y S(O)p, en donde el heterociclo es sustituido con 0-3 Rb; alternativamente, dos R7 pueden formar un anillo carbocíclico o heterocíclico de 5 a 7 miembros que comprende: átomos de carbono y 0-3 heteroátomos en el anillo seleccionados de O, N, NR7b, y S(O)p, en donde el anillo carbocíclico o heterocíclico es sustituido con 0-3 R7c; R7b es, independientemente cada vez que se presenta, H, alquilo C1-4, alquiloC1-4C(O)-, fenilo-C(O)-, bencilo-C(O)-, bencilo-S(O)2-, alquiloC1-4NHC(O)-, (alquiloC1-4)2NC(O)-, fenilo-NHC(O)-, bencilo-NHC(O)-, alquiloC1-4-S(O)2-, fenilo-S(O)2-, fenilo sustituido con 0-3 Rb, o bencilo sustituido con 0-3 Rb; R7c es, independientemente cada vez que se presenta, H, F, Cl, Br, I, OCF3, CF3, ORc, SRc, CN, NO2, -NR12R13, -C(O)Rc, -C(O)ORc, -C(O)NR12R13, -NR14C(O)Rd, -S(O)pNR12R13, -S(O)Rd, -S(O)2Rd, alquilo C1-4, fenilo sustituido con 0-3 Rb, o bencilo sustituido con 0-3 Rb; R11 es, independientemente cada vez que se presenta, H, alquilo C1-6 substituido con 1-5 fluor, -(CRfRf)rC(O)NR12R13, alquilo C1-8 substituido con 0-2 Ra, alquenilo C2-8 substituido con 0-2 Ra, alquinilo C2-8 substituido con 0-2 Ra, alquiloC1-6C(O)-, cicloalquiloC3-6-alquiloC1-3-C(O)-, cicloalquiloC3-6C(O)-, fenilo- C(O)-, bencilo-C(O)-, alquiloC1-6NHC(O)-, (alquiloC1-6)2NC(O)-, fenilo-NHC(O)-, bencilo-NHC(O)-, fenilo-alquiloC1-6NC(O)-, bencilo-alquiloC1-6NC(O)-, alquiloC1-4-S(O)2-, fenilo-S(O)2-, bencilo-S(O)2-, -(CRfRf)r-carbocicloC3-10, o -(CRfRf)r- heterociclo de 5 a 10 miembros que comprenden: átomos de carbono y 1-4 heteroátomos seleccionados de N, NRf, O, y S(O)p; en donde el fenilo, bencilo, carbociclo, y heterociclo son sustituidos con 0-3 Rb; R12 es, independientemente cada vez que se presenta, H, alquilo C1-6 substituido con 1-5 fluor, -(CRfRf)r-C(O)NRfRf, alquilo C1-6, alquiloC1-6C(O)-, alquiloC1-4OC(O)-, ariloC6-10-CH2-OC(O)-, ariloC6-10-CH2-C(O)-, alquiloC1-4-C(O)O-alquiloC1-4-OC(O)-, ariloC6-10-C(O)O-alquiloC1-4-OC(O)-, alquiloC1-6-NHC(O)-, ariloC6-10-NHC(O)-, (heteroarilo de 5 a 10 miembros)-NHC(O)-, (heteroarilo de 5 a 10 miembros)-CH2-OC(O)-, (heteroarilo de 5 a 10 miembros)-C(O)-, ariloC6-10-alquiloC0-4-C(O)-, alquiloC 1-6-S(O)2-, ariloC6-10-S(O)2-, (heterorilo de 5 a 10 miembros)-S(O)2-, o ariloC6-10-alquiloC1-4-S(O)2-, -(CRfRf)n-ariloC6-10, -(CRfRf)n-heterociclo de 5 a 10 miembros; en donde el alquilo, fenilo y arilo son sustituidos con 0-2 Rg; el heteroarilo de 5 a 10 miembros es sustituido con 0-2 Rg y comprende: átomos de carbono y 1-4 heteroátomos seleccionados de N, NRf, O, y S(O)p; el heterociclo de 5 a 10 miembros es sustituido con 0-2 Rg y comprende: átomos de carbono y 1-4 heteroátomos seleccionados de N, NRf, O, y S(O)p; R13 es, independientemente cada vez que se presenta, H, alquilo C1-6, o -(CH2)n-fenilo; alternativamente, R12 y R13, cuando se enlazan al mismo nitrogeno, se combinan para formar un anillo heterocíclico de 5 a 10 miembros que comprenden: átomos de carbono y 1-2 heteroátomos adicionales seleccionados de N, NRf, O, y S(O)p; R14 es, independientemente cada vez que se presenta, H, alquilo C1-6, sustituido con 0-2 R14a, alquenilo C2-6 substituido con 0-2 R14a, alquinilo C2-6 substituido con 0-2 R14a, (CH2)r- carbocicloC3-10 substituido con 0-3 Rg, o (CH2)r-heterociclo de 5 a 10 miembros que comprenden: átomos de carbono y 1-4 heteroátomos seleccionados de N, NRf, O, y S(O)p, en donde el heterociclo es sustituido con 0-3 Rg; R14a es, independientemente cada vez que se presenta, H, alquilo C1-4, ORf, Cl, F, Br, I, =O, CF3, CN, NO2, NR12R13, -C(O)Rf, -C(O)ORf-, -C(O)NR12R13, o -S(O)pRf; Ra es, independiente cada vez que se presenta, H, F, OCF3, CF3, -(CRfRf)rORc, -(CRfRf)rSRc, CN, -(CRfRf)rNR12R13, - (CRfRf)rC(O)Rc, -(CRfRf)rC(O)ORc, -(CRfRf)r-C(O)NR12R13, -(CRfRf)r-NR14C(O)Rd -(CRfRf)rS(O)pNR12R13, -(CRfRf)rS(O)Rd, -(CRfRf)rS(O)2Rd, alquilo C1-4 substituido con 1-5 fluor, (CH2)r-carbocicloC3-10 substituido con 0-3 Re, o (CH2)r-heterociclo de 5 a 10 miembros que comprenden: átomos de carbono y 1-4 heteroátomos seleccionados de N, NRf, O, y S(O)p, en donde el heterociclo es sustituido con 0-3 Re; Rb es, independientemente cada vez que se presenta, H, =O, F, Cl, Br, I, -(CH2)r-ORc, SRc, CN, NO2, CF3, OCF3, -(CRfRf)rNR12R13, -C(O)Rc, -(CH2)r-C(O)ORc, -(CH2)r C(O)NR12R13, -NR14C(O)Rd, -S(O)PNR12R13, -S(O)Rd, -S(O)2Rd, haloalquilo C1-4, haloalquiloxi C1-4, alquilo C1-4 substituido con 0-2 Ra, alquenilo C2-6 substituido con 0-2 Ra, alquinilo C2-6 substituido con 0-2 Ra, (CH2)r-carbocicloC3-10 substituido con 0-3 Re, o (CH2)r-heterociclo de 5 a 10 miembros que comprenden: átomos de carbono y 1-4 heteroátomos seleccionados de N, NRf, O, y S(O)p, en donde el heterociclo es sustituido con 0-3 Re; Rc es, independientemente cada vez que se presenta, H, -OP(O)(OEt)2, alquilo C1-8 substituido con 0-2 Re, alquenilo C2-8 substituido con 0-2 Re, alquinilo C2-8 substituido con 0-2 Re, (CRfRf)r-cicloalquiloC3-8 substituido con 0-2 Re, (CRfRf)r-ariloC6-10 substituido con 0-2 Re, o (CRfRf)r-heterociclo de 5 a 10 miembros que comprenden: átomos de carbono y 1-4 heteroátomos seleccionados de N, NRf, O, y S(O)p, en donde el heterociclo es sustituido con 0-2 Re; Rd es, independientemente cada vez que se presenta, CF3, OH, alcoxi C1-4, alquilo C1-6, (CH2)r-carbocicloC3-10 substituido con 0-2 Re, o (CH2)r-heterociclo de 5 a 10 miembros que comprenden: átomos de carbono y 1-4 heteroátomos seleccionados de N, NRf, O, y S(O)p, en donde el heterociclo es sustituido con 0-2 Re; Re es, independientemente cada vez que se presenta, H, =O, -(CH2)r-ORf, F, Cl, Br, I, CN, NO2, -(CH2)r-NR12R13, -C(O)Rf, -(CH2)r-C(O)ORf, -NR14C(O)Rf, -(CH2)r-C(O)NR12R13, -SO2NR12R13, - NR14SO2NR12R13, -NR14SO2-alquiloC1-4, -NR14SO2CF3, -NR14SO2-fenilo, -S(O)2CF3, -S(O)p-alquiloC1-4, -S(O)p-fenilo, -(CF2)rCF3, Si(alquiloC1-4)3, alquilo C1-8 substituido con 0-2 Rg, alquenilo C2-8 substituido con 0-2 Rg, alquinilo C2-8 substituido con 0-2 Rg, (CH2)r-cicloalquiloC3-8 substituido con 0-2 Rg, (CH2)r-ariloC6-10 substituido con 0-2 Rg, o (CH2)r-heterociclo de 5 a 10 miembr
ARP060100185A 2005-01-19 2006-01-18 Compuestos de heteroarilo como inhibidores del receptor p2y1, composiciones farmaceuticas que los contienen y su uso en la manufactura de un medicamento para el tratamiento de un trastorno tromboembolico AR053011A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US64528505P 2005-01-19 2005-01-19
US74931705P 2005-12-09 2005-12-09

Publications (1)

Publication Number Publication Date
AR053011A1 true AR053011A1 (es) 2007-04-18

Family

ID=36579581

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060100185A AR053011A1 (es) 2005-01-19 2006-01-18 Compuestos de heteroarilo como inhibidores del receptor p2y1, composiciones farmaceuticas que los contienen y su uso en la manufactura de un medicamento para el tratamiento de un trastorno tromboembolico

Country Status (13)

Country Link
US (2) US7645778B2 (es)
EP (1) EP1954696B1 (es)
JP (1) JP2008527043A (es)
KR (1) KR20070100894A (es)
AR (1) AR053011A1 (es)
AT (1) ATE499370T1 (es)
AU (1) AU2006206611A1 (es)
DE (1) DE602006020327D1 (es)
MX (1) MX2007008434A (es)
NO (1) NO20073665L (es)
PE (1) PE20061120A1 (es)
TW (1) TW200638934A (es)
WO (1) WO2006078621A2 (es)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7470712B2 (en) * 2004-01-21 2008-12-30 Bristol-Myers Squibb Company Amino-benzazoles as P2Y1 receptor inhibitors
US7550499B2 (en) 2004-05-12 2009-06-23 Bristol-Myers Squibb Company Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
JP2008500284A (ja) 2004-05-12 2008-01-10 ブリストル−マイヤーズ　スクイブ　カンパニー 血栓症の治療に有用なｐ２ｙ１レセプターのウレアアンタゴニスト
US7714002B2 (en) * 2005-06-27 2010-05-11 Bristol-Myers Squibb Company Carbocycle and heterocycle antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
US7728008B2 (en) 2005-06-27 2010-06-01 Bristol-Myers Squibb Company N-linked heterocyclic antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
WO2007002584A1 (en) * 2005-06-27 2007-01-04 Bristol-Myers Squibb Company Linear urea mimics antagonists of p2y1 receptor useful in the treatment of thrombotic conditions
WO2007002635A2 (en) * 2005-06-27 2007-01-04 Bristol-Myers Squibb Company C-linked cyclic antagonists of p2y1 receptor useful in the treatment of thrombotic conditions
JP2009500351A (ja) * 2005-07-04 2009-01-08 ドクター レディズ ラボラトリーズ リミテッド Ａｍｐｋアクチベータとしてのチアゾール誘導体
JP2009526868A (ja) * 2006-02-15 2009-07-23 アボット・ラボラトリーズ 新規なアセチル−ＣｏＡカルボキシラーゼ（ＡＣＣ）阻害薬およびこれらの糖尿病、肥満および代謝症候群における使用
WO2007118149A2 (en) * 2006-04-07 2007-10-18 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical Lollege Thiazole and thiophene analogues, and their use in treating autoimmune diseases and cancers
AR060901A1 (es) * 2006-05-12 2008-07-23 Jerini Ag Compuestos heterociclicos para la inhibicion de integrinas y uso de estos
US7960569B2 (en) * 2006-10-17 2011-06-14 Bristol-Myers Squibb Company Indole antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
JP4941971B2 (ja) * 2007-01-29 2012-05-30 独立行政法人産業技術総合研究所 アルキルチオ置換含窒素複素環化合物の製造方法
US8513286B2 (en) 2007-02-22 2013-08-20 Syngenta Crop Protection Llc Iminipyridine derivatives and their uses as microbiocides
JP5527923B2 (ja) * 2007-03-28 2014-06-25 公益財団法人相模中央化学研究所 パーフルオロアルキル基を有する複素環化合物およびその製造方法
EP2132203A1 (en) * 2007-04-10 2009-12-16 Bristol-Myers Squibb Company Thiazolyl compounds useful as kinase inhibitors
CA2699718C (en) 2007-09-21 2014-05-27 Array Biopharma Inc. Pyridin-2-yl-amino-1, 2, 4-thiadiazole derivatives as glucokinase activators for the treatment of diabetes mellitus
BRPI0818658A2 (pt) 2007-10-09 2015-04-14 Merck Patent Ges Mit Beschränkter Haftung Derivados de piridina úteis como ativadores de glicoquinase
JO2784B1 (en) * 2007-10-18 2014-03-15 شركة جانسين فارماسوتيكا ان. في 5,3,1 - Triazole substitute derivative
CN101827836B (zh) * 2007-10-18 2014-02-19 詹森药业有限公司 三取代的1,2,4-三唑化合物
WO2010012793A1 (en) * 2008-08-01 2010-02-04 Bayer Cropscience Sa Fungicide aminothiazole derivatives
CA2745266C (en) * 2008-12-03 2018-04-10 Yue Xu Stem cell cultures
US9138309B2 (en) 2010-02-05 2015-09-22 Allergan, Inc. Porous materials, methods of making and uses
EP2560488B1 (en) 2010-04-23 2015-10-28 Cytokinetics, Inc. Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use
AR081626A1 (es) 2010-04-23 2012-10-10 Cytokinetics Inc Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos
AR081331A1 (es) 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
EP2603498B1 (en) * 2010-08-10 2016-11-09 Octeta Therapeutics, LLC Novel synthesis for thiazolidinedione compounds
US8759380B2 (en) 2011-04-22 2014-06-24 Cytokinetics, Inc. Certain heterocycles, compositions thereof, and methods for their use
HK1209742A1 (en) 2012-11-20 2016-04-08 沃泰克斯药物股份有限公司 Compounds useful as inhibitors of indoleamine 2,3-dioxygenase
US9643963B2 (en) * 2013-11-14 2017-05-09 Avista Pharma Solutions, Inc. Antiparasitic compounds
JP6469238B2 (ja) 2015-09-18 2019-02-13 科研製薬株式会社 ビアリール誘導体及びそれを含有する医薬
DE102018113646B4 (de) 2018-06-07 2021-06-24 Helmholtz-Zentrum Dresden - Rossendorf E.V. 2-Phenoxypyridin-3-amin-Derivate und deren Verwendung
TWI787523B (zh) 2018-06-15 2022-12-21 漢達生技醫藥股份有限公司 達沙替尼十二烷基硫酸鹽之結晶
CN114072395A (zh) 2019-04-26 2022-02-18 新基公司 杂环化合物及其治疗蠕虫感染和疾病的用途
CR20220325A (es) 2019-12-20 2022-08-19 Tenaya Therapeutics Inc Fluoroalquil-oxadiazoles y sus usos
EP4095134A1 (en) 2021-05-25 2022-11-30 UCL Business Ltd Polycyclic compounds for the treatment of neurological indications
EP4094762A1 (en) 2021-05-25 2022-11-30 UCL Business Ltd Treatment of neurological indications
CN119431404A (zh) * 2024-10-15 2025-02-14 江南大学 一种fsp1抑制剂fsen3的制备方法

Family Cites Families (93)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3118888A (en) * 1964-01-21 Acylated s-triazines and process for their preparation
NL280954A (es) * 1961-07-14
US4179563A (en) * 1978-05-19 1979-12-18 Warner-Lambert Company 3-Aryloxy-substituted-aminopyridines and methods for their production
US4186199A (en) * 1978-11-02 1980-01-29 American Hoechst Corporation Indolo-,1,2-dihydroindolo-, and 1,2,6,7-tetrahydroindolo [1,7-ab][1,5] benzodiazepines
EP0028489B1 (en) 1979-11-05 1983-10-05 Beecham Group Plc Enzyme derivatives, and their preparation
JPS56166180A (en) * 1980-05-28 1981-12-21 Chugai Pharmaceut Co Ltd Dibenzoxazepine derivative and its preparation
JPS56167649A (en) 1980-05-30 1981-12-23 Chugai Pharmaceut Co Ltd Diphenyl ether derivative
US4663453A (en) * 1983-05-18 1987-05-05 Hoechst-Roussel Pharmaceuticals Inc. Benzo[b]pyrrolo[3,2,1-jk][1,4]benzodiazepines having dopamine receptor activity
US4761411A (en) 1983-05-18 1988-08-02 Hoechst-Roussel Pharmaceuticals Inc. Dihydrobenzopyrrolobenzodiazepines useful for treating pyschoses
JPS62280847A (ja) 1986-05-30 1987-12-05 Konica Corp 新規なマゼンタカプラ−を含有するハロゲン化銀写真感光材料
US4840947A (en) * 1986-10-14 1989-06-20 Hoechst-Roussel Pharmaceuticals, Inc. Antiinflammatory and analgesic piperidin-4-yl-tetracyclic benzodiazepines and use thereas
JP2577222B2 (ja) * 1987-04-10 1997-01-29 興和株式会社 新規な置換アニリド誘導体
JPH0339740A (ja) 1989-07-06 1991-02-20 Konica Corp 転写型熱現像カラー感光材料
JP2951434B2 (ja) 1991-04-18 1999-09-20 三菱製紙株式会社 電子写真感光体
NZ264063A (en) 1993-08-13 1995-11-27 Nihon Nohyaku Co Ltd N-(2-phenylpyrid-3-yl)- and n-(4-phenylpyrimidin-5-yl)-n'-phenylurea derivatives and pharmaceutical compositions
JP3395285B2 (ja) 1993-10-06 2003-04-07 日本製紙株式会社 感熱記録体
US5547966A (en) * 1993-10-07 1996-08-20 Bristol-Myers Squibb Company Aryl urea and related compounds
US5612359A (en) * 1994-08-26 1997-03-18 Bristol-Myers Squibb Company Substituted biphenyl isoxazole sulfonamides
DE4443641A1 (de) 1994-12-08 1996-06-13 Bayer Ag Substituierte Carbonsäureamide
JPH11503110A (ja) * 1995-02-17 1999-03-23 スミスクライン・ビーチャム・コーポレイション Ｉｌ−８受容体拮抗剤
KR19980703048A (ko) * 1995-03-20 1998-09-05 피터쥐.스트링거 5-치환-3-(1,2,3,6-테트라히드로피리딘-4-일)- 및 3-(피페리딘-4-일)-1ｈ-인돌: 신규한 5-ｈｔ1ｆ 아고니스트
US6143764A (en) * 1995-11-07 2000-11-07 Kirin Beer Kabushiki Kaisha Quinoline and quinazoline derivatives inhibiting platelet-derived growth factor receptor autophosphorylation and pharmaceutical compositions containing the same
PL329212A1 (en) * 1996-03-25 1999-03-15 Lilly Co Eli Tetrahydro-beta-carbolynic compounds
CA2241687A1 (en) 1996-10-30 1998-05-07 Kenneth A. Jacobson P2y receptor antagonists
US6187797B1 (en) * 1996-12-23 2001-02-13 Dupont Pharmaceuticals Company Phenyl-isoxazoles as factor XA Inhibitors
US6020357A (en) * 1996-12-23 2000-02-01 Dupont Pharmaceuticals Company Nitrogen containing heteroaromatics as factor Xa inhibitors
TW536540B (en) * 1997-01-30 2003-06-11 Bristol Myers Squibb Co Endothelin antagonists: N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide and N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-4'-(2-oxazolyl)[1,1'-biphe
US5858289A (en) 1997-02-24 1999-01-12 Global Consulting, Inc. Process for preparing compressed shape of ceramic fiber
ZA985247B (en) 1997-06-19 1999-12-17 Du Pont Merck Pharma Guanidine mimics as factor Xa inhibitors.
US6022884A (en) * 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
NZ503491A (en) * 1997-11-10 2002-08-28 Bristol Myers Squibb Co 2-substituted amino-1,3-benzothiazole derivatives useful as protein tyrosine kinase inhibitors
JP2002508366A (ja) 1997-12-12 2002-03-19 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー キノリンピペラジンおよびキノリンピペリジン誘導体、それらの製造方法、ならびに複合的５−ｈｔ１ａ、５−ｈｔ１ｂおよび５−ｈｔ１ｄ受容体アンタゴニストとしてのそれらの用途
US7517880B2 (en) * 1997-12-22 2009-04-14 Bayer Pharmaceuticals Corporation Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
PT1042305E (pt) 1997-12-22 2005-10-31 Bayer Pharmaceuticals Corp Inibicao de quinase p38 utilizando difenilureias simetricas e assimetricas
US6329395B1 (en) * 1998-06-08 2001-12-11 Schering Corporation Neuropeptide Y5 receptor antagonists
EE200100006A (et) 1998-07-06 2002-06-17 Bristol-Myers Squibb Company Bifenüülsulfoonamiidid kui duaalse angiotensiin-endoteliini retseptori antagonistid
SK4222001A3 (en) 1998-10-06 2001-10-08 Dainippon Pharmaceutical Co 2,3-disubstituted pyridine derivatives, process for the preparation thereof, drug compositions containing the same and intermediates for the preparation
ATE290524T1 (de) 1998-10-20 2005-03-15 Takeda Pharmaceutical Aromatische aminderivate, verfahren zu ihrer herstellung und mittel, die diese enthalten
GB9823873D0 (en) * 1998-10-30 1998-12-30 Pharmacia & Upjohn Spa 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents
GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
RU2242474C2 (ru) * 1999-03-12 2004-12-20 Бёрингер Ингельхайм Фармасьютиклз, Инк. Соединения, пригодные в качестве противовоспалительных агентов
US6548529B1 (en) 1999-04-05 2003-04-15 Bristol-Myers Squibb Company Heterocyclic containing biphenyl aP2 inhibitors and method
HUP0202708A3 (en) 1999-04-15 2004-12-28 Bristol Myers Squibb Co Cyclic protein tyrosine kinase inhibitors, pharmaceutical compositions containing them and their use
AU5413600A (en) 1999-06-14 2001-01-02 Eli Lilly And Company Compounds
CO5200760A1 (es) 1999-06-16 2002-09-27 Smithkline Beecham Corp Antagonistas del receptor de la il-8 ceptor il-8
JP2001089412A (ja) 1999-09-22 2001-04-03 Otsuka Pharmaceut Co Ltd ベンゼン誘導体またはその医薬的に許容される塩
WO2001023358A1 (en) 1999-09-27 2001-04-05 Sagami Chemical Research Center Pyrazole derivatives, intermediates for the preparation thereof, processes for the preparation of both and herbicides containing the derivatives as the active ingredient
MY125533A (en) 1999-12-06 2006-08-30 Bristol Myers Squibb Co Heterocyclic dihydropyrimidine compounds
DE19962924A1 (de) 1999-12-24 2001-07-05 Bayer Ag Substituierte Oxazolidinone und ihre Verwendung
WO2001051490A1 (en) 2000-01-14 2001-07-19 The Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services Methanocarba cycloalkyl nucleoside analogues
WO2001055146A1 (en) 2000-01-29 2001-08-02 Lg Chem Investment Ltd. FACTOR Xa INHIBITORS WITH ARYL-AMIDINES AND DERIVATIVES, AND PRODRUGS THEREOF
US6906063B2 (en) * 2000-02-04 2005-06-14 Portola Pharmaceuticals, Inc. Platelet ADP receptor inhibitors
JP2003521543A (ja) 2000-02-07 2003-07-15 アボット ゲーエムベーハー ウント カンパニー カーゲー ２−ベンゾチアゾリル尿素誘導体およびそのプロテインキナーゼ阻害剤としての使用
AU2000240570A1 (en) 2000-03-29 2001-10-08 Knoll Gesellschaft Mit Beschraenkter Haftung Pyrrolopyrimidines as tyrosine kinase inhibitors
WO2001074793A2 (en) * 2000-04-03 2001-10-11 3-Dimensional Pharmaceuticals, Inc. Substituted thiazoles and the use thereof as inhibitors of plasminogen activator inhibitor-1
AR035216A1 (es) 2000-12-01 2004-05-05 Astrazeneca Ab Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios
US6693196B2 (en) * 2001-01-31 2004-02-17 The Procter & Gamble Company Couplers for use in oxidative hair dyeing
WO2002064211A1 (en) 2001-02-09 2002-08-22 Merck & Co., Inc. Thrombin inhibitors
AU2002305260A1 (en) 2001-04-27 2002-11-11 Vertex Pharmaceuticals Incorporated Pyrazole derived kinase inhibitors
BR0209485A (pt) 2001-05-08 2004-07-06 Schering Ag Antranilamidapiridinamidas seletivas como inibidores vegfr-2 e vegfr-3
WO2003007955A2 (en) 2001-07-20 2003-01-30 Cancer Research Technology Limited Biphenyl apurinic/apyrimidinic site endonuclease inhibitors to treat cancer
AU2002325381A1 (en) * 2001-07-31 2003-02-24 Bayer Healthcare Ag Naphthylurea and naphthylacetamide derivatives as vanilloid receptor 1 (vr1) antagonists
MXPA04000920A (es) 2001-08-06 2004-04-02 Pharmacia Italia Spa Derivados de aminoisoxazol activos como inhibidores de la cinasa.
CN101357914A (zh) 2001-09-21 2009-02-04 百时美施贵宝公司 含有内酰胺的化合物及其衍生物作为Xa因子的抑制剂
JP2005518365A (ja) * 2001-11-27 2005-06-23 メルク　エンド　カムパニー　インコーポレーテッド ４−アミノキノリン化合物
JP2003192587A (ja) * 2001-12-26 2003-07-09 Bayer Ag 尿素誘導体
JP2005513154A (ja) 2001-12-26 2005-05-12 バイエル・ヘルスケア・アクチェンゲゼルシャフト 尿素誘導体
US20030216396A1 (en) * 2002-02-11 2003-11-20 Bayer Corporation Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors
EP1478358B1 (en) * 2002-02-11 2013-07-03 Bayer HealthCare LLC Sorafenib tosylate for the treatment of diseases characterized by abnormal angiogenesis
AU2003210969A1 (en) * 2002-02-11 2003-09-04 Bayer Corporation Aryl ureas with raf kinase and angiogenesis inhibiting activity
DE10213228A1 (de) * 2002-03-25 2003-10-16 Bayer Ag Cyclopenten-Derivate
RU2004135386A (ru) * 2002-05-06 2005-07-20 Вертекс Фармасьютикалз Инкорпорейтед (Us) Тиадиазолы или оксадиазолы и их применение в качестве ингибиторов протеинкиназы jak
WO2004002481A1 (en) 2002-06-27 2004-01-08 Novo Nordisk A/S Aryl carbonyl derivatives as therapeutic agents
US20060058395A1 (en) 2002-08-01 2006-03-16 Neurosearch A/S Compounds useful for the treatment of diseases responsive to antiangiogenetic therapy
CA2495284A1 (en) 2002-09-05 2004-03-18 Neurosearch A/S Diarylurea derivatives and their use as chloride channel blockers
EP1402888A1 (en) 2002-09-18 2004-03-31 Jerini AG The use of substituted carbocyclic compounds as rotamases inhibitors
US20040209930A1 (en) * 2002-10-02 2004-10-21 Carboni Joan M. Synergistic methods and compositions for treating cancer
MXPA05005409A (es) 2002-11-21 2005-08-03 Neurosearch As Derivados de arilureido y su uso medico.
WO2004054617A1 (ja) * 2002-12-13 2004-07-01 Kyowa Hakko Kogyo Co., Ltd. 中枢疾患の予防および／または治療剤
US7056889B2 (en) * 2002-12-16 2006-06-06 Kimberly-Clark, Worldwide, Inc. Compounds that bind P2Y2 or P2Y1 receptors
TWM252710U (en) * 2003-07-18 2004-12-11 Huei-Chiun Shiu Annealing equipment
EP1661879A4 (en) 2003-08-04 2006-11-29 Ono Pharmaceutical Co A DIPHENYL ETHER COMPOUND, PROCESS FOR THE PRODUCTION AND USE THEREOF
WO2005019240A2 (en) * 2003-08-13 2005-03-03 Amgen, Inc. Melanin concentrating hormone receptor antagonists
KR101122708B1 (ko) 2003-12-26 2012-03-26 마사토시 하기와라 Ｓｒ 단백질 인산화 제어 방법, 및 유효성분으로서 ｓｒ 단백질 활성 제어제를 함유하는 항바이러스제
US7470712B2 (en) * 2004-01-21 2008-12-30 Bristol-Myers Squibb Company Amino-benzazoles as P2Y1 receptor inhibitors
US7550499B2 (en) 2004-05-12 2009-06-23 Bristol-Myers Squibb Company Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
JP2008500284A (ja) * 2004-05-12 2008-01-10 ブリストル−マイヤーズ　スクイブ　カンパニー 血栓症の治療に有用なｐ２ｙ１レセプターのウレアアンタゴニスト
JP4319958B2 (ja) 2004-09-15 2009-08-26 株式会社グリーンセイジュ 蒸留水製造システム
WO2007002584A1 (en) * 2005-06-27 2007-01-04 Bristol-Myers Squibb Company Linear urea mimics antagonists of p2y1 receptor useful in the treatment of thrombotic conditions
US7728008B2 (en) * 2005-06-27 2010-06-01 Bristol-Myers Squibb Company N-linked heterocyclic antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
US7714002B2 (en) * 2005-06-27 2010-05-11 Bristol-Myers Squibb Company Carbocycle and heterocycle antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
WO2007002635A2 (en) * 2005-06-27 2007-01-04 Bristol-Myers Squibb Company C-linked cyclic antagonists of p2y1 receptor useful in the treatment of thrombotic conditions
US7960569B2 (en) 2006-10-17 2011-06-14 Bristol-Myers Squibb Company Indole antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions

Also Published As

Publication number Publication date
KR20070100894A (ko) 2007-10-12
WO2006078621A2 (en) 2006-07-27
EP1954696A2 (en) 2008-08-13
US7645778B2 (en) 2010-01-12
AU2006206611A1 (en) 2006-07-27
EP1954696B1 (en) 2011-02-23
US8273772B2 (en) 2012-09-25
US20060173002A1 (en) 2006-08-03
MX2007008434A (es) 2007-07-25
DE602006020327D1 (de) 2011-04-07
US20100093689A1 (en) 2010-04-15
ATE499370T1 (de) 2011-03-15
PE20061120A1 (es) 2006-10-13
TW200638934A (en) 2006-11-16
WO2006078621A9 (en) 2008-06-19
NO20073665L (no) 2007-10-18
WO2006078621B1 (en) 2006-10-26
JP2008527043A (ja) 2008-07-24
WO2006078621A3 (en) 2006-10-05

Similar Documents

Publication Publication Date Title
AR053011A1 (es) Compuestos de heteroarilo como inhibidores del receptor p2y1, composiciones farmaceuticas que los contienen y su uso en la manufactura de un medicamento para el tratamiento de un trastorno tromboembolico
AR047449A1 (es) Amino-benzazoles como inhibidores del receptor p2y1, composiciones farmaceuticas y metodos de tratamiento
ES3029140T3 (en) Substituted aminothiazoles as dgkzeta inhibitors for immune activation
AR055669A1 (es) Derivados de 3h - imidazo[4, 5 -b]piridina como inhibidores selectivos de gsk3, metodos e internediarios para su preparacion, composiciones farmaceuticas que los contienen y su uso para la elaboracion de un medicamento para el tratamiento de enfermedades neurodegenerativas y mentales.
BR112015029512A2 (pt) derivados de pirazolopirrolidina e seu uso no tratamento de doenças
ME02203B (me) Hinolin i hinoksalin derivati kao inhibitori kinaza
ME02409B (me) Novi heterociklični derivati i njihova upotreba u tretmanu neuroloških poremećaja
JP2018524390A5 (es)
ATE517882T1 (de) Chinolinderivate
JP2013512903A5 (es)
BR112015029491A2 (pt) derivados de imidazopirrolidinona e seu uso no tratamento de doença
BR112015029401A8 (pt) derivados de pirazolo-pirrolidin-4-ona, seus usos, e composição e combinação farmacêuticas
AR057131A1 (es) Derivados de purina como inmunomodulador
AR086676A1 (es) Derivados de alcoholes 1-fenil-2-piridinil alquilicos como inhibidores de fosfodiesterasa
HRP20090468T1 (hr) Urea antagonisti p2y1 receptora korisni u liječenju trombotičkih stanja
JP2013509392A5 (es)
AR067412A1 (es) Moduladores de propiedades farmaceuticas de productos terapeuticos
AR065531A1 (es) Derivados de pirimidina, procesos de obtencion y composiciones farmaceuticas.
BR112014001908A2 (pt) derivados aza heterocíclicos substituídos
ECSP056115A (es) ANTAGONISTAS DEL RECEPTOR A2a DE 2-ALQUINIL- Y 2-ALQUENIL-PIRAZOLO-[4,3-e]-1,2,4-TRIAZOLO-[1,5-c]-PIRIMIDINA ADENOSINA
PE20181017A1 (es) Compuestos heteroarilo y su uso como farmacos terapeuticos
HK1201534A1 (en) Pharmaceutical compounds
JP2022501434A (ja) 血液癌を治療するための併用療法
AR045913A1 (es) Derivados olefinicos de 8-azabiciclo[3,2,1]octanos como antagonistas de receptores muscarinicos de acetilcolina
AR056867A1 (es) Antagonistas heterociclicos n- enlazados del receptor de p2y1 utiles en el tratamiento de condiciones tromboticas. composiciones farmaceuticas.

Legal Events

Date Code Title Description
FB Suspension of granting procedure