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    • 3. 发明授权
    • Pyrimidine A2B selective antagonist compounds, their synthesis and use
    • 嘧啶A2B选择性拮抗剂化合物,其合成和用途
    • US07501407B2
    • 2009-03-10
    • US10992239
    • 2004-11-18
    • Arlindo CastelhanoBryan McKibbenArno SteinigEric Collington
    • Arlindo CastelhanoBryan McKibbenArno SteinigEric Collington
    • C07D403/12C07D403/14A61K31/505
    • C07D239/48C07D401/12C07D403/12
    • The subject invention provides compounds having the structure: wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R2 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R3 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R2 and R3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R3 is oxygen; R4 and R5 are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R4NR5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms; R12 is hydrogen, alkyl, halogen or cyano; and n is 0, 1, 2, 3 or 4, or an enantiomer, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A2b adenosine receptor by administering a therapeutically effective amount of the compounds of the invention.
    • 本发明提供具有以下结构的化合物:其中R 1是取代或未取代的苯基或含有1至5个杂原子的5-6元杂环或杂芳族环; R 2是氢或取代或未取代的烷基,-C(O) - 烷基,-C(O)-O-烷基,烷氧基,环烷基,烯基,单环或双环芳基,杂芳基或杂环部分; R 3是氢或取代或未取代的烷基,-C(O) - 烷基,-C(O)-O-烷基,烷氧基,环烷基,烯基,单环或双环芳基,杂芳基或杂环部分,或R 2和R 3是 连接形成杂环; 其中虚线表示可以存在或不存在的第二键,并且当存在时,R3是氧; R 4和R 5各自独立地是取代或未取代的烷基,-C(O) - 烷基,-C(O)-O-烷基,烷氧基,环烷基,链烯基,单环或双环芳基,杂芳基或杂环部分或R4NR5一起形成 含有1至6个杂原子的取代或未取代的单环或双环,杂环或杂芳基部分; R 12是氢,烷基,卤素或氰基; 和n为0,1,2,3或4或其对映异构体或其特异性互变异构体或其药学上可接受的盐,以及通过施用治疗有效量的化合物治疗与A2b腺苷受体相关的疾病的方法 的本发明。
    • 4. 发明授权
    • Pyrrolopyrimidine A2B selective antagonist compounds, their synthesis and use
    • US07645754B2
    • 2010-01-12
    • US10536119
    • 2007-06-19
    • Arlindo CastelhanoBryan McKibbenArno Steinig
    • Arlindo CastelhanoBryan McKibbenArno Steinig
    • C07D487/04A61K31/519A61P11/06
    • C07D487/04
    • The subject invention provides compounds having the structure: wherein, R1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NRaRb, —NRaRb, —NRaC(═O)NRaRb, —NRaC(═O)ORa, —OC(═O)NRaRb, or —NHC(═O) Ra; R2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NRaRb, —NRaRb, —NRaC(═O)NRaRb, —NRaC(═O)ORa, —OC(═O)NRaRb, or —NHC(═O)Ra, or R1, R2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH2)2OH or —CH2C(═O)OH; R3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C1-C15)alkyl, (C1-C15)alkoxy, or —NRaRb; R4 is hydrogen or substituted or unsubstituted (C1-C15)alkyl; R5 is —(CH2)mOR6, —CHNOR7, —C(═O)NR8R9, —(CH2)mC(═O)OR10, —(CH2)kC(═O)NR11R12; wherein R6 is a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R7 is hydrogen, or a substituted or unsubstituted (C1-C30)alkyl, (C1-C30)alkylaryl; R8 and R9 are each independently hydrogen, or a substituted or unsubstituted (C1-C30)alkyl, (C1-C30)alkylaryl, (C1-C30)alkylamino, (C1-C30)alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R8, N, and R9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R10 is hydrogen or a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R11, N and R12 together form a 4-8 membered heterocyclic ring; Ra and Rb are each independently hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3, or a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A2b adenosine receptor in a subject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.
    • 5. 发明申请
    • PYRROLOPYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE
    • US20080261943A1
    • 2008-10-23
    • US10536119
    • 2007-06-19
    • Arlindo CastelhanoBryan McKibbenArno Steinig
    • Arlindo CastelhanoBryan McKibbenArno Steinig
    • A61K31/519C07D487/04
    • C07D487/04
    • The subject invention provides compounds having the structure: wherein, R1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NRaRb, —NRaRb, —NRaC(═O)NRaRb, —NRaC(═O)ORa, —OC(═O)NRaRb, or —NH C(═O) Ra; R2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NRaRb, —NRaRb, —NRaC(═O)NRaRb, —NRaC(═O)ORa, —OC(═O)NRaRb, or —NHC(═O)Ra, or R1, R2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH2)2OH or —CH2C(═O)OH; R3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C1-C15)alkyl, (C1-C15)alkoxy, or —NRaRb; R4 is hydrogen or substituted or unsubstituted (C1-C15)alkyl; R5 is —(CH2)mOR6, —CHNOR7, —C(═O)NR8R9, —(CH2)mC(═O)OR10, —(CH2)kC(═O)NR11R12; wherein R6 is a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R7 is hydrogen, or a substituted or unsubstituted (C1-C30)alkyl, (C1-C30)alkylaryl; R8 and R9 are each independently hydrogen, or a substituted or unsubstituted (C1-C30)alkyl, (C1-C30)alkylaryl, (C1-C30)alkylamino, (C1-C30)alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R8, N, and R9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R10 is hydrogen or a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R11, N and R12 together form a 4-8 membered heterocyclic ring; Ra and Rb are each independently hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3, or a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A2b adenosine receptor in a subject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.