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1. 发明授权

US06916804B2 Pyrimidine A2b selective antagonist compounds, their synthesis and use 失效
标题翻译：嘧啶A2b选择性拮抗剂化合物，其合成和用途
公开(公告)号：US06916804B2
公开(公告)日：2005-07-12
申请号：US10326204
申请日：2002-12-20
申请人： Arlindo Castelhano , Bryan McKibben , Arno Steinig , Eric Collington
发明人： Arlindo Castelhano , Bryan McKibben , Arno Steinig , Eric Collington
IPC分类号： C07D243/08 , A61K31/506 , A61K31/513 , A61K31/519 , A61K31/5377 , A61K31/55 , A61K31/551 , A61P1/00 , A61P1/12 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/06 , A61P17/00 , A61P17/04 , A61P19/02 , A61P27/02 , A61P35/00 , A61P37/08 , A61P43/00 , C07D239/42 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D411/12 , C07D413/12 , C07D417/12 , C07D471/10 , C07D487/04 , C07D239/02 , A61K31/505 , A61K31/535 , C07D413/00
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12
摘要： 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.
摘要翻译：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 3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R 3为氧; 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，烯基，单环或双环芳基，杂芳基或杂环部分或R 4 NR 5一起形成含有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，或其对映异构体或特定的互变异构体或其药学上可接受的盐，以及通过以下方式治疗与Aβ2-2腺苷受体相关的疾病的方法：施用治疗有效量的本发明化合物。

2. 发明申请

US20050119271A1 Pyrimidine A2B selective antagonist compounds, their synthesis and use 失效
标题翻译：嘧啶A2B选择性拮抗剂化合物，其合成和用途
公开(公告)号：US20050119271A1
公开(公告)日：2005-06-02
申请号：US10992239
申请日：2004-11-18
申请人： Arlindo Castelhano , Bryan McKibben , Arno Steinig , Eric Collington
发明人： Arlindo Castelhano , Bryan McKibben , Arno Steinig , Eric Collington
IPC分类号： C07D243/08 , A61K31/506 , A61K31/513 , A61K31/519 , A61K31/5377 , A61K31/55 , A61K31/551 , A61P1/00 , A61P1/12 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/06 , A61P17/00 , A61P17/04 , A61P19/02 , A61P27/02 , A61P35/00 , A61P37/08 , A61P43/00 , C07D239/42 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D411/12 , C07D413/12 , C07D417/12 , C07D471/10 , C07D487/04 , C07D43/02
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12
摘要： 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.
摘要翻译：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 3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R 3为氧; 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，烯基，单环或双环芳基，杂芳基或杂环部分或R 4 NR 5一起形成含有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，或其对映异构体或特定的互变异构体或其药学上可接受的盐，以及通过以下方式治疗与Aβ2-2腺苷受体相关的疾病的方法：施用治疗有效量的本发明化合物。

3. 发明授权

US07501407B2 Pyrimidine A2B selective antagonist compounds, their synthesis and use 失效
标题翻译：嘧啶A2B选择性拮抗剂化合物，其合成和用途
公开(公告)号：US07501407B2
公开(公告)日：2009-03-10
申请号：US10992239
申请日：2004-11-18
申请人： Arlindo Castelhano , Bryan McKibben , Arno Steinig , Eric Collington
发明人： Arlindo Castelhano , Bryan McKibben , Arno Steinig , Eric Collington
IPC分类号： C07D403/12 , C07D403/14 , A61K31/505
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12
摘要： 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.
摘要翻译：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

US07645754B2 Pyrrolopyrimidine A2B selective antagonist compounds, their synthesis and use 失效
公开(公告)号：US07645754B2
公开(公告)日：2010-01-12
申请号：US10536119
申请日：2007-06-19
申请人： Arlindo Castelhano , Bryan McKibben , Arno Steinig
发明人： Arlindo Castelhano , Bryan McKibben , Arno Steinig
IPC分类号： C07D487/04 , A61K31/519 , A61P11/06
CPC分类号： C07D487/04
摘要： 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

US20080261943A1 PYRROLOPYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE 失效
公开(公告)号：US20080261943A1
公开(公告)日：2008-10-23
申请号：US10536119
申请日：2007-06-19
申请人： Arlindo Castelhano , Bryan McKibben , Arno Steinig
发明人： Arlindo Castelhano , Bryan McKibben , Arno Steinig
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： 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.

6. 发明申请

US20050043332A1 Pyrrolo[2,3d]pyrimidine compositions and their use 失效
标题翻译：吡咯并[2,3d]嘧啶组合物及其用途
公开(公告)号：US20050043332A1
公开(公告)日：2005-02-24
申请号：US10816329
申请日：2004-03-31
申请人： Arlindo Castelhano , Bryan McKibben , David Witter
发明人： Arlindo Castelhano , Bryan McKibben , David Witter
IPC分类号： A61K31/519 , A61P1/00 , A61P1/12 , A61P9/00 , A61P11/00 , A61P11/06 , A61P13/12 , A61P25/00 , A61P27/14 , A61P27/16 , A61P29/00 , A61P37/08 , C07D487/04
CPC分类号： C07D487/04 , A61K31/519
摘要： Novel deazapurines are disclosed which are useful for the treatment of adenosine receptor stimulated diseases.
摘要翻译：公开了可用于治疗腺苷受体刺激的疾病的新型脱氮嘌呤。

7. 发明申请

US20050090513A1 Compounds specific to adenosine a1 and a3 receptors and uses thereof 失效
标题翻译：对腺苷a1和α3受体特异的化合物及其用途
公开(公告)号：US20050090513A1
公开(公告)日：2005-04-28
申请号：US10497451
申请日：2002-11-27
申请人： Arlindo Castelhano , Bryan McKibben , Douglas Werner , David Witter
发明人： Arlindo Castelhano , Bryan McKibben , Douglas Werner , David Witter
IPC分类号： A61K31/519 , A61K45/00 , A61P7/10 , A61P9/00 , A61P9/06 , A61P9/10 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/12 , A61P25/20 , A61P25/28 , A61P27/02 , A61P27/06 , A61P27/16 , A61P37/08 , A61P43/00 , C07D487/02 , C07D487/04 , C07D519/00
CPC分类号： C07D487/04
摘要： This invention pertains to compounds which specifically inhibit the adenosine A1 and A3 receptors and the use of these compounds to treat a disease associated with A3 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
摘要翻译：本发明涉及特异性抑制腺苷A 1和A 3 N受体的化合物以及这些化合物用于治疗受试者中与A3腺苷受体有关的疾病的用途，其包括向受试者施用治疗有效量的化合物。

8. 发明申请

US20080070936A1 Compounds specific to adenosine A1 receptors and uses thereof 审中-公开
标题翻译：对腺苷A1受体特异的化合物及其用途
公开(公告)号：US20080070936A1
公开(公告)日：2008-03-20
申请号：US11903147
申请日：2007-09-20
申请人： Arlindo Castelhano , Bryan McKibben , David Witter
发明人： Arlindo Castelhano , Bryan McKibben , David Witter
IPC分类号： A61K31/519 , A61P11/00 , A61P25/00 , A61P9/00
CPC分类号： C07D487/04 , A61K31/519
摘要： This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.
摘要翻译：本发明涉及特异性抑制腺苷A 1受体的化合物以及这些化合物用于治疗受试者中Aβ1腺苷受体相关疾病的用途。

9. 发明申请

US20060035921A1 N3-substituted imidazopyridine c-Kit inhibitors 失效
标题翻译： N 3取代的咪唑并吡啶c-Kit抑制剂
公开(公告)号：US20060035921A1
公开(公告)日：2006-02-16
申请号：US10921418
申请日：2004-08-16
申请人： Arlindo Castelhano , Andrew Crew , Han-Qing Dong , Radoslaw Laufer , An-Hu Li , Li Qiu , Colin Sambrook Smith , Tao Zhang
发明人： Arlindo Castelhano , Andrew Crew , Han-Qing Dong , Radoslaw Laufer , An-Hu Li , Li Qiu , Colin Sambrook Smith , Tao Zhang
IPC分类号： C07D471/02 , A61K31/4745
CPC分类号： C07D471/04
摘要： Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐或N-氧化物可用于治疗癌症。

10. 发明申请

US20060009645A1 Naphthylene derivatives as cytochrome P450 inhibitors 失效
标题翻译：萘衍生物作为细胞色素P450抑制剂
公开(公告)号：US20060009645A1
公开(公告)日：2006-01-12
申请号：US10889520
申请日：2004-07-12
申请人： Vanessa Smith , Anthony Nigro , Mark Mulvihill , Cara Cesario , Patricia Beck , Arlindo Castelhano
发明人： Vanessa Smith , Anthony Nigro , Mark Mulvihill , Cara Cesario , Patricia Beck , Arlindo Castelhano
IPC分类号： C07D249/08 , C07D233/61
CPC分类号： C07D233/64
摘要： Compounds of the formula and pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, G1, Q1, Z, R1, R2, R3, R4a, R4b, R5a, and R5b are defined herein, inhibit the cytochrome P450RAI enzyme and are useful for the treatment and/or prevention of various diseases and conditions which respond to treatment by retinoids and by naturally occurring retinoic acid.
摘要翻译：下式的化合物及其药学上可接受的盐，其中n 1，n 2，n 3，n 4，G 1，Q 1，Z，R 1 R 2，R 3，R 4，R 4a，R 4b，R 5a，本文定义的R 5b是抑制细胞色素P 450 RAI酶，并且可用于治疗和/或预防响应于维甲酸和天然的治疗的各种疾病和病症发生视黄酸。

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