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1. 发明授权

US06903128B2 Non-peptidyl inhibitors of VLA-4 dependent cell binding useful in treating inflammatory, autoimmune, and respiratory diseases 失效
公开(公告)号：US06903128B2
公开(公告)日：2005-06-07
申请号：US10702539
申请日：2003-11-05
申请人： Allen J. Duplantier , Louis S. Chupak , Anthony J. Milici , Wan F. Lau
发明人： Allen J. Duplantier , Louis S. Chupak , Anthony J. Milici , Wan F. Lau
IPC分类号： A61K31/135 , A61K31/137 , A61K31/198 , A61K31/275 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/436 , A61K31/519 , A61K31/522 , A61K31/56 , A61K31/58 , A61K31/606 , A61K31/635 , A61K31/675 , A61K38/00 , A61K38/21 , A61P1/00 , A61P3/00 , A61P3/10 , A61P9/10 , A61P11/06 , A61P11/08 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P29/00 , A61P37/00 , A61P37/04 , A61P37/06 , C07C229/34 , C07C233/47 , C07C275/42 , C07C311/06 , C07D233/64 , C07D235/10 , C07D235/14 , C07D261/08 , C07D277/22 , C07D277/38 , C07D413/04 , C07D235/04 , C07D263/54
CPC分类号： C07D413/04 , C07C229/34 , C07C233/47 , C07C311/06 , C07D235/14 , C07D261/08
摘要： There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.0): and pharmaceutically acceptable salts and other prodrug derivatives thereof, wherein: A is (C1-C6) alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl optionally substituted with 0 to 3 R9; or is a member selected from the group consisiting of the following radicals: A1-NHC(═O)NH-A2-, A1-NHC(═O)O-A2-, A1-OC(═O)NH-A2-, A1-NHSO2NH-A2-, A1-NHC(═O)-A2-, A1-C(═O)NH-A2-, A1-NHSO2-A2-, A1-SO2NH-A2-, A1-(CH2)rO-A2-, A1-O(CH2)r-A2, A1-(CH2)r-A2-, where A1 and A2 are each independently selected from the group consisting of hydrogen, aryl, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, cycloalkyl, heteroaryl, and heterocyclyl substituted with 0 to 3 R9; B is a member independently selected from the group consisting of the following: E is a single bond; —O—; —NR10—; —CH═CH—; —CC—; S(═O)q; —CR11R12NR10—; or —CR11R12—; X is —O—; —C(═O)—; —S(═O)q—; or —NR10—; X1, X2 and X3 are each independently selected from the group consisting of CH, CR9 or N; Y is a single bond; —C(═O)—; —C(═S)—; or —S(═O)2—; R7 is (C1-C6) alkyl; (CH2)kOR5; (CH2)kNR6C(═O)R5; (CH2)kNR6C(═O)OR5; (CH2)kNR6SO2R5; (CH2)kNR6R5; F; CF3; OCF3; aryl, substituted with 0 to 3 R9; heterocyclyl, substituted with 0 to 3 R9; heteroaryl, substituted with 0 to 3 R9; cycloalkyl, substituted with 0 to 3 R9; or R7 may be taken together with R8 to form a cycloalkyl or heterocyclyl ring; or R7 may be taken together with R11 to form a cycloalkyl or heterocyclyl ring; and R8 is hydrogen; F; (C1-C6) alkyl or (C1-C6) alkoxy.

2. 发明授权

US06667331B2 Non-peptidyl inhibitors of VLA-4 dependent cell binding useful in treating inflammatory, autoimmune, and respiratory diseases 失效
标题翻译：用于治疗炎症，自身免疫和呼吸道疾病的VLA-4依赖性细胞结合的非肽基抑制剂
公开(公告)号：US06667331B2
公开(公告)日：2003-12-23
申请号：US10171286
申请日：2002-06-12
申请人： Allen J. Duplantier , Louis S. Chupak , Anthony J. Milici , Wan F. Lau
发明人： Allen J. Duplantier , Louis S. Chupak , Anthony J. Milici , Wan F. Lau
IPC分类号： A61K314025
CPC分类号： C07D413/04 , C07C229/34 , C07C233/47 , C07C311/06 , C07D235/14 , C07D261/08
摘要： There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.0): and pharmaceutically acceptable salts and other prodrug derivatives thereof, wherein: A is (C1-C6) alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl as defined herein; where said alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with 0 to 3 R9; or is a member selected from the group consisiting of the following radicals: A1—NHC(═O)NH—A2—, A1—NHC(═O)O—A2—, A1—OC(═O)NH—A2—, A1—NHSO2NH—A2—, A1—NHC(═O)—A2—, A1—C(═O)NH—A2—, A1—NHSO2—A2—, A1—SO2NH—A2—, A1—(CH2)rO—A2—, A1—O(CH2)r—A2—, A1—(CH2)r—A2—, where A1 is aryl and A2 is aryl or pyridyl; where said aryl or pyridyl group is substituted with 0 to 3 R9; —B is oxazolinyl or isoxazolinyl; wherein said oxazolinyl and said isoxazolinyl may be optionally substituted with R9; R2 is hydrogen or methyl; R3 is taken together with R4 and the carbon and nitrogen atoms to which it is attached to form a pyrrolidinyl group substituted with 0 to 3 R13; and the remaining variables are as defined in the specification.
摘要翻译：公开了一种非肽基化合物，其中所述化合物是可用于治疗炎性，自身免疫性和呼吸系统疾病的VLA-4抑制剂，其中所述化合物包含式（1.0.0）化合物及其药学上可接受的盐和其中：A为本文定义的（C 1 -C 6）烷基，环烷基，芳基，杂芳基或杂环基; 其中所述烷基，环烷基，芳基，杂芳基或杂环基任选被0至3个R 9取代; 或者是选自以下基团的基团：A 1 -NHC（= O）NH-A 2 - ，A 1 -NHC（= O）OA 2 - ，A < 1 -OC（= O）NH-A 2 - ，A 1 -NHSO 2 NH-A 2 - ，A 1 -NHC（= O）-A 2 - ，A 1 -C（= O）NH-A 2 - ，A 1 -NHSO 2 -A 2 - ，A 1 -SO 2 NH-A 2 - ，A 1 - （CH 2） A 2 - ，A 1 -O（CH 2）r A 2 - ，A 1 - （CH 2）r A 2 - ，其中A 1是芳基，A 2是芳基或吡啶基其中所述芳基或吡啶基被0至3个R 9取代; -B是恶唑啉基或异恶唑啉基; 其中所述恶唑啉基和所述异唑啉基可以任选被R 9取代; R 2是氢或甲基; R 3与R 4一起并与其连接的碳原子和氮原子一起形成被0至3个R 13取代的吡咯烷基;其余的变量如本说明书中所定义。

3. 发明授权

US06306887B1 Non-peptidyl inhibitors of VLA-4 dependent cell binding useful in treating inflammatory, autoimmune, and respiratory diseases 失效
标题翻译：用于治疗炎症，自身免疫和呼吸道疾病的VLA-4依赖性细胞结合的非肽基抑制剂
公开(公告)号：US06306887B1
公开(公告)日：2001-10-23
申请号：US09338832
申请日：1999-06-23
申请人： Louis S. Chupak , Allen J. Duplantier , Anthony J. Milici
发明人： Louis S. Chupak , Allen J. Duplantier , Anthony J. Milici
IPC分类号： A61K3142
CPC分类号： C07D207/333 , C07D231/06 , C07D231/12 , C07D233/64 , C07D241/08 , C07D249/08 , C07D257/04 , C07D261/04 , C07D261/08 , C07D263/10 , C07D263/32 , C07D271/06 , C07D277/26 , C07D277/30 , C07D307/58 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/10 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/10 , C07D417/12
摘要： Compounds of Formula (1.0.0): are described wherein A is for example aryl, heteroaryl or heterocyclyl, Y is preferably —C(═O)—; B is independently selected from a group of moieties, the most preferred of which are those of partial Formulas (1.1.2) and (1.1.6): and E is a single bond; oxygen; 1,1-cyclopropyl; C(CH3)2; CF2; or a bridging moiety of partial Formula (1.9.0): where R1a is hydrogen when R1 has the meaning of a mono-valent substituent; and R1a is a single bond when R1 has the meaning of a di-valent substituent. Said compounds are useful in methods of treating or preventing an inflammatory, autoimmune or respiratory diseases by inhibiting cell adhesion and consequent or associated pathogenic processes subsequently mediated by VLA-4.
摘要翻译：描述式（1.0.0）的化合物：其中A为例如芳基，杂芳基或杂环基，Y优选为-C（= O） - ; B独立地选自一组部分，其中最优选的是部分式（1.1.2）和（1.1.6）的部分：和E是单键; 氧; 1,1-环丙基; C（CH 3）2; CF2; 或部分式（1.9.0）的桥连部分：其中当R 1具有1价取代基的含义时，R 1a为氢; 当R 1具有二价取代基的意义时，R 1a为单键。所述化合物可用于通过抑制随后由VLA-4介导的细胞粘附和随后或相关的致病过程来治疗或预防炎性，自身免疫性或呼吸系统疾病的方法。

4. 发明授权

US06668527B2 Non-peptidyl inhibitors of VLA-4 dependent cell binding useful in treating inflammatory, autoimmune, and respiratory diseases 失效
标题翻译：用于治疗炎症，自身免疫和呼吸道疾病的VLA-4依赖性细胞结合的非肽基抑制剂
公开(公告)号：US06668527B2
公开(公告)日：2003-12-30
申请号：US10170289
申请日：2002-06-12
申请人： Allen J. Duplantier , Louis S. Chupak , Anthony J. Milici , Wan F. Lau
发明人： Allen J. Duplantier , Louis S. Chupak , Anthony J. Milici , Wan F. Lau
IPC分类号： A61K314025
CPC分类号： C07D413/04 , C07C229/34 , C07C233/47 , C07C311/06 , C07D235/14 , C07D261/08
摘要： There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.0): and pharmaceutically acceptable salts and other prodrug derivatives thereof, wherein: A is (C1-C6) alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl as defined herein; where said alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with 0 to 3 R9; or is a member selected from the group consisiting of the following radicals: A1-NHC(═O)NH-A2-, A1-NHC(═O)O-A2-, A1-OC(═O)NH-A2-, A1-NHSO2NH-A2-, A1-NHC(═O)-A2-, A1-C(═O)NH-A2-, A1-NHSO2-A2-, A1SO2NH-A2-, A1-(CH2)rO-A2-, A1-O(CH2)rA2-, A1-(CH2)rA2-, where A1 is aryl and A2 is aryl or pyridyl where said aryl or pyridyl group is substituted with 0 to 3 R9; —B is oxazolinyl or isoxazolinyl which may be optionally substituted with R9; R2 and R3 are each independently selected from the group consisting of hydrogen and (C1-C6) alkyl substituted with 0 to 3 R13; -R4 is hydrogen; or (C1-C6) alkyl optionally substituted with R13; and the remaining variables are defined as set forth in the specification.
摘要翻译：公开了一种非肽基化合物，其中所述化合物是可用于治疗炎性，自身免疫性和呼吸系统疾病的VLA-4抑制剂，其中所述化合物包含式（1.0.0）化合物及其药学上可接受的盐和其中：A为本文定义的（C 1 -C 6）烷基，环烷基，芳基，杂芳基或杂环基; 其中所述烷基，环烷基，芳基，杂芳基或杂环基任选被0至3个R 9取代; 或者是选自以下基团的基团：A 1 -NHC（= O）NH-A 2 - ，A 1 -NHC（= O）OA 2 - ，A < 1 -OC（= O）NH-A 2 - ，A 1 -NHSO 2 NH-A 2 - ，A 1 -NHC（= O）-A 2 - ，A 1 -C（= O）NH-A 2 - ，A 1 -NHSO 2 -A 2 - ，A 1 SO 2 NH-A 2 - ，A 1 - （CH 2） A 1 -O（CH 2）r A 2 - ，A 1 - （CH 2）r A 2 - ，其中A 1为芳基，A 2为芳基或吡啶基其中所述芳基或吡啶基被0至3个R 9取代; -B是可以任选被R 9取代的恶唑啉基或异唑啉基; R 2和R 3各自独立地选自氢和被0至3个R 13取代的（C 1 -C 6）烷基; -R 4是氢; 或任选被R 13取代的（C 1 -C 6）烷基; 并且其余变量被定义为说明书中所阐述的。

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