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公开(公告)号：US06872735B2
公开(公告)日：2005-03-29
申请号：US10618178
申请日：2003-07-11
申请人： Daniel J. Burdick , Mark S. Stanley , David Oare , Mark E. Reynolds , Thomas R. Gadek , James C. Marsters
发明人： Daniel J. Burdick , Mark S. Stanley , David Oare , Mark E. Reynolds , Thomas R. Gadek , James C. Marsters
IPC分类号： C07D277/06 , A61K31/197 , A61K31/198 , A61K31/341 , A61K31/351 , A61K31/385 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/403 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/445 , A61K31/4458 , A61K31/4462 , A61K31/4465 , A61K31/4525 , A61P1/04 , A61P11/06 , A61P17/06 , A61P19/02 , A61P29/00 , A61P37/06 , C07C233/83 , C07D207/16 , C07D211/60 , C07D211/62 , C07D307/54 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12
CPC分类号： C07D405/12 , A61K31/198 , A61K31/40 , A61K31/44 , C07D207/16 , C07D277/06 , C07D307/54 , C07D417/12
摘要： The invention relates to novel compounds having formula (I) wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation and autoimmune diseases.
摘要翻译： 本发明涉及具有式（I）的新化合物，其中Cy，X，Y，L和R1-6如本文所定义。 这些化合物结合CD11 / CD18粘附受体如淋巴细胞功能相关抗原-1（LFA-1），因此可用于治疗由LFA-1介导的疾病如炎症和自身免疫性疾病。
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公开(公告)号：US06667318B2
公开(公告)日：2003-12-23
申请号：US09994546
申请日：2001-11-26
申请人： Daniel J. Burdick , Mark S. Stanley , David Oare , Mark E. Reynolds , Thomas R. Gadek , James C. Marsters
发明人： Daniel J. Burdick , Mark S. Stanley , David Oare , Mark E. Reynolds , Thomas R. Gadek , James C. Marsters
IPC分类号： A61K314525
CPC分类号： C07D405/12 , A61K31/198 , A61K31/40 , A61K31/44 , C07D207/16 , C07D277/06 , C07D307/54 , C07D417/12
摘要： The invention relates to novel compounds having formula (I) wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation and autoimmune diseases.
摘要翻译： 本发明涉及具有式（I）的新化合物，其中Cy，X，Y，L和R1-6如本文所定义。 这些化合物结合CD11 / CD18粘附受体如淋巴细胞功能相关抗原-1（LFA-1），因此可用于治疗由LFA-1介导的疾病如炎症和自身免疫性疾病。
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3.发明授权Hydrazono-benzazulene derivatives, pharmaceutical compositions and intermediates 失效肼基 - 苯并薁衍生物，药物组合物和中间体公开(公告)号：US06277845B1
公开(公告)日：2001-08-21
申请号：US09509263
申请日：2000-07-07
申请人： Denis Carniato , Thomas R. Gadek , Francois Goubet , Jean-Francois Gourvest , Jochen Knolle , Robert S. McDowell , Karl-Heinz Scheunemann
发明人： Denis Carniato , Thomas R. Gadek , Francois Goubet , Jean-Francois Gourvest , Jochen Knolle , Robert S. McDowell , Karl-Heinz Scheunemann
IPC分类号： C07D23350
CPC分类号： C07C333/04 , C07C49/747 , C07C323/22 , C07D233/52
摘要： Compounds of the formula wherein the substituents are as defined in the application and their pharmaceutically acceptable acid and base salts thereof which are useful for preventing loss of bone matrix.
摘要翻译： 取代基中的取代基的化合物如本申请中所定义，并且其药学上可接受的酸和碱盐可用于防止骨基质的损失。
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4.发明授权N-(.omega., (.omega.-1)-dialkyloxy)- and N-(.omega., (.omega.-1)-dialkenyloxy)-alk-1-yl-N,N,N-tetrasubstituted ammonium lipids and uses therefor 失效N-（ω，（ω-1） - 二烷氧基） - 和N-（ω，（ω-1） - 二烯氧基） - 烷基-1-基-N，N，N-四取代的铵脂质及其用途
公开(公告)号：US5208036A
公开(公告)日：1993-05-04
申请号：US614412
申请日：1990-11-16
IPC分类号： A61K9/127 , A61K47/18 , C07D453/02 , C12N15/88
CPC分类号： A61K47/186 , A61K9/0014 , A61K9/0019 , A61K9/1272 , C07D453/02 , C12N15/88 , Y10S435/829
摘要： This invention relates to compounds of the formula ##STR1## or an optical isomer thereof wherein R.sup.1 and R.sup.2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R.sup.3, R.sup.4 and R.sup.5 are the same or different and are alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or when two or three of R.sup.3, R.sup.4, and R.sup.5 are taken together to form quinuclidino, piperidino, pyrrolidino, or morpholino; n is 1 to 8; and X is a pharmaceutically acceptable anion.
摘要翻译： 本发明涉及式I的化合物或其旋光异构体，其中R 1和R 2相同或不同，为6至24个碳原子的烷基或烯基; R 3，R 4和R 5相同或不同，为碳原子数为1〜8的烷基，芳基，碳原子数为7〜11的芳烷基，或者当R3，R4，R5中的2个或3个为一起形成亚硝酰基，哌啶子基 ，吡咯烷子基或吗啉代; n为1至8; X是药学上可接受的阴离子。
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5.发明授权N[.omega.,(.omega.-1)-dialkyloxy]- and N-[.omega.,(.omega.-1)-dialkenyloxy]-alk-1-yl-N,N,N-tetrasubstituted ammonium lipids and uses therefor 失效N [ω，（ω-1） - 二烷氧基] - 和N- [ω，（ω-1） - 二烯氧基] -alk -1-基-N，N，N-四取代的铵脂质及其用途
公开(公告)号：US4897355A
公开(公告)日：1990-01-30
申请号：US114809
申请日：1987-10-29
IPC分类号： A61K9/127 , A61K47/18 , C07D453/02 , C12N5/02 , C12N15/88
CPC分类号： C07D453/02 , A61K47/186 , A61K9/0014 , A61K9/0019 , A61K9/1272 , C12N15/88 , Y10S435/829
摘要： This invention relates to compounds of the formula ##STR1## or an optical isomer thereof wherein R.sup.1 and R.sup.2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R.sup.3, R.sup.4 and R.sup.5 are the same or different and are alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or when two or three of R.sup.3, R.sup.4, and R.sup.5 are taken together to form quinuclidino, piperidino, pyrrolidino, or morpholino; n is 1 to 8; and X is a pharmaceutically acceptable anion.
摘要翻译： 本发明涉及式I的化合物或其旋光异构体，其中R 1和R 2相同或不同，为6至24个碳原子的烷基或烯基; R3，R4和R5相同或不同，为碳原子数为1〜8的烷基，芳基，碳原子数为7〜11的芳烷基，或者当R3，R4，R5中的两个或三个为一体时，可以形成奎宁二基，哌啶子基 ，吡咯烷子基或吗啉代; n为1至8; X是药学上可接受的阴离子。
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6.发明授权Benzofurane derivatives, their preparation process, their use as medicaments and the pharmaceutical compositions containing them 失效苯并呋喃衍生物，其制备方法，它们作为药物的用途以及含有它们的药物组合物公开(公告)号：US06586442B2
公开(公告)日：2003-07-01
申请号：US10180253
申请日：2002-06-26
申请人： Denis Carniato , Jean-Francois Gourvest , Jochen Knolle , Anurschirwan Peyman , Sarah C. Bodary , Thomas R. Gadek
发明人： Denis Carniato , Jean-Francois Gourvest , Jochen Knolle , Anurschirwan Peyman , Sarah C. Bodary , Thomas R. Gadek
IPC分类号： A61K31505
CPC分类号： C07D405/12
摘要： A compound of the formula wherein the substituents are as defined in the specification and its pharmaceutically acceptable salts and it prodrug useful for treating osteoporosis.
摘要翻译： 取代基中的取代基的化合物如说明书及其药学上可接受的盐所定义，并且其用于治疗骨质疏松症的前药。
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7.发明授权Tricyclic compounds, their preparation process and the intermediates of this process, their use as medicaments and the pharmaceutical compositions containing them 有权三环化合物，其制备方法和该方法的中间体，它们作为药物的用途和含有它们的药物组合物公开(公告)号：US06459001B1
公开(公告)日：2002-10-01
申请号：US09769018
申请日：2001-01-25
申请人： Serge Bernard , Denis Carniato , Jean-Francois Gourvest , Jean-Georges Teutsch , Jochen Knolle , Hans-Ulrich Stilz , Volkmar Wehner , Sarah C. Bodary , Thomas R. Gadek , Robert S. McDowell , Robert M. Pitti
发明人： Serge Bernard , Denis Carniato , Jean-Francois Gourvest , Jean-Georges Teutsch , Jochen Knolle , Hans-Ulrich Stilz , Volkmar Wehner , Sarah C. Bodary , Thomas R. Gadek , Robert S. McDowell , Robert M. Pitti
IPC分类号： C07C25182
CPC分类号： C07D239/18 , C07C45/516 , C07C45/63 , C07C45/673 , C07C45/71 , C07C49/747 , C07C49/755 , C07C281/12 , C07C281/18 , C07C337/08 , C07C2603/30 , C07D233/52 , C07C49/753
摘要： The subject of the invention is the products of formula (I): in which R1, R2, R3, R4, R5 and G are as defined in the description, the dotted lines represent an optional second bond, as well as the addition salts with acids and bases and the esters, their preparation process and the intermediates of this process, their use as medicines and the pharmaceutical compositions containing them.
摘要翻译： 本发明的主题是式（I）的产物：其中R1，R2，R3，R4，R5和G如说明书中所定义，虚线代表任选的第二键，以及与 酸和碱和酯，它们的制备方法和该方法的中间体，它们作为药物的用途和含有它们的药物组合物。
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8.发明授权N-[.omega., (.omega.-1)-dialkyloxy]- and N-[.omega., (.omega.-1)-dialkenyloxy]-alk-1-yl-N, N, N-tetrasubstituted ammonium lipids and uses therefor 失效N- [ω，（ω-1） - 二烷氧基] - 和N- [ω，（ω-1） - 二烯氧基] -alk -1-基-N，N，N-四取代的铵脂质及其用途
公开(公告)号：US5622712A
公开(公告)日：1997-04-22
申请号：US237807
申请日：1994-05-04
CPC分类号： C07D453/02 , A61K47/186 , A61K9/0014 , A61K9/0019 , A61K9/1272 , C12N15/88 , Y10S435/829
摘要： This invention relates to compounds of the formula ##STR1## or an optical isomer thereof wherein R.sup.1 and R.sup.2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R.sup.3, R.sup.4, R.sup.5 are the same or different and are alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or when two or three of R.sup.3, R.sup.4, and R.sup.5 are taken together to form quinuclidino, piperidino, pyrrolidino, or morpholino; n is 1 to 8; and X is a pharmaceutically acceptable anion.
摘要翻译： 本发明涉及式I的化合物或其旋光异构体，其中R 1和R 2相同或不同，为6至24个碳原子的烷基或烯基; R 3，R 4，R 5相同或不同，为碳原子数为1〜8的烷基，芳基，碳原子数为7〜11的芳烷基，或者当R3，R4，R5中的2个或3个相同时，可以形成奎宁二基，哌啶子基 ，吡咯烷子基或吗啉代; n为1至8; X是药学上可接受的阴离子。
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9.发明授权N-[1, (1-1)-dialkyloxy]-and N-[1, (1-1)-dialkenyloxy]-alk-1-yl-n,n,n-tetrasubstituted ammonium lipids and uses therefor 失效N- [1，（1,1-） - 二烷氧基] - 和N- [1，（1,1-） - 二烯氧基] -alk-1-yl-n，n，n-四取代的铵脂，
公开(公告)号：US5545412A
公开(公告)日：1996-08-13
申请号：US415962
申请日：1995-04-03
CPC分类号： A61K47/186 , A61K9/0014 , A61K9/0019 , A61K9/1272 , C07D453/02 , C12N15/88 , Y10S435/829
摘要： This invention relates to compounds of the formula ##STR1## or an optical isomer thereof wherein R.sup.1 and R.sup.2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R.sup.3, R.sup.4 and R.sup.5 are the same or different and are alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or when two or three of R.sup.3, R.sup.4, and R.sup.5 are taken together to form quinuclidino, piperidino, pyrrolidino, or morpholino, n is 1 to 8; and X is a pharmaceutically acceptable anion.
摘要翻译： 本发明涉及式I的化合物或其旋光异构体，其中R 1和R 2相同或不同，为6至24个碳原子的烷基或烯基; R 3，R 4和R 5相同或不同，为碳原子数为1〜8的烷基，芳基，碳原子数为7〜11的芳烷基，或者当R3，R4，R5中的2个或3个为一起形成亚硝酰基，哌啶子基 ，吡咯烷子基或吗啉代，n为1-8; X是药学上可接受的阴离子。
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10.发明授权N-[.omega.,(.omega.-1)-dialkyloxy]- and N-[.omega.,(.omega.-1)-dialkenyloxy]-alk-1-yl-N,N,N,-tetrasubstituted ammonium lipids and uses therefor 失效N- [ω，（ω-1） - 二烷氧基] - 和N- [ω，（ω-1） - 二烯氧基] -alk -1-基-N，N，N， - 四取代的铵脂质及其用途
公开(公告)号：US5366737A
公开(公告)日：1994-11-22
申请号：US15738
申请日：1993-02-10
IPC分类号： A61K9/127 , A61K47/18 , C07D453/02 , C12N5/02 , C12N15/88 , A61K37/22 , A61K9/70 , B01J13/02 , C12N1/20
CPC分类号： C07D453/02 , A61K47/186 , A61K9/0014 , A61K9/0019 , A61K9/1272 , C12N15/88 , Y10S435/829
摘要： This invention relates to compounds of the formulaor an optical isomer thereof wherein R.sup.1 and R.sup.2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R.sup.3, R.sup.4 and R.sup.5 are the same or different and are alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or when two or three of R.sup.3, R.sup.4, and R.sup.5 are taken together to form quinuclidino, piperidino, pyrrolidino, or morpholino; n is 1 to 8; and X is a pharmaceutically acceptable anion.
摘要翻译： 本发明涉及下式的化合物或其光学异构体，其中R 1和R 2相同或不同，为6至24个碳原子的烷基或链烯基; R 3，R 4和R 5相同或不同，为碳原子数为1〜8的烷基，芳基，碳原子数为7〜11的芳烷基，或者当R3，R4，R5中的2个或3个为一起形成亚硝酰基，哌啶子基 ，吡咯烷子基或吗啉代; n为1至8; X是药学上可接受的阴离子。
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