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1. 发明授权

US4431644A Antihypertensive agents 失效
标题翻译：抗高血压药
公开(公告)号：US4431644A
公开(公告)日：1984-02-14
申请号：US355638
申请日：1982-03-08
申请人： Elizabeth M. Smith , Joseph T. Witkowski , Ronald J. Doll
发明人： Elizabeth M. Smith , Joseph T. Witkowski , Ronald J. Doll
IPC分类号： C07D209/44 , A61K38/00 , A61K38/55 , A61P9/12 , C07D207/444 , C07D209/46 , C07D209/48 , C07D215/48 , C07D217/26 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81 , C07D285/24 , A61K31/40 , A61K31/54 , C07D417/12
CPC分类号： C07K5/0222 , A61K38/00 , Y10S514/869
摘要： Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2 and R.sup.4 are independently selected from hydrogen and lower alkyl; R.sup.3 is hydrogen, lower alkyl or amino lower alkyl; A and B taken together with the carbons to which they are attached form an alkylene ring having six carbon atoms or A and B are hydrogen; and Z is ##STR2## are disclosed. The compounds are useful as anti-hypertensive agents.
摘要翻译：式“IMAGE”的化合物及其药学上可接受的盐，其中R 1，R 2和R 4独立地选自氢和低级烷基; R3是氢，低级烷基或氨基低级烷基; A和B与它们所连接的碳一起形成具有6个碳原子的亚烷基环或A和B是氢; 而Z是 + TR 。该化合物可用作抗高血压药。

2. 发明授权

US4431645A Antihypertensive agents 失效
标题翻译：抗高血压药
公开(公告)号：US4431645A
公开(公告)日：1984-02-14
申请号：US355639
申请日：1982-03-08
申请人： Elizabeth M. Smith , Joseph T. Witkowski
发明人： Elizabeth M. Smith , Joseph T. Witkowski
IPC分类号： A61K38/00 , C07K5/02 , C07D285/24 , A61K31/40 , A61K31/54 , C07D417/12
CPC分类号： C07K5/0222 , A61K38/00 , Y10S514/869
摘要： Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently selected from hydrogen or lower alkyl; n is 1 or 0; A and B taken together with the carbons to which they are attached form an alkylene ring having six carbon atoms or A and B are hydrogen; and Z is ##STR2## The compounds are useful as hypertensive agents.
摘要翻译：式I的化合物及其药学上可接受的盐，其中R 1，R 2，R 3和R 4独立地选自氢或低级烷基; n为1或0; A和B与它们所连接的碳一起形成具有6个碳原子的亚烷基环或A和B是氢; 并且Z是 + TR 该化合物可用作高血压药物。

3. 发明授权

US08691831B2 Heterocyclic aspartyl protease inhibitors 有权
标题翻译：杂环天门冬氨酰蛋白酶抑制剂
公开(公告)号：US08691831B2
公开(公告)日：2014-04-08
申请号：US13416140
申请日：2012-03-09
申请人： Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voight , Corey O. Strickland , Elizabeth M. Smith , Andrew W. Stamford , William J. Greenlee , Robert D. Mazzola, Jr. , John P. Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoxiang Liu , Tao Guo , Thuy X. E. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey A. Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
发明人： Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voight , Corey O. Strickland , Elizabeth M. Smith , Andrew W. Stamford , William J. Greenlee , Robert D. Mazzola, Jr. , John P. Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoxiang Liu , Tao Guo , Thuy X. E. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey A. Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07D233/88 , A61K31/4168 , A61K31/4178 , C07D239/22 , C07D401/06 , C07D401/10 , C07D403/06 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/10 , C07D417/14 , C07D495/10
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula I are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
摘要翻译：公开了式I化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂化物，其中式I中的每个变量如说明书中所定义; 以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经退行性疾病的方法，以及抑制人类免疫缺陷病毒，plasmepins，组织蛋白酶D和原生动物酶。还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m1激动剂或m2拮抗剂组合治疗认知或神经变性疾病的方法。

4. 发明授权

US08685967B2 Substituted triazolopyridines and analogs thereof 失效
标题翻译：取代的三唑并吡啶类及其类似物
公开(公告)号：US08685967B2
公开(公告)日：2014-04-01
申请号：US13262990
申请日：2010-04-05
申请人： Ginny D. Ho , Elizabeth M. Smith , Eugenia Y. Kiselgof , Kallol Basu , Zheng Tan , Brian McKittrick , Deen Tulshian
发明人： Ginny D. Ho , Elizabeth M. Smith , Eugenia Y. Kiselgof , Kallol Basu , Zheng Tan , Brian McKittrick , Deen Tulshian
IPC分类号： A61K31/437 , A61K31/5377 , A61P25/18 , A61P3/00 , A61P25/28 , A61P25/24 , A61P3/04 , A61P3/10 , C07D471/04 , A61P25/00
CPC分类号： C07D471/04
摘要： The present invention relates to substituted triazolopyridines and analogs thereof, the use of the compounds as phosphodiesterase 10 (PDE10) inhibitors for the treatment of PDE10-modulated disorders, to pharmaceutical compositions comprising the compounds.
摘要翻译：本发明涉及取代的三唑并吡啶类及其类似物，该化合物作为磷酸二酯酶10（PDE10）抑制剂用于治疗PDE10调节的病症的药物组合物用于包含该化合物的药物组合物。

5. 发明申请

US20130018066A1 HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 有权
公开(公告)号：US20130018066A1
公开(公告)日：2013-01-17
申请号：US13551315
申请日：2012-07-17
申请人： Zhaoning Zhu , Brian A. McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voigt , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X.H. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse
发明人： Zhaoning Zhu , Brian A. McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voigt , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X.H. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse
IPC分类号： A61K31/4245 , A61P9/00 , A61P25/00 , C07D413/10 , A61P31/18 , A61P33/02 , A61K31/505 , C07D271/07 , A61K31/4439 , A61P25/28
CPC分类号： C07D233/46 , C07D233/70 , C07D233/88 , C07D239/22 , C07D239/70 , C07D271/07 , C07D273/00 , C07D401/04 , C07D401/08 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/12 , C07D405/10 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/06
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

6. 发明授权

US08114879B2 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：哌嗪衍生物可用作CCR5拮抗剂
公开(公告)号：US08114879B2
公开(公告)日：2012-02-14
申请号：US12055900
申请日：2008-03-26
申请人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
发明人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
IPC分类号： A61K31/497 , C07D403/00
CPC分类号： C07D401/06 , A61K31/496 , A61K45/06 , C07D211/58 , C07D401/10 , C07D401/12 , C07D405/12 , C07D409/06 , C07D413/06 , A61K2300/00
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
摘要翻译：使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R1是氢或烷基; R 2是取代的苯基，取代的杂芳基，芴基，二苯基甲基或任选取代的苯基或杂芳基 - 烷基; R 3是氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R4，R5和R7是氢或烷基; R6是氢，烷基或烯基; 公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

7. 发明授权

US07700603B2 Heterocyclic aspartyl protease inhibitors 有权
公开(公告)号：US07700603B2
公开(公告)日：2010-04-20
申请号：US11149027
申请日：2005-06-09
申请人： Zhaoning Zhu , Brian A McKittrick , Zhong-Yue Sun , Yuanzan C Ye , Johannes H Voigt , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X. H. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Gang Qian , Dawit Tadesse
发明人： Zhaoning Zhu , Brian A McKittrick , Zhong-Yue Sun , Yuanzan C Ye , Johannes H Voigt , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X. H. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Gang Qian , Dawit Tadesse
IPC分类号： A01N43/54 , C07D239/02 , C07D239/42 , C07D401/04
CPC分类号： C07D233/46 , C07D233/70 , C07D233/88 , C07D239/22 , C07D239/70 , C07D271/07 , C07D273/00 , C07D401/04 , C07D401/08 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/12 , C07D405/10 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/06
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

8. 发明申请

US20090258868A1 HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 有权
标题翻译：异源ASPARTYL蛋白酶抑制剂
公开(公告)号：US20090258868A1
公开(公告)日：2009-10-15
申请号：US12331787
申请日：2008-12-10
申请人： Zhaoning Zhu , Brian A. McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voigt , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X.H. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse
发明人： Zhaoning Zhu , Brian A. McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voigt , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X.H. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse
IPC分类号： A61K31/5355 , C07D401/02 , A61K31/4439 , C07D233/02 , A61K31/4166 , C07D239/24 , A61K31/505 , C07D241/10 , A61K31/497 , C07D261/02 , A61K31/42 , A61K31/454 , C07D277/20 , A61K31/426 , C07D235/04 , A61K31/4184 , C07D211/00 , A61K31/4545 , C07D471/02 , A61K31/4375 , C07D413/14 , A61K31/5377 , C07D487/02 , A61K31/519 , C07D271/06 , A61K31/4245 , C07D273/04 , A61P9/00 , A61P25/00
CPC分类号： C07D233/46 , C07D233/70 , C07D233/88 , C07D239/22 , C07D239/70 , C07D271/07 , C07D273/00 , C07D401/04 , C07D401/08 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/12 , C07D405/10 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/06
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
摘要翻译：公开了式I化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂化物，其中W是键，-C（-S） - ， - S（O） - ， - S（O） -C（ - ） - ， - O - ， - C（R6）（R7） - ， - N（R5） - 或-C（-N（R5） X是-O - ， - N（R 5） - 或-C（R 6）（R 7） - ; 条件是当X是-O-时，U不是-O-，-S（O） - ， - S（O）2 - ， - C（-O） - 或-C（-NR 5） - ; U是一个键，-S（O） - ， - S（O）2 - ， - C（O） - ， - O - ， - （O）（OR 15） - ， - （C（R6）（R7））b-或-N（R5） - ; 其中b为1或2; 条件是当W是-S（O） - ， - S（O）2 - ， - O-或-N（R 5） - 时，U不是-S（O） - ， - S（O） -O-或-N（R 5） - ; 条件是当X为-N（R5） - 且W为-S（O） - ， - S（O）2 - ， - O-或-N（R5） - 时，则U不为键; 并且R1，R2，R3，R4，R5，R6和R7如说明书中所定义; 以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经变性疾病的方法以及抑制人类免疫缺陷病毒，plasmepins，组织蛋白酶D 和原生动物酶。还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m1激动剂或m2拮抗剂组合治疗认知或神经变性疾病的方法。

9. 发明授权

US06689765B2 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：可用作CCR5拮抗剂的哌嗪衍生物
公开(公告)号：US06689765B2
公开(公告)日：2004-02-10
申请号：US10061011
申请日：2002-01-30
申请人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
发明人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
IPC分类号： A61K31695
CPC分类号： C07D401/06 , A61K31/496 , A61K45/06 , C07D211/58 , C07D401/10 , C07D401/12 , C07D405/12 , C07D409/06 , C07D413/06 , A61K2300/00
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v, host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
摘要翻译：使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，萘基，芴基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R 4，R 5，R 5和R 5独立地选自氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基， R 7为氢或烷基; R 6为氢，烷基或烯基;用于治疗HIV，实体器官移植排斥，移植物v，宿主病，关节炎，类风湿性关节炎，炎性肠病，特应性皮炎，公开了牛皮癣，哮喘，过敏或多发性硬化，以及新化合物，包含它们的药物组合物，以及本发明的CCR5拮抗剂与用于治疗可用于治疗炎性疾病的HIV或药物。

10. 发明授权

US5298492A Diamino acid derivatives as antihypertensives 失效
标题翻译：二氨基酸衍生物作为抗高血压药
公开(公告)号：US5298492A
公开(公告)日：1994-03-29
申请号：US925338
申请日：1992-08-04
申请人： Bernard R. Neustadt , Elizabeth M. Smith , Deen Tulshian
发明人： Bernard R. Neustadt , Elizabeth M. Smith , Deen Tulshian
IPC分类号： A61K38/55 , A61K38/00 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P43/00 , C07D209/20 , C07K1/113 , C07K5/02 , C07K5/062 , C07K5/065 , C07K5/078 , C07K14/81 , A61K31/17
CPC分类号： C07K5/022 , C07D209/20 , A61K38/00
摘要： Novel diamino acid derivative dual inhibitors of neutral endopeptidase and angiotensin converting enzyme of the formula ##STR1## wherein: Z is amino, lower alkylamino, di-(lower alkyl)amino R.sup.9 C(O)NH-- or an optionally substituted guanidino group;R.sup.1 is hydrogen or R.sup.7 R.sup.8 N--;R.sup.2 is hydrogen, lower alkyl, cyclolower alkyl, aryllower alkyl or heteroaryllower alkyl; and R.sup.3 is hydrogen, lower alkyl or cyclolower alkyl; or R.sup.2 and R.sup.3, together with the carbon to which they are attached, comprise a 3-7 membered carboxyclic ring;R.sup.4 is hydrogen, lower alkyl, aryl lower alkyl or heteroaryllower alkyl;R.sup.5 and R.sup.6 are independently hydroxy, lower alkoxy, amino, aryllower alkoxy, lower alkylamino and di-(lower alkyl)amino;R.sup.7 is R.sup.9 C(O)-- or R.sup.10 SO.sub.2 --; and R.sup.8 is hydrogen, lower alkyl, aryllower alkyl or aryl; or R.sup.7 and R.sup.8, together with the nitrogen to which they are attached, comprise a 5-7 membered ring;R.sup.9 is lower alkyl, aryllower alkyl, aryl, heteroaryllower alkyl, heteroaryl, lower alkoxy, aryllower alkoxy, amino, alkylamino or dialkylamino;R.sup.10 is lower alkyl, aryl lower alkyl, aryl, heteroaryl lower alkyl, amino, lower alkylamino, di-(lower alkyl)amino or heteroaryl;n is 1, 2, 3, 4 or 5; and m is 1, 2, 3, 4 or 5;or a pharmaceutically acceptable addition salt thereof, useful in the treatment of cardiovascular disorders, are disclosed.
摘要翻译：新型二氨基酸衍生物双中性内肽酶抑制剂和式（*化学结构*）的血管紧张素转换酶其中：Z为氨基，低级烷基氨基，二 - （低级烷基）氨基R9C（O）NH-或任选取代的胍基 ; R1是氢或R7R8N-; R2是氢，低级烷基，环状烷基，芳基低级烷基或杂芳基低级烷基; 并且R 3是氢，低级烷基或环己烷基; 或R 2和R 3与它们所连接的碳一起包含3-7元羧基环; R4是氢，低级烷基，芳基低级烷基或杂芳基低级烷基; R5和R6独立地是羟基，低级烷氧基，氨基，芳基低级烷氧基，低级烷基氨基和二（低级烷基）氨基; R7是R9C（O） - 或R10SO2-; R8是氢，低级烷基，芳基低级烷基或芳基; 或R 7和R 8与它们所连接的氮一起包含5-7元环; R 9是低级烷基，芳基低级烷基，芳基，杂芳基低级烷基，杂芳基，低级烷氧基，芳基低级烷氧基，氨基，烷基氨基或二烷基氨基; R 10是低级烷基，芳基低级烷基，芳基，杂芳基低级烷基，氨基，低级烷基氨基，二 - （低级烷基）氨基或杂芳基; n为1,2,3,4或5; m为1,2,3,4或5; 或其药学上可接受的加成盐，其可用于治疗心血管疾病。

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