公开(公告)号：US5804587A

公开(公告)日：1998-09-08

申请号：US755936

申请日：1996-11-25

申请人： Thomas Lee Cupps ,  Peter J. Maurer ,  Jeffrey J. Ares ,  Raymond T. Henry ,  Russell James Sheldon ,  Glen E. Mieling ,  Sophie E. Bogdan

发明人： Thomas Lee Cupps ,  Peter J. Maurer ,  Jeffrey J. Ares ,  Raymond T. Henry ,  Russell James Sheldon ,  Glen E. Mieling ,  Sophie E. Bogdan

IPC分类号： C07D401/12 ,  C07D403/12 ,  A61K31/47

CPC分类号： C07D401/12

摘要： The subject invention relates to compounds having the structure: ##STR1## as defined in the claims, and to pharmaceutical compositions containing such compounds, and the use of such compounds for preventing or treating of disorders modulated by alpha-2 adrenoceptors.

摘要翻译： 本发明涉及具有如权利要求中定义的结构的化合物和含有这些化合物的药物组合物，以及这些化合物用于预防或治疗由α-2肾上腺素受体调节的疾病的用途。

公开(公告)号：US5965595A

公开(公告)日：1999-10-12

申请号：US756085

申请日：1996-11-25

申请人： Peter J. Maurer ,  Jeffrey J. Ares ,  William L. Seibel ,  Daniel P. Walker ,  Russell James Sheldon ,  Raymond T. Henry

发明人： Peter J. Maurer ,  Jeffrey J. Ares ,  William L. Seibel ,  Daniel P. Walker ,  Russell James Sheldon ,  Raymond T. Henry

IPC分类号： A61K31/4178 ,  C07D405/12 ,  A61K31/415

CPC分类号： A61K31/4178 ,  C07D405/12

摘要： The subject invention relates to compounds having the structure: ##STR1## wherein (a) n is an integer from 1 to about 3;(b) X and Y are each independently selected from O, S and CH.sub.2, with at least one of X and Y being O or S;(c) R is unsubstituted, straight or branched chain alkanyl or alkanoxy having from 1 to about 3 non-hydrogen atoms; and(d) R' is selected from hydrogen, methyl, cyano, and halo;pharmaceutical compositions containing such compounds; and the use of such compounds for preventing or treating of disorders modulated by alpha-2 adrenoceptors.

摘要翻译： 本发明涉及具有以下结构的化合物：其中（a）n为1至约3的整数; （b）X和Y各自独立地选自O，S和CH 2，X和Y中的至少一个是O或S; （c）R是未取代的，具有1至约3个非氢原子的直链或支链烷基或烷氧基; 和（d）R'选自氢，甲基，氰基和卤素; 含有这些化合物的药物组合物; 以及这些化合物用于预防或治疗由α-2肾上腺素受体调节的疾病的用途。

公开(公告)号：US5399584A

公开(公告)日：1995-03-21

申请号：US15771

申请日：1993-02-10

申请人： Jeffrey J. Ares ,  Sunil V. Kakodkar ,  Gary R. Kelm ,  Peter D. Murray ,  Jared L. Randall ,  Candice L. Slough

发明人： Jeffrey J. Ares ,  Sunil V. Kakodkar ,  Gary R. Kelm ,  Peter D. Murray ,  Jared L. Randall ,  Candice L. Slough

IPC分类号： A61K31/35 ,  A61K31/38 ,  A61K31/19 ,  A61K31/40 ,  A61K49/00

CPC分类号： A61K31/38 ,  A61K31/35 ,  Y10S514/922 ,  Y10S514/925 ,  Y10S514/926 ,  Y10S514/927

摘要： The subject invention relates to methods for preventing or treating damage to the mucosal lining of the gastrointestinal tract of a human or lower animal by administering a safe and effective amount of a compound having the structure: ##STR1## wherein X and Y are each independently selected from O and S; R.sup.1, R.sup.2 and R.sup.3 are each independently selected from hydrogen, hydroxy, halo, unsubstituted or monosubstituted straight or branched C.sub.1 -C.sub.4 alkanyl, and unsubstituted or substituted straight or branched C.sub.1 -C.sub.4 alkanoxy; and each of R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is hydrogen or, if one or more of R.sup.1, R.sup.2 and R.sup.3 is other than hydrogen, each of R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is selected from hydrogen, halo, trifluoromethyl, and unsubstituted straight or branched C.sub.1 -C.sub.4 alkanyl.

摘要翻译： 本发明涉及通过施用安全有效量的具有以下结构的化合物来预防或治疗对人或其以下动物的胃肠道粘膜的损伤的方法：其中X和Y各自独立地选择 从O和S; R 1，R 2和R 3各自独立地选自氢，羟基，卤素，未取代或单取代的直链或支链C 1 -C 4烷基，以及未取代或取代的直链或支链C 1 -C 4烷氧基; R 4，R 5，R 6和R 7各自为氢，或者如果R 1，R 2和R 3中的一个或多个不是氢，则R 4，R 5，R 6和R 7各自选自氢，卤素，三氟甲基和未取代的直链 或支链C 1 -C 4烷基。

公开(公告)号：US5914342A

公开(公告)日：1999-06-22

申请号：US159698

申请日：1998-09-24

申请人： Peter J. Maurer ,  Jeffrey J. Ares ,  William L. Seibel ,  Daniel P. Walker ,  Russell James Sheldon ,  Raymond T. Henry

发明人： Peter J. Maurer ,  Jeffrey J. Ares ,  William L. Seibel ,  Daniel P. Walker ,  Russell James Sheldon ,  Raymond T. Henry

IPC分类号： A61K31/4178 ,  C07D405/12 ,  A61K31/415

CPC分类号： C07D405/12 ,  A61K31/4178

摘要： The subject invention relates to compounds having the structure: ##STR1## wherein (a) n is an integer from 1 to about 3;(b) X and Y are each independently selected from O, S and CH.sub.2, with at least one of X and Y being O or S;(c) R is unsubstituted, straight or branched chain alkanyl or alkanoxy having from 1 to about 3 non-hydrogen atoms; and(d) R' is selected from hydrogen, methyl, cyano, and halo; pharmaceutical compositions containing such compounds; and the use of such compounds for preventing or treating of disorders modulated by alpha-2 adrenoceptors.

摘要翻译： 本发明涉及具有以下结构的化合物：其中（a）n为1至约3的整数; （b）X和Y各自独立地选自O，S和CH 2，X和Y中的至少一个是O或S; （c）R是未取代的，具有1至约3个非氢原子的直链或支链烷基或烷氧基; 和（d）R'选自氢，甲基，氰基和卤素; 含有这些化合物的药物组合物; 以及这些化合物用于预防或治疗由α-2肾上腺素受体调节的疾病的用途。

公开(公告)号：US5578607A

公开(公告)日：1996-11-26

申请号：US326564

申请日：1994-10-20

申请人： Thomas L. Cupps ,  Peter J. Maurer ,  Jeffrey J. Ares

发明人： Thomas L. Cupps ,  Peter J. Maurer ,  Jeffrey J. Ares

IPC分类号： A61K31/437 ,  A61P9/12 ,  C07D401/12 ,  C07D403/12 ,  A61H31/47

CPC分类号： C07D401/12

摘要： The subject invention relates to compounds having the structure: ##STR1## wherein: (a) R is unsubstituted C.sub.1 -C.sub.3 alkanyl or alkenyl;(b) R' is selected from unsubstituted C.sub.1 -C.sub.3 alkanyl or alkenyl; unsubstituted C.sub.1 -C.sub.3 alkylthio or alkoxy; hydroxy; thiol; and halo; and(c) R" is selected from hydrogen; unsubstituted C.sub.1 -C.sub.3 alkanyl or alkenyl; methyl monosubstituted with hydroxy, thiol or amino; unsubstituted C.sub.1 -C.sub.3 alkylthio or alkoxy; amino; unsubstituted amide; unsubstituted or C.sub.1 -C.sub.3 substituted amido; halo; unsubstituted sulfoxide; unsubstituted sulfonyl; and cyano;pharmaceutical compositions containing such compounds, and the use of such compounds for preventing or treating respiratory, ocular, and/or gastrointestinal disorders.

摘要翻译： 本发明涉及具有以下结构的化合物：其中：（a）R是未取代的C 1 -C 3烷基或链烯基; （b）R'选自未取代的C 1 -C 3烷基或烯基; 未取代的C 1 -C 3烷硫基或烷氧基; 羟基; 硫醇 和光环; 和（c）R“选自氢; 未取代的C 1 -C 3烷基或链烯基; 用羟基，硫醇或氨基单取代的甲基; 未取代的C 1 -C 3烷硫基或烷氧基; 氨基; 未取代的酰胺; 未取代或C1-C3取代的酰氨基; 光环; 未取代的亚砜; 未取代的磺酰基; 和氰基; 含有这些化合物的药物组合物，以及这些化合物用于预防或治疗呼吸系统，眼部和/或胃肠疾病的用途。