摘要:
The invention provides methods of making and using compounds of the formula shown, which are inhibitors of human plasmin and plasma kallikrein. (Formula I) The compounds are useful for the prevention of blood loss, and as components of fibrin adhesives.
摘要:
Arene connected polyamine macroring derivatives represented by general formula I, pharmaceutically acceptable salts or hydrates thereof which have anti-HIV activities, in which the definitions of substituents are as same as those in description. Preparation methods of compounds of formula I. Pharmaceutical compositions containing compounds of formula I or their pharmaceutically acceptable salts or hydrates. The uses of aforementioned compounds in preparing medicaments which are used to treat or prevent diseases associated with HIV.
摘要:
This invention relates to pharmaceutically acceptable salts of compounds of formula (I) wherein: W is N or N + -O - ; R 2 is an optionally substituted C 1 to C 18 hydrocarbyl group wherein up to three C atoms may optionally be replaced by N, O and/or S atoms. R 3 is -(CR 11 R 12 ) m -X-(CR 13 R 14 ) p -R 9 ; m is 0, 1, 2, 3 or 4; p is 0, 1 or 2; X is a bond, -CR 15 =CR 16 -, -C≡C-, C(O)NH, NHC(O), C(O)NMe, NMeC(O), C(O)O, NHC(O)NH, NHC(O)O, OC(O)NH, NH, O, CO, SO 2 , SO 2 NH, C(O)NHNH, R 9 is H ; C 1 to C 6 alkyl ; or phenyl, naphthyl, pyridyl, benzimidazolyl, indazolyl, quinolinyl, isoquinolinyl, tetrahydroisoquinolinyl, indolinyl, isoindolinyl, indolyl, isoindolyl or 2-pyridonyl substituted with -L-Q. R 4 is an optionally substituted C 1 to C 18 hydrocarbyl group wherein up to three C atoms may optionally be replaced by N, O and/or S atoms ; and Such salts are useful, for example, for the treatment of gastrin related disorders.
摘要翻译:本发明涉及式(I)化合物的药学上可接受的盐,其中:W是N或N + O - ; R 2是任选取代的C 1 -C 18烃基,其中最多三个C原子可以任选地被N,O和/或S原子替代。 R 3是 - (CR 11 R 12)m -X-(CR 13 R 14)p -R 9; m为0,1,2,3或4; p为0,1或2; X是一个键,-CR 15 = CR 16 - ,-C = C - ,C(O)NH,NHC(O),C(O)NMe,NMeC(O),C(O)O ,NHC(O)NH,NHC(O)O,OC(O)NH,NH,O,CO,SO 2,SO 2 NH,C(O)NHNH,R 9是H; C1至C6烷基; 或苯基,萘基,吡啶基,苯并咪唑基,吲唑基,喹啉基,异喹啉基,四氢异喹啉基,二氢吲哚基,异吲哚啉基,吲哚基,异吲哚基或被-L-Q取代的2-吡啶酮基。 R 4是任选取代的C 1至C 18烃基,其中最多三个C原子可以任选地被N,O和/或S原子替代; 并且这样的盐可用于例如用于治疗胃泌素相关病症。
摘要:
The invention concerns a method for preparing cyclic urea compounds from at least an activated carbamic acid derivative containing an unprotected primary or secondary amine function, comprising a cyclization step which consists in a reaction between the primary or secondary amine function and the carbamic acid function of said carbamic acid derivative(s).
摘要:
The invention concerns a method for preparing cyclic urea compounds from at least an activated carbamic acid derivative containing an unprotected primary or secondary amine function, comprising a cyclization step which consists in a reaction between the primary or secondary amine function and the carbamic acid function of said carbamic acid derivative(s).
摘要:
The present invention provides compounds of Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are Factor VIIa inhibitors which may be used as medicaments.
摘要:
The present invention relates generally to novel macrocycles of Formula (I) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, C, D, L, M, W, Z 1 , Z 2 , Z 3 , Z 4 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , and R 10 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
摘要翻译:本发明一般涉及式(I)的新型大环或其立体异构体,互变异构体,药学上可接受的盐,溶剂合物或前药,其中变量A,B,C,D,L,M,W,Z 1 Z 2,Z 3,Z 4,R 1,R 2,R 2, R 3,R 4,R 4,R 5,R 6,R 7, R 8,R 9,R 10和R 10如本文所定义。 这些化合物是可用作药物的因子VIIa的选择性抑制剂。
摘要:
The present invention is concerned with benzotriazepinone derivatives, their intermediates, uses thereof and processes for their production. In particular, the present invention relates to parathyroid hormone (PTH) and parathyroid hormone related protein (PTHrp) receptor ligands, (PTH-l or PTH/PTHrp receptor ligands). The invention also relates to methods of preparing such ligands and to compounds which are useful as intermediates in such methods.