摘要:
Compounds of the formula Ia or Ib: wherein A, B, X, Y, Z, W, k, R1, R2, R3, R4 and R5 are those defined herein, and compositions comprising the same. The present invention also provides methods for preparing compounds of formula I and using the same in treating p38 mediated disorders in a subject.
摘要:
This invention relates to an alpha-1 A receptor partial agonist, which is represented by Formula I: and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing formula I, methods for their use as therapeutic agents, and methods of preparation thereof.
摘要:
This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II: wherein Ar is optionally substituted aryl or heteroaryl, R1–R4 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts thereof. The invention further relates to processes for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for their use as therapeutic agents.
摘要:
This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: wherein m, A, X, Y, R1, R2, R3, R4 and R5 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
摘要:
Compounds of the formula (I): and pharmaceutically acceptable salts or prodrugs thereof, wherein m, R1, R2, R3, R4, R5 and R6 are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula (I).
摘要:
This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II: wherein Ar is optionally substituted aryl or heteroaryl, R1-R4 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts thereof. The invention further relates to processes for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for their use as therapeutic agents.
摘要:
This invention relates to compounds which are generally alpha1A/B-receptor antagonists and which are represented by Formula I: wherein the substituents are as defined in the specification; or pharmaceutically acceptable salts, hydrates, or N-oxides thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and a process for their preparation.
摘要:
The present invention concerns novel compounds represented by the Formula: ##STR1## wherein: A is R.sup.1.sub.q (R.sup.3 R.sup.60 N).sub.m (Z)(NR.sup.2).sub.n ; m and q are each 0 or 1, with the proviso that when q is 1, m is 0 and when q is 0, m is 1; Z is C.dbd.O or SO.sub.2 ; n is 1 with the proviso that, when Z is C.dbd.O, m is 1; X is --NH--, --CH.sub.2 --, or --OCH.sub.2 --; Y is 2-imidazoline, 2-oxazoline, 2-thiazoline, or 4-imidazole; R.sup.1 is H, lower alkyl, or phenyl, with the proviso that, when R.sup.1 is H, m is 1; R.sup.2, R.sup.3, R.sup.60 are each independently H, lower alkyl, or phenyl; R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are each independently hydrogen, lower alkyl, --CF.sub.3, lower alkoxy, halogen, phenyl, lower alkeny, hydroxyl, lower alkylsulfonamido, or lower cycloalkyl, wherein R.sup.2 and R.sup.7 optionally may be taken together to form alkylene or alkenylene of 2 to 3 atoms in an unsubstituted or optionally substituted 5- or 6-membered ring, wherein the optional substituents on the ring are halo, lower alkyl, or --CN, with the proviso that, when R.sup.7 is hydroxyl or lower alkylsulfonamido, then X is not --NH-- when Y is 2-imidazoline. The compounds include pharmaceutically acceptable salts of the above. In the above formula A may be, for example, (R.sup.1 SO.sub.2 NR.sup.2 --), (R.sup.3 R.sup.60 NSO.sub.2 NR.sup.2 --), or (R.sup.3 R.sup.60 NCONR.sup.2 --). The invention also includes the use of the above compounds, and compositions containing them, as alpha.sub.1A/1L agonists in the treatment of various disease states such as urinary incontinence, nasal congestion, priapism, depression, anxiety, dementia, senility, Alzheimer's, deficiencies in attentiveness and cognition, and eating disorders such as obesity, bulimia, and anorexia.
摘要翻译:本发明涉及由下式表示的新化合物:其中:A为R 1q(R 3 R 60 N)m(Z)(NR 2)n; m和q各自为0或1,条件是当q为1时,m为0,当q为0时,m为1; Z是C = O或SO 2; n为1,条件是当Z为C = O时,m为1; X是-NH-,-CH 2 - 或-OCH 2 - ; Y是2-咪唑啉,2-恶唑啉,2-噻唑啉或4-咪唑; R 1为H,低级烷基或苯基,条件是当R 1为H时,m为1; R 2,R 3,R 60各自独立地为H,低级烷基或苯基; R4,R5,R6和R7各自独立地为氢,低级烷基,-CF3,低级烷氧基,卤素,苯基,低级烯基,羟基,低级烷基亚磺酰氨基或低级环烷基,其中R2和R7任选地可以一起形成亚烷基 或未取代或任选取代的5元或6元环中2至3个原子的亚烯基,其中环上任选取代基为卤素,低级烷基或-CN,前提条件是当R 7为羟基或低级烷基亚磺酰氨基 那么当Y是2-咪唑啉时,X不是-NH-。 所述化合物包括上述药学上可接受的盐。 在上述式A中可以是例如(R 1 SO 2 NR 2 - ),(R 3 R 60 NSO 2 NR 2 - )或(R 3 R 60 NCONR 2 - )。 本发明还包括上述化合物和含有它们的组合物作为α1A/ 1L激动剂在治疗各种疾病状态如尿失禁,鼻充血,阴茎异常勃起,抑郁,焦虑,痴呆,衰老,阿尔茨海默病,阿尔茨海默病, 注意力和认知,以及进食障碍,如肥胖,贪食症和厌食症。
摘要:
This invention relates to an alpha-1A receptor partial agonist, which is represented by Formula I: and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing formula I, methods for their use as therapeutic agents, and methods of preparation thereof.
摘要:
Compounds of the Formula: where R1-R6 are those defined herein and methods for producing the same. Also provided are pharmaceutical compositions comprising a Compound of Formula I and methods for their use as therapeutic agents.