摘要:
The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R1 to R9 are as defined herein.
摘要:
Provided are a novel derivative of 5-carbamoyl adamantan-2-yl amide of Formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof for inhibiting the activity of 11β-hydroxystreroid dehydrogenase type 1 (11b-HSD1) or for preventing and/or treating various diseases mediated by 11β-hydroxystreroid dehydrogenase type 1.
摘要:
The present invention is directed to novel inhibitors of system Xc−, also known as the cystine/glutamate antiporter. The present invention is further directed to methods of treating and detecting cancer that overexpresses system Xc− which includes but is not limited to gliomas (including glioblastoma), triple negative breast cancer, and bladder cancer. The present invention is further directed to methods of treating seizures including epileptic seizures.
摘要:
The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
摘要翻译:本发明涉及通式I的化合物,其中R是任选被R 7取代的杂芳基; 或R是任选被R 8取代的杂环烷基或杂环烯基; 或R为X,其中X为-NR 11 R 12; 其药学上可接受的盐,水合物或溶剂合物,用于单独或与一种或多种其它药学活性化合物组合用于治疗,用于预防,治疗或改善响应刺激的中性粒细胞氧化性突发的反应的疾病或病症 的角质形成细胞IL-8释放或响应于坏死的诱导。
摘要:
Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C═Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ═O or ═S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.Also disclosed is a method of treating a subject with cancer by administering to the subject a compound of Structural Formula (I) in combination with Paclitaxel or an analog of Paclitaxel.
摘要翻译:公开了由结构式(I)表示的化合物:Y是共价键,亚苯基或取代或未取代的直链烃基。 此外,Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。 优选Y为共价键或-C(R 7 R 8) - 。 R 1和R 2独立地是芳基或取代的芳基,R 3和R 4独立地是-H,脂族基团,取代的脂族基团,芳基或取代的芳基。 R5-R6独立地是-H,脂族基团,取代的脂族基团,芳基或取代的芳基。 R 7和R 8各自独立地为-H,脂族或取代的脂族基团,或者R 7为-H且R 8为取代或未取代的芳基,或者R 7和R 8一起为C 2 -C 6取代或未取代的亚烷基 。 Z为═O或═S。 还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。 还公开了通过向受试者施用结合式(I)的化合物与紫杉醇或紫杉醇的类似物组合来治疗患有癌症的受试者的方法。
摘要:
The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R1 to R9 are as defined herein.
摘要:
The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.
摘要:
The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases.A compound of the general formula (II): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.; a pharmaceutically acceptable salt or a hydrate thereof.
摘要:
Disclosed is a compound useful as a type I 11βhydroxysteroid dehydrogenase inhibitor. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkenyl or the like, One of R2 and R3 is a group of the formula: —C(═O)—Y—R4, wherein Y is —NR9— or the like, R4 is optionally substituted cycloalkyl or the like, R9 is hydrogen or optionally substituted alkyl, W is optionally substituted alkylene, The other is a group of the formula: —V—R5, wherein V is a bond, —O— or the like, R6 is hydrogen or optionally substituted alkyl, R5 is hydrogen, optionally substituted alkyl or the like, X is a bond, —S—, —SO— or the like, U is a bond or optionally substituted alkylene, R7 is hydrogen or optionally substituted alkyl, Z is —S—, —O— or —NR8—, R8 is hydrogen, optionally substituted alkyl or the like.
摘要:
The present invention relates to compounds and methods for inducing synthesis and secretion of insulin from pancreatic beta cells. The methods may take place in vitro, ex vivo such as in isolates from adult mammalian tissue, or in vivo. Compounds and methods described herein may find use in the treatment of diabetes.