摘要:
Compounds of general formula (I): wherein R1, R2, R3 and R4 are independently hydrogen, halo, C1-C6 alkyl, —O(C1-C6 alkyl), —CON(R9)2, —SOR9, —SO2R9, —SO2N(R9)2, —N(R9)2, —NR9COR9, —CO2R9, —COR9, —SR9, —OH, —NO2 or —CN; each R9 is independently hydrogen or C1-C6 alkyl; R5 and R6 are each independently hydrogen, or C1-C6 alkyl or together with the carbon atom to which they are attached form a C3-C7 cycloalkyl group; R7 is hydrogen or C1-C6 alkyl n is 1 or 2; X is a bond or, when n is 2, X may also be a NR9 group; wherein R9 is as defined above; when X is a bond R8 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, biphenyl or a 9-14 membered bicyclic or tricyclic heteroaryl group; when X is a NR9 group R8 may additionally be phenyl, naphthyl or a 5-7 membered heteroaromatic ring; and the R8 group is optionally substituted with one or more substituents selected from halo, C1-C6 alkyl, —O(C1-C6)alkyl, aryl, —O-aryl, heteroaryl, —O-heteroaryl, —CON(R9)2, —SOR9, —SO2R9, SO2N(9)2, —N(9)2, —NR9COR9, —CO2R9, —COR9, —SR9, —OH, —NO2 or —CN; wherein R9 is as defined above; and their pharmaceutically acceptable salts, hydrates, solvates, complexes and prodrugs are useful in the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
摘要:
The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.
摘要:
The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder.
摘要:
The invention relates to compounds of formula (I) wherein X, R1, R2, R3, R8, R9 have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
摘要:
Benzimidazole, indole and benzolactam boronic acid compounds, analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) in a subject in need thereof.
摘要:
Indole boronic acid compounds, and analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) in a subject in need thereof.
摘要:
The present invention relates to piperidine derivatives of formula (I) ##STR1## wherein R.sup.1 is a C.sub.1-4 alkoxy group; R.sup.2 is ##STR2## R.sup.3 is a hydrogen or halogen atom; R.sup.4 and R.sup.5 may each independently represent a hydrogen or halogen atom, or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trifluoromethyl group; R.sup.6 is a hydrogen atom, a C.sub.1-4 alkyl, (CH.sub.2).sub.m cyclopropyl, --S(O).sub.n C.sub.1-4 alkyl, phenyl, NR.sup.7 R.sub.8, CH.sub.2 C(O)CF.sub.3 or trifluoromethyl group; R.sup.7 and R.sup.8 may each independently represent a hydrogen atom, or a C.sub.1-4 alkyl or acyl group; x represents zero or 1; n represents zero, 1 or 2; m represents zero or 1; and pharmaceutically acceptable salts and solvates thereof; to processes for their preparation; and their use in the treatment of conditions mediated by tachykinins.
摘要翻译:本发明涉及式(I)的哌啶衍生物其中R 1为C 1-4烷氧基; R 2是氢或卤素原子; R 4和R 5可各自独立地表示氢或卤素原子,或C 1-4烷基,C 1-4烷氧基或三氟甲基; R6是氢原子,C1-4烷基,(CH2)环丙基,-S(O)nC1-4烷基,苯基,NR7R8,CH2C(O)CF3或三氟甲基; R 7和R 8可各自独立地表示氢原子或C 1-4烷基或酰基; x表示零或1; n表示0,1或2; m表示0或1; 及其药学上可接受的盐和溶剂合物; 进行准备; 及其用于治疗由速激肽介导的病症。
摘要:
The invention provides compounds of the general formula (I): ##STR1## or a physiologically acceptable salt, solvate (e.g. hydrate) or a metabolically labile ester thereof.The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.
摘要:
The present invention relates to methods for the characterization of enzymes or of enzyme-compound complexes, wherein the enzyme is obtained from a protein preparation with the help of at least one broad spectrum ligand immobilized on a solid support and wherein the enzyme is characterized by mass spectrometry. These methods are useful for the screening of non-immobilized compound libraries, selectivity profiling of lead compounds and mechanism of action studies in living cells.
摘要:
The present invention relates to a series of novel compounds having the formula (I) wherein: X is NR3 or O; n is 1 or 2; A is a bicyclic carbocycle and R1 and R2 are as described herein. The compounds are useful as DPP-IV inhibitors, such as for the treatment of diabetes.