摘要:
Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4 and R7 are defined in the specification, Z is SO or SO2, and Ar is an aromatic or heteroaromatic group as defined herein.
摘要:
Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula (I) or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4 and R7 are defined in the specification, Z is SO or SO2, and Ar is an aromatic or heteroaromatic group as defined herein.
摘要:
Disclosed are compounds for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade. Said compounds are of Formula I or a solvate, hydrate, pharmaceutically acceptable salt, or prodrug thereof; wherein Ra, Rb, and Rc are defined in the specification, as are A Z, Q, R1 and R2.
摘要:
The present invention is directed to conjugated complement cascade inhibitors, and a method of treating a patient using a conjugated complement cascade inhibitor.
摘要:
The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要:
The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: R1, R2, R9, R10, Ra, Rd and M are defined herein; X is a bivalent radical of: an alkane, a cycloalkane, an optionally-substituted arene, an optionally-substituted heteroarene, an optionally-substituted arylalkane or an optionally-substituted heteroarylalkane; and R3 is —CO2Rd, —CO2M, —OH, —NHRd, —SO2Rd, —NHCONHRd, optionally-substituted amidino or optionally-substituted guanidino; or R3—X— is hydrogen or an electron pair; R4 is oxygen or —NR9R10; R5 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; and R6, R7 and R8 are independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkylalkyl, aralkyl or heteroarylalkyl, each of which is optionally substituted; or R6 and R7, together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted 1 to 3 times with Ra.
摘要翻译:本发明涉及新的1,4-二氮杂,其药物组合物及其作为HDM2-p53相互作用抑制剂的用途。 化合物具有式I:或其溶剂合物,水合物或其药学上可接受的盐; 其中:R 1,R 2,R 9,R 10,R SUP, >,R d和M在本文中定义; X是二价基团:烷烃,环烷烃,任选取代的芳烃,任选取代的杂芳烃,任选取代的芳基烷烃或任选取代的杂芳基烷烃; 和R 3是-CO 2 R 2,-CO 2 M,-OH,-NHR 0 任选取代的脒基或任选取代的胍基;其中R 1,R 2,R 3,R 4, 或R 3 -X-是氢或电子对; R 4是氧或-NR 9 R 10; R 5是环烷基,芳基,杂芳基,环烷基烷基,芳烷基,杂芳基烷基或饱和或部分不饱和的杂环,其各自任选被取代; R 6和R 8独立地是氢,烷基,环烷基,芳基,杂芳基,饱和或部分不饱和的杂环,环烷基烷基 ,芳烷基或杂芳基烷基,其各自任选被取代; 或R 6和R 7与它们所连接的碳原子一起形成3-至7-元碳环,任选地被R 1取代1至3倍, SUP> a SUP>。
摘要:
The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: R1, R2, R9, R10, Ra, Rd and M are defined herein;X is a bivalent radical of: an alkane, a cycloalkane, an optionally-substituted arene, an optionally-substituted heteroarene, an optionally-substituted arylalkane or an optionally-substituted heteroarylalkane; andR3 is —CO2Rd, —CO2M, —OH, —NHRd, —SO2Rd, —NHCONHRd, optionally-substituted amidino or optionally-substituted guanidino;or R3—X— is hydrogen or an electron pair;R4 is oxygen or —NR9R10;R5 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; andR6, R7 and R8 are independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkylalkyl, aralkyl or heteroarylalkyl, each of which is optionally substituted; or R6 and R7, together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted 1 to 3 times with Ra.
摘要翻译:本发明涉及新的1,4-二氮杂,其药物组合物及其作为HDM2-p53相互作用抑制剂的用途。 化合物具有式I:或其溶剂合物,水合物或其药学上可接受的盐; 其中:R 1,R 2,R 9,R 10,R a, >,R d和M在本文中定义; X是二价基团:烷烃,环烷烃,任选取代的芳烃,任选取代的杂芳烃,任选取代的芳基烷烃或任选取代的杂芳基烷烃; 和R 3是-CO 2 R 2,-CO 2 M,-OH,-NHR 0 任选取代的脒基或任选取代的胍基;其中R 1,R 2,R 3,R 4, 或R 3 -X-是氢或电子对; R 4是氧或-NR 9 R 10; R 5是环烷基,芳基,杂芳基,环烷基烷基,芳烷基,杂芳基烷基或饱和或部分不饱和的杂环,其各自任选被取代; R 6和R 8独立地是氢,烷基,环烷基,芳基,杂芳基,饱和或部分不饱和的杂环,环烷基烷基 ,芳烷基或杂芳基烷基,其各自任选被取代; 或R 6和R 7与它们所连接的碳原子一起形成3-至7-元碳环,任选地被R 1取代1至3倍, SUP> a SUP>。
摘要:
The invention is directed to acylhydrazones compounds of Formula I: where R1, R2 and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要:
This invention relates to a novel thieno[2,3-d]pyrimidine, Z, and its therapeutic and prophylactic uses, wherein X, R1 and R2 are defined in the specification. Disorders treated and/or prevented include Parkinson's Disease.
摘要:
This invention relates to a novel thieno[2,3-d]pyrimidine, Z, and its therapeutic and prophylactic uses, wherein X, R1 and R2 are defined in the specification. Disorders treated and/or prevented include Parkinson's Disease.