摘要:
Treatment of Diseases caused by Disturbances of the Activity of the Androgen Receptor uses of compounds of Formula (I): (as defined herein), for the treatment of diseases caused by disturbances of the activity of androgen receptor are provided: Formula (I). Isolated compounds of Formula (I) are also provided.
摘要:
This invention relates to compounds of the formula (I) which are thyroid receptor ligands, and are preferably selective for the thyroid hormone receptor β, to methods of preparing such compounds and to methods for using such compounds such as in the regulation of metabolism.
摘要:
New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR′R″) or an acylsulphonamide (CONHSO2R′) derivative, or a pharmaceutically acceptable salt thereof, and all stereoisomers thereof; or when n is equal to or greater than one, R4 may be a heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR′R″). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5=H). In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a T3 regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.
摘要翻译:提供了具有通式(I)的新甲状腺受体配体,其中:n为0至4的整数; R 1是卤素,三氟甲基或1至6个碳的烷基或3至7个碳的环烷基; R 2和R 3相同或不同,为氢,卤素,1至4个碳的烷基或3至5个碳的环烷基,R 1, SUB 2和R 3不是氢; R 4是羧酸酰胺(CONR'R“)或酰基磺酰胺(CONHSO 2 R')衍生物或其药学上可接受的盐及其所有立体异构体; 或当n等于或大于1时,R 4可以是可被取代或未取代的杂芳族部分,或胺(NR'R“)。 R 5是氢或酰基(例如乙酰基或苯甲酰基)或能够生物转化以产生游离酚结构(其中R 5 = H)的其它基团。 此外,提供了一种用于预防,抑制或治疗与代谢功能障碍相关的疾病或依赖于T 3 N调节基因的表达的方法,其中如上所述的化合物以 治疗有效量。 与代谢功能障碍相关或依赖于T 3受体基因表达的这种疾病的实例包括肥胖症,高胆固醇血症,动脉粥样硬化,心律失常,抑郁症,骨质疏松症,甲状腺机能减退,甲状腺肿,甲状腺癌以及 青光眼,充血性心力衰竭和皮肤疾病。
摘要:
New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR′R″) or an acylsulphonamide (CONHSO2R′) derivative, or a pharmaceutically acceptable salt thereof, and all stereolsom thereof; or when n is equal to or greater than one, R4 may be heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR′R″). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5—H). In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependant upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a T3 regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.
摘要翻译:提供了具有通式(I)的新甲状腺受体配体,其中:n为0至4的整数; R 1是卤素,三氟甲基或1至6个碳的烷基或3至7个碳的环烷基; R 2和R 3相同或不同,为氢,卤素,1至4个碳的烷基或3至5个碳的环烷基,R 1, SUB 2和R 3不是氢; R 4是羧酸酰胺(CONR'R“)或酰基磺酰胺(CONHSO 2 R')衍生物或其药学上可接受的盐及其所有立体异构体; 或当n等于或大于1时,R 4可以是可被取代或未取代的杂芳族部分,或胺(NR'R“)。 R 5是氢或酰基(如乙酰基或苯甲酰基)或能够生物转化以产生游离酚结构的其它基团(其中R 5 -H)。 此外,提供了一种用于预防,抑制或治疗与代谢功能障碍相关的疾病或依赖于T 3 N调节基因的表达的方法,其中如上所述的化合物以 治疗有效量。 与代谢功能障碍相关或依赖于T 3受体基因表达的这种疾病的实例包括肥胖症,高胆固醇血症,动脉粥样硬化,心律失常,抑郁症,骨质疏松症,甲状腺机能减退,甲状腺肿,甲状腺癌以及 青光眼,充血性心力衰竭和皮肤疾病。
摘要:
Compounds of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which R1 to R9 have meanings as defined in the Specification, are useful as estrogen receptor ligands.
摘要:
Various technologies and techniques are disclosed for observing the real-world performance of components and using the collected data to improve other user experiences. Configuration data, usage data, and user experience data are collected for components on observed solution instances. The configuration data, usage data, and user experience data are analyzed to generate component diagnostic data that can be used to make recommendations to one or more advised solution instances as to how to correct a problem being experienced on the one or more advised solution instances. In one implementation, the component diagnostic data generated includes a reputation rating for each of the components.
摘要:
Exemplary methods, computer-readable media, and systems for maintaining an inbound network path to a host in a sleep or a hibernation mode behind a plurality of network address translators (NAT) or firewalls. A network interface card (NIC) of a host is configured to periodically send or receive keep-alive packets. These packets enable network mappings that would ordinarily expire while a host is in a sleep or a hibernation mode. Power is maintained on the NIC while the host is in such mode, and the NIC responds as programmed including waking a host upon a certain event, such as receiving a data packet matching a preconfigured signature. During such time, the host may be in a wake on LAN mode.
摘要:
Architecture that facilitates validation of a data mapping of data from a data source to a data target. There is included a signature generation component that generates a source signature of all or a portion of the data source and a target signature of all or a corresponding portion of the data target, and a sampling component that obtains a sample of the source data a corresponding sample of the target data. The data signatures and data samples are compared respectively and processed with a processing component to determine the status of the validation process.
摘要:
The invention provides compounds of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, for use in the treatment or prophylaxis of condition mediated by an androgen receptor.
摘要:
New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or differential hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid thereof; or when n is equal to or greater than one, R4 may be heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR′R″). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5—H). In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependant upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a T3 regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.
摘要翻译:提供了具有通式(I)的新甲状腺受体配体,其中:n为0至4的整数; R 1是卤素,三氟甲基或1至6个碳的烷基或3至7个碳的环烷基; R 2和R 3是相同或不同的氢,卤素,1至4个碳的烷基或3至5个碳的环烷基,R 1, 2和R 3不是氢; R 4是其羧酸; 或当n等于或大于1时,R 4可以是可被取代或未取代的杂芳族部分,或胺(NR'R“)。 R 5是氢或酰基(如乙酰基或苯甲酰基)或能够生物转化以产生游离酚结构的其它基团(其中R 5 -H)。 此外,提供了一种用于预防,抑制或治疗与代谢功能障碍相关的疾病或依赖于T 3 N调节基因的表达的方法,其中如上所述的化合物以 治疗有效量。 与代谢功能障碍相关或依赖于T 3受体基因表达的这种疾病的实例包括肥胖症,高胆固醇血症,动脉粥样硬化,心律失常,抑郁症,骨质疏松症,甲状腺机能减退,甲状腺肿,甲状腺癌以及 青光眼,充血性心力衰竭和皮肤疾病。