摘要:
The present invention relates to compounds and methods from the treatment of cancer. The invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods for the treatment of cancer using the compounds of the presentation invention or pharmaceutical compositions comprising compounds of the present invention.
摘要:
This invention provides compounds which are useful as inhibitors of protein tyrosine phosphatases (PTPases). As inhibitors of PTPases, the compounds of the invention are useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include type I diabetes, type II diabetes, immune dysfunction, AIDS, autoimmunity, glucose intolerance, obesity, cancer, psoriasis, allergic diseases, infectious diseases, inflammatory diseases, diseases involving the modulated synthesis of growth hormone or the modulated synthesis of growth factors or cytokines which affect the production of growth hormone, or Alzheimer's disease.
摘要:
The present invention relates to certain substituted 17.beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), especially those of formula (IG) ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;R.sup.3c is hydrogen;R.sup.4c is hydrogen, lower alkyl, lower cycloalkyl, lower alkenyl, alkanoyl of 2-6 carbons, --(CH.sub.2).sub.m CO.sub.2 R.sup.16, --(CH.sub.2).sub.m Ar.sup.a, --(CH.sub.2).sub.n 'CONR.sup.17 R.sup.18, --(CH.sub.2).sub.n 'NR.sup.17 R.sup.18 or --(CH.sub.2).sub.n 'OR.sup.16, wherein R.sup.16 is hydrogen, lower alkyl or lower alkenyl; R.sup.17 and R.sup.18 are independently hydrogen, lower alkyl lower cycloalkyl or lower alkenyl; Ar.sup.a is an aromatic group of 6 to 12 carbons; n' is 0 or an integer from 1 to 5; m is an integer from 1 to 5;R.sup.19 and R.sup.20 are independently hydrogen or lower alkyl, or taken together R.sup.19 and R.sup.20 form a carbonyl group (.dbd.O);R.sup.5c is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, or NR.sup.21 R.sup.22, wherein R.sup.21 and R.sup.22 are independently hydrogen, lower alkyl or lower alkenyl;and pharmaceutically acceptable salts thereof, their preparation, medical use and pharmaceutical formulations.
摘要:
A method for manufacturing a thin film structural system including a thin film structure includes depositing a reinforcing material in a liquid form in a predefined pattern on a thin film membrane, and transforming the reinforcing material in the predefined pattern to form a reinforcing element connected to the thin film membrane. The reinforcing material may be deposited in a melted form and solidified by cooling, may be transformed by a light or laser induced chemical reaction, or may be deposited and solidified such that the reinforcing element is at least partially embedded in the thin film membrane. The predefined pattern may redistribute loads around a damaged portion of the thin film structure, or define a hinge, a folding line, a stiffening feature. The reinforcing element may be electrically, optically or thermally conductive, to communicate with a device included in the system. The system may be a space structure.
摘要:
The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof These compounds are useful in the treatment of RAGE-mediated diseases such as Alzheimer's Disease.The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use of such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.
摘要:
A system according to the present invention including a main utility distribution panel which through corresponding circuit breakers, directly powers facility power line circuits which remain powered continuously, and an ‘off-peak’ utility distribution panel being powered by the main utility distribution panel through a contactor (relay, switch, etc.) controlled by a 24 hour timer, and the ‘off-peak’ utility distribution panel in turn powers facility power line circuits which may be de-energized to provide zero power draw from the main utility distribution panel during a selected time period as provided by the timer, which generally corresponds to periods when the facility is unoccupied and/or the equipment and appliances are turned off.
摘要:
The present invention provides azole derivatives of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I), and their use in treating human or animal disorders. The compounds of the invention can be useful as inhibitors of protein tyrosine phosphatases and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.
摘要:
This invention provides azoles which may be useful as inhibitors of protein tyrosine phosphatases (PTPases). The present invention provides compounds of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds and their use in treating human or animal disorders. The compounds of the invention may be useful as inhibitors of protein tyrosine phosphatases and thus can be useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes, Type II diabetes.
摘要:
The present invention provides imidazole derivatives of Formula (I-IV), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I-IV), and their use in treating human or animal disorders. The compounds of the invention inhibit protein tyrosine phosphatase 1B and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.
摘要:
The present invention relates to a portable multi-use receptacle. The device is particularly useful as a receptacle for collecting and holding tree and shrub trimmings or leaves. The device consists of a basin-like structure having a flat rigid base. The base has an outer wall attached to the periphery thereof. The outer base has an opening therein between about 1/8 and about 1/3 of the periphery. The base has a second substantially shorter wall bridging the opening of the first wall along the periphery of the base. The base has a third wall corresponding approximately in height to the second wall. The third wall extends inward from one juncture of the first and second walls to the center portion of the base and then outward to the other juncture of the first and second walls. In this manner a walled, wedge-shaped section is defined in the base. The wedge-shaped area is removeable to obtain a walled substantially wedge-shaped opening in the base that is of a size to receive the trunk of a tree or shrub that is to be trimmed.