摘要:
Novel mercaptophenyl naphthyl methane compounds, their pharmaceutically acceptable salts and compositions comprised thereof are useful for the prevention or treatment of various medical indications associated with estrogen dependent diseases or syndromes related to osteoporosis, bone loss, bone formation, cardiovascular disorders, neurodegenerative disorders, menopausal disorders, physiological disorders, diabetes disorders, prostatic carcinoma, cancer of breast, cancer of uterus, cancer of the cervix and cancer of the colon, threatened or habitual abortion, obesity, ovarian development or function, post-partum lactation and depression.
摘要:
The present invention relates to compounds of the formula I in which substituents R2 and R3 are arranged in trans-configuration: wherein: R1 is H or C1-C6 alkyl; C3-C7 cycloalkyl; R2 is phenyl, optionally substituted with 1 to 5 substituents independently selected from the group comprising OH, C1-C6-alkyl, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkoxy and phenyl, wherein R4 is C1-C6 alkyl; R3 is phenyl substituted with OR5 wherein R5 has the formula (II), (III) or (IV) wherein Y is chosen from NHR4, NR42, NHCOR4, NHSO2R4, CONHR4, CONR4, CONR42, COOH, COOR4, SO2R4, SOR4, SONHR4, SONR42, a C3-C7 heterocyclic ring, saturated or unsaturated, containing one or two heteroatoms independently selected from the group consisting of O, S and N, optionally being substituted with 1 to 3 substituents independently selected from the group comprising H, OH, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkyl and C1-C6-alkoxy, preferably NHR4, NR24, or a nitrogen heterocycle, wherein R4 is as defined above, and the esters, ethers, and salts of the compounds of formula I, optionally along pharmaceutically acceptable excipients, a process for the preparation of the same, and a method of preventing and/or treating estrogen-related disease conditions in a subject using compounds of formula 1, or its salts, optionally along with pharmaceutically acceptable excipients.
摘要:
Novel mercaptophenyl naphthyl methane compounds, their pharmaceutically acceptable salts and compositions comprised thereof are useful for the prevention or treatment of various medical indications associated with estrogen dependent diseases or syndromes related to osteoporosis, bone loss, bone formation, cardiovascular disorders, neurodegenerative disorders, menopausal disorders, physiological disorders, diabetes disorders, prostatic carcinoma, cancer of breast, cancer of uterus, cancer of the cervix and cancer of the colon, threatened or habitual abortion, obesity, ovarian development or function, post-partum lactation and depression.
摘要:
The present invention relates to compounds of the formula I in which substituents R2 and R3 are arranged in trans-configuration: wherein: R1 is H or C1-C6 alkyl; C3-C7 cycloalkyl; R2 is phenyl, optionally substituted with 1 to 5 substituents independently selected from the group comprising OH, C1-C6-alkyl, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkoxy and phenyl, wherein R4 is C1-C6 alkyl; R3 is phenyl substituted with OR5 wherein R5 has the formula (II), (III) or (IV) wherein Y is chosen from NHR4, NR42, NHCOR4, NHSO2R4, CONHR4, CONR4, CONR42, COOH, COOR4, SO2R4, SOR4, SONHR4, SONR42, a C3-C7 heterocyclic ring, saturated or unsaturated, containing one or two heteroatoms independently selected from the group consisting of O, S and N, optionally being substituted with 1 to 3 substituents independently selected from the group comprising H, OH, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkyl and C1-C6-alkoxy, preferably NHR4, NR24, or a nitrogen heterocycle, wherein R4 is as defined above, and the esters, ethers, and salts of the compounds of formula I, optionally along pharmaceutically acceptable excipients, a process for the preparation of the same, and a method of preventing and/or treating estrogen-related disease conditions in a subject using compounds of formula 1, or its salts, optionally along with pharmaceutically acceptable excipients.
摘要:
Novel mercaptophenyl naphthyl methane compounds, their pharmaceutically acceptable salts and compositions comprised thereof are useful for the prevention or treatment of various medical indications associated with estrogen dependent diseases or syndromes related to osteoporosis, bone loss, bone formation, cardiovascular disorders, neurodegenerative disorders, menopausal disorders, physiological disorders, diabetes disorders, prostatic carcinoma, cancer of breast, cancer of uterus, cancer of the cervix and cancer of the colon, threatened or habitual abortion, obesity, ovarian development or function, post-partum lactation and depression.
摘要:
This invention relates to novel {overscore (ω)}-substituted-naphthyloxy-amino alkanes, their preparation and use as antihyperglycemic agents and for the treatment and prevention of cardiovascular disorders (CVS) such as lipid lowering effects.
摘要:
The present invention provides a system and a method for distending a body tissue cavity of a subject by continuous flow irrigation such that minimal or negligible fluid turbulence is present inside the cavity, such that any desired cavity pressure can be created and maintained for any desired outflow rate. The present invention also provides a method for accurately determining the rate of fluid loss, into the subject's body system, during any endoscopic procedure without utilizing any deficit weight or fluid volume calculation or flow rate sensor. The system and the methods of the present invention described above can be used in any endoscopic procedure requiring continuous flow irrigation few examples of such endoscopic procedures being hysteroscopic surgery, arthroscopic surgery, trans uretheral surgery, endoscopic surgery of the brain and endoscopic surgery of the spine.
摘要:
A continuous flow irrigation endoscope and a continuous flow irrigation fluid management system, both designed to be compatible to each other and meant to function as a single system. The endoscope and the fluid management system are synergistic to each other such that both enhance the efficiency of each other. The system allows a body tissue cavity to be distended by continuous flow irrigation so that the detached tissue pieces and waste fluid present inside a body tissue cavity are continuously automatically evacuated from the tissue cavity without causing the cavity to collapse at any stage and without the need of withdrawing the endoscope or a part of the endoscope from the tissue cavity.
摘要:
Methods and products of Transport co-polymerization (“TCP”) that are useful for preparations of low Dielectric Constant (“ε”) thin films are disclosed. Transport co-polymerization (“TCP”) of reactive intermediates that are generated from a first precursor with a general structural formula (Z)m—Ar—(CX′X″Y)n (VI) with a second reactive intermediate that is generated from a cage compound (e.g. Fullerenes, Methylsilsesquioxane, Hydrosilsesquioxane, and Adamantanyl) or a cyclic-compounds (e.g. Cyclo-Siloxanes and 2,2-Paracyclophanes) results in co-polymer films that are useful for making porous low ε (≦2.0) thin films. The porous thin films of this invention consist of nano-pores with uniform pore distribution thus retain high rigidity thus are suitable for manufacturing of future ICs using copper as conductor. Preparation methods and stabilization processes for low k co-polymers that consist of sp2C—Z and HC-sp3Cα—X bonds are also revealed. A preparation method is achieved by controlling the substrate temperature and feed rate of the major precursors. One stabilization process includes a post annealing of as-deposited co-polymer films under the presence of hydrogen under high temperatures. The reductive annealing of these films is conducted at temperatures from −20° C. to −50° C. to +20° C. to +50° C. of their Reversible Crystal Transformation (“CRT”) temperatures, then quenching the resulting films to −20° C. to −50° C. below their “CRT” temperatures. The reductive annealing is conducted before the as-deposited film was removed from a deposition system and still under the vacuum. “Re-stabilization” processes of co-polymer surfaces that are exposed to reactive plasma etching are also disclosed; thus, further coating by barrier metal, cap layer or etch-stop layer can be safely applied.
摘要:
A system for distending body tissue cavities of subjects by continuous flow irrigation during endoscopic procedures, the system including: a fluid source reservoir containing a non viscous physiologic fluid meant for cavity distension; a fluid supply conduit tube connecting the fluid source reservoir to an inlet port of a variable speed positive displacement inflow pump and an outlet port of the said inflow pump being connectable to an inflow port of an endoscope instrument through an inflow tube for pumping the fluid at a controlled flow rate into the cavity, the flow rate of the said inflow pump being termed as the inflow rate; an inflow pressure transducer being located anywhere in the inflow tube between the outlet port of the inflow pump and the inflow port of the endoscope; an outflow port of the endoscope being connectable to a waste fluid collecting container via a waste fluid carrying tube, and characterized in that an active inflow pressure pulsation dampening means is connected to the inflow tube for dampening the pressure pulsations inside the cavity created by the positive displacement inflow pump.