专利号:US-6448413-B1 优先权日:1999-06-10 标题:Process for the synthesis of a-nor-seco compounds with sterane skeleton 发明人:SANTA CSABA; TUBA ZOLTAN; MAHO SANDOR; SZELES JANOS; BALOGH GABOR; BRLIK JANOS; TRISCHLER FERENC; SZILAGYI GABRIELLA; BAKCSI ERIKA 权利人:RICHTER GEDEON VEGYESZET 摘要:The invention relates to a new process for the synthesis of 17β-hydroxy-17α-methyl-1,3-seco-2-nor-5α-androstane-3-acid derivatives of formula (I) n wherein the meaning of Z is carboxyl or formyl group and n to the new secoindoxylidene carboxylic acid derivatives of formula (II) n wherein R 1 and R 2 independently are C 1 -C 4 alkyl or alkoxy group, hydrogen or halogen atom—which are intermediates for preparing the compounds of formula (I). n The 17β-hydroxy-17α-methyl-1,3-seco-2-nor-5α-androstane-3-acid derivatives of formula (I) are intermediates in the synthesis of oxandrolon (17β-hydroxy-17α-methyl-2-oxa-5α-androstane-3-one), which is used as anabolic in therapy.
专利号:US-2025249051-A1 优先权日:2024-02-06 标 题 :Microbiome composition for improving muscle strength using heat-treated fermented culture complex of lactiplantibacillus plantarum km2 发明人:SUNG MOON-HEE 权利人:KOOKMINBIO CORP 摘要:The present disclosure relates to a microbiome composition for improving muscle strength using a heat-treated fermented culture complex of KM2 Lactiplantibacillus plantarum, wherein the composition according to the present disclosure increased synthesis of myoproteins and showed an effect of inhibiting degradation of myoproteins and animal tests showed an effect of improving muscle strength and increasing leg muscle mass through the increase in grip strength, travel distance, and speed, as well as results in which hamstring muscle strength is improved and muscle mass increases even in a clinical trial. In addition, it was found that the beneficial bacteria increased through an increase in the diversity of intestinal microflora that changed with muscle reduction and improvement in the microflora composition, while the harmful bacteria decreased.
专利号:US-2013035307-A1 优先权日:2010-01-26 标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers 发明人:PRESTWICH GLENN D; KENNEDY THOMAS P 权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P 摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.
专利号:US-2022118123-A1 优先权日:2019-02-22 标 题 :Combination of ar antagonists and targeted thorium conjugates 发明人:HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY 权利人:BAYER AG; BAYER AS 摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.
专利号:US-6333317-B1 优先权日:1997-03-28 标 题:Regulation of amyloid precursor protein (APP) expression by administration of an estrogenic compound 发明人:LEE ROBERT K K; WURTMAN RICHARD J 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:It has been discovered that lipophilic hormones that interact with cytosolic or nuclear receptors regulate APP expression and synthesis, through modification of APP mRNA stability and/or regulation of APP gene transcription and translation activities. These studies demonstrate that the treatment of brain cells with estrone or 17β-estradiol results in a reduction in the level of APP holoprotein expression, without a concomitant change in the total level of cell protein. The reduction in the level of APP holoprotein caused by estrone or 17β-estradiol is also expected to reduce the production of neurotoxic APP fragments. In as much as estrogen deficiency in postmenopausal women is associated with a higher incidence of Alzheimer's disease, this discovery opens the possibility that estrogen therapy may prevent some of the neurodegenerative and cognitive changes associated with Alzheimer's disease, aging and other disease conditions associated with such neurodegenerative and cognitive decline.
专利号:US-5902603-A 优先权日:1995-09-14 标题 :Polyurethane hydrogel drug reservoirs for use in transdermal drug delivery systems, and associated methods of manufacture and use 发明人:CHEN TUNG-FEN; CHIANG CHIA-MING; JONA JANAN; JOSHI PRITI; RAMDAS ASHA 权利人:CYGNUS THERAPEUTIC SYSTEMS 摘要:High capacity drug reservoirs are provided for incorporation into transdermal drug delivery systems. The drug reservoirs are hydrogels formulated from polyurethanes crosslinked with diisocyanate crosslinking agents or cured with radiation in the presence of a photoinitator. Drug loading as high as 65 to 70 wt. % or higher can be achieved by absorbing drug formulation into the reservoir after hydrogel synthesis. Methods for making and using transdermal systems containing such reservoirs are provided as well.
参考文献:10.1186/1752-153x-6-153 摘要:Khan NT, Bibi M, Yousuf S, Qureshi IH, Atta-Ur-Rahman N, Al-Majid AM, Mesaik MA, Khalid AS, Sattar SA, Atia-Tul-Wahab N, Choudhary MI. Synthesis of some potent immunomodulatory and anti-inflammatory metabolites by fungal transformation of anabolic steroid oxymetholone. Chem Cent J. 2012 Dec 10;6(1):153.