专利号:WO-2023122754-A1 优先权日:2021-12-23 标 题 :Processes and intermediates for preparing gb13, gb22 and himgaline 发明人:LANDWEHR ELEANOR; SHENVI RYAN; BAKER MEGHAN; OGUMA TAKUYA 权利人:SCRIPPS RESEARCH INST 摘要:Provided herein are processes for the streamlined synthesis of Galbulimima alkaloids, such as himbadine, isolated from Galbulimima belgraveana and G. baccatta, trees endemic to the rainforests of Northern Australia and Papua New Guinea, as well as analogs thereof, such as GB13, GB16, GB22, and himgaline, and further including intermediates useful in the synthesis of these and related compounds.
专利号:US-6316437-B1 优先权日:1999-09-30 标题:Spirohydantoin compounds and uses thereof 发明人:HOFFMAN JACOB M 权利人:MERCK & CO INC 摘要:Spirohydantoin compounds and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
专利号:US-9051289-B2 优先权日:2013-09-26 标 题 :Process and intermediates for preparing GPR40 agonists 发明人:DAHMANN GEORG; WAGNER HOLGER; ECKHARDT MATTHIAS; FRANK MARKUS; SANTAGOSTINO MARCO; SCHNAUBELT JUERGEN; STERTZ UWE; PACHUR THORSTEN 权利人:DAHMANN GEORG; WAGNER HOLGER; ECKHARDT MATTHIAS; FRANK MARKUS; SANTAGOSTINO MARCO; SCHNAUBELT JUERGEN; STERTZ UWE; PACHUR THORSTEN; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to compounds of formula I n nwherein R S denotes F or CF 3 , R a denotes H or C 1-4 -alkyl and Z denotes a leaving group or an optionally substituted or protected hydroxyl group, suitable as intermediates in the synthesis of indanyloxydihydrobenzofuranylacetic acids, which are GPR40 agonists, to a process for preparing these intermediates and to the process for preparing the GPR40 agonists making use of an asymmetric catalytic hydrogenation reaction in the presence of a transition metal catalyst and a chiral auxiliary.
专利号:US-5504104-A 优先权日:1993-11-19 标 题:Tricyclic pyrone derivatives as protease inhibitors and antiviral agents 发明人:ELLSWORTH EDMUND L; TAIT BRADLEY D 权利人:WARNER LAMBERT CO 摘要:The present invention relates to novel substituted tricyclic pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The tricyclic pyrone derivatives are useful in the development of therapies for the treatment of vital infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized tricyclic pyrones and of related structures.
专利号:EP-1339683-B1 优先权日:2000-11-27 标题 :Estrogen receptor modulators 发明人:WILKENING ROBERT R; PARKER DANN LEROY JR; WILDONGER KENNETH J; MENG DONGFANG; RATCLIFFE RONALD W 权利人:MERCK & CO INC 摘要:The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.