专利号:US-2012172350-A1 优先权日:2009-09-11 标题 :Histamine h3 inverse agonists and antagonists and methods of use thereof 发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN 权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
专利号:WO-0102375-A1 优先权日:1999-07-01 标 题:Process for synthesizing oxadiazoles 发明人:DENER JEFFREY MARK; LY CUONG QUOC 权利人:AXYS PHARM INC; DENER JEFFREY MARK; LY CUONG QUOC 摘要:The present invention relates to a process for the synthesis of a single as well as large array of oxadiazole based organic compounds. These oxadiazole based organic compounds are represented by compounds of formula (I).
专利号:WO-0034226-A1 优先权日:1998-12-10 标 题 :Polyamine transport inhibitors 发明人:POULIN RICHARD; AUDETTE MARIE; CHAREST-GAUDREALT RENE 权利人:UNIV LAVAL; ILEX ONCOLOGY INC; POULIN RICHARD; AUDETTE MARIE; CHAREST GAUDREALT RENE 摘要:The application discloses synthetic derivatives of original polyamines in which a carbon atom to the original polyamine comprises an amide group inhibits the e cellular uptake of a natural polyamine by specifically binding a cellular transporter for a natural polyamine . The synthetic derivatives are used to inhibit the activity of a natural polyamine transporter, in the treatment of disorders involving unrestrained cell proliferation and/or differentiation where control of polyamine transport is required When used in combination with a n inhibitor of polyamine synthesis.
专利号:EP-2305808-B1 优先权日:2001-06-20 标 题:Templated molecules and methods for using such molecules 发明人:PEDERSEN HENRIK; GOULIAEV ALEX HAAHR; SAMS CHRISTIAN KLARNER; SLØK FRANK ABILGAARD; FRESKGÃ…RD PER-OLA; HOLTMANN ANETTE; OLSEN EVA KAMPMANN; HUSEMOEN GITTE NYSTRUP; FELDING JAKOB; FRANCH THOMAS; THISTED THOMAS; HYLDTOFT LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER 权利人:NUEVOLUTION AS 摘要:The present invention relates to a method for synthesising templated molecules. In one aspect of the invention, the templated molecules are linked to the template which templated the synthesis thereof. The intion allows the generation of libraries which can be screened for e.g . therapeutic activity.
专利号:US-6949679-B1 优先权日:1998-04-21 标 题 :Polyamine transport inhibitors 发明人:POULIN RICHARD; AUDETTE MARIE; CHAREST-GAUDREAULT RENE 权利人:UNIV LAVAL 摘要:The present invention describes the design, synthesis and therapeutic use of a variety of novel inhibitors of polyamine transport. The main feature of this class of transport inhibitors is to incorporate a linker or side chain that prevents the uptake of polyamines and helps to conjugate polyamine analogs to form dimers with high inhibitory potency against polyamine uptake. These new compounds incorporate features that are designed to maximize their chemical and metabolic stability and their ability to bind to the polyamine transporter, and to minimize their toxicity by preventing their absorption by the cells. The purpose of such inhibitors is to prevent the uptake or salvaging of circulating polyamines by rapidly proliferating cells such as tumor cells, in order to potentiate the effect of therapeutic inhibitors of polyamine biosynthesis such as alpha-difluoromethylornithene.
专利号:US-9688980-B2 优先权日:2001-06-20 标 题 :Templated molecules and methods for using such molecules 发明人:PEDERSEN HENRIK; GOULIAEV ALEX HAAHR; FRANCH THOMAS; SAMS CHRISTIAN KLARNER; OLSEN EVA KAMPMANN; SLOK FRANK ABILGAARD; HUSEMOEN GITTE NYSTRUP; FELDING JAKOB; HYLDTOFT LENE; NORREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRODER; THISTED THOMAS; FRESKGARD PER-OLA; HOLTMANN ANETTE 权利人:NUEVOLUTION AS; NUEVOLUTION 摘要:The present invention relates to a method for synthesising templated molecules. In one aspect of the invention, the templated molecules are linked to the template which templated the synthesis thereof. The intion allows the generation of libraries which can be screened for e.g. therapeutic activity.
参考文献:10.1023/b:modi.0000006827.35029.e4 摘要:Kolb J, Beck B, Almstetter M, Heck S, Herdtweck E, Dömling A. New MCRs: the first 4-component reaction leading to 2,4-disubstituted thiazoles. Mol Divers. 2003;6(3-4):297–313. doi: 10.1023/b:modi.0000006827.35029.e4.