专利号:US-2011028688-A1 优先权日:2006-06-21 标 题 :Crystal structure of ox40l and ox40l complexed with ox40 receptor 发明人:HYMOWITZ SARAH; COMPAAN MCGUINN DEANNE 权利人:GENENTECH INC 摘要:The present disclosure provides crystals of and structural coordinates of mOX40L, hOX40L, hOX40 receptor and complexes thereof. The crystals and crystal structures are useful, for example, in the design and synthesis of modulators of mOX40L, hOX40L, and/or hOX40 receptor.
专利号:US-7309799-B2 优先权日:2004-06-01 标 题:Methods for the synthesis of milnacipran and congeners thereof 发明人:BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V 权利人:COLLEGIUM PHARMACEUTICAL INC 摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.
专利号:US-11993606-B2 优先权日:2015-10-16 标题:Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof 发明人:MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; PANGAN AILEEN L; SONG IN-HO; KLÜNDER BEN; VOSS JEFFREY W; PADLEY ROBERT J; CAMP HEIDI S 权利人:ABBVIE INC 摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).
专利号:US-11976077-B2 优先权日:2015-10-16 标 题 :Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-α]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms therof 发明人:PANGAN AILEEN L; TEIXEIRA HENRIQUE D; MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; KLÜNDER BEN; VOSS JEFFREY W; PADLEY ROBERT J; CAMP HEIDI S 权利人:ABBVIE INC 摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and atopic dermatitis), kits, methods of synthesis, and products-by-process.
专利号:US-11512092-B2 优先权日:2015-10-16 标题 :Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof 发明人:ALLIAN AYMAN; JAYANTH JAYANTHY; MOHAMED MOHAMED-ESLAM F; MULHERN MATHEW; NORDSTROM FREDRIK LARS; OTHMAN AHMED A; ROZEMA MICHAEL J; BHAGAVATULA LAKSHMI; MARROUM PATRICK J; MAYER PETER T; SHEIKH AHMAD Y; BORCHARDT THOMAS B; KLÜNDER BEN 权利人:ABBVIE INC 摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).
专利号:US-7799829-B2 优先权日:2006-07-28 标 题 :Acyloxyalkyl carbamate prodrugs of α-amino acids, methods of synthesis and use 发明人:DAI XUEDONG; GANGAKHEDKAR ARCHANA; XIANG JIA-NING; GALLOP MARK A 权利人:XENOPORT INC 摘要:Acyloxyalkyl carbamate prodrugs of α-amino acids, pharmaceutical compositions thereof, methods of making acyloxyalkyl carbamate prodrugs of α-amino acids and methods of using acyloxyalkyl carbamate prodrugs of α-amino acids, and pharmaceutical compositions thereof to treat a disease are disclosed. Acyloxyalkyl carbamate prodrugs of α-amino acids suitable for oral administration using sustained release dosage forms are also disclosed.
参考文献:10.1007/s00484-009-0300-x 摘要:Matsumoto S, Shimodozono M, Etoh S, Shimozono Y, Tanaka N, Kawahira K. Beneficial effects of footbaths in controlling spasticity after stroke. International Journal of Biometeorology. 2010 Feb 17;54(4):465–73. doi: 10.1007/s00484-009-0300-x. 参考文献:10.1007/s00228-005-0028-4 摘要:Zesiewicz TA, Pathak A, Sullivan KL, Shamayev M, Hauser RA. Treatment of chorea with levetiracetam. European Journal of Clinical Pharmacology. 2005 Dec 01;62(1):87. doi: 10.1007/s00228-005-0028-4. 参考文献:10.1107/s1600536811008348 摘要:John P, Khan IU, Akkurt M, Ramzan MS, Sharif S. 5-Chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-2,1,3-benzothiadiazol-4-amine (tizanidine). Acta Crystallogr E Struct Rep Online. 2011 Mar 12;67(4):o838–9. doi: 10.1107/s1600536811008348. 参考文献:10.1155/2011/403808 摘要:Handy CR, Krudy C, Boulis N, Federici T. Pain in Amyotrophic Lateral Sclerosis: A Neglected Aspect of Disease. Neurology Research International. 2011;2011():1–8. doi: 10.1155/2011/403808. 参考文献:10.1111/j.1526-4610.2011.01956.x 摘要:Aurora SK. Implications of current clinical trials focused on medication overuse and therapeutic prophylaxis. Headache. 2011 Jul;51 Suppl 2():93–100. doi: 10.1111/j.1526-4610.2011.01956.x.