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1. 发明申请

WO2014031581A8 PROCESS FOR THE SYNTHESIS OF SUBSTITUTED GAMMA LACTAMS 审中-公开
公开(公告)号：WO2014031581A8
公开(公告)日：2014-02-27
申请号：PCT/US2013/055685
申请日：2013-08-20
申请人： ALLERGAN, INC. , DINH, Danny, T. , GARST, Michael, E. , OLD, David, W. , SYAGE, Elizabeth, T. , GORIN, Boris, I. , LANTHIER, Christopher, M. , OUDENES, Jan
发明人： DINH, Danny, T. , GARST, Michael, E. , OLD, David, W. , SYAGE, Elizabeth, T. , GORIN, Boris, I. , LANTHIER, Christopher, M. , OUDENES, Jan
IPC分类号： C07D409/12
摘要： The present invention provides synthetic processes for the preparation of a variety of well-defined substituted gamma lactams. The compounds that can be prepared by the process of the invention are useful for treating a variety of conditions. In some embodiments of the invention, the compounds are useful for treating ocular disorders, such as, for example, glaucoma, lowering of elevated intraocular pressure, and the like. In other embodiments, the compounds are useful for treating irritable bowel disease. In further embodiments, the compounds are useful in promoting hair growth. In still further embodiments, the compounds are useful in promoting wound healing, scar reduction, and the like.

2. 发明申请

WO2006107598A3 CONJUGATES OF PHOTOACTIVE COMPOUND AND A BULKING GROUP FOR ENHANCING PHOTODYNAMIC THERAPY 审中-公开
公开(公告)号：WO2006107598A3
公开(公告)日：2006-10-12
申请号：PCT/US2006/010359
申请日：2006-03-22
申请人： ALLERGAN, INC. , BURKE, James, A. , SYAGE, Elizabeth, T. , GARST, Michael, E. , WHEELER, Larry, A.
发明人： BURKE, James, A. , SYAGE, Elizabeth, T. , GARST, Michael, E. , WHEELER, Larry, A.
IPC分类号： A61K47/48 , A61K41/00 , A61P27/02
摘要： A chemical conjugate for administration to a patient undergoing photodynamic therapy includes a photoactive compound coupled to a leakage reducing agent that is structured to reduce leakage of the photoactive compound from a patient ' s vasculature . The leakage reducing agent may be a bulking agent to sterically reduce the permeability of the photoactive compound through the blood vessel, or it may be a ligand that binds to endothelial cells of a patient's choriocapillaries . The conjugate may be used in methods of reducing secondary damage associated with photodynamic therapy.

3. 发明申请

WO1995011229A1 1,11-DIESTERS OF PROSTAGLANDIN-F2'alpha' HAVING A POLAR ESTER GROUP AT C-1 审中-公开
标题翻译：在C-1上具有极性酯基团的前列腺素-21α的1,11-
公开(公告)号：WO1995011229A1
公开(公告)日：1995-04-27
申请号：PCT/US1994011856
申请日：1994-10-17
申请人： ALLERGAN, INC.
发明人： ALLERGAN, INC. , GARST, Michael, E. , SYAGE, Elizabeth, T. , ROOF, Michael, B. , WOODWARD, David, F. , CHAN, Ming, Fai
IPC分类号： C07C405/00
CPC分类号： A61K31/557 , C07C405/00
摘要： Compounds of formula (I) where the hatched lines indicate alpha ( alpha ) configuration, a solid triangle is used to indicate beta ( beta ) configuration, lines on both sides of a double bond indicate cis (Z) configuration, and lines on opposite sides of the double bond indicate trans (E) configuration; R1 is alkyl of 1 - 10 carbons, C1 - C10-alkylphenyl, phenyl-C1 - C10alkyl, or alkenyl of 2 to 10 carbons and having 1 to 3 double bonds; R2 is Z - OR3, Z - OCOR3, Z - OCONHR3, Z - OCOOR3, Z - NR4R5, Z - NR4COR3, Z - NR4SO2R3, Z - COOR3, Z - CONR4R5, Z - CHO; Z is (CH2)n where n is 1 - 6, or Z is an alkenyl group having 2 to 6 carbons and 1 or 2 double bonds, R3 is H, alkyl of 1 - 6 carbons, alkenyl of 2 to 6 carbons or phenyl, R4 and R5 independently are H or alkyl of 1 to 6 carbons, have ocular hypotensive activity.
摘要翻译：其中阴影线表示α（α）构型，实心三角形用于表示β（β）构型的式（I）化合物，双键两侧的线表示顺式（Z）构型，相对侧上的线双键表示反式（E）构型; R1是1-10个碳原子的烷基，C1-C10烷基苯基，苯基C1-C10烷基或2至10个碳原子的烯基并具有1至3个双键; R2是Z-OR3，Z-OCOR3，Z-OCONHR3，Z-OCOOR3，Z-NR4R5，Z-NR4COR3，Z-NR4SO2R3，Z-COOR3，Z-CONR4R5，Z-CHO; Z是（CH 2）n，其中n是1-6，或Z是具有2至6个碳的烯基和1或2个双键，R3是H，1-6个碳原子的烷基，2至6个碳原子的链烯基或苯基，R4和R5独立地是H或1至6个碳的烷基，具有眼睛低血压活性。

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