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51. 发明申请

WO1997016729A1 COMBINATORIAL DIHYDROBENZOPYRAN LIBRARY 审中-公开
标题翻译：组合二氢苯并噻吩库
公开(公告)号：WO1997016729A1
公开(公告)日：1997-05-09
申请号：PCT/US1996017982
申请日：1996-11-04
申请人： PHARMACOPEIA, INC.
发明人： PHARMACOPEIA, INC. , BALDWIN, John, J. , DILLARD, Lawrence, W. , LI, Ge , READER, John, C. , ZENG, Wenguang
IPC分类号： G01N33/53
CPC分类号： C40B40/04 , C07B2200/11 , C07C205/59 , C07D311/08 , C07D311/22 , C07D311/96 , C07D491/10 , C07D493/10 , C07D495/10 , C12Q1/00 , C40B40/00 , C40B50/14 , G01N33/573
摘要： Combinatorial libraries are disclosed which are represented by Formula (I), wherein S is a solid support; T'-L- is an identifier residue; and -L'-II' is a ligand/linker residue. These libraries contain dihydrobenzopyrans of Formula (II) which interact (i.e., as agonists or antagonists) with alpha adrenergic receptors, dopamine receptors, sigma -opiate receptors, and K channels and are inhibitors of carbonic anhydrase isozymes. They are useful in the treatment of ocular diseases such as glaucoma.
摘要翻译：公开了由式（I）表示的组合文库，其中S是固体支持物; T'-L-是标识符残基; 和-L'-II'是配体/接头残基。这些文库含有与α肾上腺素能受体，多巴胺受体，σ-受体和K +通道相互作用（即作为激动剂或拮抗剂）的式（II）的二氢苯并吡喃，是碳酸酐酶同功酶的抑制剂。它们可用于治疗眼部疾病如青光眼。

52. 发明申请

WO1997010200A1 PROCESS FOR THE PURIFICATION OF DIPHENYL ETHER COMPOUNDS 审中-公开
标题翻译：二苯醚化合物的纯化方法
公开(公告)号：WO1997010200A1
公开(公告)日：1997-03-20
申请号：PCT/GB1996001893
申请日：1996-08-06
申请人： ZENECA LIMITED , BROWN, Stephen, Martin , GOTT, Brian, David , GRAY, Thomas , TAVANA, Seyed, Mehdi
发明人： ZENECA LIMITED
IPC分类号： C07C201/16
CPC分类号： C07C303/44 , C07C201/16 , C07C311/51 , C07C205/59
摘要： A process for the purification of a compound of general formula (I), wherein R is hydrogen or C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl (any of which may optionally be substituted with one or more substituents selected from halogen and OH) or COOH, COH, COOR , COR , CONR R or CONHSO2R ; R and R are each independently hydrogen or C1-C4 alkyl optionally substituted with one or more halogen atoms; R is a halogen atom or a group R ; R is hydrogen or halo; R is C1-C4 alkyl, C2-C4 alkenyl or C2-C4 alkynyl, any of which may optionally be substituted with one or more halogen atoms, or halo; or where appropriate, a salt thereof; from a mixture containing the compound of general formula (I) together with one or more isomers or di-nitrated analogues thereof; the process comprising dissolving the mixture in a suitable crystallisation solvent and recrystallising the product from the resulting crystallisation solution; characterised in that the crystallisation solution contains not more than 25 % loading of the compound of general formula (I) wherein loading is defined as: weight of pure compound of formula (I) x 100/weight of pure compound of formula (I) + weight of solvent, and in that the temperature to which the solution is cooled for crystallisation is not greater than about 30 DEG C.
摘要翻译：用于纯化通式（I）的化合物的方法，其中R 1是氢或C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基（其任何一个可以任选地被一个或多个取代基取代选自卤素和OH）或COOH，COH，COOR 4，COR 6，CONR 4 R 5或CONHSO 2 R 4; R 4和R 5各自独立地为氢或任选被一个或多个卤素原子取代的C 1 -C 4烷基; R 6是卤素原子或基团R 4; R 2是氢或卤素; R 3是C 1 -C 4烷基，C 2 -C 4烯基或C 2 -C 4炔基，其中任何一个可以任选地被一个或多个卤素原子或卤素取代; 或其合适的盐; 由含有通式（I）的化合物的混合物与一种或多种异构体或其二硝化类似物一起混合; 所述方法包括将所述混合物溶解在合适的结晶溶剂中并从所得结晶溶液中重结晶产物; 其特征在于结晶溶液含有不超过25％的通式（I）化合物的负载量，其中负载量定义为：式（I）的纯化合物的重量×100 /式（I）的纯化合物的重量+ 溶剂的重量，并且溶液冷却至结晶的温度不大于约30℃。

53. 发明申请

WO1995024186A1 SULFONAMIDE DERIVATIVES AND THEIR USE 审中-公开
标题翻译：磺酰胺衍生物及其用途
公开(公告)号：WO1995024186A1
公开(公告)日：1995-09-14
申请号：PCT/US1995003223
申请日：1995-03-10
申请人： PHARMACOPEIA, INC. , BALDWIN, John, J. , OHLMEYER, Michael, H., J. , HENDERSON, Ian
发明人： PHARMACOPEIA, INC.
IPC分类号： A61K31/095
CPC分类号： C07D285/125 , C07C205/59 , C07C311/16 , C07C311/39 , C07D211/22 , C07D211/46 , C07D211/62 , C07D307/68 , C07D333/38 , C07D401/12 , C07D401/14 , C40B40/00
摘要： Combinatorial libraries are disclosed which are represented by the formula (I): (T'-L)q- -C(O)-L'-II' wherein: is a solid support; T'-L- is an identifier residue; and -L'-II' is a ligand/linker residue. These libraries contain aryl sulfonamides, N-acyl derivatives, and N-substituted pyrrolidines and piperidines of the formula: Y-A-CO-R which are inhibitors of serine proteases and carbonic anhydrase isozymes. They are useful in the treatment of hyper-coagulation disease and ocular diseases such as glaucoma.
摘要翻译：公开了由式（I）表示的组合文库：（T'-L）q -C（O）-L'-II'其中：S是固体载体; T'-L-是标识符残基; 和-L'-II'是配体/接头残基。这些文库含有作为丝氨酸蛋白酶和碳酸酐酶同功酶抑制剂的芳基磺酰胺，N-酰基衍生物和N-取代的吡咯烷和下式的分子式为：Y-A-CO-R 1的哌啶。它们可用于治疗高凝血性疾病和眼部疾病如青光眼。

54. 发明申请

WO1994019315A1 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO1994019315A1
公开(公告)日：1994-09-01
申请号：PCT/SE1994000152
申请日：1994-02-22
申请人： AKTIEBOLAGET ASTRA , THE UNIVERSITY OF MARYLAND , BJÖRK, Susanna, Karin, Maria , GOTTHAMMAR, Kristina, Birgitta , LINDERBERG, Mats, Torbjörn , LUTHMAN, Per, Johan , PERSSON, Kerstin, Margareta, Irma , SCHWARCZ, Robert
发明人： AKTIEBOLAGET ASTRA , THE UNIVERSITY OF MARYLAND
IPC分类号： C07C229/64
CPC分类号： C07C205/59 , C07C205/26 , C07C205/37 , C07C229/64 , C07C229/70 , C07C255/59 , C07C2602/10
摘要： The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA, of general formula (I), wherein R and R are the same or different and selected from H and alkyl; X is selected from alkylthio, arylthio, aryloxy, halogen and cyano; R , R are the same or different and selected from halogen, methyl, fluoroalkyl, cyano and Z-R wherein Z is selected from CHn, NHm, O, S, SO2 and CO wherein n = 1 or 2; m = 0 or 1 and R is selected from alkyl, aryl and fluoroalkyl; or R and R together form a saturated or unsaturated ring system Y-V-Z wherein Y and Z, independently of each other, are as defined for Z above and V is selected from C1-C3 alkylene or alkenylene, -N = , -N = N- and (a), wherein R7 = H or alkyl; or a pharmaceutically acceptable salt thereof, methods and intermediates for their preparation, novel pharmaceutical compositions and the use thereof for inhibiting the enzyme 3-hydroxy-anthranilate oxygenase, 3-HAO, responsible for the production of the endogenous neurotoxin quinolinic acid, QUIN.
摘要翻译：本发明涉及通式（I）的3-羟基邻氨基苯甲酸3-HANA的新衍生物，其中R 1和R 2相同或不同并且选自H和烷基; X选自烷硫基，芳硫基，芳氧基，卤素和氰基; R 3，R 4相同或不同，并且选自卤素，甲基，氟烷基，氰基和ZR 5，其中Z选自CH n，NH m，O，S，SO 2和CO，其中n = 1或 2; m = 0或1，R 5选自烷基，芳基和氟烷基; 或R 3和R 4一起形成饱和或不饱和的环系YVZ，其中Y和Z彼此独立地如上述Z所定义，V选自C 1 -C 3亚烷基或亚烯基，-N = ，-N = N-和（a），其中R7 = H或烷基; 或其药学上可接受的盐，其制备方法和中间体，新型药物组合物及其用于抑制负责产生内源性神经毒素喹啉酸QUIN的3-羟基 - 邻氨基苯甲酸加氧酶3-HAO的用途。

55. 发明申请

WO1994002465A1 INHIBITORS OF c-AMP PHOSPHODIESTERASE AND TNF 审中-公开
标题翻译： c-AMP磷酸二酯酶和TNF的抑制剂
公开(公告)号：WO1994002465A1
公开(公告)日：1994-02-03
申请号：PCT/GB1993001597
申请日：1993-07-28
申请人： RHONE-POULENC RORER LIMITED , FENTON, Garry , MORLEY, Andrew, David , PALFREYMAN, Malcolm, Norman , RATCLIFFE, Andrew, James , SHARP, Brian, William , STUTTLE, Keith, Alfred, James , THURAIRATNAM, Sukanthini , VACHER, Bernard, Yvon, Jack
发明人： RHONE-POULENC RORER LIMITED
IPC分类号： C07D213/75
CPC分类号： C07D213/75 , C07C43/225 , C07C45/004 , C07C45/292 , C07C45/71 , C07C47/575 , C07C49/84 , C07C59/58 , C07C59/60 , C07C59/62 , C07C65/21 , C07C65/24 , C07C65/42 , C07C69/76 , C07C69/92 , C07C205/59 , C07C217/88 , C07C235/56 , C07C255/60 , C07C275/34 , C07C311/29 , C07C311/46 , C07C317/40 , C07C323/42 , C07C327/48 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07D213/50 , C07D213/89 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/03 , C07D409/12
摘要： This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
摘要翻译：本发明涉及通过各种连接与芳基部分连接的用于抑制肿瘤坏死因子的苯基化合物的药物用途。本发明还涉及含有这些化合物的化合物及其制备方法和药物组合物。此外，本发明涉及化合物抑制环AMP磷酸二酯酶的药物用途。

56. 发明申请

WO1992012953A1 CERTAIN 2-(2'METHYL-3',4'-TRISUBSTITUTED BENZOYL)-1,3-CYCLOHEXANEDIONES 审中-公开
标题翻译：某些2-（2'METHYL-3'，4'-取代苯甲酰基）-1,3-环己烷
公开(公告)号：WO1992012953A1
公开(公告)日：1992-08-06
申请号：PCT/US1991009541
申请日：1991-12-19
申请人： NGUYEN, Nhan, H.
IPC分类号： C07C49/84
CPC分类号： A01N41/10 , A01N39/00 , C07C49/84 , C07C65/03 , C07C65/21 , C07C205/45 , C07C205/59 , C07C317/46 , C07C323/62 , C07C2601/14
摘要： Herbicidal compounds of structural formula (I), wherein R1 is hydrogen or C¿1?-C4 alkyl; R?2¿ is hydrogen or C¿1?-C4 alkyl; R?3¿ is hydrogen or C¿1?-C4 alkyl; R4 is hydroxy, hydrogen or C1-C4 alkyl; or R?3 and R4¿ together are carbonyl (=O) with the proviso that R?1, R2, R5 and R6¿ are C¿1?-C4 alkyl; R?5¿ is hydrogen or C¿1?-C4 alkyl; R?6¿ is hydrogen, C¿1?-C4 alkyl, C1-C4 alkylthio, or C1-C4 alkylsulfonyl, with the proviso that when R?6 is C¿1-C4 alkylthio or C1-C4 alkylsulfonyl, then R3 and R4 are not together carbonyl; R7 is methyl or ethyl; and R8 is (1) halogen; (2) nitro; or (3) RbSOn- wherein n is the integer 0 or 2, and Rb is (a) C¿1?-C4 alkyl; and its salts.

57. 发明申请

WO1992007837A1 HETEROCYCLIC DIONE DERIVATIVES AS PESTICIDES AND PLANT GROWTH REGULATORS 审中-公开
标题翻译：作为杀虫剂和植物生长调节剂的杂环二氢衍生物
公开(公告)号：WO1992007837A1
公开(公告)日：1992-05-14
申请号：PCT/EP1991002014
申请日：1991-10-23
申请人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ-PATENT-GMBH , SANDOZ LTD.
发明人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ-PATENT-GMBH , SANDOZ LTD. , LEE, Shy-Fuh
IPC分类号： C07D265/02
CPC分类号： A01N43/72 , C07C205/59 , C07D265/02
摘要： The present invention concerns substituted 3,5-dioxo-3,4,5,6-tetrahydrooxazines as herbicides, processes and intermediates for their preparation, compositions containing them and their use as herbicides and acaricides.
摘要翻译：本发明涉及取代的3,5-二氧代-3,4,5,6-四氢恶嗪作为除草剂，其制备方法和中间体，含有它们的组合物及其作为除草剂和杀螨剂的用途。

58. 发明申请

WO1991015478A1 CROP-SELECTIVE HERBICIDAL SULFONAMIDES 审中-公开
标题翻译：选择性除草剂磺酰胺
公开(公告)号：WO1991015478A1
公开(公告)日：1991-10-17
申请号：PCT/US1991001075
申请日：1991-02-26
申请人： E.I. DU PONT DE NEMOURS AND COMPANY , MOON, Marcus, P.
发明人： E.I. DU PONT DE NEMOURS AND COMPANY
IPC分类号： C07D239/42
CPC分类号： C07D521/00 , A01N47/36 , C07C205/58 , C07C205/59 , C07C255/41 , C07C309/89 , C07C323/62 , C07F7/10
摘要： This invention relates to novel sulfonamides and their use as crop selective herbicides. Compounds of the instant invention have demonstrated excellent control of weeds coupled with corn safety.
摘要翻译：本发明涉及新型磺酰胺及其作为作物选择性除草剂的用途。本发明的化合物已经显示了对玉米和玉米安全性的良好控制。

59. 发明申请

WO1990005712A1 CERTAIN 2-(2',3',4'-TRISUBSTITUTED BENZOYL)-1,3-CYCLOHEXANEDIONES 审中-公开
标题翻译：某些2-（2'，3'，4'-三唑基苯甲酰基）-1,3-环己烷
公开(公告)号：WO1990005712A1
公开(公告)日：1990-05-31
申请号：PCT/US1989005056
申请日：1989-11-17
申请人： ICI AMERICAS INC.
发明人： ICI AMERICAS INC. , MICHAELY, William, J.
IPC分类号： C07C49/84
CPC分类号： A01N39/00 , A01N41/10 , C07C39/26 , C07C49/84 , C07C65/03 , C07C205/45 , C07C205/59 , C07C317/24 , C07C2601/14
摘要： Herbicidal compounds of structural formula (I), wherein X is oxygen or sulfur; R is chlorine or bromine; R1 is hydrogen or C¿1?-C4 alkyl; R?2¿ is hydrogen or C¿1?-C4 alkyl; R?3¿ is hydrogen or C¿1?-C4 alkyl; R?4¿ is hydroxy, hydrogen or C¿1?-C4 alkyl; or R?3 and R4¿ together are carbonyl (=O) with the proviso that R?1, R2, R5 and R6¿ are all C¿1?-C4 alkyl; R?5¿ is hydrogen or C¿1?-C4 alkyl; R?6¿ is hydrogen, C¿1?-C4 alkyl, C1-C4 alkylthio, or C1-C4 alkylsulfonyl, with the proviso that when R?6 is C¿1-C4 alkylthio or C1-C4 alkylsulfonyl, then R?3 and R4¿ are not together carbonyl; R7 is methyl or ethyl; and R8 is (1) halogen; (2) nitro; or (3) RbSOn-wherein n is the integer 0 or 2; and Rb is (a) C¿1?-C3 alkyl; and their salts.

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