公开(公告)号：EP1292308B1

公开(公告)日：2010-06-09

申请号：EP01925013.3

申请日：2001-04-13

Applicant: Temple University - Of The Commonwealth System of Higher Education

Inventor： REDDY, E., Premkumar ,  REDDY, M., V., Ramana

IPC: A61K31/495 ,  A61K31/435 ,  A61K31/40 ,  A61K31/385 ,  A61K31/275 ,  C07D241/04

CPC classification number: C07D207/333 ,  C07C317/10 ,  C07D213/34 ,  C07D277/36 ,  C07D307/10 ,  C07D333/18 ,  C07D333/42 ,  C07D333/48

Abstract: Sulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents:wherein:Q1 is selected from the group consisting of(a) a phenyl radical according to formula II whereinR1, R2, R3, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, amino, C1-C6 trifluoroalkoxy and trifluoromethyl;(b) an aromatic radical selected from the group consisting of 1-naphthyl, 2-naphthyl and 9-anthryl; and(c) an aromatic radical according to formula III whereinn1 is 1 or 2,Y1 and Y2 are independently selected from the group consisting of hydrogen, halogen, and nitro, andX1 is selected from the group consisting of oxygen, nitrogen, sulfur andandQ2 is selected from the group consisting of(d) a phenyl radical according to formula II, as defined above;(e) an aromatic radical selected from the group consisting of 1-naphthyl, 2-naphthyl and 9-anthryl;(f) an aromatic radical according to formula IV whereinn1 is 1 or 2,Y3 and Y4 are independently selected from the group consisting of hydrogen, halogen, and nitro, andX2, X3 and X4 are independently selected from the group consisting of carbon, oxygen, nitrogen, sulfur and provided that not all of X2, X3 and X4 may be carbon; and(g) 1-piperazinyl;provided that at least one of Q1 or Q2 is other than a phenyl radical according to formula II;or a pharmaceutically acceptable salt thereof.Sulfones of formula V are also useful as antiproliferative agents, including, for example, anticancer agents:wherein:X is sulfur or oxygen; Ya and Yb are independently selected from the group consisting of hydrogen, halogen, and nitro; and R1-R5 are defined as above;or a pharmaceutically acceptable salt thereof.

公开(公告)号：EP1633336A4

公开(公告)日：2008-10-29

申请号：EP04752597

申请日：2004-05-19

Applicant: IRM LLC

Inventor： PAN SHIFENG ,  GAO WENQI ,  GRAY NATHANAEL S ,  MI YUAN ,  FAN YI

IPC: C07D211/28 ,  A61K20060101 ,  A61K31/135 ,  A61K31/195 ,  A61K31/41 ,  A61K31/66 ,  C07F9/28

CPC classification number: C07D205/04 ,  C07C251/48 ,  C07C251/52 ,  C07C251/54 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/16 ,  C07D211/60 ,  C07D213/30 ,  C07D213/53 ,  C07D213/61 ,  C07D217/04 ,  C07D295/06 ,  C07D307/10 ,  C07D307/12 ,  C07D307/52 ,  C07D333/12 ,  C07D333/16 ,  C07D333/22

公开(公告)号：EP1466898A1

公开(公告)日：2004-10-13

申请号：EP02790937.3

申请日：2002-12-27

Applicant: DAIICHI PHARMACEUTICAL CO., LTD.

Inventor： YASUKOUCHI,T. ,  ITO, Masayuki ,  KUBOTA, Hideki ,  MIYAUCHI, Satoru ,  SAITO, Masanori

IPC: C07C317/14 ,  C07C317/18 ,  C07C317/24 ,  C07C317/28 ,  C07C317/44 ,  C07C323/09 ,  C07C323/65 ,  C07F7/18 ,  A61K31/10 ,  A61K31/12 ,  A61K31/192 ,  A61K31/216 ,  A61K31/235 ,  A61K31/255 ,  A61K31/27

CPC classification number: C07D213/34 ,  C07D207/325 ,  C07D211/24 ,  C07D211/54 ,  C07D213/61 ,  C07D213/65 ,  C07D213/71 ,  C07D213/74 ,  C07D213/82 ,  C07D215/12 ,  C07D215/36 ,  C07D233/64 ,  C07D233/68 ,  C07D233/84 ,  C07D235/06 ,  C07D235/28 ,  C07D239/26 ,  C07D239/38 ,  C07D257/04 ,  C07D263/22 ,  C07D263/32 ,  C07D277/26 ,  C07D277/36 ,  C07D277/76 ,  C07D295/096 ,  C07D307/10 ,  C07D307/38 ,  C07D309/08 ,  C07D311/56 ,  C07D333/18 ,  C07D335/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06

Abstract: Provided are novel compounds having an inhibitory activity against production or secretion of β-amyloid protein. They embrace compounds represented by the following formula (1):
and capable of being replaced with a variety of substituents; and salts thereof, and solvates of any one of them.

Abstract translation: 提供了具有抑制β-淀粉样蛋白生成或分泌活性的新化合物。 它们包括由下式（1）表示的化合物：并且能够被各种取代基取代; 及其盐，以及它们中任何一种的溶剂合物。

公开(公告)号：EP0874809B1

公开(公告)日：2003-08-27

申请号：EP96944684.8

申请日：1996-12-19

Applicant: SmithKline Beecham plc

Inventor： HINKS, Jeremy, David c/o GlaxoSmithKline ,  TAKLE, Andrew, Kenneth ,  HUNT, Eric

IPC: C07C271/36 ,  C07C271/64 ,  A61K31/325 ,  A61K31/33

CPC classification number: C07D203/08 ,  C07C271/32 ,  C07C271/36 ,  C07C271/64 ,  C07C271/66 ,  C07C281/02 ,  C07C307/06 ,  C07C311/08 ,  C07C311/39 ,  C07C311/53 ,  C07C317/44 ,  C07C323/60 ,  C07C331/14 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2603/82 ,  C07D203/20 ,  C07D207/16 ,  C07D209/08 ,  C07D211/62 ,  C07D213/40 ,  C07D213/70 ,  C07D213/75 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D231/14 ,  C07D239/38 ,  C07D241/24 ,  C07D249/04 ,  C07D249/10 ,  C07D257/04 ,  C07D261/18 ,  C07D271/113 ,  C07D277/36 ,  C07D277/80 ,  C07D285/06 ,  C07D285/125 ,  C07D295/088 ,  C07D295/205 ,  C07D295/215 ,  C07D307/10 ,  C07D307/66 ,  C07D307/68 ,  C07D317/66 ,  C07D333/34 ,  C07D333/38 ,  C07D401/06 ,  C07D417/06 ,  C07D451/02 ,  C07D453/02 ,  C07D455/02 ,  C07D471/08 ,  C07D487/08 ,  C07D513/04 ,  C07H15/24

公开(公告)号：EP1292308A1

公开(公告)日：2003-03-19

申请号：EP01925013.3

申请日：2001-04-13

Applicant: Temple University of the CommonwealthSystem of Higher Education

Inventor： REDDY, E., Premkumar ,  REDDY, M., V., Ramana

IPC: A61K31/495 ,  A61K31/435 ,  A61K31/40 ,  A61K31/385 ,  A61K31/275 ,  C07D241/04

CPC classification number: C07D207/333 ,  C07C317/10 ,  C07D213/34 ,  C07D277/36 ,  C07D307/10 ,  C07D333/18 ,  C07D333/42 ,  C07D333/48

Abstract: Sulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents:wherein:Q1 is selected from the group consisting of(a) a phenyl radical according to formula II whereinR1, R2, R3, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, amino, C1-C6 trifluoroalkoxy and trifluoromethyl;(b) an aromatic radical selected from the group consisting of 1-naphthyl, 2-naphthyl and 9-anthryl; and(c) an aromatic radical according to formula III whereinn1 is 1 or 2,Y1 and Y2 are independently selected from the group consisting of hydrogen, halogen, and nitro, andX1 is selected from the group consisting of oxygen, nitrogen, sulfur andandQ2 is selected from the group consisting of(d) a phenyl radical according to formula II, as defined above;(e) an aromatic radical selected from the group consisting of 1-naphthyl, 2-naphthyl and 9-anthryl;(f) an aromatic radical according to formula IV whereinn1 is 1 or 2,Y3 and Y4 are independently selected from the group consisting of hydrogen, halogen, and nitro, andX2, X3 and X4 are independently selected from the group consisting of carbon, oxygen, nitrogen, sulfur and provided that not all of X2, X3 and X4 may be carbon; and(g) 1-piperazinyl;provided that at least one of Q1 or Q2 is other than a phenyl radical according to formula II;or a pharmaceutically acceptable salt thereof.Sulfones of formula V are also useful as antiproliferative agents, including, for example, anticancer agents:wherein:X is sulfur or oxygen; Ya and Yb are independently selected from the group consisting of hydrogen, halogen, and nitro; and R1-R5 are defined as above;or a pharmaceutically acceptable salt thereof.

公开(公告)号：EP1020439A1

公开(公告)日：2000-07-19

申请号：EP98901574.8

申请日：1998-02-10

Applicant: Japan Tobacco Inc.

Inventor： SHINKAI, Hisashi, Central Pharmaceutical Res. Inst ,  MAEDA, Kimiya, Central Pharmaceutical Res. Inst. ,  OKAMOTO, Hiroshi, Central Pharmaceutical Res. Inst

IPC: C07C323/40 ,  C07C323/63 ,  C07C323/65 ,  C07D207/16 ,  C07D207/28 ,  C07D211/62 ,  C07D213/81 ,  C07D307/68 ,  C07D333/38 ,  A61K31/165 ,  A61K31/18 ,  A61K31/255 ,  A61K31/34 ,  A61K31/38 ,  A61K31/40 ,  A61K31/44

CPC classification number: C07D307/10 ,  A61K31/164 ,  A61K31/18 ,  A61K31/33 ,  A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/435 ,  A61K31/44 ,  C07C311/14 ,  C07C311/15 ,  C07C311/21 ,  C07C323/40 ,  C07C323/41 ,  C07C323/42 ,  C07C327/30 ,  C07C329/10 ,  C07C329/20 ,  C07C333/04 ,  C07C333/08 ,  C07C333/10 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/08 ,  C07C2602/22 ,  C07C2602/28 ,  C07C2603/74 ,  C07D211/34 ,  C07D213/80 ,  C07D213/81 ,  C07D307/68 ,  C07D333/38 ,  Y02P20/55

Abstract: The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I):
wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X 1 , X 2 , X 3 , and X 4 may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents -CO- or -SO 2 -, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof. The compounds represented by the formula (I) can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity and, therefore, is expected to be useful as a new type of a preventive or therapeutic agent for atherosclerosis or hyperlipidemia.

Abstract translation: 本发明提供一种CETP活性抑制剂，其包含作为活性成分的由式（I）表示的化合物：其中R表示直链或支链烷基; 直链或支链烯基; 低级卤代烷基; 取代或未取代的环烷基; 取代或未取代的环烯基; 取代或未取代的环烷基烷基; 取代或未取代的芳基或取代或未取代的杂环基可以相同或不同，表示氢原子，卤素原子，低级烷基，低级卤代烷基; 低级烷氧基; 氰基; 硝基; 酰基; 或芳基，Y表示-CO-或-SO 2 - ，Z表示氢原子或巯基保护基，或前药化合物，其药学上可接受的盐或水合物或溶剂化物。 由式（I）表示的化合物可以增加HDL，同时通过选择性抑制CETP活性降低LDL，因此预期可用作动脉粥样硬化或高脂血症的新型预防或治疗剂。

公开(公告)号：EP0749421A1

公开(公告)日：1996-12-27

申请号：EP95911960.0

申请日：1995-02-24

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： TUNG, Roger, Dennis ,  SALITURO, Francesco, Gerald ,  DEININGER, David, D. ,  MURCKO, Mark, Andrew ,  NOVAK, Perry, Michael ,  BHISETTI, Govinda, Rao

IPC: A61K31 ,  A61P31 ,  A61P43 ,  C07C311 ,  C07D211 ,  C07D213 ,  C07D217 ,  C07D231 ,  C07D233 ,  C07D235 ,  C07D241 ,  C07D249 ,  C07D261 ,  C07D263 ,  C07D277 ,  C07D307 ,  C07D309 ,  C07D317 ,  C07D319 ,  C07D333 ,  C07D335 ,  C07D401 ,  C07D487 ,  C07D493 ,  C07D521

CPC classification number: C07D213/30 ,  C07C311/29 ,  C07C311/41 ,  C07C2601/08 ,  C07D211/60 ,  C07D213/70 ,  C07D213/81 ,  C07D213/82 ,  C07D217/24 ,  C07D217/26 ,  C07D231/38 ,  C07D233/54 ,  C07D233/64 ,  C07D233/76 ,  C07D233/84 ,  C07D233/88 ,  C07D233/90 ,  C07D235/06 ,  C07D235/28 ,  C07D241/04 ,  C07D249/18 ,  C07D261/08 ,  C07D263/22 ,  C07D263/32 ,  C07D263/56 ,  C07D263/58 ,  C07D277/06 ,  C07D277/26 ,  C07D277/36 ,  C07D277/46 ,  C07D307/10 ,  C07D307/20 ,  C07D309/08 ,  C07D309/10 ,  C07D317/18 ,  C07D317/34 ,  C07D319/06 ,  C07D333/36 ,  C07D333/38 ,  C07D333/48 ,  C07D335/02 ,  C07D401/06 ,  C07D493/04

Abstract: This invention relates to a novel class of sulfonamides that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.

Abstract translation: PCT No.PCT / US95 / 02420 Sec。 371日期：1996年4月1日 102（e）日期1996年4月1日PCT提交1995年2月24日PCT公布。 WO95 / 24385 PCT公开号 日期1995年9月14日本发明提供了一类新颖的式I的磺酰胺化合物，它们是天冬氨酰蛋白酶抑制剂：本发明还提供包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制HIV-1和HIV-2蛋白酶活性，因此可有利地用作针对HIV-1和HIV-2病毒的抗病毒剂。 本发明还提供了使用本发明的化合物和组合物来抑制天冬氨酰蛋白酶活性的方法和用于治疗病毒感染的方法。

公开(公告)号：EP0163533A3

公开(公告)日：1986-12-30

申请号：EP85303797

申请日：1985-05-30

Applicant: MONTEFLUOS S.P.A.

Inventor： FONTANA, ALBERTO ,  MODENA, SILVANA ,  MOGGI, GIOVANNI

IPC: C07B31/00 ,  C07B37/02 ,  C07C27/00 ,  C07C29/44 ,  C07C31/34 ,  C07C41/00 ,  C07C41/30 ,  C07C43/12 ,  C07C67/00 ,  C07C67/347 ,  C07C69/14 ,  C07D307/10 ,  C07D319/12 ,  C07C41/18 ,  C07C67/28 ,  C07C69/63 ,  C07D319/10

CPC classification number: C07D307/10 ,  C07C29/44 ,  C07C41/01 ,  C07C41/30 ,  C07C43/12 ,  C07C67/293 ,  C07D319/12 ,  C07C31/34 ,  C07C69/63

公开(公告)号：EP0090516A1

公开(公告)日：1983-10-05

申请号：EP83301224.8

申请日：1983-03-08

Applicant: PFIZER INC.

Inventor： Eggler, James Frederick ,  Johnson, Michael Ross ,  Melvin, Lawrence Sherman

IPC: C07D471/04 ,  A61K31/47 ,  C07D455/04 ,  C07D491/147 ,  C07C49/755 ,  C07C69/675 ,  C07D311/92 ,  C07C93/26 ,  C07C103/42

CPC classification number: C07D207/08 ,  C07C33/20 ,  C07C205/33 ,  C07C309/00 ,  C07C2603/26 ,  C07D211/34 ,  C07D307/10 ,  C07D307/16 ,  C07D309/04 ,  C07D311/78 ,  C07D455/04 ,  C07D471/04

Abstract: Tricyclic benzo fused compounds of the formula
and pharmaceutically acceptable cationic and acid addition salts thereof, wherein n is zero, 1 or 2, and t is 1 or 2; M is CH or N, R 1 is H or certain acyl groups; Q is CO 2 R 4 , COR S , C(OR 7 )R 5 R 6 , CN, CONR 9 R 10 , CH 2 NR 9 R 10 , CH 2 NHCOR 11 , CH 2 NHSO 2 R 12 , 5-tetrazolyl or when n is 1, Q and OR 1 together form a lactone or certain reduced derivatives thereof; and Z is certain alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl groups, are valuable central nervous system active agents, methods for their use, pharmaceutical compositions containing them and certain intermediates therefor.

Abstract translation: 式（I）的三环苯并稠合化合物及其药学上可接受的阳离子和酸加成盐，其中n为0,1或2，t为1或2; M是CH或N，R 1是H或某些酰基; Q是CO2R4，COR5，C（OR7）R5R6，CN，CONR9R10，CH2NR9R10，CH2NHCOR11，CH2NHSO2R12，5-四唑基或当n为1时，Q和OR1一起形成内酯或其某些还原的衍生物; Z是某些烷基，烷氧基，烷氧基烷基，芳烷基，芳烷氧基，芳氧基烷基或芳烷氧基烷基，是有价值的中枢神经系统活性剂，其使用方法，含有它们的药物组合物及其某些中间体。

公开(公告)号：EP2802561B1

公开(公告)日：2017-07-26

申请号：EP13700279.6

申请日：2013-01-08

Applicant: Studiengesellschaft Kohle mbH

Inventor： LIST, Benjamin ,  CORIC, Ilija ,  VELLALATH, Sreekumar

IPC: C07C317/14 ,  C07C409/44

CPC classification number: C07F9/65746 ,  B01J31/0264 ,  B01J31/0271 ,  B01J2231/52 ,  B01J2231/70 ,  C07C231/06 ,  C07D209/08 ,  C07D209/12 ,  C07D239/90 ,  C07D307/10 ,  C07D307/20 ,  C07D319/08 ,  C07D327/06 ,  C07D339/08 ,  C07D493/10 ,  C07F9/657154 ,  C07F9/65744 ,  C07C233/05

Abstract: The invention relates to chiral imidodiphosphates and derivatives thereof having the general formula I, The compounds are suitable as chiral Brønsted acid catalysts, phase-transfer catalysts, chiral anions for organic salts, metal salts or metal complexes for catalysis.

Abstract translation: 本发明涉及具有通式I的手性亚氨基二磷酸酯及其衍生物，所述化合物适合作为手性布朗斯台德酸催化剂，相转移催化剂，用于有机盐的手性阴离子，用于催化的金属盐或金属络合物。