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1. 发明授权

EP1175383B1 GLUCOCORTICOID RECEPTOR MODULATORS 有权
标题翻译：糖皮质激素受体调节剂
公开(公告)号：EP1175383B1
公开(公告)日：2018-03-14
申请号：EP00911172.5
申请日：2000-03-27
申请人： Pfizer Products Inc.
发明人： DOW, Robert, Lee , LIU, Kevin, Kun-Chin , MORGAN, Bradley, Paul , SWICK, Andrew, Gordon
IPC分类号： C07C35/42 , A61K31/05 , A61K31/122 , A61K31/325 , A61K31/4402 , A61K31/4406 , A61K31/4409 , C07C49/675 , C07C271/44 , C07D213/40 , C07D213/30 , C07D213/75 , C07D241/18 , C07D241/20 , C07D295/12
CPC分类号： C07D455/06 , C07C49/747 , C07C49/755 , C07C69/76 , C07C215/74 , C07C235/66 , C07C251/44 , C07C251/52 , C07C251/60 , C07C255/53 , C07C255/54 , C07C271/44 , C07C271/52 , C07C281/04 , C07C307/02 , C07C309/65 , C07C309/66 , C07C309/73 , C07C311/04 , C07C311/08 , C07C311/51 , C07C317/18 , C07C333/04 , C07C2603/00 , C07C2603/26 , C07D207/09 , C07D211/46 , C07D213/22 , C07D213/30 , C07D213/40 , C07D213/75 , C07D231/40 , C07D231/56 , C07D239/34 , C07D241/18 , C07D241/20 , C07D249/08 , C07D249/14 , C07D257/04 , C07D271/06 , C07D271/07 , C07D277/24 , C07D277/28 , C07D277/56 , C07D295/088 , C07D295/13 , C07D295/185 , C07D295/205 , C07D303/14 , C07D317/36 , C07D333/16 , C07D413/04
摘要： The present invention provides non-steroidal compounds of formula I which are selective modulators (i.e., agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides intermediates and processes for preparing these compounds.

2. 发明授权

EP1598332B1 Indanones and carbamates, and their use in the preparation of anthropodicidal oxadiazines 失效
标题翻译： Indanone und Carbamat，und ihre Verwendung in der Herstellung von arthropoziden Oxadiazinen
公开(公告)号：EP1598332B1
公开(公告)日：2007-10-24
申请号：EP05014510.1
申请日：1995-04-17
申请人： E.I. DU PONT DE NEMOURS AND COMPANY
发明人： Annis, Gary David , Shapiro, Rafael , Mccann, Stephen Frederick
IPC分类号： C07C69/757 , C07B53/00 , C07D273/04 , C07C65/21 , C07C281/04 , C07C63/68 , C07C69/76 , C07C69/92 , C07C271/66 , C07C271/28 , C07C269/06
CPC分类号： C07D273/04 , C07B2200/07 , C07C63/68 , C07C65/21 , C07C69/757 , C07C69/76 , C07C69/92 , C07C271/66 , C07C281/04 , C07C2602/08

3. 发明授权

EP0900210B1 ANTIVIRALLY ACTIVE HETEROCYCLIC AZAHEXANE DERIVATIVES 失效
标题翻译：具有抗病毒作用杂环衍生物azahexane
公开(公告)号：EP0900210B1
公开(公告)日：2005-02-09
申请号：EP97919355.4
申请日：1997-04-14
申请人： Novartis AG , Novartis Pharma GmbH
发明人： FÄSSLER, Alexander , BOLD, Guido , CAPRARO, Hans-Georg , LANG, Marc , KHANNA, Satish, Chandra
IPC分类号： C07D277/28 , C07D257/04 , C07D213/42 , C07D333/20 , C07D241/12 , A61K31/425 , A61K31/44 , A61K31/395 , A61K31/495 , C07C271/22 , C07D303/36
CPC分类号： C07D213/42 , C07C271/22 , C07C281/02 , C07C281/04 , C07D241/12 , C07D257/04 , C07D277/28 , C07D333/20 , Y02P20/55
摘要： There are described compounds of formula (I*) wherein R1 is lower alkoxycarbonyl, R2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, R3 is phenyl that is unsubsituted or substituted by one or more lower alkoxy radicals, or C4-C8cycloalkyl, R4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (-SO-) and sulfonyl (-SO2-) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl, R5, independently of R2, has one of the meanings mentioned for R2, and R6, independently of R1, is lower alkoxycarbonyl, or salts thereof, provided that at least one salt-forming group is present. The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS. They exhibit outstanding pharmacodynamic properties.

4. 发明授权

EP0933346B1 NOVEL p-TERPHENYL COMPOUNDS 失效
标题翻译：新的对三联苯CONNECTIONS
公开(公告)号：EP0933346B1
公开(公告)日：2003-12-10
申请号：EP97933837.3
申请日：1997-07-30
申请人： SHIONOGI & CO., LTD.
发明人： KAWADA, Kenji , OHTANI, Mitsuaki , SUZUKI, Ryuji , ARIMURA, Akinori
IPC分类号： C07C15/14 , C07C25/18 , C07C43/20 , C07C47/575 , C07C65/24 , C07C69/734 , C07C69/78 , C07C205/38 , C07C217/80 , C07C233/80 , C07C235/46
CPC分类号： C07D213/30 , C07C15/14 , C07C43/225 , C07C43/23 , C07C43/253 , C07C43/315 , C07C45/68 , C07C47/57 , C07C47/575 , C07C59/64 , C07C59/70 , C07C65/24 , C07C65/28 , C07C69/712 , C07C69/734 , C07C69/94 , C07C205/35 , C07C205/37 , C07C217/20 , C07C217/76 , C07C217/80 , C07C229/52 , C07C233/25 , C07C233/27 , C07C233/80 , C07C235/60 , C07C251/38 , C07C251/60 , C07C255/54 , C07C271/28 , C07C275/32 , C07C281/04 , C07C281/10 , C07C307/10 , C07C309/65 , C07C309/66 , C07C309/73 , C07C311/08 , C07C311/21 , C07C311/29 , C07C317/22 , C07C327/42 , C07D215/14 , C07D239/54 , C07D295/30 , C07D307/42 , C07D309/22 , C07D317/54 , C07D319/20 , C07D333/28 , C07D333/38 , C07D333/54 , C09K2019/123
摘要： Selective IgE production inhibitors which contain substances inhibiting the production of IgE in the process of the differentiation of matured B cells into antibody-producing cells and the production of the antibody thereby while not or scarcely inhibiting the production of IgG, IgM and/or IgA to be produced simultaneously with IgE; compounds represented by general formula (I); a process for producing the same; and drugs containing the same. In said formula R to R represent each hydrogen, halogeno, lower alkyl, lower alkoxy, etc.; X represents O-, -CH2-, -NR - or -S(O)p-; and Y represents lower alkyl or lower alkenyl.

5. 发明公开

EP1335908A2 PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA AGONISTS 有权
标题翻译：过氧化物酶体增殖物激活受体α激动剂
公开(公告)号：EP1335908A2
公开(公告)日：2003-08-20
申请号：EP01989704.0
申请日：2001-11-09
申请人： ELI LILLY AND COMPANY
发明人： MANTLO, Nathan, Bryan , COLLADO CANO, Ivan , DOMINIANNI, Samuel, James , ETGEN, Garret, Jay, Junior , GARCIA-PAREDES, Cristina , JOHNSTON, Richard, Duane , LETOURNEAU, Michael, Edward , MARTINELLI, Michael, John , MAYHUGH, Daniel, Ray , SAEED, Ashraf , THOMPSON, Richard, Craig , WANG, Xiadong , COFFEY, David, Scott , SCHMID, Christopher, Randall , VICENZI, Jeffrey, Thomas , XU, Yanping
IPC分类号： C07D249/12 , A61K31/4196 , C07D401/06 , C07D413/06 , C07D409/06 , C07D409/12 , C07D417/12 , C07D405/06 , A61K31/4439 , A61K31/427 , C07C257/22 , C07C281/04 , C07C281/06
CPC分类号： C07C281/06 , C07C257/22 , C07C281/04 , C07D249/12 , C07D401/06 , C07D405/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/12
摘要： he present invention is directed to compounds represented by the following structural formula (I'), and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy. Additionally, R4 is H, halo, a substituted or unsubstituted group selected from C1-C5 alkyl, C1-C5 alkoxy, C3-C6 cycloalkyl, arylC0-C4alkyl and phenyl, or R3 and R4 are combined to form a C3-C4 cycloalkyl.

6. 发明公开

EP1172357A1 Verfahren zur Herstellung von Hydrazincarbonsäureestern und Zwischenprodukte dieses Verfahrens 失效
标题翻译：一种用于制备这种方法的Hydrazincarbonsäureestern和中间产物的方法
公开(公告)号：EP1172357A1
公开(公告)日：2002-01-16
申请号：EP01126454.6
申请日：1996-01-31
申请人： BAYER AG
发明人： Wroblowsky, Hans-Jürgen, Dr.
IPC分类号： C07C281/04 , C07C281/02
CPC分类号： C07C281/02 , C07C281/04 , C07D249/12
摘要： Die vorliegende Erfindung betrifft ein Verfahren zur Herstellung von Hydrazincarbonsäureestern der allgemeinen Formel (II)
in welcher R, R 1 , R 2 die in der Beschreibung angegebene Bedeutung haben,
dadurch gekennzeichnet, dass man entsprechende Hydrazincarbonsäureester der allgemeinen Formel (III)
in welcher R und R 1 die in der Beschreibung angegebenen Bedeutungen haben, mit Aminoverbindungen der allgemeinen Formel (IV)

H 2 N-R 2 (IV)

in welcher R 2 die in der Beschreibung angegebene Bedeutung hat,
gegebenenfalls in Gegenwart eines Säureakzeptors und gegebenenfalls in Gegenwart eines Verdünnungsmittels bei Temperaturen zwischen 0°C und 100°C umsetzt. Die Erfindung betrifft ebenfalls die Zwischenprodukte der Formel (III) und Verfahren zu deren Herstellung.
摘要翻译： Aminoalkylidene - 肼羧酸酯是通过与氨基化合物一氯substituiertem肼羧酸酯的反应来制备。式（I）的aminoalkylidene - 肼羧酸酯的生产方法包括用式chloroalkylidene - 肼羧酸酯的反应（II）在式氨基化合物（III）任选地在酸接受体存在下，在0稀释剂 -100度C. R =烷基或芳基（各自任选substituiertem）; [R <1> =卤代烷基; [R <2> = H; OH; NH2; 或烷基，烯基，炔基，烷氧基，单或二烷基氨基，环烷基，环烷基烷基，苯基或苯基（其各自任选substituiertem）。因此独立权利要求中包括了：（A）chloroalkylidene - 肼羧酸酯（II）是新的; 和（B）化合物的制备（II），其包括卤代乙酰肼羧酸酯（IV）与磺酰氯任选地在酸接受体和稀释剂存在的反应在0-100℃下

7. 发明公开

EP0900210A1 ANTIVIRALLY ACTIVE HETEROCYCLIC AZAHEXANE DERIVATIVES 失效
标题翻译：具有抗病毒作用杂环衍生物azahexane
公开(公告)号：EP0900210A1
公开(公告)日：1999-03-10
申请号：EP97919355.0
申请日：1997-04-14
申请人： Novartis AG
发明人： FÄSSLER, Alexander , BOLD, Guido , CAPRARO, Hans-Georg , LANG, Marc , KHANNA, Satish, Chandra
IPC分类号： A61K31 , A61P31 , C07C271 , C07C281 , C07D213 , C07D241 , C07D257 , C07D277 , C07D303 , C07D333
CPC分类号： C07D213/42 , C07C271/22 , C07C281/02 , C07C281/04 , C07D241/12 , C07D257/04 , C07D277/28 , C07D333/20 , Y02P20/55
摘要： There are described compounds of formula (I*) wherein R1 is lower alkoxycarbonyl, R2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, R3 is phenyl that is unsubsituted or substituted by one or more lower alkoxy radicals, or C4-C8cycloalkyl, R4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (-SO-) and sulfonyl (-SO2-) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl, R5, independently of R2, has one of the meanings mentioned for R2, and R6, independently of R1, is lower alkoxycarbonyl, or salts thereof, provided that at least one salt-forming group is present. The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS. They exhibit outstanding pharmacodynamic properties.

8. 发明授权

EP0468727B1 Process for producing hydrazone derivative 失效
标题翻译：一种用于生产腙衍生物的过程。
公开(公告)号：EP0468727B1
公开(公告)日：1994-12-28
申请号：EP91306663.5
申请日：1991-07-22
申请人： KUREHA CHEMICAL INDUSTRY CO., LTD.
发明人： Ishizuka, Makoto , Wakasugi, Takashi
IPC分类号： C07C281/04
CPC分类号： C07C281/04

9. 发明授权

EP0726258B1 Verfahren und neue Zwischenprodukte zur Herstellung von Triazolinonen 失效
标题翻译：方法和新的中间体的三唑酮的制备
公开(公告)号：EP0726258B1
公开(公告)日：2002-05-29
申请号：EP96101303.4
申请日：1996-01-31
申请人： BAYER AG
发明人： Wroblowsky, Heinz-Jürgen
IPC分类号： C07D249/12 , C07C281/02 , C07C281/04
CPC分类号： C07C281/02 , C07C281/04 , C07D249/12

10. 发明公开

EP1187817A1 CATHECOL HYDRAZONE DERIVATIVES, PROCESS FOR PREPARING THE SAME AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 有权
标题翻译： KATECHOLHYDRAZON衍生物，PROCESS FOR THEIR和药物组合物含有它们的
公开(公告)号：EP1187817A1
公开(公告)日：2002-03-20
申请号：EP99922643.4
申请日：1999-05-28
申请人： Cheil Jedang Corporation
发明人： YOUN, Yong, SikPungrym Apartment 107-205 , XIANG, Myung, Xik , SUH, Byoung, Chol , KIM, Jong, Hoon , LEE, Kwang, HyukHwasung Villa , KIM, Eui, KyungKachimaeul Apt. 1007-1212 , SHIN, Jae, Kyu , RHEE, Chung, Keun
IPC分类号： C07D239/42 , A61K31/15 , C07C251/86 , C07C281/04 , C07C281/14 , C07C337/08 , C07D213/18 , C07D215/42 , C07D233/52 , C07D295/28
CPC分类号： C07D213/77 , C07C251/86 , C07C281/04 , C07C281/14 , C07C281/18 , C07C337/08 , C07C2601/08 , C07D213/81 , C07D215/42 , C07D233/88 , C07D239/42 , C07D295/30
摘要： The present invention provides novel cathecol hydrazone derivatives of formula (I) or pharmaceutically acceptable salts thereof, wherein R1 is C¿1-7? alkyl or C3-7 cycloalkyl; R?2¿ is hydrogen, hydroxy, C¿1-5? alkyl or -CH2CH2C(=O)NH2; R?3 and R4¿ are independently hydrogen, C¿1-7? alkyl, -C(=X)-R?5¿, or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one or two selected from a group consisting of halogen, C¿1-6? alkoxy, nitro, trifluoromethyl, C1-6 alkyl and carboxyl, or R?3 and R4¿ are directly bonded by C¿3-4? containing oxygen, sulfur or nitrogen to form a heterocyclic ring, X is oxygen, sulfur or NH and R?5¿ is C¿1-7? alkyl, -NHR?6¿, CONH¿2? or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one selected from a group consisting of halogen, C1-6 alkoxy, nitrile, trifluoromethyl, C1-6 alkyl and carboxyl, and R?6¿ is hydrogen, hydroxy, NH¿2?, C1-5 alkoxy, C1-5 alkyl, pyridyl or phenyl.

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