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1. 发明公开

EP0595989A1 NOVEL BENZOPYRIDO PIPERYLIDENE COMPOUNDS, COMPOSITIONS, METHODS OF MANUFACTURE AND METHODS OF USE 失效
标题翻译： BENZOPYRIDO哌啶基化合物作为PAF拮抗剂。
公开(公告)号：EP0595989A1
公开(公告)日：1994-05-11
申请号：EP92916482.0
申请日：1992-07-17
申请人： SCHERING CORPORATION
发明人： WONG, Jesse, K. , PIWINSKI, John, J. , GREEN, Michael, J.
IPC分类号： A61K31 , A61P11 , A61P29 , A61P37 , C07D491 , C07D495
CPC分类号： C07D491/04 , C07D495/04
摘要： On décrit un composé de formule I, ou un sel ou un solvate pharmaceutiquement acceptable dudit composé, formule dans laquelle: R est sélectionné dans le groupe comprenant: H, Cl, Br, F et I; T représente C ou N, la ligne pointillée liée à T représentant une liaison double lorsque T représente C, absente lorsque T représente N; et X représente O ou bien S à condition que T représente N lorsque X représente O. On décrit également une composition pharmaceutique comprenant un composé de Formule I ainsi qu'un vecteur pharmaceutiquement acceptable. De plus, l'invention concerne une méthode de traitement de l'asthme, des allergies et/ou des inflammations qui consiste à administrer à un mammifère nécessitant un tel traitement une quantité efficace d'un composé de formule I.

2. 发明公开

EP0412988A1 FUSED POLYCYCLIC COMPOUNDS, COMPOSITIONS, METHODS OF MANUFACTURE AND THEIR USE AS PAF ANTAGONISTS, ANTIHISTAMINES AND/OR ANTIINFLAMMATORY AGENTS 失效
标题翻译：缩合多环化合物，组合物的制备方法及其作为PAF拮抗药，抗组胺药及/或代理人消炎。
公开(公告)号：EP0412988A1
公开(公告)日：1991-02-20
申请号：EP89905353.0
申请日：1989-04-26
申请人： SCHERING CORPORATION
发明人： FRIARY, Richard, J. , GREEN, Michael, J. , PIWINSKI, John, J.
IPC分类号： C07D209 , A61K31 , A61P7 , A61P29 , A61P37 , A61P43 , C07D231 , C07D235 , C07D237 , C07D239 , C07D241 , C07D249 , C07D261 , C07D263 , C07D277 , C07D333 , C07D401 , C07D403 , C07D409 , C07D413 , C07D417 , C07D471 , C07D495 , C07D498 , C07D513
CPC分类号： C07D413/14 , C07D231/54 , C07D235/02 , C07D249/16 , C07D263/52 , C07D277/60 , C07D401/04 , C07D401/14 , C07D403/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04 , C07D417/14
摘要： L'invention concerne des composés hétérocycliques polycycliques fusionnés de la formule (I), leur utilisation comme antogonistes du PAF (facteur d'agrégation de plaquettes), des antihistamines et/ou des agents anti-inflammatoires, des procédés de fabrication ainsi que des compositions pharmaceutiques comprenant lesdits composés.

3. 发明授权

EP0912515B1 1,4-DI-SUBSTITUTED PIPERIDINES AS MUSCARINIC ANTAGONISTS 失效
标题翻译： 1,4-二取代哌啶ALS毒蕈碱拮抗剂
公开(公告)号：EP0912515B1
公开(公告)日：2002-11-13
申请号：EP97932321.9
申请日：1997-07-08
申请人： SCHERING CORPORATION
发明人： ASBEROM, Theodros , LOWE, Derek, B. , GREEN, Michael, J.
IPC分类号： C07D211/58 , C07D405/12 , C07D405/14 , A61K31/445
CPC分类号： C07D405/12 , A61K45/06 , C07D211/58
摘要： 1,4-Di-substituted piperidine muscarinic antagonists of formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein X is a bond, -O-, -S-, -SO-, -SO2-, -CO-, -C(OR7)2-, -CH2-O-, -O-CH2-, -CH=CH-, -CH2-, -CH(C1-C6 alkyl)-, -C(C1-C6 alkyl)2-, -CONR?17-, -NR17¿CO-, -SO¿2NR?17- or -NR17SO2-; R is C3-C6 cycloalkyl, (a), (b), (c), (d), (e), optionally substituted phenyl or optionally substituted pyridyl; R1 is H, -CN, -CF¿3?, alkyl, cycloalkyl, cycloalkenyl, alkenyl, -COR?15¿, -COO(alkyl, aryl, heteroaryl, alkylaryl or alkylheteroaryl), alkylaryl, alkylheteroaryl or -CON(R13)2; R2 is cycloalkyl, cycloalkenyl, t-butoxycarbonyl or optionally substituted 4-piperidinyl; R?3 and R4¿ are H, halo, -CF¿3?, alkyl, alkoxy or -OH; R?5 and R6¿ are H, alkyl, -CF¿3?, alkoxy, -OH, alkylcarbonyl, alkoxycarbonyl, R?13¿CONH-, R14OCONH-, R13NHCONH- or NH¿2?CONR?13-; R7¿ is H or alkyl, or the two R7 groups may form -(CH¿2?)2-4; R?13¿ is H, alkyl, cycloalkyl, -(alkyl)COOR15, aryl, heteroaryl, alkylaryl, alkylheteroaryl and adamantyl; R14 is H or alkyl; R15 is H, C¿1?-C20 alkyl, C1-C6 cycloalkyl, aryl or heteroaryl; and R?17¿ is H, C¿1?-C6 alkyl, aryl or heteroaryl; useful for treating cognitive disorders such as Alzheimer's disease are disclosed, as well as pharmaceutical compositions and methods of preparation. Also disclosed are combinations of compounds of formula (I) capable of enhancing ACh release with ACh'ase inhibitors.

4. 发明授权

EP0535152B1 Bis-benzo or benzopyrido cyclo hepta piperidene, piperidylene and piperazine compounds as PAF antagonists and compositions thereof. 有权转让
标题翻译：双 - 苯并或Benzopyrido环庚piperiden亚哌啶基，哌嗪衍生物作为PAF拮抗剂和组合物。
公开(公告)号：EP0535152B1
公开(公告)日：1995-08-09
申请号：EP91913317.3
申请日：1991-06-21
申请人： SCHERING CORPORATION
发明人： PIWINSKI, John, J. , GREEN, Michael, J. , WONG, Jesse
IPC分类号： C07D401/12 , A61K31/44 , A61K31/495 , C07D401/06 , C07D213/89 , C07D491/04 , C07D495/04
CPC分类号： C07D213/89 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D491/04 , C07D495/04
摘要： Bis-benzo or benzopyrido piperidene, piperidylidene and piperazine compounds of formula (I), and pharmaceutically acceptable salts thereof are disclosed, wherein Z represents -(C(Ra)2)m-Y-(C(Ra)2)n- or (α). The compounds of formula (I) possess anti-allergic and anti-inflammatory activity. Methods for preparing and using the compounds are also described.

5. 发明公开

EP0411048A1 NOVEL BENZOPYRIDO PIPERIDINE, PIPERIDYLIDENE AND PIPERAZINE COMPOUNDS, COMPOSITIONS, METHODS OF MANUFACTURE AND METHODS OF USE 失效
标题翻译： BENZOPYRIDOPIPERIDIN-，-PIPERIDYLIDEN-和哌嗪化合物，组合物的生产和使用方法。
公开(公告)号：EP0411048A1
公开(公告)日：1991-02-06
申请号：EP89905928.0
申请日：1989-04-26
申请人： SCHERING CORPORATION
发明人： PIWINSKI, John, J. , WONG, Jesse, K. , GREEN, Michael, J. , GANGULY, Ashit, K. , VILLANI, Frank, J.
IPC分类号： C07D221 , A61K31 , A61P11 , A61P29 , A61P37 , C07D401 , C07D491 , C07D495 , C07F9
CPC分类号： C07D401/04 , C07D401/14 , C07D491/04 , C07D495/04
摘要： On a mis au point de nouveaux composés de benzopyrido piperidine, piperidylidène et piperazine de la formule générale (I), utiles pour le traitement de l'asthme, d'allergies et d'inflammations. On a également mis au point de nouvelles compositions pharmaceutiques contenant lesdits composés ainsi que des procédés de production de ces derniers.

6. 发明公开

EP0938483A2 MUSCARINIC ANTAGONISTS 失效
标题翻译：毒蕈碱受体拮抗剂
公开(公告)号：EP0938483A2
公开(公告)日：1999-09-01
申请号：EP97936296.0
申请日：1997-08-06
申请人： SCHERING CORPORATION
发明人： LOWE, Derek, B. , CHANG, Wei, K. , KOZLOWSKI, Joseph, A. , BERGER, Joel, G. , McQUADE, Robert , BARNETT, Allen , SHERLOCK, Margaret , TOM, Wing , DUGAR, Sundeep , CHEN, Lian-Yong , CLADER, John, W. , CHACKALAMANNIL, Samuel , WANG, Yuguang , McCOMBIE, Stuart, W. , TAGAT, Jayaram, R. , VICE, Susan, F. , VACCARO, Wayne, D. , GREEN, Michael, J. , BROWNE, Margaret, E. , BOYLE, Craig, D. , JOSIEN, Hubert, B. , ASBEROM, Theodros
IPC分类号： C07D211 , A61K31 , A61K45 , A61P25 , C07D239 , C07D257 , C07D295 , C07D401 , C07D405 , C07D409 , C07D413
CPC分类号： C07D405/14 , C07C2601/14 , C07D211/24 , C07D211/32 , C07D239/34 , C07D257/04 , C07D295/03 , C07D295/088 , C07D295/092 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D405/12 , C07D409/14
摘要： Di-N-substituted piperazine or 1,4 di-substituted piperidine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) wherein R, R?1, R2, R3, R4, R21, R27, R28¿, X, Y and Z as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.

7. 发明授权

EP0618913B1 IMIDAZOLYL OR IMIDAZOYLALKYL SUBSTITUTED WITH A FOUR OR FIVE MEMBERED NITROGEN CONTAINING HETEROCYCLIC RING 失效
标题翻译：咪唑基或咪唑基烷基取代的4-或5-元含氮杂环
公开(公告)号：EP0618913B1
公开(公告)日：1996-08-14
申请号：EP93901329.8
申请日：1992-12-17
申请人： SCHERING CORPORATION
发明人： SHIH, Neng-Yang , ASLANIAN, Robert , LUPO, Andrew, Jr. , PIWINSKI, John, J. , GREEN, Michael, J. , GANGULY, Ashit, K.
IPC分类号： C07D401/06 , A61K31/415 , C07D403/06
CPC分类号： C07D403/04 , C07D403/06
摘要： Disclosed is a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier and an effective amount of a compound of formula (I). Further disclosed is a method of treating allergy (for example asthma), inflammation, hypertension, raised intraocular pressure (such as glaucoma)--i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypo motility and acidic secretion of the gastrointestinal tract, hypo and hyerpactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimers, schizophrenia, and migraine) comprising administering an effective amount of a compound of formula (I) to a patient in need of such treatment.

8. 发明授权

EP0553191B1 PYRIDINE AND PYRIDINE N-OXIDE DERIVATIVES OF DIARYLMETHYL- PIPERIDINES OR PIPERAZINES, COMPOSITIONS AND USE THEREOF 失效
标题翻译：二芳基哌啶或哌嗪，组合物和应用吡啶和吡啶N-氧化物衍生物。
公开(公告)号：EP0553191B1
公开(公告)日：1995-05-17
申请号：EP91918503.3
申请日：1991-10-08
申请人： SCHERING CORPORATION
发明人： PIWINSKI, John, J. , WONG, Jesse , GREEN, Michael, J. , SEIDL, Vera , FRIARY, Richard
IPC分类号： C07D401/14 , A61K31/44 , C07D409/14 , C07D417/14 , C07D401/06 , A61K31/445 , A61K31/38 , A61K31/495
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D417/14
摘要： Pyridine and pyridine N-oxide derivatives of diaryl methyl piperidines or piperazines represented by structural formula (1.0) and pharmaceutically acceptable salts thereof are disclosed, which possess anti-allergic and anti-inflammatory activity. Pharmaceutical compositions containing and methods of using the compounds are also described.

9. 发明授权

EP1318994B1 SUBSTITUTED IMIDAZOLES AS DUAL HISTAMINE H1 AND H3 AGONISTS OR ANTAGONISTS 有权
标题翻译：取代咪唑一举两得组胺H1和H3激动剂或拮抗剂
公开(公告)号：EP1318994B1
公开(公告)日：2008-02-27
申请号：EP01973119.9
申请日：2001-09-18
申请人： Schering Corporation
发明人： SHIH, Neng-Yang , SOLOMON, Daniel, M. , PIWINSKI, John, J. , LUPO, Andrew, T., Jr. , GREEN, Michael, J.
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D401/14
摘要： The present invention discloses novel substituted imidazole compounds which have dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, inflammatory and CNS-related diseases and others.

10. 发明授权

EP0729459B1 PHENYL-ALKYL IMIDAZOLES AS H3-RECEPTOR ANTAGONISTS 失效
标题翻译：苯的咪唑AS H3受体拮抗剂
公开(公告)号：EP0729459B1
公开(公告)日：2003-03-12
申请号：EP95902442.3
申请日：1994-11-10
申请人： SCHERING CORPORATION
发明人： ASLANIAN, Robert, G. , GREEN, Michael, J. , SHIH, Neng-Yang
IPC分类号： C07D233/54 , A61K31/415 , C07D401/12
CPC分类号： C07D233/64 , C07D401/12
摘要： The invention provides novel phenyl-alkyl-imidazoles of formula (I) wherein A, R1, R2, m and n are as defined in the specification, and the group —(CH¿2?)n—A—R?1¿ is at the 3- or 4-position, together with their pharmaceutically acceptable salts. These phenyl-alkyl-imidazoles and salts have valuable pharmacological properties, especially CNS activities and activity against inflammatory disease.

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