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公开(公告)号：EP3668832A1
公开(公告)日：2020-06-24
申请号：EP18760225.5
申请日：2018-08-13
申请人： Allergan, Inc.
发明人： HEIN, Christopher, D. , DUONG, Tien, T. , SINHA, Santosh , LI, Ling , NGUYEN, Jeremiah, H. , OLD, David, W. , BURK, Robert , VISWANATH, Veena , RAO, Sandhya , DONELLO, John, E.
IPC分类号： C07C211/52 , C07D215/42 , C07D333/54 , C07D307/36 , C07D307/79 , A61P17/00 , A61P29/00 , A61K31/341
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2.发明授权6-SUBSTITUTED INDOLE-3-CARBOXYLIC ACID AMIDE COMPOUNDS HAVING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR ANTAGONIST BIOLOGICAL ACTIVITY 有权与鞘氨醇-1-磷酸受体拮抗剂的6-取代的吲哚-3-CARBOXYLSÄUREAMIDVERBINDUNGEN生物活性
公开(公告)号：EP2238109B1
公开(公告)日：2014-12-31
申请号：EP08870363.2
申请日：2008-07-10
申请人： ALLERGAN, INC.
IPC分类号： C07D209/42 , C07D405/04 , A61K31/404 , A61P9/00
CPC分类号： C07D209/42 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
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3.发明授权SUBSTITUTED TETRAHYDRONAPHTHALENE AND DIHYDRONAPHTHALENE DERIVATIVES HAVING RETINOID AND/OR RETINOID ANTAGONIST-LIKE BIOLOGICAL ACTIVITY 失效WITH A维甲酸和/或类似类视黄醇拮抗剂生物活性的取代四氢化萘和二氢萘衍生物，
公开(公告)号：EP0915825B1
公开(公告)日：2004-05-06
申请号：EP97933997.5
申请日：1997-06-19
申请人： Allergan, Inc.
发明人： VULIGONDA, Vidyasagar , TENG, Min , BEARD, Richard, L. , JOHNSON, Alan, T. , LIN, Yuan , CHANDRARATNA, Roshantha, A. , SONG, Tae, K. , WONG, Harold, N. , DUONG, Tien, T. , GILLETT, Samuel, J.
IPC分类号： C07C69/587 , A61K31/19 , C07C69/78 , C07C245/10 , A61K31/655 , C07C235/66 , C07D309/12 , A61K31/35
CPC分类号： C07C251/44 , C07C69/587 , C07C69/76 , C07C233/81 , C07C245/10 , C07C309/65 , C07C317/44 , C07C323/55 , C07C2602/10 , C07D277/30 , C07D309/12 , C07D317/20 , C07D317/24 , C07D317/26 , C07D333/24 , C07D339/08 , C07D409/10
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4.发明公开6-SUBSTITUTED INDOLE-3-CARBOXYLIC ACID AMIDE COMPOUNDS HAVING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR ANTAGONIST BIOLOGICAL ACTIVITY 有权与鞘氨醇-1-磷酸受体拮抗剂的6-取代的吲哚-3-CARBOXYLSÄUREAMIDVERBINDUNGEN生物活性
公开(公告)号：EP2238109A1
公开(公告)日：2010-10-13
申请号：EP08870363.2
申请日：2008-07-10
申请人： ALLERGAN, INC.
IPC分类号： C07D209/42 , C07D405/04 , A61K31/404 , A61P9/00
CPC分类号： C07D209/42 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, o, A, A1, A2, X, Z, R1, R3, R2, p, q and r are as defined in the specification. These compounds are useful for treating a disease or condition selected from the group consisting of glaucoma, dry eye, angiogenesis, cardiovascular conditions and diseases, and wound healing
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公开(公告)号：EP2300456A1
公开(公告)日：2011-03-30
申请号：EP09751286.7
申请日：2009-05-18
申请人： Allergan, Inc.
发明人： BEARD, Richard, L. , VULIGONDA, Vidyasagar , DUONG, Tien, T. , VU, Thong , DONELLO, John, E. , GARST, Michael, E. , RODRIGUES, Gerard, A.
IPC分类号： C07D401/12 , A61K31/517
CPC分类号： C07D401/12
摘要： A compound represented by the structural formula (I): Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
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6.发明授权N-ARYL SUBSTITUTED TETRAHYDROQUINOLINES LIGANDS FOR RETINOID RECEPTORS HAVING AGONIST, ANTAGONIST OR INVERSE AGONIST TYPE ACTIVITY 失效N-二芳基取代的四氢喹啉配体与激动剂，拮抗剂或反相激动剂作用维甲酸
公开(公告)号：EP0937045B1
公开(公告)日：2004-04-28
申请号：EP97913959.9
申请日：1997-10-29
申请人： Allergan, Inc.
发明人： BEARD, Richard, L. , TENG, Min , COLON, Diana, F. , DUONG, Tien, T. , CHANDRARATNA, Roshantha, A.
IPC分类号： C07D215/14 , A61K31/44 , C07D215/22 , A61K31/445 , C07D215/48
CPC分类号： C07D215/227 , C07D215/06 , C07D215/12 , C07D215/18 , C07D215/48
摘要： Compounds of formula (1) where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid inverse agonist-like biological activity.
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7.发明授权SYNTHESIS AND USE OF RETINOID COMPOUNDS HAVING NEGATIVE HORMONE AND/OR ANTAGONIST ACTIVITIES 失效合成和应用具有负激素和/或拮抗作用的类维生素
公开(公告)号：EP0991636B1
公开(公告)日：2005-03-02
申请号：EP98932821.6
申请日：1998-06-24
申请人： ALLERGAN, INC.
发明人： KLEIN, Elliott, S. , JOHNSON, Alan, T. , STANDEVEN, Andrew, M. , BEARD, Richard, L. , GILLETT, Samuel, J. , DUONG, Tien, T. , NAGPAL, Sunil , VULIGONDA, Vidyasagar , TENG, Min , CHANDRARATNA, Roshantha, A.
IPC分类号： C07D311/58 , C07C233/81 , C07F7/18 , A61K31/215 , A61K31/335
CPC分类号： C07C57/50 , C07C63/33 , C07C63/49 , C07C63/66 , C07C63/72 , C07C63/74 , C07C65/19 , C07C65/28 , C07C65/38 , C07C69/618 , C07C69/76 , C07C69/90 , C07C69/94 , C07C233/81 , C07C233/87 , C07C245/10 , C07C327/48 , C07C2602/10 , C07C2602/28 , C07D213/55 , C07D277/30 , C07D307/54 , C07D311/58 , C07D333/24 , C07D335/06 , C07F7/0818
摘要： Aryl-substituted and aryl and (3-oxo-1-propenyl)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.
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8.发明授权BENZOPYRAN AND BENZOTHIOPYRAN DERIVATIVES HAVING RETINOID ANTAGONIST LIKE ACTIVITY 有权苯并吡喃和以维A拮抗剂样活性苯并噻衍生物
公开(公告)号：EP1042313B1
公开(公告)日：2004-04-28
申请号：EP98964231.9
申请日：1998-12-21
申请人： Allergan, Inc.
发明人： KLEIN, Elliott, S. , JOHNSON, Alan, T. , STANDEVEN, Andrew, M. , BEARD, Richard, L. , GILLETT, Samuel, J. , DUONG, Tien, T. , NAGPAL, Sunil , VULIGONDA, Vidyasagar , TENG, Min , CHANDRARATNA, Roshantha, A.
IPC分类号： C07D335/06 , C07D311/58 , C07D213/55 , C07D277/30 , C07D333/24 , C07D307/54 , C07D409/04 , C07D409/06 , C07C69/78 , C07C233/65 , C07C327/48 , A61K31/44 , A61K31/335 , A61K31/38 , A61K31/425
CPC分类号： C07D335/06 , C07D213/55 , C07D277/30 , C07D307/54 , C07D311/58 , C07D333/24 , C07D409/04 , C07D417/04
摘要： 2,2-Dialkyl- 4-aryl-substituted benzopyran and benzothiopyran derivatives of formula (I) where the symbols have the meaning described in the specification, have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action or RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists.
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