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公开(公告)号：EP0356866A3
公开(公告)日：1991-03-27
申请号：EP89115400.7
申请日：1989-08-21
CPC分类号： C07F9/4469 , C07F9/4028 , C07F9/4037 , C07F9/4078
摘要： Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesterolemic agents are provided which have the structure
wherein Q is
or a bond;
n is 1 to 4; X is O, -NH- or -NR⁴-;
R, R¹ and R 1a are the same or different and are H, lower alkyl, lower alkenyl, or a metal ion;
R² and R³ may be the same or different and are H or halogen; and
R⁴ is lower alkyl;
with the proviso that when X is oxygen, n is 2, 3, or 4. A method for using such compounds to inhibit cholesterol biosynthesis is also provided.-
公开(公告)号：EP3209671B1
公开(公告)日：2019-03-27
申请号：EP15787031.2
申请日：2015-09-16
发明人： BHARATE, Sandip , KUMAR, Ajay , MANDA, Sudhakar , JOSHI, Prashant , BHARATE, Sonali , WANI, Abubakar , SHARMA, Sadhana , VISHWAKARMA, Ram
IPC分类号： C07F9/655 , C07F9/40 , A61K31/665 , A61K31/663 , A61P25/28
CPC分类号： C07F9/65515 , C07F9/4031 , C07F9/4034 , C07F9/4037 , C07F9/404 , C07F9/405
摘要： The present invention relates to the alkylidene phosphonate esters of formula I wherein, R1 is selected from a group consisting of hydrogen or alkyl group; R2 is selected from a group consisting of hydrogen, hydroxy, alkyl, alkoxy, nitro, halogen, amino, N- substituted alkylamino; alkyl group is selected from a group consisting of methyl, ethyl and isopropyl; Ar is selected from a group consisting of aryl, substituted aryl, fused aryl, heteroaryl, and substituted heteroaryl. The present invention particularly relates to synthesis and p-glycoprotein induction activity of the alkylidene phosphonate esters. In addition, the invention relates to methods of using compounds for treating or preventing Alzheimer's disease.
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公开(公告)号：EP2001486A2
公开(公告)日：2008-12-17
申请号：EP07758756.6
申请日：2007-03-16
IPC分类号： A61K31/663
CPC分类号： C07F9/4037 , C07F9/3843 , C07F9/3856 , C07F9/3865 , C07F9/3869 , C07F9/3873 , C07F9/4028 , C07F9/404 , C07F9/4046 , C07F9/5414 , C07F9/5728 , C07F9/581 , C07F9/65061 , C07F9/655345 , C07F9/655363 , C07F9/723
摘要： The invention provides, inter alia, novel bisphosphonate compounds and methods of making and using. In embodiments, the invention provides compounds and methods in connection with research and therapeutic applications, e.g., for tumor cell growth inhibition, activation of gammadelta T cells, inhibition of farnesyldiphosphate (FPPS) and/or undecaprenyldiphosphate synthase enzymes, bone resorption diseases, cancer, immune disorders, immunotherapy, and infectious diseases. In regards to certain embodiments, a surprising advance has been the recognition that certain structural features can significantly enhance the activity of the compounds. For example, the presence of particular cationic species e.g., phosphonium, sulfonium, and arsonium moieties can contribute to desirable functional activity when positioned near a bisphosphonate moiety. In other embodiments of non-nitrogen containing bisphosphonates, terphenyl and benzyl bisphosphonate compounds and methods are provided. Further variations are also provided.
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公开(公告)号：EP2001486A4
公开(公告)日：2010-12-29
申请号：EP07758756
申请日：2007-03-16
申请人： UNIV ILLINOIS
发明人： OLDFIELD ERIC , SONG YONGCHENG , ZHANG YONGHUI , SANDERS JOHN M
IPC分类号： A61K31/663 , C07F9/38 , C07F9/40
CPC分类号： C07F9/4037 , C07F9/3843 , C07F9/3856 , C07F9/3865 , C07F9/3869 , C07F9/3873 , C07F9/4028 , C07F9/404 , C07F9/4046 , C07F9/5414 , C07F9/5728 , C07F9/581 , C07F9/65061 , C07F9/655345 , C07F9/655363 , C07F9/723
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公开(公告)号：EP1001918A1
公开(公告)日：2000-05-24
申请号：EP98932402.5
申请日：1998-07-09
申请人： F2 Chemicals Limited
CPC分类号： C07F9/4037 , C07F9/4006
摘要： A method for the preparation of a fluorinated phosphonate having the formula (RO)2PO.CFR'.R'' comprises treating a phosphonate of the formula (RO)2PO.CHR'R'', or a metal salt thereof, with fluorine. R is an alkyl group, R' is hydrogen or alkyl and R'' is hydrogen, alkyl or another group.
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公开(公告)号：EP0479813A1
公开(公告)日：1992-04-15
申请号：EP90909051.0
申请日：1990-06-19
申请人： HUHTAMAKI OY
CPC分类号： C07F9/4037 , C07F9/4081
摘要： Dérivés nouveaux d'acide bisphosphonique pharmaceutiquement actifs de formule (I) dans laquelle R1, R2, R3 et R4 sont indépendamment alkyle C1-C22, alkényle C2-C22, alkynyle C2-C22, cycloalkyle C3-C10, cycloalkényle C3-C10, aryle, aralkyle, silyle, ou hydrogène; dans la formule (I), au moins un des groupes R1, R2, R3 et R4 est hydrogène et au moins un des groupes R1, R2, R3 et R4 est différent de l'hydrogène, Q1 est hydrogène, fluor, chlore, brome, ou iode, et Q2 est chlore, brome ou iode, y compris les stéréoisomères, tels que les isomères géométriques et les isomères optiquement actifs, des composés, ainsi que les sels pharmaceutiquement acceptables des composés.
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7.发明授权COMPOSES INHIBITANT SELECTIVEMENT LES LYMPHOCYTES T GAMMA 9 DELTA 2 有权ŤGAMMA DELTA 9 2淋巴细胞的化合物SELEKTIF抑制剂
公开(公告)号：EP1165573B1
公开(公告)日：2004-01-21
申请号：EP00917119.0
申请日：2000-04-04
申请人： INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM) , SANGSTAT MEDICAL CORPORATION
发明人： BELMANT, Christian , BONNEVILLE, Marc , PEYRAT, Marc, Alix , FOURNIE, Jean-Jacques , KOZIKOWSKI, Alan, P.
CPC分类号： C12N5/0636 , A61K2035/122 , C07F9/4028 , C07F9/4037 , C07F9/4075 , C07F9/65505 , C12N2501/999
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8.发明公开COMPOSES INHIBITANT SELECTIVEMENT LES LYMPHOCYTES T GAMMA 9 DELTA 2 有权ŤGAMMA DELTA 9 2淋巴细胞的化合物SELEKTIF抑制剂
公开(公告)号：EP1165573A1
公开(公告)日：2002-01-02
申请号：EP00917119.0
申请日：2000-04-04
申请人： INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM) (E.P.S.T.) , SANGSTAT MEDICAL CORPORATION
发明人： BELMANT, Christian , BONNEVILLE, Marc , PEYRAT, Marc, Alix , FOURNIE, Jean-Jacques , KOZIKOWSKI, Alan, P.
CPC分类号： C12N5/0636 , A61K2035/122 , C07F9/4028 , C07F9/4037 , C07F9/4075 , C07F9/65505 , C12N2501/999
摘要： The invention concerns compounds of formula CH3-R1-(CH2)2-R2 wherein: R1 is selected among a tertiary alcohol; a 1,2-diol; a halohydrine; an epoxide; an alkene; an aldehyde or an α-hydroxyaldehyde; and R2 is selected among a methylenediphosphonate; a difluoromethylenediphosphonate; or a monofluoromethylenediphosphonate. The invention also concerns the uses of said compounds as selective inhibitors of Tη9δ2 lymphocytes, and their uses, in particular for therapeutic purposes.
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公开(公告)号：EP0356866A2
公开(公告)日：1990-03-07
申请号：EP89115400.7
申请日：1989-08-21
CPC分类号： C07F9/4469 , C07F9/4028 , C07F9/4037 , C07F9/4078
摘要： Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesterolemic agents are provided which have the structure
wherein Q is
or a bond;
n is 1 to 4; X is O, -NH- or -NR⁴-;
R, R¹ and R 1a are the same or different and are H, lower alkyl, lower alkenyl, or a metal ion;
R² and R³ may be the same or different and are H or halogen; and
R⁴ is lower alkyl;
with the proviso that when X is oxygen, n is 2, 3, or 4.
A method for using such compounds to inhibit cholesterol biosynthesis is also provided.摘要翻译： 提供了可用作胆固醇生物合成抑制剂，因此作为低胆固醇血症药物的化合物，其具有结构
，其中Q是 或键; n为1至4; X是O，-NH-或-NR 4 - ; R 1，R 1和R 1a相同或不同，为H，低级烷基，低级链烯基或金属离子; R 2和R 3可以相同或不同，为H或卤素; 和R 4是低级烷基; 条件是当X是氧时，n是2,3或4.还提供了使用这些化合物抑制胆固醇生物合成的方法。 -
公开(公告)号：EP3209671A1
公开(公告)日：2017-08-30
申请号：EP15787031.2
申请日：2015-09-16
发明人： BHARATE, Sandip , KUMAR, Ajay , MANDA, Sudhakar , JOSHI, Prashant , BHARATE, Sonali , WANI, Abubakar , SHARMA, Sadhana , VISHWAKARMA, Ram
IPC分类号： C07F9/655 , C07F9/40 , A61K31/665 , A61K31/663 , A61P25/28
CPC分类号： C07F9/65515 , C07F9/4031 , C07F9/4034 , C07F9/4037 , C07F9/404 , C07F9/405
摘要： The present invention relates to the alkylidene phosphonate esters of formula I wherein, R1 is selected from a group consisting of hydrogen or alkyl group; R2 is selected from a group consisting of hydrogen, hydroxy, alkyl, alkoxy, nitro, halogen, amino, N- substituted alkylamino; alkyl group is selected from a group consisting of methyl, ethyl and isopropyl; Ar is selected from a group consisting of aryl, substituted aryl, fused aryl, heteroaryl, and substituted heteroaryl. The present invention particularly relates to synthesis and p-glycoprotein induction activity of the alkylidene phosphonate esters. In addition, the invention relates to methods of using compounds for treating or preventing Alzheimer's disease.
摘要翻译： 本发明涉及式I的亚烷基膦酸酯，其中R 1选自氢或烷基; R2选自氢，羟基，烷基，烷氧基，硝基，卤素，氨基，N-取代的烷基氨基; 烷基选自甲基，乙基和异丙基; Ar选自由芳基，取代的芳基，稠合的芳基，杂芳基和取代的杂芳基组成的组。 本发明特别涉及亚烷基膦酸酯的合成和p-糖蛋白诱导活性。 另外，本发明涉及使用化合物治疗或预防阿尔茨海默氏病的方法。
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