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81. 发明授权

US5436359A Hydroquinone derivatives and intermediates for production thereof 失效
标题翻译：对苯二酚衍生物及其制备中间体
公开(公告)号：US5436359A
公开(公告)日：1995-07-25
申请号：US30880
申请日：1993-03-12
申请人： Hirotomo Masuya , Masayoshi Yamaoka
发明人： Hirotomo Masuya , Masayoshi Yamaoka
IPC分类号： C07C69/732 , C07C309/42 , C07C309/58 , C07D211/90 , C07D213/30 , C07D213/80 , C07F7/18 , C07F9/12 , C07H15/203 , C07H15/26 , C07F7/08
CPC分类号： C07D213/30 , C07C309/42 , C07C309/58 , C07C69/732 , C07D211/90 , C07D213/80 , C07F7/1852 , C07F7/1856 , C07F9/12 , C07H15/203 , C07H15/26
摘要： There are disclosed novel hydroquinone derivatives of the formulas: ##STR1## The derivatives of the formula (I) have various pharmacological activities such as antioxidation in living bodies and are useful as medicaments, and the derivatives of the formula (II) are intermediates for the production thereof.
摘要翻译：公开了以下结构式的新型氢醌衍生物：式（I）和（II）式（I）的衍生物具有各种药理活性，例如活体中的抗氧化作用，可用作药物，衍生物式（II）的化合物是其制备的中间体。

82. 发明授权

US5428160A Substituted imidazo[5-a]pyridine derviatives and other substituted bicyclic derivatives 失效
标题翻译：取代的咪唑并[5-a]吡啶衍生物和其它取代的双环衍生物
公开(公告)号：US5428160A
公开(公告)日：1995-06-27
申请号：US632584
申请日：1990-12-21
申请人： Leslie J. Browne
发明人： Leslie J. Browne
IPC分类号： C07D213/38 , C07D213/40 , C07D213/55 , C07D213/65 , C07D213/84 , C07D213/89 , C07D233/54 , C07D471/04 , C07D487/04 , C07F7/10 , C07F7/18 , C07D417/04 , C07D491/04
CPC分类号： C07D213/40 , C07D213/38 , C07D213/55 , C07D213/65 , C07D213/84 , C07D213/89 , C07D233/64 , C07D471/04 , C07D487/04 , C07F7/10 , C07F7/1856
摘要： Disclosed are compounds of formula I ##STR1## wherein R.sub.1 represents hydrogen, lower alkyl, substituted lower alkyl, nitro, halogen, free, etherified or esterified hydroxy, free, etherified, oxidised etherified or esterified mercapto, unsubstituted, mono- or disubstituted amino, ammonio, free or functionally modified sulfo, free or functionally modified formyl, C.sub.2 -C.sub.20 -acyl, cyano, free or functionally modified carboxy; and R.sub.2 represents hydrogen, lower alkyl, substituted lower alkyl, halogen; free, etherified or esterified hydroxy; free, etherified, oxidised etherified or esterified mercapto; free or functionally modified carboxy, or acyl; the 7,8-dihydro derivatives thereof; and compounds of the formula I* ##STR2## wherein n denotes 0, 1, 2, 3, or 4, and R.sub.1 and R.sub.2 are as defined above under formula I and salts thereof; e.g. as aromatase inhibitors; pharmaceutical compositions containing these compounds; the use of these compounds for the treatment of conditions responsive to e.g. aromatase inhibition in mammals; processes and intermediates for preparing these compounds.
摘要翻译：公开了式I化合物其中R 1表示氢，低级烷基，取代的低级烷基，硝基，卤素，游离的，醚化的或酯化的羟基，游离的，醚化的，氧化的醚化或酯化的巯基，未取代的单 - 或游离或官能改性的磺酰基，C 2 -C 20酰基，氰基，游离的或官能改性的羧基; 并且R 2表示氢，低级烷基，取代的低级烷基，卤素; 游离的，醚化的或酯化的羟基; 游离，醚化，氧化醚化或酯化巯基; 游离或官能改性的羧基或酰基; 其7,8-二氢衍生物; 和式I *的化合物（I *），其中n表示0,1,2,3或4，并且R 1和R 2如上文通式I及其盐所定义; 例如作为芳香酶抑制剂; 含有这些化合物的药物组合物; 使用这些化合物来治疗响应于例如细胞的病症。哺乳动物中的芳香酶抑制作用; 制备这些化合物的方法和中间体。

83. 发明授权

US5409911A Prostaglandin analog for treating osteoporosis 失效
标题翻译：前列腺素类似物用于治疗骨质疏松症
公开(公告)号：US5409911A
公开(公告)日：1995-04-25
申请号：US944149
申请日：1992-09-11
申请人： Peter C. Tyler , Robert N. Young , Gideon A. Rodan
发明人： Peter C. Tyler , Robert N. Young , Gideon A. Rodan
IPC分类号： A61K31/557 , A61K31/5575 , A61K31/66 , A61K31/675 , A61K51/04 , A61P3/00 , A61P3/14 , A61P19/10 , A61P43/00 , C07C405/00 , C07F7/18 , C07F9/38 , C07F9/553 , C07F9/572
CPC分类号： C07F9/5537 , A61K51/0402 , C07C405/0041 , C07F7/1856 , C07F9/3873
摘要： This invention relates to a prostaglandin-bisphosphonate compound of the formula: ##STR1## and its pharmaceutically acceptable salts. The claimed compounds are effective as delivery agents of prostaglandins to treat osteoporosis and related bone diseases. The claimed compounds also simultaneously deliver a bisphosphonate which inhibits bone resorption and delivers prostaglandins which increase bone formation in vivo.
摘要翻译：本发明涉及下式的前列腺素二膦酸化合物及其药学上可接受的盐。所要求保护的化合物作为前列腺素的递送剂是有效的，以治疗骨质疏松症和相关的骨疾病。所要求保护的化合物还同时递送抑制骨吸收的双膦酸盐，并递送增加体内骨形成的前列腺素。

84. 发明授权

US5378707A Aryl-propyl-amines endowed with antifungal activity 失效
标题翻译：具有抗真菌活性的芳基 - 丙基胺
公开(公告)号：US5378707A
公开(公告)日：1995-01-03
申请号：US155545
申请日：1993-11-22
申请人： Giovanni Camaggi , Lucio Filippini , Marilena Gusmeroli , Carlo Garavaglia , Luigi Mirenna
发明人： Giovanni Camaggi , Lucio Filippini , Marilena Gusmeroli , Carlo Garavaglia , Luigi Mirenna
IPC分类号： A01N43/84 , A01N33/10 , A01N43/40 , A01N43/54 , A01N55/00 , A01N55/10 , A01P3/00 , C07D213/64 , C07D213/643 , C07D239/34 , C07D265/30 , C07D295/096 , C07D413/06 , C07F7/08 , C07F7/10 , C07F7/18
CPC分类号： C07D213/643 , A01N33/10 , A01N43/40 , A01N43/54 , A01N55/00 , C07D239/34 , C07D295/096 , C07F7/0812 , C07F7/1856 , C07C2101/02 , C07C2101/08
摘要： Aryl-propyl-aminic compounds having the following formula ##STR1## have high activity and are useful in the agricultural field as fungicides.
摘要翻译：具有下式（I）的芳基 - 丙基 - 氨基化合物具有高活性，并且在农田中用作杀真菌剂。

85. 发明授权

US5378695A Vitamin D analogues 失效
公开(公告)号：US5378695A
公开(公告)日：1995-01-03
申请号：US62154
申请日：1993-05-17
申请人： Martin J. Calverley , Kai Hansen , Lise Binderup
发明人： Martin J. Calverley , Kai Hansen , Lise Binderup
IPC分类号： C07C401/00 , C07F7/18 , C07F9/117
CPC分类号： C07F7/1864 , C07C401/00 , C07F7/1856 , C07F9/117
摘要： ##STR1## The present invention relates to compounds of formula (I), in which formula R stands for an alkyl group containing from 7 to 12 carbon atoms optionally substituted with a hydroxy group; and derivatives of the compounds of formula (I) in which one or more hydroxy groups have been transformed into --O-acyl or --O-glycosyl or phosphate ester groups, such masked groups being hydrolyzable in vivo, in pure form or in mixtures. The present compounds find use in both the human and veterinary practice in the treatment and prophylaxis of autoimmune diseases, including diabetes mellitus, hypertension, inflammatory diseases such as rheumatoid arthritis and asthma as well as diseases characterized by abnormal cell differentiation and/or cell proliferation, and/or imbalance in the immune system.

86. 发明授权

US5354879A Optically active intermediate and method for production thereof 失效
标题翻译：光学活性中间体及其制备方法
公开(公告)号：US5354879A
公开(公告)日：1994-10-11
申请号：US969249
申请日：1993-02-19
申请人： Toshiro Konoike , Yoshitaka Araki
发明人： Toshiro Konoike , Yoshitaka Araki
IPC分类号： C07D207/48 , C07C315/04 , C07C317/46 , C07F7/18 , C07F9/40 , C07F9/535 , C07F7/08
CPC分类号： C07F9/5352 , C07C315/04 , C07D207/48 , C07F7/1852 , C07F7/1856 , C07F7/1892 , C07F9/4006 , Y02P20/55
摘要： The present invention relates to a synthetic method of optically active starting materials for various medicaments, which are represented by Formula (I): ##STR1## wherein R.sup.1 is hydrogen or hydroxy protecting group; * is an asymmetric carbon; R.sup.2 ' is hydrogen or an optionally substituted lower alkyl; and Q is --CH.dbd.P(Ph).sub.3, --CH.sub.2 P(O)(OMe).sub.2, or --CH.sub.2 S(O)Me, in high optical purity on a large scale.In more detail, the present invention provides intermediates and a method for the production thereof for synthesizing optically active compounds which are able to inhibit activities of HMG-CoA reductase and are, therefore, useful for inhibition of cholesterol biosynthesis.
摘要翻译： PCT No.PCT / JP92 / 00611 Sec。 371日期：1993年2月19日 102（e）日期1993年2月19日PCT提交1992年5月14日PCT公布。出版物WO92 / 22560 本发明涉及由式（I）表示的各种药物的光学活性起始原料的合成方法：其中R 1为氢或羟基保护基; *是不对称碳; R2'是氢或任选取代的低级烷基; 并且Q是大规模的高光学纯度的-CH = P（Ph）3，-CH 2 P（O）（OMe）2或-CH 2 S（O）Me）。更详细地说，本发明提供了能够抑制HMG-CoA还原酶的活性的光学活性化合物的制备的中间体及其制造方法，因此可用于抑制胆固醇生物合成。

87. 发明授权

US5350696A 2-acetyl-6-cyanopyridines and their use as intermediates in the synthesis of oligo-2,6-pyridines 失效
标题翻译： 2-乙酰基-6-氰基吡啶并且它们用作合成低聚-2,6-吡啶的中间体
公开(公告)号：US5350696A
公开(公告)日：1994-09-27
申请号：US46221
申请日：1993-04-13
申请人： Robert A. Snow , Daniel J. Delecki , Chandra R. Shah , K. Robert Hollister
发明人： Robert A. Snow , Daniel J. Delecki , Chandra R. Shah , K. Robert Hollister
IPC分类号： C07D213/84 , C07D405/06 , C07F7/18 , C07D405/12
CPC分类号： C07D213/84 , C07D405/06 , C07F7/1856
摘要： The present invention is directed to 2-acetyl-6-cyanopyridine compounds that are useful as intermediates in the synthesis of oligo-2,6-pyridines. The present invention is also directed to new, simpler, less expensive methods for synthesizing such oligopyridines using the novel 2-acetyl-6-cyanopyridine compounds as intermediates.
摘要翻译：本发明涉及可用作合成低聚-2,6-吡啶的中间体的2-乙酰基-6-氰基吡啶化合物。本发明还涉及使用新颖的2-乙酰基-6-氰基吡啶化合物作为中间体合成这种低聚吡啶的新的，更简单的，更便宜的方法。

88. 发明授权

US5334740A Cyclohexanetriol derivatives 失效
标题翻译：环己烷三醇衍生物
公开(公告)号：US5334740A
公开(公告)日：1994-08-02
申请号：US851943
申请日：1992-03-13
申请人： Takashi Takahashi , Manzo Shiono
发明人： Takashi Takahashi , Manzo Shiono
IPC分类号： C07C69/732 , C07C33/14 , C07C35/17 , C07C43/178 , C07C43/188 , C07C43/196 , C07C47/267 , C07C49/337 , C07C49/35 , C07C69/734 , C07C401/00 , C07D261/20 , C07D311/74 , C07D311/76 , C07D317/20 , C07D317/46 , C07D493/04 , C07D498/04 , C07F7/18 , C07D311/02 , C07D262/20 , C07C69/74
CPC分类号： C07D493/04 , C07D261/20 , C07D311/76 , C07D317/46 , C07F7/1856 , Y02P20/55
摘要： Cyclohexanetriol derivatives represented by the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different, and each denotes a hydrogen atom or a protecting group of a hydroxyl group,X denotes an oxygen atom, .dbd.CHCH.sub.2 OR.sup.4, .dbd.CHCHO or .dbd.CHCO.sub.2 R.sup.5, Y denotes a hydrogen atom and Z denotes --OR.sup.6, or Y and Z together form a single bond; or X and Z together form .dbd.NO--, .dbd.CHCH(OR.sup.7)O-- or .dbd.CHCO.sub.2 -- and Y is a hydrogen atom, R.sup.4 and R.sup.6 denote a hydrogen atom or a protecting group of a hydroxyl group respectively, R.sup.5 denotes a lower alkyl group, and R.sup.7 denotes a hydrogen atom or a lower alkyl group.Said derivatives are useful as synthetic intermediates of 1-hydroxyvitamin D derivatives.
摘要翻译：式中，R 1，R 2和R 3相同或不同，表示氢原子或羟基保护基，X表示氧原子，= CHCH 2 OR 4 = CHCHO或= CHCO 2 R 5表示的环己烷三醇衍生物，Y表示氢原子，Z表示-OR6，或Y和Z一起形成单键; 或X和Z一起形成= NO-，= CHCH（OR7）O-或= CHCO2-，Y为氢原子，R4和R6分别表示氢原子或羟基的保护基，R5表示低级烷基，R7表示氢原子或低级烷基。所述衍生物可用作1-羟基维生素D衍生物的合成中间体。

89. 发明授权

US5318989A Cytotoxic bicyclo [7.3.1.]tridec-4-ene-2,6-diyne compounds and process for the preparation thereof 失效
标题翻译：细胞毒性双环[7.3.1]三癸-4-烯-2,6-二炔化合物及其制备方法
公开(公告)号：US5318989A
公开(公告)日：1994-06-07
申请号：US993184
申请日：1992-12-18
申请人： John F. Kadow , Mark D. Wittman
发明人： John F. Kadow , Mark D. Wittman
IPC分类号： C07C45/67 , C07C49/733 , C07C323/22 , C07F7/18 , C07F15/06 , A61K31/21 , C07D241/36 , C07D303/00
CPC分类号： C07F15/06 , C07C323/22 , C07C45/673 , C07C49/733 , C07F7/1856 , C07C2102/48
摘要： The present invention relates to a novel and efficient process for the preparation of 8-hydroxybicyclo[7.3.1]tridec-4-ene-2,6-diyne ring system which is part of the aglycone of esperemicin and to novel cytotoxic antitumor agents having said bicyclic ring system. The present invention also provides a method for treating mammalian malignant tumors by administering to an animal in need of such treatment an antitumor effective amount of a compound of the present invention.
摘要翻译：本发明涉及一种新颖有效的制备8-羟基双环[7.3.1]十三碳-4-烯-2,6-二炔环体系的方法，该系是作为异丙肾上腺苷的糖苷配基的一部分，以及新型细胞毒性抗肿瘤剂，其具有所述双环系统。本发明还提供了通过向需要这种治疗的动物施用抗肿瘤有效量的本发明化合物来治疗哺乳动物恶性肿瘤的方法。

90. 发明授权

US5300668A Certain esters of 1-(4-X-methylphenyl)cyclopent-3-ene-1-carboxylic acid, wherein X is a trialkylsilyloxy, bromo or hydroxy group, as intermediates 失效
标题翻译： 1-（4-X-甲基苯基）环戊-3-烯-1-羧酸的某些酯，其中X是三烷基甲硅烷氧基，溴或羟基，作为中间体
公开(公告)号：US5300668A
公开(公告)日：1994-04-05
申请号：US43959
申请日：1993-03-10
申请人： Paul A. Dasilva Jardine
发明人： Paul A. Dasilva Jardine
IPC分类号： C07D471/00 , A61K31/00 , C07C69/74 , C07C69/757 , C07F7/18 , C07C62/32 , C07C61/20
CPC分类号： C07F7/1856 , C07C69/74 , C07C69/757 , C07F7/1852
摘要： 1-[4'-(2"-Ethyl-5",7"-dimethylimidazo[4,5-b]pyridin-3-yl)methylphenyl]cyclopent-3-ene-1-carboxylic acid and its pharmaceutically acceptable salts inhibit angiotensin II in mammals and are useful in treating conditions such as hypertension, congestive heart failure and glaucoma and as the active ingredient in pharmaceutical compositions for treating such conditions.
摘要翻译： 1- [4' - （2“ - 乙基-5”，7“ - 二甲基咪唑并[4,5-b]吡啶-3-基）甲基苯基]环戊-3-烯-1-羧酸及其药学上可接受的盐在哺乳动物中抑制血管紧张素II，并且可用于治疗诸如高血压，充血性心力衰竭和青光眼的病症，并且用作用于治疗这些病症的药物组合物中的活性成分。

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