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61. 发明授权

US5747541A Substituted benzoylguanidines, a process for their preparation, their use as medicament of diagnostic agent, and medicament comprising them 失效
标题翻译：取代的苯甲酰胍，其制备方法，它们作为诊断剂的药物，以及包含它们的药物
公开(公告)号：US5747541A
公开(公告)日：1998-05-05
申请号：US873825
申请日：1997-06-12
申请人： Andreas Weichert , Joachim Brendel , Heinz-Werner Kleemann , Hans Jochen Lang , Jan-Robert Schwark , Udo Albus , Wolfgang Scholz
发明人： Andreas Weichert , Joachim Brendel , Heinz-Werner Kleemann , Hans Jochen Lang , Jan-Robert Schwark , Udo Albus , Wolfgang Scholz
IPC分类号： A61K49/00 , A61K31/155 , A61K31/165 , A61P1/16 , A61P3/08 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07C277/00 , C07C279/22 , C07C231/02 , C07C235/50
CPC分类号： C07C279/22
摘要： The present invention relates to substituted benzoylguanidines, a process for their preparation, their use as medicament or diagnostic agent, and medicament comprising them.
摘要翻译：本发明涉及取代的苯甲酰胍，其制备方法，它们作为药物或诊断剂的用途，以及包含它们的药物。

62. 发明授权

US5728879A Bisguanidine salts and a method for releasing a base using the same salts 失效
标题翻译：双胍盐和使用相同盐释放碱的方法
公开(公告)号：US5728879A
公开(公告)日：1998-03-17
申请号：US829814
申请日：1997-03-25
申请人： Jiro Tsukahara , Kiyoshi Takeuchi , Hideaki Satoh , Shun-ichi Ishikawa , Keizo Ogawa , Tomomi Ishino
发明人： Jiro Tsukahara , Kiyoshi Takeuchi , Hideaki Satoh , Shun-ichi Ishikawa , Keizo Ogawa , Tomomi Ishino
IPC分类号： B41M5/323 , B41M5/30 , C07C279/12 , C07C317/44 , C07D233/48 , C07D295/12 , C07D295/215 , C09K3/00 , G03C1/43 , G03C1/498 , G03C1/61 , G03C8/40 , C07C277/00 , C07D241/00
CPC分类号： C07D295/215 , B41M5/30 , C07C279/12 , C07C317/44 , C07D233/48 , G03C1/43 , G03C1/49845 , G03C1/615 , G03C8/4086
摘要： A bisguanidine salt selected from the group consisting of a 4-(phenylsulfonyl)phenylsulfonylacetic acid salt of N,N'-bis(1,3-diethylguanyl)ethylenediamine, a 4-(phenylsulfonyl)phenylsulfonylacetic acid salt of N,N'-bis(1,3-diisopropylguanyl)ethylenediamine, a 4-(phenylsulfonyl)phenylsulfonylacetic acid salt of N,N'-bis-(imidazoline-2-yl)ethylenediamine, a 4-(phenylsulfonyl)-phenylsulfonylacetic acid salt of 1,4-bis(1,3-diisopropylguanyl)piperazine, a 4-(phenylsulfonyl)phenylsulfonylacetic acid salt of 1,4-bis(1,3-diethylguanyl)piperazine, a 4-(4-methylphenylsulfonyl)phenylsulfonylacetic acid salt of N,N'-bis(1,3-diethylguanyl)ethylenediamine and a 4-(4-ethylphenylsulfonyl)phenylsulfonylacetic acid salt of 1,4-bis(1,3-diethylguanyl)piperazine which can be used as a base precursor which is rapidly decomposed by heat treatment at 120.degree. C. or less to release a base.
摘要翻译：选自N，N'-双（1,3-二乙基鸟苷基）乙二胺的4-（苯基磺酰基）苯基磺酰基乙酸盐，N，N'-双（1,3-二异丙基脒基）乙二胺，N，N'-双 - （咪唑啉-2-基）乙二胺的4-（苯基磺酰基）苯磺酰基乙酸盐，1,4- 哌嗪，1,4-双（1,3-二乙基鸟嘌呤）哌嗪的4-（苯基磺酰基）苯基磺酰基乙酸盐，N，N'的4-（4-甲基苯基磺酰基）苯基磺酰基乙酸盐，（1,3-二乙基鸟苷基）乙二胺和1,4-双（1,3-二乙基鸟苷基）哌嗪的4-（4-乙基苯基磺酰基）苯磺酰基乙酸盐，其可用作通过热快速分解的基础前体在120℃或更低温度下处理以释放碱。

63. 发明授权

US5688952A �(Benzodioxan benzofuran or benzopyran) alkylamino!alkyl substituted guanidines 失效
标题翻译： [（苯并二恶烷苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍
公开(公告)号：US5688952A
公开(公告)日：1997-11-18
申请号：US632228
申请日：1996-04-15
申请人： Guy Rosalia Eugene Van Lommen , Marcel Frans Leopold De Bruyn , Walter Jacobus Joseph Janssens
发明人： Guy Rosalia Eugene Van Lommen , Marcel Frans Leopold De Bruyn , Walter Jacobus Joseph Janssens
IPC分类号： C07C279/00 , C07D307/78 , A61K31/34 , A61K31/343 , A61K31/35 , A61K31/352 , A61K31/415 , A61K31/443 , A61K31/445 , A61K31/505 , A61K31/53 , A61P9/00 , A61P9/02 , A61P25/04 , C07C277/00 , C07D307/81 , C07D311/58 , C07D319/08 , C07D319/20 , C07D405/06 , C07D405/12 , C07D405/14 , C07D403/02 , C07D403/14
CPC分类号： C07D405/12 , C07D307/81 , C07D311/58 , C07D319/20 , C07D405/14
摘要： The present invention is concerned with vasoconstricive �(benzodioxan, benzofuran or benzopyran)alkylamino!alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is a bivalent C.sub.1-3 alkanediyl radical; A is a bivalent radical of formula: ##STR2## wherein each R.sup.5 is hydrogen or C.sub.1-4 alkyl; wherein each R.sup.6 is hydrogen or C.sub.1-4 alkyl; Alk.sup.2 is C.sub.2-15 alkanediyl or C.sub.5-7 cycloalkanediyl; and each p is 0, 1 or 2; provided that �2-�(2,3- dihydro-1,4-benzodioxin-2-yl)methyl!amino!ethyl guanidine is excluded. Pharmaceuticals which are useful as vasoconstrictors. Compositions comprising said guanidine derivatives as active ingredients, processes for preparing said guanidine derivatives and novel N-cyano guanidine, intermediates; and a use as a medicine are described.
摘要翻译：本发明涉及具有下式的[（苯并二恶烷，苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍，（I）其药学上可接受的酸加成盐及其立体化学异构形式，其中X是O，CH 2 或直接债券; R1是氢或C1-6烷基; R2是氢，C1-6烷基，C3-6烯基或C3-6炔基; R3是氢或C1-6烷基; 或者R 2和R 3可以一起形成式 - （CH 2）m - 的二价基团，其中m为4或5; 或R 1和R 2一起形成式-CH = CH-或式 - （CH 2）n - 的二价基团，其中n为2,3或4; 或者当R 1和R 2一起形成式-CH = CH-CH =，-CH = CH-N =或-CH = N-CH =的二价基团时，R 3可以表示键。 R4是氢或C1-6烷基; Alk1是二价C 1-3烷二基; （a）其中每个R 5为氢或C 1-4烷基;（e）其中每个R 5为氢或C 1-4烷基;（c）其中每个R 6是氢或C 1-4烷基; Alk2是C2-15烷二基或C5-7环烷二基; 每个p为0,1或2; 条件是排除[2 - [（2,3-二氢-1,4-苯并二恶英-2-基）甲基]氨基]乙基胍。可用作血管收缩药物的药物。包含所述胍衍生物作为活性成分的组合物，制备所述胍衍生物的方法和新的N-氰基胍，中间体; 并描述了作为药物的用途。

64. 发明授权

US5677448A Sulfonamidocarboxamides 失效
标题翻译：磺酰胺酰胺
公开(公告)号：US5677448A
公开(公告)日：1997-10-14
申请号：US689743
申请日：1996-08-13
申请人： Jean Ackermann , David Banner , Klaus Gubernator , Kurt Hilpert , Gerard Schmid
发明人： Jean Ackermann , David Banner , Klaus Gubernator , Kurt Hilpert , Gerard Schmid
IPC分类号： A61K31/445 , A61K20060101 , A61K31/155 , A61K31/18 , A61K31/33 , A61K31/435 , A61K31/4427 , A61K31/452 , A61K31/47 , A61K31/535 , A61K31/5375 , A61K31/63 , A61K31/675 , A61K38/00 , A61P7/02 , C07C231/00 , C07C237/16 , C07C277/00 , C07C279/16 , C07C279/18 , C07C279/20 , C07C311/00 , C07C311/19 , C07D20060101 , C07D211/18 , C07D211/26 , C07D211/28 , C07D211/36 , C07D211/56 , C07D265/06 , C07D265/28 , C07D265/30 , C07D295/00 , C07D401/12 , C07D401/14 , C07D413/12 , C07F9/59 , C07K5/06 , C07K5/068 , C07K5/072 , C07K5/078 , C07D211/14
CPC分类号： C07D265/30 , C07D211/26 , C07D401/12 , C07D413/10 , C07D413/12 , C07K5/06026 , C07K5/06086 , C07K5/06104 , C07K5/06113 , C07K5/06139 , A61K38/00
摘要： Sulfonamidocarboxamides of the formula ##STR1## wherein A, M, Q, X and Y have the significance given in the description, as well as hydrates, solvates and salts thereof, which inhibit thrombin-induced blood platelet aggregation and clotting of fibrinogen in plasma, as described. The compounds of formula I can be prepared by amidination of a cyclic amino group standing for grouping X or by C(O)N(Q) amide formation.
摘要翻译：其中A，M，Q，X和Y具有在说明书中给出的含义的磺酰胺酰胺，其水合物，溶剂化物和盐，其抑制血浆中凝血酶诱导的血小板聚集和纤维蛋白原凝结，如上所述。式I的化合物可以通过用于分组X或通过C（O）N（Q）酰胺形成的环状氨基的酰胺化来制备。

65. 发明授权

US5041662A Process for the production of guanidine nitrate from urea and ammonium nitrate 失效
标题翻译：用于从尿素和硝酸铵生产硝酸胍的方法
公开(公告)号：US5041662A
公开(公告)日：1991-08-20
申请号：US488497
申请日：1990-03-02
申请人： Clemens Grambow , Wolfgang Kristof , Peter Reitsamer , Kurt Scheinost
发明人： Clemens Grambow , Wolfgang Kristof , Peter Reitsamer , Kurt Scheinost
IPC分类号： B01J21/08 , C07B61/00 , C07C277/00 , C07C279/02
CPC分类号： C07C277/00
摘要： The present invention provides a process for the production of guanidine nitrate by the reaction of urea and excess ammonium nitrate in the presence of a silicon dioxide catalyst at an elevated temperature, wherein the molten reaction mixture containing the dispersed catalyst is passed in a cycle, a branch current of the reaction mixture is continuously separated off by filtration in such a manner that the catalyst remains in circulation and consumed urea and ammonium nitrate are supplemented corresponding to the removal of the product.
摘要翻译：本发明提供了一种通过在二氧化硅催化剂的存在下在升高的温度下通过尿素和过量硝酸铵的反应来生产硝酸胍的方法，其中含有分散的催化剂的熔融反应混合物在一个循环中通过，反应混合物的分支电流通过过滤连续分离，使得催化剂保持循环并且消耗尿素和硝酸铵，同时除去产物。

66. 发明授权

US4939291A Process for the preparation of mercaptoethansulfonic acid and sodium salt thereof 失效
标题翻译：巯基乙磺酸及其钠盐的制备方法
公开(公告)号：US4939291A
公开(公告)日：1990-07-03
申请号：US346320
申请日：1989-05-01
申请人： Alberto Reiner
发明人： Alberto Reiner
IPC分类号： B01J27/232 , B01J27/00 , C07B61/00 , C07C20060101 , C07C67/00 , C07C277/00 , C07C279/00 , C07C313/00 , C07C319/20 , C07C323/00 , C07C323/66
CPC分类号： C07C303/32 , C07C319/02 , C07C327/26
摘要： For the preparation of saline derivatives of mercaptoethansulfonic acid belonging to the class of the salts of alkali metals and of the salts with basic aminoacids, the sodium salt of the acid is obtained with a process comprising the reaction between sodium bromoethansulfonate with thiobenzoic acid and sodium bicarbonate and subsequent reaction of the resulting sodium benzoylethansulfonate with ammonia in water solution.
摘要翻译：为了制备属于碱金属盐类和碱式氨基酸类的巯基乙磺酸的盐水衍生物，该酸的钠盐是通过包括溴代二磺酸钠与硫代苯甲酸和碳酸氢钠之间的反应的方法得到的随后将所得的苯基乙烷磺酸钠与氨在水溶液中反应。

67. 发明授权

US4690916A Nona and decapeptide analogs of LHRH useful as LHRH antagonists 失效
标题翻译： LHRH的壬基和十肽类似物可用作LHRH拮抗剂
公开(公告)号：US4690916A
公开(公告)日：1987-09-01
申请号：US671153
申请日：1984-11-13
申请人： John J. Nestor, Jr. , Brian Vickery
发明人： John J. Nestor, Jr. , Brian Vickery
IPC分类号： A61K38/04 , A61K38/00 , A61K38/22 , A61P13/02 , A61P15/00 , A61P43/00 , C07C277/00 , C07C279/14 , C07K1/113 , C07K7/06 , C07K7/23 , C07K14/575 , A61K37/43 , C07K7/20
CPC分类号： C07K7/23 , A61K38/00 , Y10S514/80 , Y10S930/13
摘要： Synthetic nonapeptide and decapeptide LHRH antagonist analogues having a halo lower alkyl guanadino-substituted amino acyl residue at position six are disclosed herein.
摘要翻译：在本文中公开了在6位具有卤代低级烷基瓜那丁取代的氨基酰基残基的合成的非肽和十肽LHRH拮抗剂类似物。

68. 发明公开

US20230373881A1 SIMPLE ASTATINE CONCENTRATION METHOD 审中-公开
公开(公告)号：US20230373881A1
公开(公告)日：2023-11-23
申请号：US17923341
申请日：2021-05-06
申请人： TOKYO INSTITUTE OF TECHNOLOGY , FUKUSHIMA MEDICAL UNIVERSITY
发明人： Hiroshi TANAKA , Kazuhiro TAKAHASHI , Miho SUZUKI
IPC分类号： C07B59/00 , C07D319/06 , C07C277/00 , C01B7/00
CPC分类号： C07B59/002 , C07D319/06 , C07B59/001 , C07C277/00 , C01B7/00 , C07B2200/05
摘要： In order to produce high yields of astatine-211 without contamination of chloride ions, provided is a method for producing astatine-211, including (1) a step of generating astatine-211 by irradiating bismuth with α rays; (2) a step of heating the astatine-211 generated in step (1) to vaporize; (3) a step of cooling the astatine-211 that has been vaporized in step (2) and collecting the astatine-211 with a volatile and polar solvent to obtain an astatine-211 solution; (4) a step of adding a weak acid salt to the astatine-211 solution obtained in step (3) to obtain an astatine-211 solution containing the weak acid salt; and (5) a step of removing the solvent from the astatine-211 solution containing the weak acid salt obtained in step (4).

69. 发明授权

US09725412B2 Polymorphic forms of perindopril (L)-arginine and process for the preparation thereof 有权
公开(公告)号：US09725412B2
公开(公告)日：2017-08-08
申请号：US14812053
申请日：2015-07-29
申请人： Mylan Laboratories Limited
发明人： Ramakoteswara Rao Jetti , Chetan Kanaiyalal Raval , Aggi Ramireddy Bommareddy , Debashish Datta
IPC分类号： C07D209/08 , C07D209/44 , C07D209/42 , C07C277/00
CPC分类号： C07D209/44 , C07C277/00 , C07D209/42
摘要： The present invention relates to novel and stable polymorphic forms of Perindopril (L)-Arginine designated as Form γ and amorphous form and processes for their preparation. The present invention also provides the novel polymorph Form γ with greater stability to heat and humidity and can be prepared on large scale by an efficient, economic and reproducible process.

70. 发明授权

US09388126B2 Sigma receptor ligands and methods of modulating cellular protein homeostasis using same 有权
标题翻译： Sigma受体配体和使用其调节细胞蛋白质体内平衡的方法
公开(公告)号：US09388126B2
公开(公告)日：2016-07-12
申请号：US14415061
申请日：2013-07-18
申请人： Drexel University
发明人： Felix J. Kim , Joseph M. Salvino
IPC分类号： C07C277/00 , A61K45/06 , C07C279/18 , A61K31/138 , A61K31/496 , A61K31/155 , A61K31/366 , A61K31/4035 , A61K31/4706 , A61K31/69 , C07D209/48 , C07D311/16
CPC分类号： A61K31/155 , A61K9/06 , A61K9/7023 , A61K31/138 , A61K31/366 , A61K31/4035 , A61K31/4706 , A61K31/496 , A61K31/69 , A61K45/06 , C07C279/18 , C07D209/48 , C07D311/16 , A61K2300/00
摘要： The present invention includes compounds useful in preventing, treating or ameliorating Sigma-related disorders or diseases. The compounds of the invention can modulate cellular protein homeostasis, which includes: translation initiation, folding, processing, transport, and degradation (including ubiquitin selective autophagy) of proteins. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound, further comprising administering an effective amount of a compound that inhibits the ubiquitin proteasome system (UPS) and/or autophagic survival pathways.
摘要翻译：本发明包括可用于预防，治疗或改善Sigma相关疾病或疾病的化合物。本发明的化合物可以调节细胞蛋白质内稳态，其包括蛋白质的翻译起始，折叠，加工，转运和降解（包括遍在蛋白选择性自噬）。本发明还包括在有需要的受试者中预防，治疗或改善与Sigma相关的病症或疾病的方法，所述方法包括向受试者施用有效量的Sigma-调节化合物。本发明还包括在有需要的受试者中预防，治疗或改善与Sigma相关的病症或疾病的方法，所述方法包括向受试者施用有效量的Sigma-调节化合物，其还包括给予有效量的一种抑制泛素蛋白酶体系统（UPS）和/或自噬存活途径的化合物。

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