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1. 发明申请

US20210205271A1 MEBENDAZOLE PRODRUGS WITH ENHANCED SOLUBILITY AND ORAL BIOAVAILABILITY 有权
公开(公告)号：US20210205271A1
公开(公告)日：2021-07-08
申请号：US16967924
申请日：2019-02-08
申请人： The Johns Hopkins University , Institute of Organic Chemistry and Biochemistry AS CR v.v.i.
发明人： Barbara Slusher , Rana Rais , Gregory Riggins , Pavel Majer , Tomas Tichy , Jan Vavra , Andrej Jancarik
IPC分类号： A61K31/4184 , A61K45/06 , C07D235/32 , C07H15/26 , C07F9/6506 , A61K31/7056 , A61K31/675 , A61K31/685 , C07D405/12
摘要： Prodrugs of mebendazole and methods for their use in treating a disease, disorder, or disorder, including cancer, are disclosed.

2. 发明申请

US20200377505A1 BENZIMIDAZOLES AND AZA-BENZIMIDAZOLES, AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：US20200377505A1
公开(公告)日：2020-12-03
申请号：US16636606
申请日：2018-08-03
申请人： Goldfinch Bio., Inc.
发明人： Mark W. Ledeboer , Jean-Christophe P. Harmange , Maolin Yu , Thomas T. Tibbitts , Matthew H. Daniels
IPC分类号： C07D487/04 , C07D235/04 , C07D235/32 , C07D409/12 , C07D403/12 , C07D413/12 , C07D409/14 , C07D401/12 , C07D401/06 , C07D405/04 , C07D417/14 , C07D413/06
摘要： Disclosed are compounds according to Formula (I) or (II), and pharmaceutical compositions comprising them. Also disclosed are therapeutic methods, e.g., of treating kidney diseases, using the compounds of Formula (I) or (II).

3. 发明授权

US09765037B2 Compositions and methods for treating toxoplasmosis, cryptosporidiosis, and other apicomplexan protozoan related diseases 有权
公开(公告)号：US09765037B2
公开(公告)日：2017-09-19
申请号：US13561896
申请日：2012-07-30
申请人： Wesley C. Van Voorhis , Wilhelmus G. J. Hol , Eric T. Larson , Dustin James Maly , Ethan Merritt , Kayode K. Ojo
发明人： Wesley C. Van Voorhis , Wilhelmus G. J. Hol , Eric T. Larson , Dustin James Maly , Ethan Merritt , Kayode K. Ojo
IPC分类号： C07D235/30 , C07D403/12 , C07D401/12 , C07D235/32 , C07D487/04
CPC分类号： C07D235/30 , C07D235/32 , C07D401/12 , C07D403/12 , C07D487/04 , Y02A50/488
摘要： Compositions and methods for the treatment of toxoplasmosis, caused by the infectious eukaryotic parasite Toxoplasma gondii (T. gondii) and for the treatment of cryptosporidiosis, caused by the infectious eukaryotic parasites Cryptosporidium parvum (C. parvum) and Cryptosporidium hominus (C. hominus) are described. In particular, the present disclosure is directed to compositions and methods for inhibiting either T. gondii calcium dependent protein kinases (TgCDPKs) or C. parvum and C. hominus calcium dependent protein kinases (CpCDPKs) using pyrazolopyrimidine and/or imidazo[1,5-a]pyrazine inhibitors, of the formula, wherein the variables X, Y, Z, L, R1, and R3 are defined herein.

4. 发明申请

US20160046625A1 BENZIMIDAZOLE AND AZABENZIMIDAZOLE COMPOUNDS THAT INHIBIT ANAPLASTIC LYMPHOMA KINASE 审中-公开
公开(公告)号：US20160046625A1
公开(公告)日：2016-02-18
申请号：US14828928
申请日：2015-08-18
申请人： AMGEN INC.
发明人： Christiane M. Boezio , Alan C. Cheng , Deborah Choquette , Richard T. Lewis , Michele H. Potashman , Karina Romero , John C. Stellwagen , Douglas A. Whittington
IPC分类号： C07D471/04 , C07D519/00 , C07D417/12 , C07D403/06 , C07D235/32 , C07D401/06
CPC分类号： C07D471/04 , C07D235/30 , C07D235/32 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D413/10 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D487/04 , C07D519/00
摘要： Compounds of Formula (I) are useful inhibitors of anaplastic lymphoma kinase. Compounds of Formula (I) have the following structure: where the definitions of the variables are provided herein.

5. 发明申请

US20150065495A1 SUBSTITUTED- 1H-BENZO[D]IMIDAZOLE SERIES COMPOUNDS AS LYSINE-SPECIFIC DEMETHYLASE 1 (LSD1) INHIBITORS 有权
标题翻译：取代的1H-苯并[D]咪唑系列化合物作为LYSINE-SPECIFIC DEMETHYLASE 1（LSD1）抑制剂
公开(公告)号：US20150065495A1
公开(公告)日：2015-03-05
申请号：US14471134
申请日：2014-08-28
申请人： University of Utah
发明人： Hariprasad Vankayalapati , Sunil Sharma , Venkataswamy Sorna
IPC分类号： C07D471/04 , C07D401/12 , C07D235/32
CPC分类号： C07D471/04 , C07D235/32 , C07D401/12
摘要： The present invention provides compounds which are useful as inhibitors of lysine-specific demethylase 1 (“LSD1”). The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to a method for preparing these compounds. The present invention also relates to a method of treating a mammalian disorder in which LSD1 levels are elevated by administering these compounds and compositions to a patient in need thereof. The present invention also relates to a method for decreasing histone demethylase activity in a mammal comprising administering to the mammal an effective amount of these compounds and compositions.
摘要翻译：本发明提供可用作赖氨酸特异性脱甲基酶1（“LSD1”）抑制剂的化合物。本发明还涉及含有这些化合物的药物组合物。本发明还涉及一种制备这些化合物的方法。本发明还涉及通过向有需要的患者施用这些化合物和组合物来治疗哺乳动物疾病的方法，其中LSD1水平升高。本发明还涉及一种用于降低哺乳动物组蛋白去甲基化酶活性的方法，包括向哺乳动物施用有效量的这些化合物和组合物。

6. 发明申请

US20050119236A1 CANCER TREATMENTS AND PHARMACEUTICAL COMPOSITIONS THEREFOR 失效
标题翻译：癌症治疗及其药物组合物
公开(公告)号：US20050119236A1
公开(公告)日：2005-06-02
申请号：US10340945
申请日：2003-01-13
申请人： James Camden
发明人： James Camden
IPC分类号： C07D235/32 , A61K31/415 , A61K31/4184 , A61P31/12 , A61P35/00 , A61K31/60
CPC分类号： A61K31/4184
摘要： A pharmaceutical composition that inhibits the growth of tumors and cancers in mammals and can be used to treat viral infections that comprises a fungicide is disclosed. The particular fungicide used is a benzimidazole derivative having the formula: wherein R is selected from the group consisting of H, carboxyl (—CO2H), hydroxyl, amino or esters (—CO2R′) wherein R′ is selected from the group consisting of alkoxy, haloalkyl, alkenyl, and cycloalkyl wherein the alkyl groups have from 1-8 carbons or CH3CH2(OCH2CH2)n— or CH3CH2CH2(OCH2CH2CH2)n— or (CH3)2CH—(OCH(CH3)CH2)n— wherein n is from 1-3, the pharmaceutically acceptable salts thereof, or mixtures thereof.
摘要翻译：公开了抑制哺乳动物肿瘤和癌症生长并可用于治疗包含杀真菌剂的病毒感染的药物组合物。特定的杀真菌剂是具有下式的苯并咪唑衍生物：其中R选自H，羧基（-CO 2 H 2 H），羟基，氨基或酯（-CO 2 R'）其中R'选自烷氧基，卤代烷基，烯基和环烷基，其中烷基具有1-8个碳或CH 3 CH 2 （OCH 2 CH 2 CH 2）n - 或CH 3 CH 2 - （OCH 2 CH 2）2 CH 2 - （CH 2）2 - （CH 2）（CH 3）2 CH-（OCH（CH 3 CH 3）CH 2）n 其中n为1-3，其药学上可接受的盐，或其混合物。

7. 发明授权

US5985870A Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors 失效
标题翻译：磺酰基烷酰氨基羟乙氨基磺酰胺逆转录病毒蛋白酶抑制剂
公开(公告)号：US5985870A
公开(公告)日：1999-11-16
申请号：US913069
申请日：1997-12-19
申请人： Daniel P Getman , Gary A. Decrescenzo , John N. Freskos , Michael L. Vazquez , James A. Sikorski , Balekudru Devadas , Srinivasan Nagarajan , Joseph J. McDonald
发明人： Daniel P Getman , Gary A. Decrescenzo , John N. Freskos , Michael L. Vazquez , James A. Sikorski , Balekudru Devadas , Srinivasan Nagarajan , Joseph J. McDonald
IPC分类号： C07C311/29 , C07C311/41 , C07C317/44 , C07D215/36 , C07D217/04 , C07D235/06 , C07D235/30 , C07D235/32 , C07D249/18 , C07D249/20 , C07D263/56 , C07D277/62 , C07D277/82 , C07D303/36 , C07D307/79 , C07D317/62 , C07D319/18 , A61K31/36 , A61K31/415
CPC分类号： C07C311/29 , C07C311/41 , C07C317/44 , C07D215/36 , C07D217/04 , C07D235/06 , C07D235/30 , C07D235/32 , C07D249/18 , C07D249/20 , C07D263/56 , C07D277/62 , C07D277/82 , C07D303/36 , C07D307/79 , C07D317/62 , C07D319/18
摘要： Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
摘要翻译： PCT No.PCT / US96 / 02682 Sec。 371 1997年12月19日第 102（e）日期1997年12月19日PCT 1996年3月7日PCT公布。 WO96 / 28418 PCT公开号日期1996年9月19日选择的磺酰基烷酰基氨基羟基胺磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。本发明涉及这种逆转录病毒蛋白酶抑制剂，更具体地涉及所选择的新化合物，用于抑制逆转录病毒蛋白酶如人免疫缺陷病毒（HIV）蛋白酶的组合物和方法，预防性地预防逆转录病毒感染或逆转录病毒的扩散，以及治疗逆转录病毒感染。

8. 发明授权

US5852046A Benzo-fused heterocyclic compounds having a 5-membered ring processes for their preparation their use as medicaments their use as diagnostic agents and medicaments containing them 失效
标题翻译：具有5元环的苯并稠合杂环化合物用于制备其作为药物的用途，作为其用作诊断剂和含有它们的药物
公开(公告)号：US5852046A
公开(公告)日：1998-12-22
申请号：US872180
申请日：1997-06-10
申请人： Hans-Jochen Lang , Andreas Weichert , Jan-Robert Schwark , Wolfgang Scholz , Udo Albus , Peter Crause
发明人： Hans-Jochen Lang , Andreas Weichert , Jan-Robert Schwark , Wolfgang Scholz , Udo Albus , Peter Crause
IPC分类号： C07D209/08 , C07D209/42 , C07D235/06 , C07D235/24 , C07D235/26 , C07D235/28 , C07D235/32 , C07D249/18 , C07D277/62 , C07D277/68 , C07D277/82 , C07D307/84 , C07D307/85 , C07D307/86 , C07D333/62 , C07D333/70 , C07D401/04 , A61K31/40 , C07D209/10
CPC分类号： C07D277/82 , C07D209/08 , C07D209/42 , C07D235/06 , C07D235/24 , C07D235/26 , C07D235/28 , C07D235/32 , C07D249/18 , C07D277/62 , C07D277/68 , C07D307/84 , C07D307/85 , C07D307/86 , C07D333/62 , C07D333/70 , C07D401/04
摘要： Benzo-fused heterocyclic compounds having a 5-membered ring, processes for their preperation, their use as medicaments, their use as diagnostic agents and medicaments containing them. Benzo-fused heterocyclic compounds having a 5-membered ring, of the formula I ##STR1## where X is N or CR(6); Y is oxygen, S or NR(7); A and B together are a bond or are both hydrogen, if, at the same time, X is CR(6) and Y is NR(7), one of the substituents R(1) to R(6) is a --CO--N.dbd.C(NH.sub.2).sub.2 group; the other respective substituents R(1) to R(6) are H, Hal or alkyl; up to two of the other substituents R(1) to R(6) are CN, NO.sub.2, N.sub.3, (C.sub.1 -C.sub.4)-alkoxy, CF.sub.3 ; up to one of the other substituents is R(8)--C.sub.n H.sub.2n --Z-- or phenyl; R(7) is H, alk(en)yl or R(8)--C.sub.n H.sub.2n --, and pharmaceutically tolerated salts there of, are described. A process f or the preparation of the compounds I which comprises reacting a compound of the formula II ##STR2## in which one of the substituents R(1)' to R(5)' is a --CO--L group and L is a leaving group which can easily be replaced nucleophilically, with guanidine, and, if appropriate, converting the product into the pharmacologically tolerated salt, furthermore is also described.
摘要翻译：具有5元环的苯并稠合杂环化合物，其制备方法，用作药物，用作诊断剂和含有它们的药物。具有5元环的苯并稠合杂环化合物，其中X为N或CR（6）;其中X为N或CR（6）; Y是氧，S或NR（7）; 如果同时X是CR（6），Y是NR（7），则取代基R（1）〜R（6）中的一个是-CO -N = C（NH 2）2基团; 其它各取代基R（1）〜R（6）为H，Hal或烷基; 最多两个其它取代基R（1）-R（6）是CN，NO 2，N 3，（C 1 -C 4） - 烷氧基，CF 3; 最多一个其它取代基是R（8）-C n H 2n-Z-或苯基; R（7）为H，烷（烯）基或R（8）-C n H 2n - 及其药学上耐受的盐。方法f或化合物I的制备，其包括使式II（II）化合物与其中一个取代基R（1）'与R（5）'为-CO-L基团的化合物反应， L是一种离去基团，其可以容易地被核苷酸替代，并且如果合适，将产物转化成药理学上耐受的盐，此外还被描述。

9. 发明授权

US5538990A Benzimidazole anthelmintics 失效
标题翻译：苯并咪唑驱蚊剂
公开(公告)号：US5538990A
公开(公告)日：1996-07-23
申请号：US185996
申请日：1994-01-14
申请人： Bernard J. Banks , Christopher J. Dutton , Alexander C. Goudie
发明人： Bernard J. Banks , Christopher J. Dutton , Alexander C. Goudie
IPC分类号： A01N47/18 , A61K31/415 , A61K31/4184 , A61P31/10 , A61P33/10 , C07D235/32 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/04 , C07D417/04 , C07D417/06 , C07D417/12 , C07D521/00 , C07D235/26
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D235/32 , C07D401/04 , C07D403/04 , C07D405/04 , C07D413/04 , C07D417/04 , C07D417/06 , C07D417/12
摘要： This invention is directed to anthelmintic benzimidazole compounds of the formula (I), ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.6 alkylthio; R.sup.2 is C.sub.1 -C.sub.4 alkyl; and R.sup.3 is C.sub.1 -C.sub.4 alkyl.
摘要翻译： PCT No.PCT / EP92 / 01578 Sec。 371日期1994年1月14日 102（e）日期1994年1月14日PCT提交1992年7月13日PCT公布。公开号WO93 / 02058 日本特开1993年2月4日本发明涉及式（I），其中R1为C1-C6烷硫基的式（I）的驱虫剂苯并咪唑化合物。 R2是C1-C4烷基; 并且R 3是C 1 -C 4烷基。

10. 发明授权

US5432187A Benzimidazole anthelmintic in the treatment of microsporidial infections 失效
标题翻译：苯并咪唑驱虫剂治疗微孢子虫感染
公开(公告)号：US5432187A
公开(公告)日：1995-07-11
申请号：US117160
申请日：1993-09-15
申请人： Brian G. Gazzard
发明人： Brian G. Gazzard
IPC分类号： A61K31/415 , A61K31/4184 , C07D235/32
CPC分类号： A61K31/415
摘要： The present inventions relates to the use of certain benzimidazole compounds in the treatment of diseases caused by microsporidia organisms, in particular the treatment of diarrhea in patients infected with human immunodeficiency virus.
摘要翻译： PCT No.PCT / GB92 / 00522 Sec。 371日期：1993年9月15日 102（e）日期1993年9月15日PCT 1991年3月10日PCT公布。公开号WO92 / 16208 日本1992年1月10日。本发明涉及某些苯并咪唑化合物在治疗由微孢子虫生物引起的疾病中的用途，特别是在感染人类免疫缺陷病毒的患者中治疗腹泻。

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