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1. 发明申请

US20230069100A1 N-(3-AMINO-3-OXOPROPYL)-2-[(1-METHYL-4-NITRO-1H-IMIDAZOL-5-YL)THIO]BENZAMIDE AND ITS USE FOR TREATING HIV INFECTION 有权
公开(公告)号：US20230069100A1
公开(公告)日：2023-03-02
申请号：US17785155
申请日：2020-12-17
申请人： The United States of America,as represented by the Secretary,Department of Health and Human Services
发明人： Daniel H. Appella , Herman Nikolayevskiy , Marco Robello , Michael T. Scerba
IPC分类号： A61K31/4164 , C07D233/92 , A61K45/06 , A61K31/675 , A61K31/513 , A61K31/5365 , A61K31/47 , A61K31/427 , A61K31/635 , A61K39/21 , A61P31/18 , A61K31/52
摘要： Disclosed is a compound of formula (I): for treating or preventing a human immunodeficiency virus (HIV) infection in a mammal, for inhibiting or preventing maturation of an immature human immunodeficiency virus (HIV) to a mature HIV, and for preventing or inhibiting a human immunodeficiency virus (HIV) infection in a mammal having at least one HIV viral particle on a surface thereof.

2. 发明授权

US11530182B2 YAP1 inhibitors that target the interaction of YAP1 with Oct4 有权
公开(公告)号：US11530182B2
公开(公告)日：2022-12-20
申请号：US17138346
申请日：2020-12-30
申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.
发明人： Srikumar Chellappan , Nicholas J. Lawrence , Sujeewa Ranatunga Mahanthe Mudiyanselage
IPC分类号： C07D211/60 , C07D401/06 , C07D401/12 , C07C237/22 , C07C251/24 , C07C255/57 , C07D211/34 , C07D211/96 , C07D233/92 , C07D241/04 , C07D401/10 , C07D403/06 , C07D405/06 , C07D405/12 , A61K45/06
摘要： Binding of the transcriptional co-activator, YAP1, to the transcription factor Oct4, induces Sox2, which is a transcription actor necessary for the self-renewal of stem-like cells from non-small cell lung cancer. The WW domain of YAP1 binds to the PPxY motif of Oct4 to induce Sox2. Delivering a peptide corresponding to the WW domain could prevent the induction of Sox2 and stemness. Similarly, peptides and mimetics of the PPxY motif would be able to inhibit sternness. Disclosed are compounds that affect the Yap1:Oct4 interaction.

3. 发明授权

US11384060B2 Amide compounds and use thereof 有权
公开(公告)号：US11384060B2
公开(公告)日：2022-07-12
申请号：US16477072
申请日：2018-01-22
申请人： ALPHALA CO., LTD.
发明人： Cheng-Ho Chung , Shi-Liang Tseng , Yung-Ning Yang , Yen-Fu Chen
IPC分类号： C07D233/92 , C07D257/04 , C07D277/66 , C07D471/04 , C07D417/04 , C07D307/81 , C07D405/04 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/12 , C07D263/57 , C07D213/56 , C07D491/04 , C07D271/06 , C07D271/10 , C07D271/113 , C07D401/04 , C07D401/12 , C07D231/18 , C07D403/04 , C07D239/34 , C07D237/14 , C07D333/60 , A61P3/10 , C07D307/79 , C07C233/92 , C07D209/08 , C07D213/90 , C07D271/07
摘要： Disclosed are compounds of formula (I) below and pharmaceutically acceptable salts thereof: (I), in which each of variables R1, R2, R3, R4, R5, A1, A2, A3, A4, X and Y is defined herein. Also disclosed are methods for reducing the glycemic level and treating glucagon-associated disorders with a compound of formula (I) or a salt thereof and a pharmaceutical composition containing same.

4. 发明申请

US20210053925A1 PROCESS FOR PRODUCTION OF 2-CHLORO-4-NITROIMIDAZOLE DERIVATIVES 有权
公开(公告)号：US20210053925A1
公开(公告)日：2021-02-25
申请号：US16965464
申请日：2018-01-29
申请人： OTSUKA PHARMACEUTICAL CO., LTD.
发明人： Petr NOVAK , Petr ZAHRADNIK , Jiri TAUCHMAN , Jan KOCI , Antonin STURC
IPC分类号： C07D233/92
摘要： An improved process for preparing 2-chloro-4-nitroimidazole derivatives which are useful intermediates in the preparation of an anti-tuberculosis drug is provided. The process may comprise the step of chlorinating nitroimidazoles with a chlorinating agent and an activating agent to give 2-chloro-4-nitroimidazole derivatives.

5. 发明授权

US10906874B2 YAP1 inhibitors that target the interaction of YAP1 with OCT4 有权
公开(公告)号：US10906874B2
公开(公告)日：2021-02-02
申请号：US16334087
申请日：2017-09-18
申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.
发明人： Srikumar Chellappan , Nicholas J. Lawrence , Sujeewa Ranatunga Mahanthe Mudiyanselage
IPC分类号： C07D211/34 , C07D405/06 , C07D401/10 , C07D211/60 , C07C237/22 , C07C251/24 , C07C255/57 , C07D211/96 , C07D233/92 , C07D241/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/12 , A61K45/06
摘要： Binding of the transcriptional co-activator, YAP1, to the transcription factor Oct4, induces Sox2, which is a transcription actor necessary for the self-renewal of stem-like cells from non-small cell lung cancer. The WW domain of YAP1 binds to the PPxY motif of Oct4 to induce Sox2. Delivering a peptide corresponding to the WAV domain could prevent the induction of Sox2 and stemness. Similarly, peptides and mimetics of the PPxY motif would be able to inhibit stemness. Disclosed are compounds that affect the Yap1:Oct4 interaction.

6. 发明授权

US10231453B2 5-substituted imidazole derivatives 有权
公开(公告)号：US10231453B2
公开(公告)日：2019-03-19
申请号：US15563414
申请日：2016-03-29
申请人： BAYER CROPSCIENCE AKTIENGESELLSCHAFT
发明人： Sebastian Hoffmann , Hendrik Helmke , Peter Dahmen , Ulrike Wachendorff-Neumann , David Bernier , Ricarda Miller , Pierre-Yves Coqueron , Pierre Genix , Sven Wittrock , Jean-Pierre Vors , Philippe Kennel , Stephane Brunet , Sebastien Naud , Ruth Meissner
IPC分类号： A01N43/50 , C07D233/58 , C07D233/60 , C07D233/68 , C07D233/74 , C07D233/84 , C07D233/92 , C07D233/61 , C07D401/06
摘要： The present invention relates to novel 5-substituted imidazolylmethyl derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.

7. 发明授权

US09255107B2 Heteroaryl alkyne compound and use thereof 有权
标题翻译：杂芳基炔化合物及其用途
公开(公告)号：US09255107B2
公开(公告)日：2016-02-09
申请号：US14441190
申请日：2013-11-27
申请人： NANJING SANHOME PHARMACEUTICAL CO., LTD.
发明人： Yong Wang , Liwen Zhao , Di Zhang , Feng Wu , Sheng Bi , Yiping Gao , Hongbin Chen , Hongyan Chen , Cang Zhang , Yang Nan , Yang Liu
IPC分类号： C07D401/14 , C07D403/14 , C07D471/04 , C07D487/04 , C07D233/92 , A61K31/4196 , A61K31/496 , C07D401/04 , C07D403/04 , A61K31/4178 , A61K31/4439 , A61K31/4985 , C07D233/64
CPC分类号： C07D487/04 , A61K31/4178 , A61K31/4196 , A61K31/4439 , A61K31/496 , A61K31/4985 , C07D233/64 , C07D233/92 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D471/04
摘要： In the field of pharmaceutical chemistry compounds of general formula I having heteroaryl alkynyl moiety or pharmaceutically acceptable salts, isomers, solvates, crystals or prodrugs thereof, and pharmaceutical compositions including these compounds, as well as uses of these compounds and compositions thereof in the manufacture of a medicament. The compounds have a strong inhibitory effect on BCR-ABL tyrosine kinase and are useful for treating diseases, such as tumors.
摘要翻译：在药物化学领域，具有杂芳基炔基部分或其药学上可接受的盐，异构体，溶剂合物，晶体或前药的通式I化合物和包括这些化合物的药物组合物，以及这些化合物及其组合物在制备药物。该化合物对BCR-ABL酪氨酸激酶具有很强的抑制作用，可用于治疗疾病如肿瘤。

8. 发明申请

US20110178308A1 METHODS FOR THE PRODUCTION OF 2-HALO-4-NITROIMIDAZOLE AND INTERMEDIATES THEREOF 有权
标题翻译： 2-羟基-4-硝基吡唑的制备方法及其中间体
公开(公告)号：US20110178308A1
公开(公告)日：2011-07-21
申请号：US13059333
申请日：2009-08-21
申请人： Guido Wuellner , Franz-Willi Herkenrath , Alexander Juelich , Yoshinori Yamada , Shuji Kawabe
发明人： Guido Wuellner , Franz-Willi Herkenrath , Alexander Juelich , Yoshinori Yamada , Shuji Kawabe
IPC分类号： C07D498/04 , C07D233/92
CPC分类号： C07D233/92
摘要： The present invention relates to a method for the production of 2-halo-4-nitroimidazole and intermediates thereof. Further, the present invention relates to a production process of 1,4-dinitroimidazole comprising subjecting 4-nitroimidazole to nitration reaction. Furthermore, the present invention relates to a production process of 4-nitroimidazole comprising subjecting imidazole to nitration reaction.
摘要翻译：本发明涉及2-卤代-4-硝基咪唑的制备方法及其中间体。此外，本发明涉及1,4-二硝基咪唑的制备方法，其包括使4-硝基咪唑进行硝化反应。此外，本发明涉及4-硝基咪唑的制备方法，其包括使咪唑进行硝化反应。

9. 发明授权

US5877326A Aqueous phase process for preparing N-substituted imidazoles 失效
标题翻译：制备N-取代咪唑的水相方法
公开(公告)号：US5877326A
公开(公告)日：1999-03-02
申请号：US914187
申请日：1997-08-19
申请人： Gisela Hieber , Klaus Ebel , Jurgen Schroder , Toni Dockner , Carsten Groning , Bernd Ruge
发明人： Gisela Hieber , Klaus Ebel , Jurgen Schroder , Toni Dockner , Carsten Groning , Bernd Ruge
IPC分类号： C07D233/58 , B01J21/12 , B01J27/16 , C07D233/54 , C07D233/68 , C07D233/90 , C07D233/91 , C07D233/92 , C07D235/06 , C07D235/08 , C07D233/56
CPC分类号： C07D235/08 , C07D233/54 , C07D233/56 , C07D233/64 , C07D233/68 , C07D233/90 , C07D233/91 , C07D233/92 , C07D235/06
摘要： A process for preparing substituted imidazoles of the formula I ##STR1## R.sup.1, R.sup.2 and R.sup.3 are identical or different and are each hydrogen, halogen, NO.sub.2, CN or a C.sub.1 -C.sub.20 -hydrocarbon radical which is unsubstituted or substituted by one or more halogens or R.sup.1 and R.sup.2 together are members of a 3- to 20-membered hydrocarbon ring which is unsubstituted or substituted by one or more halogens and/or C.sub.1 -C.sub.8 -alkyl groups and which may contain 1, 2 or 3 heteroatoms from the group consisting of nitrogen, oxygen and sulfur, andR.sup.4 is a C.sub.1 -C.sub.20 -hydrocarbon radical which is unsubstituted or substituted by one or more halogens,comprises using an aqueous phase of the imidazoles of the formula II ##STR2## where R.sup.1, R.sup.2 and R.sup.3 are as defined above with compounds of the formula IIIR.sup.4 --O--R.sup.5 IIIwhereR.sup.4 is as defined above andR.sup.5 is hydrogen or R.sup.4, it being possible in the latter case for the two R.sup.4 substituents to be identical or different,and reacting it at from 200.degree. to 550.degree. C. in the presence of a catalyst comprising oxides and/or phosphates of one or more metals of the 2nd, 3rd and 4th main group and the 4th subgroup of the Periodic Table in the presence or absence of phosphoric acid and/or phosphoric esters.
摘要翻译：制备式I的取代咪唑的方法R1，R2和R3相同或不同，各自为氢，卤素，NO2，CN或C1-C20-烃基，其未被取代或被一个或多个卤素或R 1和R 2一起是3至20元烃环的成员，其未被取代或被一个或多个卤素和/或C 1 -C 8烷基取代，并且可以含有1,2或3个来自该基团的杂原子由氮，氧和硫组成，R4是未被取代或被一个或多个卤素取代的C 1 -C 20烃基，包括使用式II的咪唑的水相，其中R 1，R 2和 R 3如上所定义，与式III的R4-O-R5III化合物，其中R 4如上定义，R 5是氢或R 4，在后一种情况下，两个R 4取代基可以相同或不同，在约200℃〜550℃下，在磷酸和/或磷酸酯存在或不存在的条件下，包含第2，第3和第4主族和第4族的周期表中的一种或多种金属的氧化物和/或磷酸盐。

10. 发明授权

US5691366A Nitro compounds, process for preparation thereof and use thereof 失效
标题翻译：硝基化合物，其制备方法及其用途
公开(公告)号：US5691366A
公开(公告)日：1997-11-25
申请号：US550735
申请日：1995-10-31
申请人： Masayuki Kato , Shigetaka Nishino , Mitsuko Hamano , Hisashi Takasugi
发明人： Masayuki Kato , Shigetaka Nishino , Mitsuko Hamano , Hisashi Takasugi
IPC分类号： A61K31/12 , A61K31/165 , A61K31/215 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/42 , A61K31/423 , A61K31/433 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/47 , A61P7/02 , A61P9/08 , C07C249/06 , C07C251/40 , C07C271/12 , C07C275/20 , C07C307/06 , C07C311/05 , C07C319/20 , C07C323/23 , C07D209/34 , C07D209/38 , C07D209/48 , C07D213/56 , C07D213/71 , C07D213/78 , C07D213/80 , C07D213/81 , C07D213/82 , C07D215/54 , C07D231/14 , C07D233/84 , C07D233/90 , C07D233/92 , C07D239/38 , C07D241/14 , C07D241/24 , C07D249/10 , C07D253/00 , C07D257/04 , C07D261/18 , C07D277/56 , C07D277/70 , C07D277/74 , C07D285/12 , C07D285/125 , C07D471/04 , C07D473/38
CPC分类号： C07D209/48 , C07C251/40 , C07C271/12 , C07C275/20 , C07C307/06 , C07C311/05 , C07D209/34 , C07D213/56 , C07D213/71 , C07D213/78 , C07D213/80 , C07D213/81 , C07D213/82 , C07D215/54 , C07D231/14 , C07D233/84 , C07D233/92 , C07D239/38 , C07D241/24 , C07D249/10 , C07D257/04 , C07D261/18 , C07D277/56 , C07D277/74 , C07D285/125 , C07D471/04 , C07D473/38
摘要： A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)-alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, and R.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4 wherein Y is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.
摘要翻译：下式的新的硝基化合物：其中R 1和R 2各自为低级烷基或低级烷氧基（低级） - 烷基，或者将“IMAGE”环化形成X为-O - ， - S-或 - NH-，m为0或1的整数，R3为氨基甲酰基，低级烷基氨基甲酰基，低级烷酰基，二低级烷基氨基磺酰基，低级烷基磺酰基，氨甲酰基或下式基团： - （Y）n -R4其中Y为-CO - ， - SO 2 - ， - COCH 2 - 或者N 2是0或1的整数，R 4是任选地被一个或多个选自低级烷基，低级烷氧基，苯基，氨基甲酰基，卤素，氨基，低级烷硫基，羟基，低级烷基磺酰基氨基和氨基甲酰基甲基及其药学上可接受的盐，其可用作血管扩张剂。

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