专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20200247777A1 DERIVATIVES OF EPA ENDOCANNABINOID EPOXIDES AS ANTI-INFLAMMATORY, ANTI-CANCEROUS, ANTI-ANGIOGENC AND ANTIPLATELET AGGREGATION COMPOUNDS 审中-公开
公开(公告)号：US20200247777A1
公开(公告)日：2020-08-06
申请号：US16648953
申请日：2018-09-20
申请人： The Board of Trustees of the University of Illinois
发明人： Aditi Das , Josephine E. Watson
IPC分类号： C07D331/02 , C07D303/46 , C07D203/08 , A61P29/00
摘要： The present disclosure provides chemical compound derivatives of a class of biological lipid mediators known as endocannabinoids and methods of synthesizing the compositions. These compounds are useful for treating cancer, reducing inflammation, reducing platelet aggregation, and reducing angiogenesis.

2. 发明申请

US20190161490A1 NOVEL ARYL ETHENE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT 审中-公开
公开(公告)号：US20190161490A1
公开(公告)日：2019-05-30
申请号：US16313351
申请日：2016-09-13
申请人： Sung Yeoun Hwang , KEMIMEDI CO.LTD
发明人： Sung Yeoun HWANG , Sung Jin CHO , Jina KIM , Jungwook CHIN , Hayoung HWANG , In-Kyu LEE , Yong-Hyun JEON , Jaetae LEE , Jae-Han JEON , Sang Wook KIM
IPC分类号： C07D487/10 , C07D487/04 , C07D295/08 , C07D203/08 , C07D205/04 , C07D207/06 , C07D209/52 , C07D209/54 , C07D249/06 , C07D401/04 , C07D405/06
摘要： The present invention relates to an aryl ethene derivative, for inhibiting an estrogen-related receptor gamma (ERRγ) activity, a prodrug of same, a solvate of same, a stereoisomer of same or pharmaceutically acceptable salts of same, and a pharmaceutical composition containing same as an active ingredient.

3. 发明授权

US10214598B2 (Meth)acrylate compound, and copolymer and homopolymer comprising repeating unit derived from same 有权
公开(公告)号：US10214598B2
公开(公告)日：2019-02-26
申请号：US15508809
申请日：2015-09-25
申请人： LG CHEM, LTD.
发明人： Kwang Seung Park , Mi Rin Lee , Jun Wuk Park , Eunsoo Huh , Sung Hyun Jeon
IPC分类号： C08F20/06 , C08F22/36 , C07C57/04 , C07D203/08 , C07C275/04 , C07C219/08 , C08L33/04 , C07C275/10 , C07C57/13 , C08F18/04 , C08F22/10
摘要： The present specification relates to a (meth)acrylate compound, and a copolymer and a homopolymer including a repeating unit derived therefrom.

4. 发明授权

US09822058B2 Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof 有权
公开(公告)号：US09822058B2
公开(公告)日：2017-11-21
申请号：US14390190
申请日：2013-03-13
申请人： CHDI FOUNDATION, INC.
发明人： Leticia M. Toledo-Sherman , Celia Dominguez , Michael Prime , William Leonard Mitchell , Peter Johnson , Naomi Went
IPC分类号： C07C62/38 , C07D307/94 , C07D309/10 , C07D215/18 , C07D311/58 , C07D317/46 , C07D317/60 , C07D319/18 , C07D233/64 , C07D235/26 , C07D403/10 , C07D405/08 , C07D405/10 , C07D405/12 , C07C317/44 , C07D413/08 , C07D413/10 , C07C323/62 , C07C229/22 , C07C229/46 , C07C229/48 , C07D257/04 , C07D203/08 , C07D263/58 , C07C235/82 , C07D207/08 , C07D271/07 , C07D207/337 , C07D295/155 , C07D305/06 , C07D305/08 , C07D307/54 , C07D307/80 , C07C69/757 , C07D203/10 , C07D307/79 , C07D413/12 , C07H15/20
CPC分类号： C07C62/38 , C07C69/757 , C07C229/22 , C07C229/46 , C07C229/48 , C07C235/82 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2602/50 , C07D203/08 , C07D203/10 , C07D207/08 , C07D207/337 , C07D215/18 , C07D233/64 , C07D235/26 , C07D257/04 , C07D263/58 , C07D271/07 , C07D295/155 , C07D305/06 , C07D305/08 , C07D307/54 , C07D307/79 , C07D307/80 , C07D307/94 , C07D309/10 , C07D311/58 , C07D317/46 , C07D317/60 , C07D319/18 , C07D403/10 , C07D405/08 , C07D405/10 , C07D405/12 , C07D413/08 , C07D413/10 , C07D413/12 , C07H15/20
摘要： Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

5. 发明授权

US09732034B2 Method and catalyst for synthesising aziridine 有权
公开(公告)号：US09732034B2
公开(公告)日：2017-08-15
申请号：US14404123
申请日：2013-05-31
申请人： University of East Anglia
发明人： Sean Patrick Bew , Sean Michael Thurston , Paolo Pesce
IPC分类号： C07D421/00 , C07D203/02 , C07D203/14 , C07D203/18 , C07D203/22 , B01J31/02 , C07D203/08 , C07D403/04 , C07D413/06 , C07F9/24
CPC分类号： C07D203/02 , B01J31/0264 , C07B2200/05 , C07D203/08 , C07D203/14 , C07D203/18 , C07D203/22 , C07D403/04 , C07D413/06 , C07F9/2483
摘要： The present invention relates to methods of synthesizing aziridines including isotopically labelled aziridines, said methods comprising contacting an imine or one or more precursors thereof with a diazo compound in the presence of a phosphoramide or a phosphoramide-derived catalyst. The present invention also relates to aziridines, modified aziridines and aziridine-derived compounds preparable by the aforementioned methods, and to phosphoramide or phosphoramide-derived catalysts suitable for use in such methods.

6. 发明授权

US09187419B2 Intermediates of sitagliptin and preparation process thereof 有权
标题翻译：西他列汀中间体及其制备方法
公开(公告)号：US09187419B2
公开(公告)日：2015-11-17
申请号：US13988261
申请日：2011-12-01
申请人： Xianhua Pan , Weijin Li , Qunhui Zhang , Libo Ruan , Wansheng Yu , Fei Deng , Tianhua Ma , Mingwang Huang , Minhuan He
发明人： Xianhua Pan , Weijin Li , Qunhui Zhang , Libo Ruan , Wansheng Yu , Fei Deng , Tianhua Ma , Mingwang Huang , Minhuan He
IPC分类号： C07C211/34 , C07C323/25 , C07C209/62 , C07D203/08 , C07D203/10 , C07D203/24 , C07D487/04 , C07C271/22 , C07C319/20 , C07F7/10
CPC分类号： C07C323/25 , C07C209/62 , C07C271/22 , C07C319/20 , C07D203/08 , C07D203/10 , C07D203/24 , C07D487/04 , C07F7/10 , C07C211/27
摘要： Disclosed are intermediates of Sitagliptin, a preparation process thereof, and a process for synthesizing Sitagliptin using these intermediates. Sitagliptin is synthesized by using chiral amino compounds as a raw material, without having to build a chiral center with a chiral asymmetric catalytic hydrogenation, and high-pressure hydrogenation is avoided.
摘要翻译：公开了西他列汀的中间体，其制备方法以及使用这些中间体合成西他列汀的方法。西他列汀以手性氨基化合物为原料合成，不需要用手性不对称催化氢化反应形成手性中心，避免了高压氢化。

7. 发明申请

US20100191000A1 METHOD FOR SYNTHESIZING AN N-UNSUBSTITUTED OR N-SUBSTITUTED AZIRIDINE 审中-公开
标题翻译：合成N-取代或N-取代的AZIRIDINE的方法
公开(公告)号：US20100191000A1
公开(公告)日：2010-07-29
申请号：US12665509
申请日：2008-06-18
申请人： Johann-Peter Melder , Martin Ernst , Till Gerlach , Ekkehard Schwab , Csaba Varszegi , Bert Sels , Dirk de Vos
发明人： Johann-Peter Melder , Martin Ernst , Till Gerlach , Ekkehard Schwab , Csaba Varszegi , Bert Sels , Dirk de Vos
IPC分类号： C07D203/08 , C25B3/02
CPC分类号： C07D203/08 , C07D203/02
摘要： Process for preparing an N-unsubstituted or N-substituted aziridine of the formula which comprises reacting an olefin of the formula I where R1 to R5 are each, independently of one another, hydrogen, a linear or branched alkyl radical having from 1 to 16 carbon atoms, a hydroxyalkyl radical having from 1 to 4 carbon atoms, a cycloalkyl radical having from 5 to 7 carbon atoms, a benzyl or phenyl radical which in each case may be substituted in the o, m or p position of the phenyl radical by methoxy, hydroxy, chlorine or alkyl radicals having from 1 to 4 carbon atoms and the radical R1 or R2 together with the radical R3 or R4 may be closed to form a 5- to 12-membered ring or the radicals R1 and R2 may be closed to form a 5- to 12-membered ring, with ammonia or a primary amine of the formula R5NH2 in the presence of iodine or bromine.
摘要翻译：制备下式的N-未取代的或N-取代的氮丙啶的方法，其包括使式I的烯烃（其中R 1至R 5）彼此独立地彼此独立地为氢，具有1至16个碳原子的直链或支链烷基原子，具有1至4个碳原子的羟基烷基，具有5至7个碳原子的环烷基，苄基或苯基，其在每种情况下可以在苯基的o，m或p位置被甲氧基取代，羟基，氯或具有1至4个碳原子的烷基和基团R 1或R 2与基团R 3或R 4一起可以封闭以形成5至12元环，或者基团R 1和R 2可以被封闭在碘或溴的存在下与氨或式R 5 NH 2的伯胺形成5-至12元环。

8. 发明授权

US07109352B2 Process for producing optically active amino acid derivatives 失效
标题翻译：光学活性氨基酸衍生物的制备方法
公开(公告)号：US07109352B2
公开(公告)日：2006-09-19
申请号：US10716430
申请日：2003-11-20
申请人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
发明人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
IPC分类号： C07D203/02 , C07D203/08
CPC分类号： C07D203/08 , C07B2200/07 , C07C227/10 , C07C227/32 , C07C227/42 , C07C229/30 , C07C303/36 , C07D203/20 , C07D203/24 , C07C311/19 , C07C229/26
摘要： An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.
摘要翻译：光学活性氨基酸衍生物是通过N-保护光学活性3-卤代丙氨酸衍生物进行环化，或环化该衍生物进行N-保护而得到光学活性N-保护的氮丙啶-2-羧酸衍生物在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物，或通过N-保护光学活性3-卤代丙氨酸衍生物，由此得到N-保护的氮丙啶 -2-羧酸，其在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物。根据该方法，可以通过简单的方法从便宜的材料制备天然和非天然旋光氨基酸。

9. 发明申请

US20050143586A1 Process for producing optically active amino acid derivatives 失效
标题翻译：光学活性氨基酸衍生物的制备方法
公开(公告)号：US20050143586A1
公开(公告)日：2005-06-30
申请号：US10716430
申请日：2003-11-20
申请人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
发明人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
IPC分类号： C07C227/10 , C07C227/32 , C07C227/42 , C07C229/26 , C07C229/30 , C07C303/36 , C07C311/19 , C07D203/08 , C07D203/20 , C07D203/24 , C07D203/16
CPC分类号： C07D203/08 , C07B2200/07 , C07C227/10 , C07C227/32 , C07C227/42 , C07C229/30 , C07C303/36 , C07D203/20 , C07D203/24 , C07C311/19 , C07C229/26
摘要： An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.
摘要翻译：光学活性氨基酸衍生物通过N-保护光学活性3-卤代丙氨酸衍生物进行环化生成，或使该衍生物环化，接着进行N-保护，从而得到光学活性N-保护的氮丙啶-2-羧酸衍生物，在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物，或通过N-保护光学活性3-卤代丙氨酸衍生物，由此得到N-保护的氮丙啶 -2-羧酸，其在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物。根据该方法，可以通过简单的方法从便宜的材料制备天然和非天然旋光氨基酸。

10. 发明授权

US5789599A Aziridine compounds, methods of preparation and reactions thereof 失效
标题翻译：氮丙啶化合物，制备方法及其反应
公开(公告)号：US5789599A
公开(公告)日：1998-08-04
申请号：US239097
申请日：1994-05-06
申请人： Franklin A. Davis , Ping Zhou , Gaddampally Venkat Reddy
发明人： Franklin A. Davis , Ping Zhou , Gaddampally Venkat Reddy
IPC分类号： C07C315/02 , C07C317/46 , C07C319/20 , C07C323/41 , C07D203/08 , C07D203/24
CPC分类号： C07D203/08 , C07C315/02 , C07C319/20 , C07D203/24
摘要： Novel N-sulfinyl-2-carboxyaziridine compounds and novel N-hydrogen-2-hydroxymethylaziridine compounds are provided. The asymmetric synthesis of N-sulfinylaziridines is readily accomplished in high diastereomeric purity and good yield by the Darzens-type reaction of the metal enolate of an .alpha.-haloester and an enantiopure sulfinimine. Ring-opening of these aziridines affords .alpha.-amino acids and the otherwise difficult to prepare syn-.beta.-hydroxy-.alpha.-amino acids, both key structural units found in many bioactive materials. The N-sulfinyl radical may be selectively removed from the novel aziridine compounds by treatment with acid or base. Alternatively, the N-sulfinyl radical may be oxidized to provide the corresponding N-sulfonyl-aziridine, or reduced to form the corresponding 1H-2-hydroxymethylaziridine, either of which may subsequently be ring-opened to provide precursors to bioactive compounds.
摘要翻译：提供新的N-亚磺酰基-2-羧基氮丙啶化合物和新的N-氢-2-羟基甲基氮丙啶化合物。 N-亚氨基氮丙啶的不对称合成通过α-卤代醇金属烯醇化物和对映异构体亚硫酰亚胺的Darzens型反应，以高非对映纯度和良好的收率容易地实现。这些氮丙啶的开环提供α-氨基酸，否则难以制备顺式-β-羟基-α-氨基酸，这是许多生物活性材料中发现的关键结构单元。通过用酸或碱处理可以从新的氮丙啶化合物中选择性地除去N-亚硫酰基。或者，N-亚硫酰基可被氧化以提供相应的N-磺酰基 - 氮丙啶，或还原形成相应的1H-2-羟甲基氮丙啶，其中之一可随后被开环以提供生物活性化合物的前体。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式