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101. 发明授权

US11649206B2 Method for producing pyrrole compound 有权
公开(公告)号：US11649206B2
公开(公告)日：2023-05-16
申请号：US17350013
申请日：2021-06-17
申请人： Takeda Pharmaceutical Company Limited
发明人： Takashi Ouchi , Giho Goh , Sunmi Kim , Jinsoon Choi , Hunsoo Park
IPC分类号： C07C253/30 , C07D207/36 , B01J23/44 , C07B61/00 , C07C255/42 , C07D401/12 , C07D207/34 , B01J8/02 , B01J21/04 , B01J29/08 , C07B31/00 , C07B41/06 , C07C255/28
CPC分类号： C07D207/36 , B01J8/0278 , B01J21/04 , B01J23/44 , B01J29/08 , C07B31/00 , C07B41/06 , C07B61/00 , C07C253/30 , C07C255/28 , C07C255/42 , C07D207/34 , C07D401/12 , B01J2523/67 , B01J2523/68 , B01J2523/69 , B01J2523/824 , B01J2523/828 , B01J2523/847
摘要： The present invention provides a production method of a 3-cyanopyrrole compound possibly useful as an intermediate for pharmaceutical products. A production method of compound (II) including subjecting compound (I) to a reduction reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst. A production method of compound (III) including subjecting compound (I) to a reduction reaction followed by a cyclization reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst.

102. 发明授权

US11066362B2 Method for producing pyrrole compound 有权
公开(公告)号：US11066362B2
公开(公告)日：2021-07-20
申请号：US16739707
申请日：2020-01-10
申请人： Takeda Pharmaceutical Company Limited
发明人： Takashi Ouchi , Giho Goh , Sunmi Kim , Jinsoon Choi , Hunsoo Park
IPC分类号： C07D207/36 , C07D207/34 , B01J23/44 , C07B61/00 , C07C253/30 , C07C255/42 , C07D401/12 , B01J8/02 , B01J21/04 , B01J29/08 , C07B31/00 , C07B41/06 , C07C255/28
摘要： The present invention provides a production method of a 3-cyanopyrrole compound possibly useful as an intermediate for pharmaceutical products. A production method of compound (II) including subjecting compound (I) to a reduction reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst. A production method of compound (III) including subjecting compound (I) to a reduction reaction followed by a cyclization reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst.

103. 发明申请

US20200165214A1 ALBICIDIN DERIVATIVES, THEIR USE AND SYNTHESIS 审中-公开
公开(公告)号：US20200165214A1
公开(公告)日：2020-05-28
申请号：US16631737
申请日：2017-12-21
申请人： TECHNISCHE UNIVERSITÄT BERLIN
发明人： Roderich SUESSMUTH , Dennis KERWAT , Stefan GRAETZ , Iraj BEHROZ , Leonard VON ECKARDSTEIN , Patrick Michael DURKIN , Marius MORKUNAS , John WESTON
IPC分类号： C07D265/30 , C07D233/90 , C07D249/04 , C07D213/56 , C07D211/34 , C07C235/64 , C07C255/28 , A61P31/04 , C07D229/02
摘要： A chemical compound is provided according to general formula (1):

104. 发明授权

US07598419B2 Compounds for modulating cell proliferation 有权
标题翻译：用于调节细胞增殖的化合物
公开(公告)号：US07598419B2
公开(公告)日：2009-10-06
申请号：US10593851
申请日：2005-03-22
申请人： Chaim M. Roifman , Peter Demin , Andrew Freywald , Thomas Grunberger , Olga Rounova , Nigel Sharfe
发明人： Chaim M. Roifman , Peter Demin , Andrew Freywald , Thomas Grunberger , Olga Rounova , Nigel Sharfe
IPC分类号： C07C255/28 , C07C255/29
CPC分类号： C07C255/41 , C07C255/42 , C07C317/46 , C07C327/44 , C07D213/40 , C07D307/52 , C07D317/58 , C07D317/60 , C07F7/1804 , C07F9/3826 , C07F9/4015
摘要： Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed.
摘要翻译：公开了可用于治疗各种细胞增殖性疾病如癌症的新型苯乙烯基丙烯腈化合物。

105. 发明申请

US20070142467A1 3-alkylaryl aspartate compounds and their use for selective enhancement of synaptic transmission 审中-公开
标题翻译： 3-烷基芳基天冬氨酸化合物及其用于选择性增强突触传递的用途
公开(公告)号：US20070142467A1
公开(公告)日：2007-06-21
申请号：US11256583
申请日：2005-10-21
申请人： Christopher Esslinger , Richard Bridges , Michael Kavanaugh
发明人： Christopher Esslinger , Richard Bridges , Michael Kavanaugh
IPC分类号： A61K31/277 , A61K31/198 , C07C255/28 , C07C229/38
CPC分类号： C07C229/36
摘要： The present invention provides an L-aspartate derivative compound represented by the following structure wherein Ar represents an aromatic group; L represents a linking moiety; R represents hydrogen, alkyl, aryl, or heteroaryl; and indicates that the stereochemistry at the 3-position can be R or S. The compounds of the invention are useful for selectively inhibiting EAAT3 and for enhancing synaptic transmission. Additionally, the inventive compounds can be used to treat a patient suffering from Alzheimers disease or a neuropathy or a neurodegenerative disease in which L-glutamate transporter activity is involved in the onset of the disease.
摘要翻译：本发明提供由以下结构表示的L-天冬氨酸衍生物化合物，其中Ar表示芳族基团; L表示连接部分; R代表氢，烷基，芳基或杂芳基; “img id =”custom-character-00001“he =”1.78mm“wi =”4.91mm“file =”US20070142467A1-20070621-P00001.TIF“alt =”custom character“img-content =”character“img- format =“tif”/>表示3位的立体化学可以是R或S.本发明的化合物可用于选择性抑制EAAT3和增强突触传递。此外，本发明的化合物可用于治疗患有阿尔茨海默病或神经病变或神经变性疾病的患者，其中L-谷氨酸转运蛋白活性参与疾病发作。

106. 发明申请

US20060100457A1 Production process of gamma-cyhalothrin 有权
标题翻译： γ-氯氟氰菊酯的生产工艺
公开(公告)号：US20060100457A1
公开(公告)日：2006-05-11
申请号：US10539265
申请日：2003-12-09
申请人： Stephen Brown , Brian Gott
发明人： Stephen Brown , Brian Gott
IPC分类号： C07C255/28
CPC分类号： C07C253/30 , C07B2200/07 , C07B2200/09 , C07C253/34 , C07C255/39 , C07C2601/02
摘要： A process for the preparation of gamma-cyahlothrin comprising a) chlorinating 1R cis-Z 3-(2-chloro-3,3,3-triflu-oro-1-propenyl)-2,2-dimethyl cyclopropanecarboxylic acid to give 1R cis-Z 3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethyl cy-clopropanecarboxylic acid chloride; b) esterifying 1R cis-Z 3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethyl cyclopropanecarboxylic acid chloride with 3-phenoxy benzaldehyde in the presence of a source of cyanide to form a diastereoisomeric mixture of cyhalothrin isomers and c) epimerising the diastereoisomeric mixture under conditions in which the least soluble diastereoisomer crystallises from solution.
摘要翻译：一种制备γ-氰基丙烯腈的方法，包括a）将1R顺式-Z-（2-氯-3,3,3-三氟-1-丙烯基）-2,2-二甲基环丙烷甲酸氯化，得到1R顺式 -Z 3-（2-氯-3,3,3-三氟-1-丙烯基）-2,2-二甲基环丙烷甲酰氯; b）在氰化源存在下，用3-苯氧基苯甲醛酯化1R顺式-Z-（2-氯-3,3,3-三氟-1-丙烯基）-2,2-二甲基环丙烷甲酰氯以形成三氟氯氰菊酯异构体的非对映异构体混合物和c）在溶液中结晶最小溶解非对映异构体的条件下使非对映异构体混合物差向异构化。

107. 发明申请

US20060069261A1 Alkynyl compounds as non nucleoside reverse transcriptase inhibitors 有权
标题翻译：炔基化合物作为非核苷逆转录酶抑制剂
公开(公告)号：US20060069261A1
公开(公告)日：2006-03-30
申请号：US11238732
申请日：2005-09-29
申请人： Pierre Bonneau , Patrick Deroy , Alexandre Gagnon , Jeffrey O'Meara , Bruno Simoneau , Christiane Yoakim
发明人： Pierre Bonneau , Patrick Deroy , Alexandre Gagnon , Jeffrey O'Meara , Bruno Simoneau , Christiane Yoakim
IPC分类号： C07D213/72 , C07C255/28
CPC分类号： C07C235/24 , C07C235/84 , C07C237/10 , C07C237/24 , C07C255/56 , C07C2601/02 , C07C2601/04 , C07D205/04 , C07D207/10 , C07D207/16 , C07D211/62 , C07D213/75 , C07D213/81 , C07D213/82 , C07D213/89 , C07D295/088 , C07D295/15 , C07D295/32 , C07D307/33
摘要： Inhibitors of HIV reverse transcriptase which are useful for the treatment of HIV infection. Exemplars of the invention are compounds of the formula wherein the substituents are as defined in the following table. R1R2R4R5R8a FCF3MeH—OH FCF3ClH—OH FCF3MeH—O—CH2CO2H ClCNClH—OH
摘要翻译：可用于治疗HIV感染的HIV逆转录酶抑制剂。本发明的实例是下式的化合物

108. 发明授权

US5108652A Cyclohexane derivatives 失效
标题翻译：环己酮衍生物
公开(公告)号：US5108652A
公开(公告)日：1992-04-28
申请号：US572313
申请日：1990-08-24
申请人： Rudolf Eidenschink , Gunther Haas , Ludwig Pohl , Michael Romer , Bernhard Scheuble , Georg Weber
发明人： Rudolf Eidenschink , Gunther Haas , Ludwig Pohl , Michael Romer , Bernhard Scheuble , Georg Weber
IPC分类号： C07C13/28 , C07C17/08 , C07C17/18 , C07C23/18 , C07C43/184 , C07C43/21 , C07C43/225 , C07C69/75 , C07C255/28 , C07C255/45 , C07D211/14 , C07D239/26 , C07D239/36 , C07D317/14 , C09K19/00 , C09K19/30 , C09K19/32 , C09K19/34 , C09K19/52 , G02F1/13
CPC分类号： C07D239/26 , C07C13/28 , C07C17/08 , C07C17/18 , C07C23/18 , C07C255/00 , C07C43/184 , C07C43/21 , C07C43/225 , C07D211/14 , C07D317/14 , C09K19/3001 , C09K19/321 , C09K19/3402 , C09K19/3441 , C09K19/3469 , C09K19/3483 , C07C2101/14 , C09K2019/3422
摘要： Cyclohexane derivatives of formula IR.sup.1--(A.sup.1).sub.m 13 Z.sup.1 --A--Z.sup.2 --(A.sup.2).sub.n --R.sup.2 Iwherein R.sup.1 and R.sup.2 are each H, an alkyl group which has 1-10 C atoms and in which one or two CH.sub.2 groups can also be replaced by 0 atoms, F, Cl, Br, CN or --O--COR, A.sup.1 and A.sup.2 are each 1,4-phenylene, 1,4-cyclohexylene, 1,3-dioxane-2,5-diyl, piperidine-1,4-diyl, 1,4-bicyclo(2,2,2)-octylene or pyrimidine-2,5-diyl groups which are unsubstituted or substituted by 1-4 F atoms, A is a 1,4-cyclohexylene group which is substituted in the 1-position and/or 4-position by alkyl, alkoxy, fluorinated alkyl or fluorinated alkoxy, each of which has 1-5 C atoms, F, Cl, Br and/or CN and which can also carry 1 or 2 further F, Cl or Br atoms and/or CN groups, Z.sup.1 and Z.sup.2 are each --CO--O--, --O--CO--, --CH.sub.2 CH.sub.2 --, --OCH.sub.2 --, --CH.sub.2 O-- or a single bond, R is an alkyl group which has 1-5 C atoms, m is 1 or 2 and n is 0 or 1, it being possible, where m=2, for the two groups A.sup.1 to be identical or different from one another; and the acid addition salts of those compounds which are basic,are suitable for use as components of liquid-crystal dielectrics.

109. 发明授权

US4699992A 3-amino-2-benzoylacrylic acid derivatives 失效
标题翻译： 3-氨基-2-苯甲酰基丙烯酸衍生物
公开(公告)号：US4699992A
公开(公告)日：1987-10-13
申请号：US775202
申请日：1985-09-12
申请人： Klaus Grohe
发明人： Klaus Grohe
IPC分类号： C07C255/42 , C07C67/00 , C07C69/618 , C07C211/00 , C07C225/16 , C07C227/00 , C07C227/16 , C07C229/24 , C07C229/34 , C07C229/36 , C07C231/00 , C07C231/12 , C07C231/14 , C07C233/02 , C07C237/16 , C07C237/20 , C07C253/00 , C07C253/30 , C07C255/28 , C07C255/30 , C07C255/56 , C07C255/58 , C07D295/04 , C07D295/14 , C07D295/145 , C07C121/78 , C07C69/533
CPC分类号： C07D295/145 , C07C255/00
摘要： Novel 3-amino-2-benzoyl-acrylic acid derivatives of the formula ##STR1## in which R.sup.1 represents the nitrile group, an ester group --COOR.sup.4 or carboxamide group ##STR2## R.sup.4 denoting C.sub.1 -C.sub.6 -alkyl, and R.sup.5 and R.sup.6 representing hydrogen or C.sub.1 -C.sub.3 -alkyl or phenyl,R.sup.2 and R.sup.3, which can be identical or different, represent a C.sub.1 -C.sub.6 -alkyl radical and, furthermore, can form, together with the nitrogen atom to which they are bonded, a 5- or 6-membered heterocyclic ring which can additionally contain as ring member the atoms or groups --O--, --S--, --SO-- or --SO.sub.2 --,X represents halogen,X.sup.1 denotes hydrogen, methyl, nitro or halogen,X.sup.2 denotes halogen or methyl, andX.sup.3 denotes hydrogen or halogen,are prepared by reacting ##STR3## The products can be converted into known antibacterials.
摘要翻译：新颖的3-氨基-2-苯甲酰基 - 丙烯酸衍生物，其中R1代表腈基，酯基-COOR4或羧酰胺基，R4代表C1-C6-烷基，R5和R6代表氢或C 1 -C 3 - 烷基或苯基，可以相同或不同的R 2和R 3表示C 1 -C 6烷基，并且还可以与它们所键合的氮原子一起形成5- 或6元杂环，其可以另外含有原子或基团-O - ， - S - ， - SO-或-SO 2 - ，X表示卤素，X 1表示氢，甲基，硝基或卤素，X 2表示卤素或甲基，X 3表示氢或卤素，可通过使产物反应成已知的抗菌剂。

110. 发明授权

US11225465B2 Albicidin derivatives, their use and synthesis 有权
公开(公告)号：US11225465B2
公开(公告)日：2022-01-18
申请号：US16631737
申请日：2017-12-21
申请人： TECHNISCHE UNIVERSITÄT BERLIN
发明人： Roderich Suessmuth , Dennis Kerwat , Stefan Graetz , Iraj Behroz , Leonard Von Eckardstein , Patrick Michael Durkin , Marius Morkunas , John Weston
IPC分类号： C07C229/02 , C07C235/64 , C07C255/28 , C07D211/34 , C07D211/66 , C07D213/56 , C07D229/02 , C07D233/64 , C07D233/90 , C07D249/04 , C07D265/30 , C07D295/15 , A61P31/04
摘要： A chemical compound is provided according to general formula (1):

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