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1. 发明授权

US12037339B2 Substituted imidazoles as GLP-1 receptor agonists 有权
公开(公告)号：US12037339B2
公开(公告)日：2024-07-16
申请号：US17380084
申请日：2021-07-20
申请人： Eccogene Inc.
发明人： Zaifang Ren , Xuefeng Sun , Jingye Zhou
IPC分类号： A61K31/4166 , C07D233/04 , C07D487/04 , C07D519/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The application relates to a compound of Formula (I):

or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of GLP-1 receptor, a pharmaceutical composition comprising a compound of Formula (I), and a method of treating or preventing a disease in which GLP-1 receptor plays a role.

2. 发明授权

US11945787B2 Substituted imidazoles for preventing and/or treating cell or tissue necrosis 有权
公开(公告)号：US11945787B2
公开(公告)日：2024-04-02
申请号：US17201201
申请日：2021-03-15
申请人： Ela Pharma Ltd
发明人： Ilana Nathan , Boris Khalfin
IPC分类号： C07D233/04 , A61K31/00 , A61K31/167 , A61K31/4045 , A61K31/415 , A61K31/4178 , A61K31/4196 , A61K31/426 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/536 , A61K45/06 , A61P25/00 , C07C233/24 , C07D233/44 , C07D233/48 , C07D265/22 , C07D275/06 , C07D277/42 , C07D277/56 , C07D405/06 , C07D417/12 , C12N5/077 , C12N15/113
CPC分类号： C07D265/22 , A61K31/00 , A61K31/167 , A61K31/4045 , A61K31/415 , A61K31/4178 , A61K31/4196 , A61K31/426 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/536 , A61K45/06 , A61P25/00 , C07C233/24 , C07D233/44 , C07D233/48 , C07D275/06 , C07D277/42 , C07D277/56 , C07D405/06 , C07D417/12 , C12N5/0669 , C12N15/1137 , C12Y304/14001 , C12Y304/21036 , C12N2310/14 , C12N2501/30 , C12N2501/999
摘要： Inhibitor compounds and agents of Cathepsin C, CELA1, CELA3A and/or structurally related molecules thereto, compositions comprising the same, and uses thereof in the inhibition and/or prevention of cell and/or tissue necrosis are described. The compounds include imidazoles of Formula VI:

wherein G1 is pyrrolidine, pyrazolidine, imidazolidine piperidine, or piperazine and G2 is alkyl, cycloalkyl, heterocycle, or aryl. The pyrrolidine, pyrazolidine, imidazolidine, piperidine, or piperazine of G1 and the alkyl, cycloalkyl, heterocycle, or aryl of G2 are optionally substituted with one or more substituents independently selected from the group consisting of halogen, NO2, CN, C1-C6 alkyl, C1-C6 haloalkyl, NH2, OH, OC1-C6 alkyl, C(O)H, C(O)C1-C6 alkyl, C(O)NH2, C(O)OH, and C(O)OC1-C6 alkyl. Variations applications for the described compounds, and combination therapies are further described as well.

3. 发明授权

US09266821B2 Process for making fatty amides 有权
标题翻译：制备脂肪酰胺的方法
公开(公告)号：US09266821B2
公开(公告)日：2016-02-23
申请号：US12580467
申请日：2009-10-16
申请人： Upali Weerasooriya , John Boorem , Brian Hodle , Aaron Boorem , Peter Radford , Howard Stevenson , G. Gerald Barr
发明人： Upali Weerasooriya , John Boorem , Brian Hodle , Aaron Boorem , Peter Radford , Howard Stevenson , G. Gerald Barr
IPC分类号： C07D233/04 , C07C231/02 , C07C233/36
CPC分类号： C07C231/02 , C07D233/04 , C07C233/36
摘要： A process for reacting, in the presence of a particular calcium containing catalyst, an amine having an active hydrogen and one or more of a fatty acid ester or a fatty acid.
摘要翻译：在特定含钙催化剂存在下使具有活性氢和一种或多种脂肪酸酯或脂肪酸的胺反应的方法。

4. 发明授权

US09179675B2 Use of sarmentine and its analogs for controlling plant pests 有权
公开(公告)号：US09179675B2
公开(公告)日：2015-11-10
申请号：US14587929
申请日：2014-12-31
申请人： Marrone Bio Innovations, Inc.
发明人： Huazhang Huang , Ratnakar Asolkar
IPC分类号： A01N37/02 , A01N37/06 , A01N37/10 , A01N37/18 , A01N43/36 , A01N43/40 , A01N43/46 , C07C233/05 , C07C233/06 , C07C233/11 , C07D295/185 , C07C57/42 , C07D207/06 , C07D211/16 , C07D233/04 , C11B1/00 , C07C57/44 , C07C69/587 , C07C233/08
CPC分类号： A01N43/36 , A01N37/02 , A01N37/06 , A01N37/10 , A01N37/18 , A01N43/40 , A01N43/46 , C07C57/42 , C07C57/44 , C07C69/587 , C07C233/05 , C07C233/06 , C07C233/08 , C07C233/11 , C07C2601/08 , C07D207/06 , C07D211/16 , C07D223/04 , C07D233/04 , C07D295/185 , C11B1/00
摘要： Methods and compositions for controlling plant pests, particularly weeds and/or plant phytopathogens using sarmentine and/or analogs thereof are disclosed.

5. 发明授权

US08546571B2 Catalytic hydrogenation of ene-carbamates 有权
标题翻译：氨基甲酸酯的催化氢化
公开(公告)号：US08546571B2
公开(公告)日：2013-10-01
申请号：US12518416
申请日：2007-12-12
申请人： David Alexander Learmonth , Antonio Zanotti-Gerosa , Gabriela Alexandra Grasa , Alexander Beliaev
发明人： David Alexander Learmonth , Antonio Zanotti-Gerosa , Gabriela Alexandra Grasa , Alexander Beliaev
IPC分类号： C07F9/00 , C07F9/50 , C07D233/00 , C07D233/04 , C07D311/00 , C07D311/04
CPC分类号： C07D311/58
摘要： A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral catalyst and a source of hydrogen, wherein: X is CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 is alkyl or aryl, wherein: the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.
摘要翻译：一种制备式A化合物的S或R对映异构体的方法，该方法包括在手性催化剂和氢源存在下使式B化合物进行不对称氢化，其中：X为CH 2，氧或硫 ; R1，R2和R3相同或不同，表示氢，卤素，烷基，烷氧基，羟基，硝基，烷基羰基氨基，烷基氨基或二烷基氨基; 并且R 4是烷基或芳基，其中：术语烷基是指含有1-6个碳原子的直链或支链的烃链，任选地被芳基，烷氧基，卤素，烷氧基羰基或羟基羰基取代; 术语芳基是指任选被烷氧基，卤素或硝基取代的苯基或萘基; 术语卤素是指氟，氯，溴或碘。

6. 发明申请

US20100036127A1 Process 有权
标题翻译：处理
公开(公告)号：US20100036127A1
公开(公告)日：2010-02-11
申请号：US12518416
申请日：2007-12-12
申请人： David Alexander Learmonth , Antonio Zanotti-Gerosa , Gabriela Alexandra Grasa , Alexander Beliaev
发明人： David Alexander Learmonth , Antonio Zanotti-Gerosa , Gabriela Alexandra Grasa , Alexander Beliaev
IPC分类号： C07F9/50 , C07D311/04 , C07D233/04
CPC分类号： C07D311/58
摘要： A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral catalyst and a source of hydrogen, wherein: X is CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 is alkyl or aryl, wherein: the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.
摘要翻译：一种制备式A化合物的S或R对映异构体的方法，该方法包括在手性催化剂和氢源存在下使式B化合物进行不对称氢化，其中：X为CH 2，氧或硫 ; R1，R2和R3相同或不同，表示氢，卤素，烷基，烷氧基，羟基，硝基，烷基羰基氨基，烷基氨基或二烷基氨基; 并且R 4是烷基或芳基，其中：术语烷基是指含有1-6个碳原子的直链或支链的烃链，任选地被芳基，烷氧基，卤素，烷氧基羰基或羟基羰基取代; 术语芳基是指任选被烷氧基，卤素或硝基取代的苯基或萘基; 术语卤素是指氟，氯，溴或碘。

7. 发明申请

US20090137175A1 Sizing Composition For Glass Fibers, Sized Glass Fibers, And Reinforced Products Comprising The Same 审中-公开
标题翻译：玻璃纤维，大小玻璃纤维及其制品的上胶组合物
公开(公告)号：US20090137175A1
公开(公告)日：2009-05-28
申请号：US12267963
申请日：2008-11-10
申请人： Jacobus Hendricus Antonius Van Der Woude , Jacob Cornelius Dijt , John Theo Penning , Ronald Boelman , Johannes Leonardus Tabak
发明人： Jacobus Hendricus Antonius Van Der Woude , Jacob Cornelius Dijt , John Theo Penning , Ronald Boelman , Johannes Leonardus Tabak
IPC分类号： B32B17/02 , C07F9/28 , C07C309/00 , B32B17/10 , C07D233/04 , C07F7/02
CPC分类号： C03C25/26 , C03C25/40 , C08J5/08 , Y10T428/249948 , Y10T428/2964 , Y10T442/3049 , Y10T442/604
摘要： The present invention provides aqueous sizing compositions for application to glass fibers as well as polymeric resins reinforced with glass fibers at least partially coated with the aqueous sizing compositions. In some embodiments, sizing compositions of the present invention demonstrate advantageous properties resulting from the presence of an acid-amine component therein.
摘要翻译：本发明提供用于玻璃纤维的水性施胶组合物以及用至少部分涂覆有水性施胶组合物的玻璃纤维增强的聚合物树脂。在一些实施方案中，本发明的施胶组合物显示出由于其中存在酸 - 胺组分而产生的有利特性。

8. 发明授权

US07365210B2 Method for the production of chiral imidazolidin-2-ones 失效
标题翻译：制备手性咪唑烷-2-酮的方法
公开(公告)号：US07365210B2
公开(公告)日：2008-04-29
申请号：US10510439
申请日：2003-04-08
申请人： Hansgeorg Ernst , Jürgen Koppenhöfer , Daniela Klein
发明人： Hansgeorg Ernst , Jürgen Koppenhöfer , Daniela Klein
IPC分类号： C07D233/04
CPC分类号： C07D233/00
摘要： The invention relates to a process for preparing chiral imidazolidin-2-ones of the formula I in which R1 is C1-C8-alkyl, cyclohexyl, phenyl, a C1-C6-alkyl-, halo-, nitro-, C1-C6-alkoxy-, C1-C6-alkylmercapto- or CF3-substituted phenyl radical, naphthyl or a C1-C6-alkyl-, halo-, nitro-, C1-C6-alkoxy- or CF3-substituted naphthyl radical, R2 is C1-C8-alkyl, C2-C8-alkenyl, cyclohexyl, phenyl or a phenyl-C1-C6-alkyl radical which may be substituted by a nitro, C1-C6-alkoxy, methylenedioxy or CF3 radical, and R3 is C1-C12-alkyl, C2-C8-alkenyl, cyclohexyl, phenyl or a C1-C6-alkyl-, halo-, nitro-, C1-C6-alkoxy-, methylenedioxy-, dialkylamino- or CF3-substituted phenyl radical, by reacting a compound of the formula II or the salt thereof in which R1, R2 and R3 have the abovementioned meaning, with urea in the presence of an involatile ammonium salt, wherein the reaction is carried out in the presence of an aprotic polar organic solvent.
摘要翻译：本发明涉及一种制备其中R 1是C 1 -C 8 - 的式I的手性咪唑烷-2-酮的方法，烷基，环己基，苯基，C 1 -C 6 - 烷基 - ，卤代 - ，硝基 - ，C 1 -C 3 - C 6 - 烷氧基 - ，C 1 -C 6 - 烷基巯基或CF 3 - 取代的苯基，萘基或C C 1 -C 6 - 烷基 - ，卤代 - ，硝基 - ，C 1 -C 6 - 烷氧基 - 或CF 3 - 取代的萘基，R 2是C 1 -C 8 - 烷基，C _{和R 3具有上述含义，在非挥发性铵盐存在下用脲进行反应，其中反应在非质子极性有机溶剂的存在下进行。}

9. 发明申请

US20050288508A1 Catalytic depolymerization of polymers containing electrophilic linkages using nucleophilic reagents 失效
公开(公告)号：US20050288508A1
公开(公告)日：2005-12-29
申请号：US11208268
申请日：2005-08-18
申请人： James Hedrick , Gregory Nyce , Robert Waymouth
发明人： James Hedrick , Gregory Nyce , Robert Waymouth
IPC分类号： C07C59/285 , C07C67/03 , C07C68/06 , C07D233/02 , C07D233/04 , C07D233/06 , C07D233/16 , C07D233/54 , C07D307/33 , C07F1/00
CPC分类号： C07D233/16 , C07C59/285 , C07C67/03 , C07C68/06 , C07D233/02 , C07D233/04 , C07D233/06 , C07D233/54 , C07D307/33 , C07F1/00 , C07C69/82 , C07C69/96
摘要： A method is provided for carrying out depolymerization of a polymer containing electrophilic linkages in the presence of a catalyst and a nucleophilic reagent, wherein production of undesirable byproducts resulting from polymer degradation is minimized. The reaction can be carried out at a temperature of 80° C. or less, and generally involves the use of an organic, nonmetallic catalyst, thereby ensuring that the depolymerization product(s) are substantially free of metal contaminants. In an exemplary depolymerization method, the catalyst is a carbene compound such as an N-heterocyclic carbene, or is a precursor to a carbene compound. The method provides an important alternative to current recycling techniques such as those used in the degradation of polyesters, polyamides, and the like.

10. 发明授权

US06137007A Enantiomer compositions of (1R,4S)-1-butyrylamino-4-(hydroxymethyl)-2-cyclopentene 失效
标题翻译：（1R，4S）-1-丁酰氨基-4-（羟甲基）-2-环戊烯的对映体组成
公开(公告)号：US06137007A
公开(公告)日：2000-10-24
申请号：US373862
申请日：1999-08-13
申请人： Christine Bernegger , Eva Maria Urban , Olwen Mary Birch , Knut Burgdorf , Frank Brux , Kay-Sara Etter , Pierre Bossard , Walter Brieden , Laurent Duc , John Gordon , Colm O'Murchu , Yves Guggisberg
发明人： Christine Bernegger , Eva Maria Urban , Olwen Mary Birch , Knut Burgdorf , Frank Brux , Kay-Sara Etter , Pierre Bossard , Walter Brieden , Laurent Duc , John Gordon , Colm O'Murchu , Yves Guggisberg
IPC分类号： C12P41/00 , C07C231/18 , C07C231/20 , C07C233/23 , C07C271/24 , C07D209/94 , C07D233/04 , C07D233/74 , C07D235/02 , C07D237/06 , C07D239/70 , C07D473/40 , C12P13/00 , C12P13/02 , C12P17/18 , C12R1/01 , C12R1/05 , C12R1/06 , C12R1/09 , C12R1/19 , C12R1/38 , C07C215/42
CPC分类号： C07C231/18 , C07C233/23 , C07C271/24 , C07D209/94 , C12P13/001 , C12P13/02 , C12P17/182 , C07B2200/07 , C07C2101/10
摘要： A novel process for the preparation of (1S,4R)- or (1R,4S)-4-(2-amino-6-chloro-9H-purin-9-yl)-2-cyclopentene-1-methanol of the formulae ##STR1## is described. This entails in the first stage (.+-.)-2-azabicyclo[2.2.1]hept-5-en-3-one of the formula ##STR2## being acylated to give a (.+-.)-2-azabicyclo[2.2.1]hept-5-en-3-one derivative of the general formula ##STR3## in which R.sup.1 denotes C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, aryl or aryloxy, the latter being reduced in the second stage to give a cyclopentene derivative of the general formula ##STR4## in which R.sup.1 has the stated meaning, the latter then being converted in the third stage biotechnologically into the (1R,4S)- or (1S,4R)-1-amino-4-(hydroxymethyl)-2-cyclopentene of the formula ##STR5## the latter being converted in the fourth stage with N-(2-amino-4,6-dichloro-5-pyrimidinyl)formamide of the formula ##STR6## into the (1S,4R)- or (1R,4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentene-1-methanol of the formulae ##STR7## and the latter being cyclized in the fifth stage in a known manner to the final product of the formula I or II.
摘要翻译：制备式（1S，4R） - 或（1R，4S）-4-（2-氨基-6-氯-9H-嘌呤-9-基）-2-环戊烯-1-甲醇的新方法，被描述。这需要在被酰化的式（+/-）-2-氮杂双环[2.2.1]庚-5-烯-3-酮的第一阶段中得到（+/-）-2-氮杂双环[2.2.1 ]庚-5-烯-3-酮衍生物，其中R 1表示C 1-4 - 烷基，C 1-4 - 烷氧基，芳基或芳氧基，后者在第二阶段中还原，得到其中R 1具有所述含义的通式，后者在第三阶段中生物技术转化为（1R，4S） - 或（1S，4R）-1-氨基-4-（羟甲基）-2-环戊烯式（1R，4S）-4 - （（1S，4R） - 或（1R，4S）-4 - 2-氨基-6-氯-5-甲酰氨基-4-嘧啶基）氨基] -2-环戊烯-1-甲醇，后者在第五阶段以已知方式环化为式I的最终产物或II。

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