公开(公告)号：US4166064A

公开(公告)日：1979-08-28

申请号：US877151

申请日：1978-02-13

申请人： Kiyoshi Kondo ,  Akira Negishi ,  Kikuo Sugimoto

发明人： Kiyoshi Kondo ,  Akira Negishi ,  Kikuo Sugimoto

IPC分类号： C07C67/30 ,  A01N20060101 ,  A01N53/00 ,  B01J31/00 ,  B01J31/02 ,  C07C20060101 ,  C07C23/04 ,  C07C61/04 ,  C07C67/00 ,  C07C67/317 ,  C07C69/74 ,  C07C253/00 ,  C07C255/39 ,  C07C313/00 ,  C07C319/20 ,  C07C323/12 ,  C07C323/19 ,  C07C323/62 ,  C07D209/48 ,  C07D209/49 ,  C07D307/42 ,  C07D307/45 ,  C07D307/54 ,  C07D317/48 ,  C07D317/50 ,  C07D317/54 ,  C07D317/60 ,  C07D319/16 ,  C07D333/16 ,  C07D333/24 ,  C07D333/26

CPC分类号： C07C67/317 ,  C07B2200/09 ,  C07C2101/02

摘要： A process is described whereby esters of 3-(2,2,2-trichloroethyl)-2,2-dimethylcyclopropane-1-carboxylic acid are prepared predominantly in their cis isomer form. The process comprises treating a 4,6,6,6-tetrachloro-3,3-dimethylhexanoate with an alkali metal tert-alkoxide under controlled conditions of temperature in the presence of a defined solvent-cosolvent mixture. The products of the process are intermediates in the production of pyrethroid insecticides.

摘要翻译： 描述了一种方法，其中3-（2,2,2-三氯乙基）-2,2-二甲基环丙烷-1-羧酸的酯主要以其顺式异构体形式制备。 该方法包括在限定的溶剂 - 共溶剂混合物的存在下，在温度控制条件下用碱金属叔醇盐处理4,6,6,6-四氯-3,3-二甲基己酸酯。 该方法的产物是生产拟除虫菊酯类杀虫剂的中间体。

公开(公告)号：US3946046A

公开(公告)日：1976-03-23

申请号：US315726

申请日：1972-12-15

申请人： Robert C. Kelly

发明人： Robert C. Kelly

IPC分类号： C07C405/00 ,  C07D263/04 ,  C07D307/93 ,  C07D307/935 ,  C07D317/12 ,  C07D317/14 ,  C07D317/26 ,  C07D319/06 ,  C07D319/16 ,  C07D307/83

CPC分类号： C07D263/04 ,  C07C405/00 ,  C07D307/93 ,  C07D307/935 ,  C07D317/12 ,  C07D317/14 ,  C07D317/26 ,  C07D319/06 ,  C07D319/16

摘要： Process for resolving a racemic mixture of an oxo-type prostaglandin intermediate by (a) converting the oxo compound by reaction with an optically active ephedrine to a mixture of oxazolidine diastereomers, (b) separating at least one oxazolidine diastereomer from said mixture, (c) hydrolyzing said oxazolidine to free the optically active oxo compound, and (d) recovering said optically active oxo compound.

摘要翻译： （a）通过与光学活性麻黄碱反应将氧代化合物与光学活性麻黄碱反应转化成恶唑烷非对映异构体的混合物来分离氧代型前列腺素中间体的外消旋混合物的方法，（b）从所述混合物中分离出至少一种恶唑烷非对映异构体，（c ）水解所述恶唑烷以游离光学活性氧化合物，和（d）回收所述光学活性氧化合物。

公开(公告)号：US3879423A

公开(公告)日：1975-04-22

申请号：US31569072

申请日：1972-12-15

申请人： UPJOHN CO

发明人： KELLY ROBERT C

IPC分类号： C07C405/00 ,  C07D263/04 ,  C07D307/93 ,  C07D307/935 ,  C07D317/12 ,  C07D317/14 ,  C07D317/26 ,  C07D319/06 ,  C07D319/16 ,  C07D13/04

CPC分类号： C07D263/04 ,  C07C405/00 ,  C07D307/93 ,  C07D307/935 ,  C07D317/12 ,  C07D317/14 ,  C07D317/26 ,  C07D319/06 ,  C07D319/16

摘要： Process for preparing (1) bycyclic lactone diols of the formula
WHEREIN W is 1-pentyl, cis 1-pent-2-enyl or 1-pent-2-ynyl, and (2) prostaglandins E3 and F3 in their racemic and optically active configurations, their enantiomorphs, their 15-epimers, and their esters; and the products prepared therein. The diols are useful intermediates in preparing prostaglandins having pharmacological utility.

摘要翻译： 制备（1）式WHEREIN W的环内酯二醇的方法是1-戊基，顺式1-戊-2-烯基或1-戊-2-炔基，和（2）前列腺素E3和F3α的外消旋和光学 活性构型，它们的对映体，它们的15-差向异构体及其酯; 及其中制备的产品。 二醇在制备具有药理学实用性的前列腺素中是有用的中间体。

公开(公告)号：US3818045A

公开(公告)日：1974-06-18

申请号：US31536772

申请日：1972-12-15

申请人： UPJOHN CO

发明人： KELLY R

IPC分类号： C07C405/00 ,  C07D263/04 ,  C07D307/93 ,  C07D307/935 ,  C07D317/12 ,  C07D317/14 ,  C07D317/26 ,  C07D319/06 ,  C07D319/16 ,  C07D5/32

CPC分类号： C07D263/04 ,  C07C405/00 ,  C07D307/93 ,  C07D307/935 ,  C07D317/12 ,  C07D317/14 ,  C07D317/26 ,  C07D319/06 ,  C07D319/16

摘要： WHEREIN W is 1-pentyl, cis 1-pent-2-enyl or 1-pent-2-ynyl, and (2) prostaglandins E3 and F3 in their racemic and optically active configurations, their enantiomorphs, and their 15-epimers; and the products prepared therein. The diols are useful intermediates in preparing prostaglandins having pharmacological utility.

Process for preparing (1) bicyclic lactone diols of the formula

摘要翻译： 制备（1）式WHEREIN W的双环内酯二醇的方法是1-戊基，顺式1-戊-2-烯基或1-戊-2-炔基，和（2）其外消旋和光学上的前列腺素E3和F3α 活性构型，它们的对映体和它们的15-差向异构体; 及其中制备的产品。 二醇在制备具有药理学实用性的前列腺素中是有用的中间体。

公开(公告)号：US3816462A

公开(公告)日：1974-06-11

申请号：US31537172

申请日：1972-12-15

申请人： UPJOHN CO

发明人： KELLY R

IPC分类号： C07C405/00 ,  C07D263/04 ,  C07D307/93 ,  C07D307/935 ,  C07D317/12 ,  C07D317/14 ,  C07D317/26 ,  C07D319/06 ,  C07D319/16 ,  C07D5/32

CPC分类号： C07D263/04 ,  C07C405/00 ,  C07D307/93 ,  C07D307/935 ,  C07D317/12 ,  C07D317/14 ,  C07D317/26 ,  C07D319/06 ,  C07D319/16

摘要： PROCESS FOR PREPARING AN OPTICALLY ACTIVE TRICYCLIC LACTONE ALDEHYDE OF THE FORMULA

4-(O=CH-)PERHYDROCYCLOPROPA(3,4)CYCLOPENTA(1,2-B)FURAN-

2-ONE

OR THE MIRROR IMAGE THEREOF, OR A RACEMIC COMPOUND OF THAT FORMULA AND THE MIRROR IMAGE THEREOF, WHEREIN $ INDICATES ATTACHMENT OF THE MOIETY TO THE CYCLOPROPANE RING IN EXO OR ENDO CONFIGURATION. THE TRICYCLIC LACTONE ALDEHYDES ARE USEFUL INTERMEDIATES IN PREPARING PROSTAGLANDINS HAVING PHARMACOLOGICAL UTILITY.

公开(公告)号：US20240101510A1

公开(公告)日：2024-03-28

申请号：US18241104

申请日：2023-08-31

申请人： Texas Crop Science

发明人： Matthew Duncton ,  Jeffrey D. Fowler ,  John Clough ,  Tanya Sabharwal ,  Simon Hiebert

IPC分类号： C07C311/21 ,  C07C247/10 ,  C07D213/42 ,  C07D215/12 ,  C07D217/12 ,  C07D237/08 ,  C07D239/26 ,  C07D241/12 ,  C07D317/58 ,  C07D319/16 ,  C07D333/34

CPC分类号： C07C311/21 ,  C07C247/10 ,  C07D213/42 ,  C07D215/12 ,  C07D217/12 ,  C07D237/08 ,  C07D239/26 ,  C07D241/12 ,  C07D317/58 ,  C07D319/16 ,  C07D333/34

摘要： Disclosed herein are apyrase inhibitors of Formula (I)




Also disclosed herein are methods for using the disclosed inhibitors, including in methods for protecting crops from pests. In one aspect the apyrase inhibitors are useful for enhancing the activity of pesticides for the protection of crops from pathogens and to support crop yield.

公开(公告)号：US20230348412A1

公开(公告)日：2023-11-02

申请号：US18000099

申请日：2021-05-26

申请人： Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd.

发明人： Fan HU ,  Yubao ZHOU ,  Li FANG ,  Haiwen HU ,  Zhongjun XU

IPC分类号： C07D319/16 ,  C07D491/056

CPC分类号： C07D319/16 ,  C07D491/056

摘要： The present invention relates to a method for preparing GLP-1 receptor agonist, specifically relates to an industrialized method for preparing a GLP-1 receptor agonist (S)-2-(3S,8S)-3-(4-(3,4-dichlorobenzyloxy)phenyl-7-((S)-1-phenylpropyl)-2,3,6,7,8,9-hexahydro-[1,4]-dioxino[2,3-g]isoquinolin-8-ylformylamino)-3-(4-(2,3-dimethylpyridin-4-yl)phenyl)propanoic acid dihydrochloride (compound I). The method utilizes compound 1 as the starting material, which undergoes nucleophilic addition, hydrolysis, reduction ammoniation, cyclization, amide condensation, hydrolysis, and salt forming reaction to give compound I. The method for preparing compound I has a total yield of more than 35%, with purity of compound I more than 98%.

公开(公告)号：US20230053726A1

公开(公告)日：2023-02-23

申请号：US17241662

申请日：2021-04-27

申请人： BioSplice Therapeutics, Inc.

发明人： Sunil Kumar KC ,  David Mark Wallace ,  John Hood ,  Charlene F. Barroga

IPC分类号： C07D411/06 ,  C07D213/50 ,  C07D317/46 ,  C07D319/16 ,  C07D327/06 ,  C07D339/08 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D263/56 ,  C07D311/58 ,  C07D317/54 ,  C07D319/18 ,  C07D231/56 ,  C07D333/54 ,  C07D235/06 ,  C07D407/06 ,  C07D413/06 ,  C07D307/80 ,  A61P25/00

摘要： The present disclosure provides γ-diketones or analogs thereof, that activate Wnt/β-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.

公开(公告)号：US20220281835A1

公开(公告)日：2022-09-08

申请号：US17627996

申请日：2020-02-24

申请人： SPECIAL PRODUCT'S LINE S.P.A.

发明人： Sabrina DALLAVALLE ,  Claudio PISANO ,  Massimiliano FLORIO ,  Claudio CAMPONESCHI

IPC分类号： C07D319/16 ,  A61P31/04 ,  C07C255/36 ,  C07C39/23 ,  C07C59/54 ,  C07C255/41 ,  C07C233/47 ,  C07C235/34 ,  C07C251/40 ,  C07C251/48 ,  C07C251/60 ,  C07C279/14

摘要： Phenol derivatives of general formula (I) and (II), wherein meanings of the substituents are indicated in the description, their pharmaceutically acceptable salts, together with the processes for their preparation, their use as antimicrobial, antibacterial, bactericide agents and the corresponding pharmaceutical compositions are disclosed.

公开(公告)号：US10941129B2

公开(公告)日：2021-03-09

申请号：US16303646

申请日：2017-05-23

申请人： Institute of Materia Medica, Chinese Academy of Medical Sciences ,  Tianjin Chase Sun Pharmaceutical Co., LTD

发明人： Zhiqiang Feng ,  Xiaoguang Chen ,  Yang Yang ,  Fangfang Lai ,  Ming Ji ,  Lijing Zhang ,  Yi Zheng ,  Nina Xue ,  Ke Wang ,  Ling Li

IPC分类号： C07D295/155 ,  C07C233/36 ,  C07C255/54 ,  C07D405/12 ,  C07C311/05 ,  C07D319/18 ,  C07D207/16 ,  C07C45/61 ,  C07C231/12 ,  C07D401/14 ,  A61P35/00 ,  C07C211/29 ,  C07C229/36 ,  C07C235/34 ,  C07D221/00 ,  C07D265/30 ,  C07D407/12 ,  C07D269/02 ,  C07C271/64 ,  C07C227/12 ,  C07C269/02 ,  C07D207/08 ,  C07D309/14 ,  C07D319/16 ,  A61K31/36 ,  A61K31/165 ,  A61K31/277 ,  A61K45/06

摘要： The present invention discloses a benzyl phenyl ether derivative, a preparation method therefor, and a pharmaceutical composition and uses thereof. Specifically, the invention relates to benzyl phenyl ether derivatives represented by formula (I), a pharmaceutically-acceptable salt thereof, a stereoisomer thereof, a preparation method therefor, a pharmaceutical composition containing the one or more compounds, and uses of the compounds in treating diseases related to PD-1/PD-L1 signal channels, such as cancers, infectious diseases and autoimmune diseases.