公开(公告)号：US20130267732A1

公开(公告)日：2013-10-10

申请号：US13994967

申请日：2011-12-13

Applicant: Miguel A. Guerra ,  Tatsuo Fukushi ,  Zai-Ming Qiu

Inventor： Miguel A. Guerra ,  Tatsuo Fukushi ,  Zai-Ming Qiu

IPC: C07C313/02

CPC classification number: C07C313/02 ,  C07C313/04

Abstract: There is provided a process for preparing a perfluorovinyl ether sulfinate, comprising: a) providing a perfluorovinyl ether sulfonyl halide; and (b) reducing the perfluorovinyl ether sulfonyl halide with a reducing agent in an organic protic solvent.

Abstract translation: 提供了制备全氟乙烯基醚亚磺酸盐的方法，包括：a）提供全氟乙烯基醚磺酰卤; 和（b）在有机质子溶剂中用还原剂还原全氟乙烯基醚磺酰卤。

公开(公告)号：US07300955B2

公开(公告)日：2007-11-27

申请号：US10789008

申请日：2004-02-27

Applicant: Jose Luis Castro Pineiro

Inventor： Jose Luis Castro Pineiro

IPC: A61K31/19 ,  A61K31/216 ,  C07C313/02 ,  C07C317/12 ,  C07C317/14

CPC classification number: C07C317/44 ,  A61K31/21 ,  C07C2601/14

Abstract: The invention provides the combined use of an inhibitor of formation or release of β-amyloid and a nitric oxide releaser for the treatment or prevention of Alzheimer's disease.

Abstract translation: 本发明提供了用于治疗或预防阿尔茨海默病的β-淀粉样蛋白形成或释放抑制剂和一氧化氮释放剂的组合使用。

公开(公告)号：US5859288A

公开(公告)日：1999-01-12

申请号：US620359

申请日：1996-03-22

Applicant: Gerard Forat ,  Jean-Manuel Mas ,  Laurent Saint-Jalmes

Inventor： Gerard Forat ,  Jean-Manuel Mas ,  Laurent Saint-Jalmes

IPC: C07B45/04 ,  C07C303/02 ,  C07C303/14 ,  C07C309/06 ,  C07C309/39 ,  C07C309/80 ,  C07C313/02 ,  C07C313/04

CPC classification number: C07C303/02 ,  C07C313/04

Abstract: The invention relates to a reagent which is useful for the synthesis of oxysulphide-containing fluorine-containing organic derivatives by reacting with an oxide of sulphur, especially sulphur dioxide, characterized in that it comprises:a) a fluorocarboxylic acid of formula E.sub.w --CF.sub.2 --COOH where E.sub.w is an electron-withdrawing group or atom which is at least partially salified by an organic or inorganic cation, andb) an aprotic polar solvent; andin that the content of releasable protons carried by its various components, including their impurities, is at most equal to half the initial molar concentration of the said fluorocarboxylic acid.This reagent can be used by heating in order to form fluorine-containing sulphinic or sulphonic acids.

Abstract translation: 本发明涉及一种用于通过与硫的氧化物，特别是二氧化硫反应来合成含氧硫化物的含氟有机衍生物的试剂，其特征在于它包括：a）式Ew-CF2-的氟代羧酸， COOH，其中Ew是吸电子基团或至少部分由有机或无机阳离子盐化的原子，和b）非质子极性溶剂; 并且由其各种组分（包括它们的杂质）携带的可释放质子的含量最多等于所述氟代羧酸的初始摩尔浓度的一半。 该试剂可以通过加热使用，以形成含氟亚磺酸或磺酸。

公开(公告)号：US4866190A

公开(公告)日：1989-09-12

申请号：US152029

申请日：1988-02-03

Applicant: Marc Tordeux ,  Bernard Langlois ,  Claude Wakselman

Inventor： Marc Tordeux ,  Bernard Langlois ,  Claude Wakselman

IPC: C07C309/06 ,  C07C67/00 ,  C07C301/00 ,  C07C303/02 ,  C07C303/32 ,  C07C309/80 ,  C07C313/00 ,  C07C313/02 ,  C07C313/04 ,  C07F1/08 ,  C07F3/06

CPC classification number: C07C313/04 ,  C07C309/00

Abstract: A process for the preparation of perhaloalkanesulfinic and -sulfonic acids and derivatives of these acids. A perhaloalkanesulfinic acid salt is prepared by contacting a metal hydroxymethanesulfinate (preferably, a sodium, zinc or copper hydroxymethanesulfinate) with a perhaloalkyl halide group, in a polar solvent. Optionally, the perhaloalkanesulfinic acid salt is then converted to a perhaloalkanesulfinic or -sulfonic acid or a derivative of either of these acids.

Abstract translation: 一种制备全卤代亚烷基亚磺酸和磺酸及其衍生物的方法。 通过在极性溶剂中使金属羟基甲基亚磺酸盐（优选钠，锌或铜羟基甲烷亚磺酸盐）与全卤烷基卤化物基团接触来制备全卤烷基亚磺酸盐。 任选地，将全卤代亚烷基亚磺酸盐转化成全卤代亚烷基亚磺酸或磺酸或这些酸中的任一种的衍生物。

公开(公告)号：US20240254075A1

公开(公告)日：2024-08-01

申请号：US18558726

申请日：2022-05-06

Applicant: Autobahn Therapeutics, Inc.

Inventor： Brian Andrew STEARNS ,  Jill Melissa BACCEI ,  Jason Randall HARRIS

IPC: C07C235/20 ,  A61K31/16 ,  A61K31/165 ,  A61K31/397 ,  A61K31/40 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/455 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/505 ,  A61K31/5375 ,  A61P25/00 ,  C07C235/16 ,  C07C235/22 ,  C07C235/24 ,  C07C243/28 ,  C07C255/29 ,  C07C259/06 ,  C07C313/02 ,  C07C317/28 ,  C07D205/04 ,  C07D213/75 ,  C07D237/20 ,  C07D237/22 ,  C07D239/42 ,  C07D241/20 ,  C07D261/14 ,  C07D295/18 ,  C07D305/08

CPC classification number: C07C235/20 ,  A61K31/16 ,  A61K31/165 ,  A61K31/397 ,  A61K31/40 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/455 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/505 ,  A61K31/5375 ,  A61P25/00 ,  C07C235/16 ,  C07C235/22 ,  C07C235/24 ,  C07C243/28 ,  C07C255/29 ,  C07C259/06 ,  C07C313/02 ,  C07C317/28 ,  C07D205/04 ,  C07D213/75 ,  C07D237/20 ,  C07D237/22 ,  C07D239/42 ,  C07D241/20 ,  C07D261/14 ,  C07D295/18 ,  C07D305/08 ,  C07C2601/02 ,  C07C2601/14

Abstract: Provided herein are fatty acid amide (FAAH) cleavable prodrugs of thyromimetics and pharmaceutical compositions comprising these compounds with at least one pharmaceutically acceptable excipient further comprising a peripherally restricted FAAH inhibitor.

公开(公告)号：US20220280496A1

公开(公告)日：2022-09-08

申请号：US17500039

申请日：2021-10-13

Applicant: AMGEN INC.

Inventor： Matthew BIO ,  Sebastien CAILLE ,  Brian COCHRAN ,  Yuanqing FANG ,  Brian M. FOX ,  Brian S. LUCAS ,  Lawrence R. MCGEE ,  Filisaty VOUNATSOS ,  Sean H. WIEDEMANN ,  Sarah WORTMAN

IPC: A61K31/451 ,  C07D211/94 ,  C07D491/048 ,  C07C309/25 ,  C07C309/04 ,  C07C313/02 ,  C07C309/35 ,  C07D498/04 ,  C07D211/76

Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

公开(公告)号：US10513483B2

公开(公告)日：2019-12-24

申请号：US16085163

申请日：2017-03-14

Applicant: SPIROCHEM AG

Inventor： Yoshikazu Suzuki ,  Daniel Jimenez-Teja ,  Christophe Salomé ,  Thomas Fessard

IPC: C07C67/343 ,  C07C45/68 ,  C07D263/16 ,  C07C235/82 ,  C07C245/18 ,  C07C67/31 ,  C07C67/313 ,  C07C67/317 ,  C07C259/08 ,  C07C1/28 ,  C07C227/18 ,  C07C231/02 ,  C07C51/353 ,  C07C231/12 ,  C07C303/22 ,  C07C303/30 ,  C07C303/40 ,  C07C313/02 ,  C07C313/04 ,  C07C313/06

Abstract: A process for the preparation of a class of molecules, namely bicyclo[1.1.1]pentanes and derivatives thereof by reaction of [1.1.1]propellane with a variety of reagents under irradiation and/or in the presence of radical initiators to obtain bicyclo[1.1.1]pentanes asymmetrically substituted at position 1 and 3, which are useful as intermediates for the preparation of asymmetrically 1,3-disubstituted bicyclo[1.1.1]pentane derivatives and various physiologically active substances or materials containing these structures.

公开(公告)号：US09801867B2

公开(公告)日：2017-10-31

申请号：US15175824

申请日：2016-06-07

Applicant: AMGEN INC.

Inventor： Matthew Bio ,  Sebastien Caille ,  Brian Cochran ,  Yuanqing Fang ,  Brian M. Fox ,  Brian S. Lucas ,  Lawrence R. McGee ,  Filisaty Vounatsos ,  Sean H. Wiedemann ,  Sarah Wortman

IPC: C07D211/76 ,  A61K31/451 ,  C07D211/94 ,  C07D491/048 ,  C07C309/25 ,  C07C309/04 ,  C07C313/02 ,  C07D498/04 ,  C07C309/35

CPC classification number: A61K31/451 ,  C07B2200/13 ,  C07C309/04 ,  C07C309/25 ,  C07C309/35 ,  C07C313/02 ,  C07D211/76 ,  C07D211/94 ,  C07D491/048 ,  C07D498/04

Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

公开(公告)号：US08354007B2

公开(公告)日：2013-01-15

申请号：US13121973

申请日：2009-09-28

Applicant: Martin Sukopp ,  Alexander Korte ,  Stefan Fülster ,  Michael Keil ,  Michael Rack

Inventor： Martin Sukopp ,  Alexander Korte ,  Stefan Fülster ,  Michael Keil ,  Michael Rack

IPC: B01D3/36 ,  C07D231/10 ,  C07C313/02

CPC classification number: C07D231/44 ,  C07C313/04

Abstract: The invention relates to a process for purifying trifluoromethanesulfinic acid by azeotropic distillation with an aromatic solvent, to processes for preparing purified trifluoromethanesulfinic acid and to the use of the purified trifluoronnethanesulfinic acid for preparing trifluoromethylsulfinylated pyrazole derivatives, especially fipronil.

Abstract translation: 本发明涉及一种通过与芳族溶剂共沸蒸馏纯化三氟甲磺酸的方法，以及用于制备纯化的三氟甲磺酸的方法，以及使用纯化的三氟甲磺酰亚胺制备三氟甲基亚硫酰化的吡唑衍生物，特别是氟虫腈。

公开(公告)号：US5614632A

公开(公告)日：1997-03-25

申请号：US439733

申请日：1995-05-12

Applicant: Mahadevan Bhupathy ,  James M. McNamara ,  Daniel R. Sidler ,  Ralph P. Volante ,  James Bergan

Inventor： Mahadevan Bhupathy ,  James M. McNamara ,  Daniel R. Sidler ,  Ralph P. Volante ,  James Bergan

IPC: C07D215/18 ,  A61K31/47 ,  A61P11/06 ,  C07C215/14 ,  C07C313/02 ,  C07C323/53 ,  C07D215/12 ,  C07D215/14

CPC classification number: C07D215/14 ,  C07C323/53 ,  C07C2101/02

Abstract: The present invention relates to a process for the preparation of a compound of formula (I) or a sodium salt thereof ##STR1## wherein HET is 7-chloroquinolin-2-yl or 6,7-difluoroquinolin-2-yl, which comprises: reacting the dilithium dianion of 1-(mercaptomethyl)cyclopropaneacetic acid with a compound of formula (II) ##STR2## wherein HET is as defined above and L is arylsulfonyl or alkylsulfonyl. The invention further provides the dicyclohexylamine salt of a compound of formula (I).

Abstract translation: 本发明涉及制备式（I）化合物或其钠盐的方法，其中HET是7-氯喹啉-2-基或6,7-二氟喹啉-2-基， 其包括：使1-（巯基甲基）环丙烷乙酸的二锂二阴离子与式（II）化合物（II）反应，其中HET如上所定义，L是芳基磺酰基或烷基磺酰基。 本发明还提供式（I）化合物的二环己基胺盐。