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序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
181 METHOD FOR PREPARING 2-NITRO-5-(PHENYLTHIO)-ANILINES PCT/EP1999/004296 1999-06-21 WO00001669A2 2000-01-13
The present invention relates to 2-nitro-5-(phenylthio)-anilines which are obtained by reacting 5-chlorine-2-nitroanilines with thiophenols and ammonia in a solvent.
182 METHOD FOR PREPARING SULFANYL-TYPE ENDOTHELIN RECEPTOR ANTAGONISTS PCT/EP1999/001209 1999-02-25 WO99044988A2 1999-09-10
The invention relates to a method for preparing sulfanyl-type endothelin receptor antagonists of general formula (I) wherein R<1> represents hydroxy, alkoxy, sulfonamidyl, amino; R<2> represents alkyl, aryl or heteroaryl, optionally substituted, and R<3>, R<4>, R<5> can be the same or different and are alkyl or aryl, optionally substituted, by means of nucleophilic reaction of a carboxylic acid derivative of formula (II) with a sulfide of formula (III), X being SR<6> or SO2R<6> and R<6> being alkyl or aryl, optionally substituted.
183 MONOESTERS OF PROBUCOL FOR THE TREATMENT OF CARDIOVASCULAR AND INFLAMMATORY DISEASE PCT/US9809773 1998-05-14 WO9851289A3 1999-05-14 MEDFORD RUSSELL M; SOMERS PATRICIA K
This invention is a method and composition for the inhibition of VCAM-1, and in particular for the treatment of cardiovascular or inflammatory disease, including atherosclerosis, that includes the administration of an effective amount of an ester of probucol.
184 IMPROVED SYNTHESIS OF SULFURIZED OLIGONUCLEOTIDES PCT/US1998/021502 1998-10-13 WO99019340A1 1999-04-22
Methods for the formation of sulfurized oligonucleotides are provided. The methods allow for the formation of phosphorothioate linkages in the oligonucleotides or derivatives, without the need for complex solvent mixtures and repeated washing or solvent changes. Oligonucleotides having from about 8, and up to about 50, nucleotides can be sulfurized according to the methods of the invention with higher yields than have been previously reported.
185 COMPOUNDS AND METHODS FOR THE INHIBITION OF THE EXPRESSION OF VCAM-1 PCT/US9809781 1998-05-14 WO9851662A2 1998-11-19 MEDFORD RUSSELL M; SOMERS PATRICIA K; HOONG LEE K; MENG CHARLES Q
This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.
186 S-nitrosothiols as smooth muscle relaxants and therapeutic uses thereof PCT/US9202560 1992-03-30 WO9217445A3 1992-12-10 STAMLER JONATHAN S; LOSCALZO JOSEPH; SLIVKA ADAM; SIMON DANIEL; BROWN ROBERT; DRAZEN JEFFREY
S-nitrosothiols exert a potent relaxant effect, mediated by guanylate cyclase, upon non-vascular smooth muscle. Such types of smooth muscle include airway, gastrointestinal, bladder, uterine and corpus cavernosal. Thus, S-nitrosothiols may be used for the treatment or prevention of disorders associated with relaxation of smooth muscle, such as airway obstruction, and other respiratory disorders, bladder dysfunction, premature labor and impotence. Additionally, S-nitrosothiols may be used to alleviate smooth muscle contraction and spasm, and thus facilitate procedures involving diagnostic instrumentation, such as endoscopy, bronchoscopy, laparoscopy and cystoscopy. Figure 2 shows the relaxation effects of various S-nitrosothiols on guinea pig trachea.
187 COATING COMPOSITION FOR A METAL SUBSTRATE PCT/US2020/013814 2020-01-16 WO2020154160A1 2020-07-30 HAYES, Robert Andrew

A composition comprising a compound having the general formula (I): F – [CF2]n – (O[CF2]n)m –( L )p – SH (Formula (I)) Each n is independently from 2 to 4, m is from 3 to 30, p is 0 or 1 and L represents a linker having the formula Oq(CF2)r(CH2)s, wherein q is 0 or 1, r is from 0 to 4 and s is from 0 to 4.

188 COMPOUNDS FOR INHIBITION OF INFLAMMATION PCT/US2019/039499 2019-06-27 WO2020006229A1 2020-01-02 WU, Hao; LIEBERMAN, Judy; HU, Jun; LIU, Xing

The present application provides chemical compounds useful, for example, in inhibiting gasdermin pore formation in a cell, inhibiting inflammasome-mediated death of a cell (pyroptosis); inhibiting cytokine secretion from a cell, inhibiting an inflammatory caspase in a cell, and/or covalently reacting with a cysteine of a gasdermin protein in a cell. These compounds are also useful in treating or preventing diseases or conditions in which inflammasome activation is implicated in pathogenesis. One example of such disease or condition is sepsis.

189 有機硫黄材料及びその製造方法 PCT/JP2016/060615 2016-03-31 WO2016159212A1 2016-10-06 妹尾 博; 小島 敏勝; 竹市 信彦; 安藤 尚功

 炭素、素、酸素及び硫黄を構成元素として含有し、ラマン分光法によって検出されたラマンスペクトルにおいて、482 cm-1付近、846 cm-1付近、1066 cm-1付近、1279 cm-1付近、及び1442 cm-1付近にピークを有し、且つ、前記1442 cm-1付近のピークが最強ピークである、有機硫黄材料は、液体有機原料を用いつつも、高容量且つ高耐熱性の有機硫黄材料である。

190 LIPOIC ACID-RESVERATROL CONJUGATES AND USES THEREOF PCT/CA2014/051259 2014-12-23 WO2015095968A1 2015-07-02 SALEH, Tarek; RAJAGOPAL, Desikan; KHAN, Bobby; KUCUKKAYA, Inan; ABD-EL-AZIZ, Alaa; CONNELL, Barry

Described are covalent conjugates between lipoic acid (LA), or a derivative thereof, and resveratrol, or a derivative thereof. As an example, the covalent conjugate may be a compound of the formula: (I). Methods using the LA-resveratrol conjugates for the treatment of diseases, disorders, or conditions related to oxidative stress are also provided.

191 METHODS AND COMPOSITIONS FOR PRODUCING DIFLUOROMETHYLENE-AND TRIFLUOROMETHYL-CONTAINING COMPOUNDS PCT/US2008/086044 2008-12-09 WO2009076345A1 2009-06-18 UMEMOTO, Teruo; SINGH, Rajendra

New methods for producing difluoromethylene-containing compounds with phenylsulfur trifluoride or a primary alkyl-substituted phenylsulfur trifluoride are disclosed. Also, new methods for producing trifluoromethyl-containing compounds with phenylsulfur trifluoride or primary alkyl-substituted phenylsulfur trifluoride are also disclosed.

192 ARYLSULFANYL COMPOUNDS AND COMPOSITIONS FOR DELIVERING ACTIVE AGENTS PCT/US2007/074534 2007-07-27 WO2008014430A1 2008-01-31 WANG, Nai, Fang; SARAF, Sushma; PUSZTAY, Stephen, V.

Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are also provided.

193 N-DEACETYLTHIOCOLCHICINE DERIVATIVES, THEIR USE AND PHARMACEUTICAL FORMULATIONS CONTAINING THEM PCT/EP2005/000987 2005-02-01 WO2005075418A2 2005-08-18 BOMBARDELLI, Ezio; FONTANA, Gabriele

Disclosed is a series of N-deacetylthiocolchicine derivatives of formula (I) in which: - the linker is a bivalent straight or branched C1-C8 alkyl residue, C3-C8 cycloalkyl, a phenylene or heterocyclic C4-C6 ring; - the G1 and G2 junctions, which can be the same or different, are - CO-, -COHN-, -CR2- groups in which R2 is hydrogen or a straight C1-C4 alkyl residue, or the G1-linker-G2 group is the -CO- group. The compounds of formula (I) have antiproliferative, antinflammatory, antiarthritic and antiviral activity.

194 PRODRUGS OF DIARYL-2-(5H)-FURANONE CYCLOOXYGENASE-2 INHIBITORS PCT/US2004034374 2004-10-18 WO2005042476A3 2005-06-09 ARRUDA JEANNIE M; MUNOZ BENITO; STEARNS BRIAN A
The invention encompasses the novel compounds of Formula (I) and Formula (II), which are prodrugs that convert in vivo to diaryl-2-(5H)-furanones useful in the treatment of cyclooxygenase-2 mediated diseases. These prodrugs are far more soluble in aqueous media than the active agents into which they convert, in vivo. As such compounds of Formula (I) and (II) are advantageous for, among other things intravenous administration. The invention also encompasses certain pharmaceutical compositions and methods for treatment of cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula (I) and Formula (II).
195 NOVEL AMIDES THAT ACTIVATE SOLUBLE GUANYLATE CYCLASE PCT/US2003/038906 2003-12-08 WO2004060859A2 2004-07-22 ANDERSON, Steven, N.; BHATIA, Pramila; KOLASA, Teodozyj; NAKANE, Masaki; PATEL, Meena, V.; ROHDE, Jeffrey, J.; XIA, Zhiren; ZHANG, Henry, Q.

Compounds of formula (I) are useful for increasing cGMP levels in a mammal.

196 COMPOUNDS PCT/GB2003/002502 2003-06-05 WO2003104189A2 2003-12-18 COOPER, Anthony, William, James; MORDAUNT, Jacqueline, Elizabeth; PEACE, Simon; SMITH, Paul, William; SMITH, Steven

The invention relates to compounds of formula (I) wherein R1 represents benzyl; R2 represents pyrazole; or a pharmaceutically acceptable derivative thereof. The invention also relates to pharmaceutical compositions containing compounds of formula (I) and to the use of compounds of formula (I) in medicine, particularly in the amelioration of a clinical condition for which a ACE and/or NEP inhibitor is indicated.

197 POTASSIUM CHANNEL MODULATORS PCT/DK2003/000004 2003-01-06 WO2003059873A1 2003-07-24 GOULIAEV, Alex, Haahr; SLÖK, Frank, Abildgaard; TEUBER, Lene; DEMNITZ, Joachim

This invention relates to novel compounds characterized by the general Formula (I) any of its enantiomers or any mixture of its enantiomers, or a pharmaceutically acceptable salt thereof, or an N-oxide thereof, useful as potassium channel modulators. More specifically the invention provides chemical compounds useful as modulators of SKCa and/or IKCa channels.

198 CARBON BLACK COUPLER PCT/US0109290 2001-03-22 WO0170866A3 2002-05-16 BURRINGTON JAMES D; RICHARDSON BENNY R; PIALET JOSEPH W; WYKOFF ANN E; SOWERBY ROGER L; LEE KENNETH W; KORNBREKKE RALPH E; GHEBREMESKEL GHEBREHIWET N; DAVIS KIRK E
A coupler is described for use in carbon black filled rubber compositions. The coupler includes an amine group and a thiol group or a polysulfidic linkage. The coupler improves the interaction of the carbon black with the rubber as measured by a decrease in the tan delta at 60 DEG C while substantially maintaining the tan delta at 0 DEG C.
199 SUBSTITUTED THIOACETAMIDES PCT/US0115752 2001-05-16 WO0187830A2 2001-11-22 BACON EDWARD R; CHATTERJEE SANKAR; DUNN DEREK; MALLAMO JOHN P; VAUGHT JEFFRY L
The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.
200 ENHANCED PROPERTIED PESTICIDES PCT/US2001/000651 2001-01-26 WO01056358A2 2001-08-09
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