子分类：
| 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 | Compositions and dosage forms for enhanced absorption of metformin | US10978141 | 2004-10-29 | US20050158374A1 | 2005-07-21 | Patrick Wong; Dong Yan; George Guittard |
| A complex comprised of metformin and a transport moiety, such as a fatty acid, is described. The complex has an enhanced absorption in the gastrointestinal tract, particularly the lower gastrointestinal tract. The complex, and compositions and dosage forms prepared using the complex, provide for absorption by the body of the drug through a period of ten to twenty-four hours, thus enabling a once-daily dosage form for metformin. | ||||||
| 182 | Fluoroalkyl/alkenyl-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing them | US28920 | 1998-02-24 | US5998481A | 1999-12-07 | Andreas Weichert; Heinz-Werner Kleemann; Hans-Jochen Lang; Jan-Robert Schwark; Udo Albus; Wolfgang Scholz |
| There are described benzoylguanidines of the formula I ##STR1## having the definitions of R(1) to R(4) indicated in the text, and their pharmaceutically tolerable salts. They are obtained by reaction of a compound II ##STR2## with guanidine. They are outstanding agents for the treatment of disorders of the cardiovascular system. | ||||||
| 183 | Quaternary bisphenolates, methods for their preparation, and uses thereof | US768871 | 1996-12-17 | US5756843A | 1998-05-26 | Jimmy Lynn Webb; Matthew Hal Littlejohn; Joseph John Caringi; Thomas Link Guggenheim; Robert Joseph Nick; Patrick Joseph McCloskey; Joseph Anthony King, Jr. |
| Quaternary salts having a double helix structure are prepared by the reaction of dihydroxyaromatic compound, preferably a bisphenol, with an alkali metal hydroxide and a quaternary salt, such as a tetraalkylammonium or hexaalkylguanidinium chloride. The quaternary salts and their alkaline hydrolysis products are useful as catalysts in various reactions, including imide formation from bisphenol salts and halo- or nitro-substituted phthalimides and redistribution and equilibration of polycarbonates. | ||||||
| 184 | [(Benzodioxan, benzofuran or benzopyran) alkylamino] alkyl substituted guanidines | US632227 | 1996-04-15 | US5607949A | 1997-03-04 | Guy R. E. Van Lommen; Marcel F. L. De Bruyn; Walter J. J. Janssens |
| The present invention is concerned with vasoconstricive [(benzodioxan, benzofuran or benzopyran)alkylamino]alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is a bivalent C.sub.1-3 alkanediyl radical; A is a bivalent radical of formula: ##STR2## wherein each R.sup.5 is hydrogen or C.sub.1-4 alkyl; wherein each R.sup.6 is hydrogen or C.sub.1-4 alkyl; Alk.sup.2 is C.sub.2-15 alkanediyl or C.sub.5-7 cycloalkanediyl; and each p is 0, 1 or 2; provided that [2-[(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amino]ethyl guanidine is excluded. Pharmaceuticals which are useful as vasoconstrictors. Compositions comprising said guanidine derivatives as active ingredients, processes for preparing said guanidine derivatives and novel N-cyano guanidine, intermediates; and a use as a medicine are described. | ||||||
| 185 | [(benzodioxan, benzofuran or benzopyran) alkylamino] alkyl substituted guanidines | US256995 | 1994-07-29 | US5541180A | 1996-07-30 | Guy R. E. Van Lommen; Marcel F. L. De Bruyn; Walter J. J. Janssens |
| The present invention is concerned with vasoconstricive [(benzodioxan, benzofuran or benzopyran)alkylamino]alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl;Alk.sup.1 is a bivalent C.sub.1-3 alkanediyl radical; A is a bivalent radical of formula: ##STR2## wherein each R.sup.5 is hydrogen or C.sub.1-4 alkyl; wherein each R.sup.6 is hydrogen or C.sub.1-4 alkyl; Alk.sup.2 is C.sub.2-15 alkanediyl or C.sub.5-7 cycloalkanediyl; and each p is 0, 1 or 2; provided that [2-[(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amino]ethyl guanidine is excluded. Pharmaceuticals which are useful as vasoconstrictors. Compositions comprising said guanidine derivatives as active ingredients, processes for preparing said guanidine derivatives and novel N-cyano guanidine, intermediates; and a use as a medicine are described. | ||||||
| 186 | Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists | US105458 | 1993-08-11 | US5336689A | 1994-08-09 | Eckard Weber; John F. W. Keana |
| Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders. | ||||||
| 187 | Compounds and method for protection of cells and tissues from irreversible injury due to lactic acidosis | US664933 | 1991-03-05 | US5312839A | 1994-05-17 | Tsutomu Nakada |
| Compounds and a method useful for protection of tissue cells in a mammalian body from irreversible damages due to lactic acidosis caused by oxygen deficiency. The protection is achieved by administering a compound having a cell membrane permeability and/or ability to cross the blood brain barrier and being able to provide a buffering action to prevent an increase in a hydrogen ion concentration over the physiologically acceptable levels. | ||||||
| 188 | N,N'-disubstituted guanidines and their use as excitatory amino acid antagonists | US487033 | 1990-03-02 | US5093525A | 1992-03-03 | Eckard Weber; John F. W. Keana |
| Disubstituted guanidines, e.g., bis-1,3-(o-isopropylphenyl)guanidine, bis-1,3-(m-isopropylphenyl)guanidine, bis-1,3-(1-naphthyl)guanidine, bis-1,3-(m-methoxyphenyl)guanidine, N-(1-naphthyl)-N'-(o-iodophenyl)-guanidine, N-(1-naphthyl)-N'-(m-ethylphenyl)guanidine, and N-(1-napthyl)-N'-(o-isoproylphenyl) guanidine, exhibit a high binding affinity to phencyclidine (PCP) receptors. These N,N'-disubstituted guanidine derivatives act as non-competitive inhibitors of glutamate-induced responses generated via the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert a neuroprotective property and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal chord ischemia, brain or spinal cord trauma, as well as being useful for the treatmnet of epilepsy, Alzheimer's disease, Amyotrophic Laterla Scherosis, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders. | ||||||
| 189 | Process for the preparation of mercaptoethansulfonic acid and sodium salt thereof | US346320 | 1989-05-01 | US4939291A | 1990-07-03 | Alberto Reiner |
| For the preparation of saline derivatives of mercaptoethansulfonic acid belonging to the class of the salts of alkali metals and of the salts with basic aminoacids, the sodium salt of the acid is obtained with a process comprising the reaction between sodium bromoethansulfonate with thiobenzoic acid and sodium bicarbonate and subsequent reaction of the resulting sodium benzoylethansulfonate with ammonia in water solution. | ||||||
| 190 | Phenol derivatives | US726824 | 1985-04-24 | US4751240A | 1988-06-14 | Jean Bowler; Graham C. Crawley; Philip N. Edwards; Alasdair T. Glen; Michael S. Large; Brian S. Tait |
| A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined phenolic nucleus including a phenyl-hydroxynaphthyl; hydroxyphenyl-naphthyl; phenyl-hydroxyindanyl, phenyl-hydroxybenzothienyl or mono-hydroxyphenyl-ethylene or vinylene nucleus; wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, wherein R.sup.1 is hydrogen, or alkyl, alkenyl, alkynyl, cycloalkyl, halogenoalkyl, alkoxyalkyl, halogenoalkoxyalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 --or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --(PO)R.sup.2 13 , --S--, --SO--or --SO.sub.2 --, wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene; wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro; or a salt thereof when appropriate. The compounds possess antioestrogenic activity and may be used for the treatment of hormone-dependent breast tumors or of anovulatory infertility. | ||||||
| 191 | Process for producing amidine sulfonic acids | US868231 | 1986-05-28 | US4656291A | 1987-04-07 | Cynthia A. Maryanoff; James N. Plampin; Robin C. Stanzione |
| An efficient synthesis of quanidines, e.g. of the formula (III), by oxidizing a thiourea, e.g. of the following formula (II): ##STR1## with H.sub.2 O.sub.2 and a molybdenum catalyst to yield an aminoiminomethane sulfonic acid which can then be reacted with an amine followed by optional transamination steps. | ||||||
| 192 | 18F-RADIOLABELED BIOMOLECULES | PCT/US2020/034243 | 2020-05-22 | WO2020242948A1 | 2020-12-03 | ZALUTSKY, Michael Rod; VAIDYANATHAN, Ganesan; ZHOU, Zhengyuan |
The application is drawn to 18F-radiolabeled residualizing agents and biomolecules and methods for radiolabeling biomolecules with radioactive fluorine atoms. The biomolecules have an affinity for particular types of cells and may specifically bind a certain cell, such as a cancer cell. Relevant biomolecules include antibodies, monoclonal antibodies, antibody fragments, peptides, other proteins, nanoparticles and aptamers. The application further provides compositions including such labeled biomolecules, as well as methods of using the labeled biomolecules and/or compositions in imaging applications. |
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| 193 | GUANIDINE-FUNCTIONALIZED PERLITE PARTICLES, ARTICLES CONTAINING THE PARTICLES, AND METHODS OF USING THE PARTICLES AND ARTICLES | PCT/US2016/022409 | 2016-03-15 | WO2016149233A1 | 2016-09-22 | KSHIRSAGAR, Manjiri T.; GRIESGRABER, George W. |
Guanidine-functionalized perlite particles are provided. Nonwoven articles are also provided, including a fibrous porous matrix and guanidine-functionalized perlite particles enmeshed in the fibrous porous matrix. Laminated articles are additionally provided, including a first substrate and a second substrate sealed to the first substrate along at least a portion of a perimeter of the first substrate. The laminated article further includes guanidine-functionalized perlite particles disposed between the first substrate and the second substrate. Methods of detecting microorganisms or target cellular analytes in a fluid sample using guanidine-functionalized particles or laminated articles are also provided. |
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| 194 | INHIBITORS OF CREATINE TRANSPORT AND USES THEREOF | PCT/US2015/028633 | 2015-04-30 | WO2015168465A1 | 2015-11-05 | MARTINEZ, Eduardo, J.; TAVAZOIE, Sohail, F. |
This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer. |
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| 195 | SCHNELL HÄRTENDE MIGRATIONSFREIE ZUSAMMENSETZUNG AUF BASIS VON SILANGRUPPEN-HALTIGEN POLYMEREN | PCT/EP2015/058326 | 2015-04-16 | WO2015158860A1 | 2015-10-22 | BURCKHARDT, Urs; CANNAS, Rita |
Die vorliegende Erfindung betrifft eine Zusammensetzung unnfassend mindestens ein Silangruppen-haltiges Polymer und mindestens einen spezifischen Amidin- oder Guanidingruppen aufweisenden Katalysator der Formel (I). Die Zusammensetzung ist emissions- und geruchsarm, weist eine gute Lagerfähigkeit auf, härtet rasch aus und bildet dabei ein mechanisch hochwertiges und beständiges Material, welches kaum zu migrationsbedingten Fehlern wie Ausschwitzen und Substratverschmutzung neigt. Sie eignet sich insbesondere als Klebstoff, Dichtstoff oder Beschichtung. |
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| 196 | METHOD OF MAKING A CYCLIC GUANIDINE FROM A GUANIDINIUM SALT AND A WEAK ACID AND COATING COMPOSITIONS CONTAINING SAME | PCT/US2011027572 | 2011-03-08 | WO2011112596A3 | 2011-11-17 | MCCOLLUM GREGORY J; HICKENBOTH CHARLES R; KARABIN RICHARD F; MORIARITY THOMAS C; ZAWACKY STEVEN R |
| The present invention is directed to a method for preparing a cyclic guanidine comprising reacting (i) a guanidinium, (ii) a polyamine, and (iii) a weak acid. The present invention is also directed to a coating composition comprising the cyclic guanidine. | ||||||
| 197 | LIGAND GUANIDINYL FUNCTIONALIZED POLYMERS | PCT/US2011/024422 | 2011-02-11 | WO2011109151A1 | 2011-09-09 | RASMUSSEN, Jerald K.; SESHADRI, Kannan; FITZSIMONS, Robert T., Jr.; HEMBRE, James I.; BOTHOF, Catherine A.; SATTERWHITE, Erin A.; GRIESGRABER, George W.; HE, Yi; HADDAD, Louis C. |
Ligand functionalized substrates, methods of making ligand functionalized substrates, and methods of using functionalized substrates are disclosed. |
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| 198 | VERFAHREN ZUR HERSTELLUNG VON FORMKÖRPERN MIT HILFE VON MISCHUNGEN VON AMINEN MIT GUANIDIN-DERIVATEN | PCT/EP2009/059237 | 2009-07-17 | WO2010010047A1 | 2010-01-28 | DAUN, Gregor; WITTENBECHER, Lars; HENNINGSEN, Michael; FLICK, Dieter; GEISLER, Joerg-Peter; SCHILLGALIES, Juergen; JACOBI, Erhard |
Der Gegenstand der vorliegenden Erfindung betrifft ein Verfahren zur Herstellung von Formkörpern, wobei zum Aushärten der Form ein Blend eingesetzt wird, dass ein oder mehrere Epoxidharze und eine Mischung enthält und innerhalb der Mischung die Härtungskomponente a) im Bereich von 0,3 bis 0,9 Aminäquivalent pro Äquivalent Epoxid des eingesetzte Epoxidharzes, eingesetzt wird und die Härterkomponente b) eine Verbindung der Formel I ist. |
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| 199 | MISCHUNGEN VON AMINEN MIT GUANIDIN-DERIVATEN | PCT/EP2009/059210 | 2009-07-17 | WO2010010045A1 | 2010-01-28 | DAUN, Gregor; WITTENBECHER, Lars; HENNINGSEN, Michael; FLICK, Dieter; GEISLER, Joerg-Peter; SCHILLGALIES, Juergen; JACOBI, Erhard |
Der Gegenstand der vorliegenden Erfindung betrifft eine Mischung enthaltend mindestens drei Härterkomponenten a1), a2) und b), wobei das Verhältnis der Härterkomponente a1) zu a2) im Bereich von 0,1 bis 10 zu 1 liegt, und die Härterkomponente b) zu 5 bis 55 Gew.-%, bezogen auf die Mischung, enthalten ist, ein Verfahren zur Herstellung dieser Mischung, die Verwendung der erfindungsgemäßen Mischung zum Härten von Epoxidharzen, die Verwendung der erfindungsgemäßen Mischung mit Epoxidharzen als Klebstoffe sowie ein mit der erfindungsgemäßen Mischung gehärtetes Epoxidharz. |
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| 200 | BIGUANIDE COMPOSITION WITH LOW TERMINAL AMINE | PCT/US2007081195 | 2007-10-12 | WO2008051733A3 | 2008-07-31 | HEILER DAVID JOSEPH |
| A polymeric biguanide composition comprising less than 18 mol% of terminal amine groups as measured by 13C NMR. The polymeric biguanide composition also is characterized by a relative increase in the molar concentration of terminal guanidine groups or terminal cyanoguanidino groups. The invention is also directed to ophthalmic compositions comprising the polymeric biguanide compositions. The polymeric biguanide compositions can be used as an antimicrobial component in an ophthalmic lens care solution, or as a preservative to in a pharmaceutical composition or other health care product. | ||||||
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