| 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 Methods for Treatment of Cancer | US14215852 | 2014-03-17 | US20140200199A1 | 2014-07-17 | Chiang J. Li; Mark A. Ashwell; Jason Hill; Magdi Moussa; Neru Munshi |
| The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent. | ||||||
| 182 | Julolidine conjugates and methods for their preparation and use | US13597323 | 2012-08-29 | US08642764B1 | 2014-02-04 | Govindaraju Thimmaiah; Debabrata Maity; Swapan Kumar Pati; Tapas Kumar Kundu; Arun Kumar Manna; Karthigeyan Dhanasekaran |
| Compounds that selectively bind to copper ions in a sample and methods of preparing and using the compounds are described. Disclosed herein are planar julolidine based compounds that display characteristic absorbance in the visible and near-infrared (NIR, 700-1000 nm) region in the presence of copper ions. Methods to detect Cu2+ ions by fluorometry and colorimetry are disclosed. | ||||||
| 183 | SMAC mimetic compounds as apoptosis inducers | US12741862 | 2008-11-05 | US08609685B2 | 2013-12-17 | Carlo Scolastico; Leonardo Pierpaolo Manzoni; Pierfausto Seneci; Laura Belvisi; Domenico Delia; Martino Bolognesi; Eloise Mastrangelo; Mario De Mayo De Mari Milani; Ilaria Motto; Carmelo Drago |
| The present invention relates to compounds conformationally constrained mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients. | ||||||
| 184 | Pyrroloquinolinyl-pyrrolidine-2,5-dione compositions and methods for preparing and using same | US13336059 | 2011-12-23 | US08470786B2 | 2013-06-25 | Mark A. Ashwell; Darin Kizer; Takahiro Murai; Daisuke Nakai; Takanori Yasukochi |
| The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing pyrroloquinolinyl-pyrrolidine-2,5-dione compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof. | ||||||
| 185 | Thienopyridine Derivatives for the Treatment and Prevention of Dengue Virus Infections | US13203351 | 2010-02-24 | US20120022046A1 | 2012-01-26 | Chelsea M. Byrd; Dongcheng Dai; Robert Jordan; Dennis E. Hruby |
| Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus. | ||||||
| 186 | Spirohydantoin compounds and methods for the modulation of chemokine receptor activity | US11159406 | 2005-06-23 | US07709642B2 | 2010-05-04 | Laval Chan Chun Kong; Christophe Moinet; Louis Vaillancourt; Monica Bubenik |
| Novel compounds represented by formula (I): wherein R1, R2, R3 and R4 are as defined herein, and pharmaceutically acceptable salts, hydrates and solvates thereof, are useful for the modulation of CCR5 chemokine receptor activity. | ||||||
| 187 | Imaging Agents Useful for Identifying AD Pathology | US12509259 | 2009-07-24 | US20100098634A1 | 2010-04-22 | Hartmuth C. Kolb; Joseph C. Walsh; Wei Zhang; Umesh B. Gangadharmath; Dhanalakshmi Kasi; Kai Chen; Anjana Sinha; Eric Wang; Gang Chen; Peter J.H. Scott; Henry Clifton Padgett; Qianwa Liang; Zhiyong Gao; Tieming Zhao; Chunfang Xia |
| Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease. | ||||||
| 188 | Production of dolasetron | US11650294 | 2007-01-05 | US07608714B2 | 2009-10-27 | Janos Hajko; Tivadar Tamas; Adrienne Kovacsne-Mezei; Erika Magyar Molnarne; Csaba Peto; Csaba Szabo |
| The present invention provides an improved process for the preparation of Dolasetron salts, in particularly Dolasetron mesylate. Also provided are intermediates for the process and methods of preparing the intermediates. | ||||||
| 189 | Spiropiperidine derivatives as melanocortin receptor agonists | US09781373 | 2001-02-12 | US20010029259A1 | 2001-10-11 | Ravi P. Nargund; Zhixiong Ye; Brenda L. Palucki; Raman K. Bakshi; Arthur A. Patchett; Leonardus H.T. Van Der Ploeg |
| Certain novel spiropiperidine compounds are agonists of melanocortin receptor(s) and are useful for the treatment, control or prevention of diseases and disorders responsive to the activation of melanocortin receptors. The compounds of the present invention are therefore useful for treatment of diseases and disorders such as obesity, diabetes, sexual dysfunction including erectile dysfunction and female sexual dysfunction. | ||||||
| 190 | Ruthenium catalyst for biarylic coupling; new steganolides | US127898 | 1987-11-05 | US4873349A | 1989-10-10 | Jean-Pierre Robin; Yannick Landais |
| A method for forming bridged biaryl compounds via the intramolecular oxidative biarylic coupling of precursor compounds containing two aromatic rings linked via a hydrocarbon chain is disclosed along with the ruthenium catalyst for its implementation and new compounds resulting therefrom. The biarylic coupling method is characterized in that the biarylic precursors are cyclized in the presence of the catalyst tetrakis(trifluoroacetate) of ruthenium (IV). | ||||||
| 191 | 7H thieno[2,3-a]quinolizines, useful as .alpha..sub.2 -andrenoceptor antagonist | US922484 | 1986-10-23 | US4717731A | 1988-01-05 | Alan C. White; Robin G. Shepherd; Barry J. Langham |
| The invention concerns thienoquinolizines of general formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts. In the formula R.sup.1 is hydrogen or lower alkyl and R.sup.2 is lower alkyl, halo(lower)alkyl, --A--NR.sup.3 R.sup.4 [where A represents a direct bond between the S and N atoms or a lower alkylene group having 1 to 3 carbon atoms in the chain between the S and N atoms and R.sup.3 and R.sup.4 each independently represent hydrogen, lower alkyl, aryl or aryl(lower)alkyl or together with the nitrogen atom to which they are attached represent a five or six membered heterocyclic ring], aryl or a heterocyclic radical or R.sup.1 is --A.sup.1 NR.sup.5.SO.sub.2 R.sup.6 [where A.sup.1 is a lower alkylene group having 1 to 3 carbon atoms in the chain between the two N atoms, R.sup.5 is hydrogen or lower alkyl and R.sup.6 is lower alkyl, halo(lower)alkyl or aryl] and R.sup.2 is lower alkyl, halo(lower)alkyl or aryl. The compounds possess .alpha..sub.2 -adrenoceptor antagonistic activity in warm blooded animals. | ||||||
| 192 | N.sub.b Quaternary derivatives of ajmaline and isoajmaline, methods and intermediate products in the manufacture of their derivatives and method of using same and pharmaceutical compositions thereof | US615757 | 1984-05-31 | US4554274A | 1985-11-19 | Wolfgang Kehrbach; Joachim Wegener; Ulrich Kuehl; Renke Budden; Gerd Buschmann |
| New quaternary derivatives of 10-bromoajmaline and 10-bromoisoajmaline are disclosed which exhibit antiarrhythmic and adrenolytic properties and which have the formula I ##STR1## wherein R represents a carbon-attached organic group containing 1 to 10 carbon atoms and A.sup.- represents an acid anion as well as pharmaceutical formulations thereof and processes and intermediates for their preparation. | ||||||
| 193 | N.sub.b -Quaternary derivatives of sandwicine and isosandwicine methods and intermediate products in the manufacture of their derivatives and methods of using same and pharmaceutical compositions thereof | US615756 | 1984-05-31 | US4552877A | 1985-11-12 | Wolfgang Kehrbach; Joachim Wegener; Ulrich Kuehl; Renke Budden; Gerd Buschmann |
| New N.sub.b -quaternary 10-bromosandwicine and 10-bromoisosandwicine derivatives are disclosed which exhibit antiarrhythmic properties and adrenolytic properties and which have the formula I ##STR1## wherein R represents a carbon-attached organic group containing 1 to 10 carbon atoms and A.sup..crclbar. represents an acid anion, as well as pharmaceutical formulations thereof and processes and intermediates for their preparation. | ||||||
| 194 | 5-Alkyl or hydroxyalkyl substituted-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines and anticonvulsant use thereof | US272864 | 1981-06-12 | US4399141A | 1983-08-16 | Paul Anderson; Marcia E. Christy; Ben E. Evans |
| 5-Substituted-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines, derivatives and pharmaceutically acceptable salts thereof are useful as anticonvulsants. | ||||||
| 195 | Process for the preparation of hydroxyamino-eburnane derivatives and octahydroindoloquinolizine intermediates | US154329 | 1980-05-29 | US4345082A | 1982-08-17 | Csaba Szantay; Lajos Szabo; Gyorgy Kalaus; Janos Sapi; Lajos Dancsi; Tibor Keve; Maria Gazdac |
| The invention relates to new hydroxyamino-eburnane derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each stand for a C.sub.1-6 alkyl group, as well as to pharmaceutically acceptable acid addition salts and optically active isomers of these compounds.These new compounds can be applied as peripheral vasodilatating agents or can be converted into other compounds, e.g. vincamine and apovincamine derivatives of valuable therapeutical effects.The compounds of the general formula (I) are prepared according to the invention by reacting a hexahydro-indoloquinolisinium derivative of the general formula (II), ##STR2## wherein R.sup.2 is as defined above and X stands for an acid residue, with a methylenemalonic acid diester derivative of the general formula (III), ##STR3## wherein R.sup.1 is as defined above, subjecting the resulting product to catalytic hydrogenation, treating the resulting product with an alkali, and reacting the resulting octahydroindoloquinolisine monoester derivative with a nitrosating agent in an acidic medium. | ||||||
| 196 | Process for making 4-methyl-4,5-dihydrotetrazolo [1,5-a] quinazolin-5-one | US49902 | 1979-06-19 | US4226994A | 1980-10-07 | John H. Marsden; Norman Harrison |
| In a process for preparing the compound 4-methyl-4,5-dihydrotetrazolo [1,5-a] quinazolin-5-one having the structural formula: ##STR1## which comprises the steps of (i) bringing anthranilic acid into reaction with cyanamide at a temperature in the range of 80.degree. to 100.degree. C.; (ii) bringing the reaction product obtained by the foregoing step (i) into reaction with hydrazine hydrate in the presence of an organic solvent; then (iii) diazotizing the hydrazino compound so formed to yield a tetrazole; and finally (iv) methylating the tetrazole, the improvement which comprises using n-butanol as the organic solvent in step (ii). | ||||||
| 197 | 세파코스포린 유도체의 제조 방법 | KR1019810000527 | 1981-02-19 | KR1019830005245A | 1983-08-03 | 위르겔블룸바하 |
| 내용없음 | ||||||
| 198 | 세파피린의 아미노산염 제조 방법 | KR1019810001076 | 1981-03-31 | KR1019830005244A | 1983-08-03 | 마르코팔시아니 |
| 내용없음 | ||||||
| 199 | 아미노산 세파드록실염의 제조 방법 | KR1019810001077 | 1981-03-31 | KR1019830005239A | 1983-08-03 | 마르코팔시아니 |
| 내용없음 | ||||||
| 200 | 리파마이신 유도체의 제조 방법 | KR1019810000443 | 1981-02-13 | KR1019830005227A | 1983-08-03 | 레오나르도바르실리 |
| 내용없음 | ||||||
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