| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 121 | Intramolecular amidation of sulfamates catalyzed by metalloporphyrins | US10790810 | 2004-03-03 | US07105660B2 | 2006-09-12 | Chi-Ming Che; Jiang-Lin Liang |
| An intramolecular amidation processes for substrates such as sulfamates using chiral and non-chiral metalloporphyrin complexes which can maximize catalytic activity, enhance efficiency, stereoselectivity and speed of amidation reactions is described. The chiral metalloporphyrin catalyzed amidation of sulfamates exhibits excellent cis-selectivity, affording cyclic sulfamidates with high enantiomeric excess values. | ||||||
| 122 | Liposomal camptothecins and uses thereof | US09896811 | 2001-06-29 | US07060828B2 | 2006-06-13 | Thomas D. Madden; Sean C. Semple |
| This invention relates to improved liposomal camptothecin compositions and methods of manufacturing and using such compositions for treating neoplasia and for inhibiting angiogenesis. | ||||||
| 123 | Process for the preparation of α-aminosubstituted carboxylic acid amides | US10433011 | 2001-12-11 | US07053211B2 | 2006-05-30 | Thorsten Hartig; Steffen Enke |
| The invention relates to a process for the preparation of α-aminosubstituted carboxylic acid amide compounds and/or their salts comprising reacting a carboxylic acid amide of a primary amine with a nitrosylating agent in the presence of a base followed by hydrolysis to give a hydroxy imino derivative followed by hydrogenation and if necessary converting a base or acid of the α-aminosubstituted carboxylic acid amide into one of its salts. | ||||||
| 124 | Process for aqueous milling of quinacridone pigments | US10988250 | 2004-11-12 | US20050187313A1 | 2005-08-25 | Yingxia He; Colin Campbell |
| The present invention is directed to an aqueous process for reducing particle size of organic pigments by milling the crude pigment in the presence of a water soluble styrene copolymer dispersant, optionally a defoamer, optionally an additive, and greater than about 10 wt. % water, and isolating the organic pigment. | ||||||
| 125 | 2,9-dichloroquinacridone pigment | US10466464 | 2003-07-15 | US20040065231A1 | 2004-04-08 | Fridolin Babler |
| A high chroma, opaque gamma 2,9-dichloroquinacridone pigment specified by its particle shape and size and characterized by C.I.E. color space values in masstone, and a process for its preparation is disclosed. The new gamma 2,9-dichloro-quinacridone pigment is especially useful for coloring coating compositons, such as automotive paints, and plastics. | ||||||
| 126 | CHEMOKINE RECEPTOR ANTAGONISTS AND METHODS OF USE THEREFOR | US09362837 | 1999-07-28 | US20020119973A1 | 2002-08-29 | JAY R. LULY; YOSHISUKE NAKASATO; ETSUO OHSHIMA; HIROKI SONE; OSAMU KOTERA; GERALDINE C.B. HARRIMAN |
| Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: 1 and physiologically acceptable salts thereof. 2 | ||||||
| 127 | Farnesyl transferase inhibiting 1,8-annelated quinolinone derivatives substituted with N- or C-linked imidazoles | US09725391 | 2000-11-29 | US20020049327A1 | 2002-04-25 | Marc Gaston Venet; Patrick Rene Angibaud; Yannick Aime Eddy Ligny; Virginie Sophie Poncelet; Gerard Charles Sanz |
| This invention concerns compounds of formula 1 the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; -A- is a bivalent radical of formula; R1 and R2 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar, ArnullC1-6alkyl, Ar-oxy, ArnullC1-6alkyloxy; or when on adjacent positions R1 and R2 taken together may form a bivalent radical; R3 and R4 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy, Ar-oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy, or when on adjacent positions R3 and R4 taken together may form a bivalent radical; R5 is an imidazolyl substituted with hydrogen or C1-6alkyl; R6 hydrogen, hydroxy, halo, cyano, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl or Ar; or a radical of formula nullOnullR7, nullSnullR8, nullNnullR8R9; and Ar is optionally substituted phenyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine. | ||||||
| 128 | NOVEL 20,21-DINOR-EBURNAMENINE | US08228300 | 1994-04-15 | US20020045637A1 | 2002-04-18 | FRANCOIS CLEMENCE; JEAN-LUC HAESSLEIN; CLAUDE OBERLANDER |
| A compound selected from the group consisting of all possible isomers or racemates of a compound of the formula 1 wherein X1, X2 and X3 are individually selected from the group consisting of hydrogen, halogen, unsubstituted or substituted alkyl of 1 to 18 carbon atoms, unsubstituted or substituted alkenyl and alkynyl of 2 to 18 carbon atoms, unsubstituted or substituted alkoxy of 1 to 7 carbon atoms, nullOH, nullCF3, nullNO21 nullNH21 mono and dialkylamino of 1 to 4 alkyl carbon atoms and unsubstituted or substituted phenyl, 2 R is selected from the group consisting of unsubstituted or substituted alkyl of 1 to 7 carbon atoms, unsubstituted or substituted alkenyl and alkynyl of 2 to 7 carbon atoms, unsubstituted or substituted phenyl and carboxy optionally salified or esterified, R1 is 3 or nullCnullCHnullR10, one of R8 and R9 is selected from the group consisting of hydrogen, unsubstituted or substituted alkyl of 1 to 6 carbon atoms, unsubstituted or substituted alkenyl and alkynyl of 2 to 6 carbon atoms, unsubstituted or substituted phenyl, esterified carboxy, nullCN and acyl of 2 to 6 carbon atoms and the other and R10 are selected from the group consisting of hydrogen, unsubstituted or substituted alkyl of 1 to 6 carbon atoms, unsubstituted or substituted alkenyl and alkynyl of 2 to 6 carbon atoms and unsubstituted or substituted phenyl and its non-toxic, pharmaceutically acceptable salts with acids or bases having anti-anoxic, anti-ischemic and neuronal protective anti-depressant activities. | ||||||
| 129 | Oxo-pyridoimidazole-carboxamides: GABA brain receptor ligands | US09761601 | 2001-01-16 | US20010011133A1 | 2001-08-02 | Bogumila Rachwal; Pamela Albaugh; Kenneth Shaw |
| Disclosed are compounds of the formula: 1 or the pharmaceutically acceptable non-toxic salts thereof where R1-R4 and A are defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors and are, therefore, useful in the diagnosis and treatment of anxiety, Down Syndrome, depression, sleep, cognitive and seizure disorders, overdose with benzodiazepine drugs and for enhancement of alertness. | ||||||
| 130 | New tetracyclic analogues of camptothecins, their preparation processes, their use as medicaments and the pharmaceutical compositions containing them | US09734167 | 2000-12-12 | US20010000521A1 | 2001-04-26 | Dennis Bigg; Olivier Lavergne; Alain Rolland; Christophe Lanco; Gerard Ulibarri |
| The invention relates to new tetracyclic analogues of camptothecin, their preparation processes, their use as medicaments and the pharmaceutical compositions containing them. Said analogues, which include in particular 3-hydroxy-3-(4-oxo-4,6-dihydroindolizino null1,2-bnull quinoline-2-yl)pentanoic acid, have a powerful biological activity inhibiting topoisomerase I and/or topoisomerase II. | ||||||
| 131 | Oxidation process using tempo | US283435 | 1999-04-01 | US6031101A | 2000-02-29 | Paul N. Devine; Eiichi Mano; Zhiguo Song; David M. Tschaen; Mangzu Zhao |
| The present invention relates to an oxidation using sodium chlorite in the presence of a catalytic amount of TEMPO and sodium hypochlorite which converts the penultimate intermediate bearing a primary alcohol to the target endothelin antagonist compound of Formula I having a carboxylic acid ##STR1## | ||||||
| 132 | Tricyclic benzazepine vasopressin antagonists | US672150 | 1996-06-27 | US5753648A | 1998-05-19 | Jay Donald Albright; Aranapakam M. Venkatesan; John P. Dusza; Fuk-Wah Sum |
| Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds. | ||||||
| 133 | 4H-pyrano[4,3-d]thiazole derivatives and process therefor | US618643 | 1975-10-01 | US4033977A | 1977-07-05 | Adolf H. Philipp; Leslie G. Humber |
| 4H-Pyrano[4,3-d]thiazole derivatives characterized by having a 4H-pyrano[4,3-d]thiazole nucleus having a phenyl substituent at position 2 and a substituent at position 4, said substituent incorporating an acidic or basic function therein, are disclosed. The nucleus is further substituted at position 4 with a lower alkyl and may be optionally substituted in the phenyl ring. The foregoing compounds possess anti-inflammatory and antidepressant activity and methods for their preparation and use are described. | ||||||
| 134 | Crystal forms of (R)-N-methylnaltrexone bromide and uses thereof | US14820916 | 2015-08-07 | US09879024B2 | 2018-01-30 | Valeriya N. Smolenskaya; Kadum A. Al Shareffi; Julio Perez; Syed M. Shah; Thomas A. Boyd |
| The present invention provides a new forms of (R)-N-methylnaltrexone, and compositions thereof, useful as a peripheral mu opioid receptor antagonist. | ||||||
| 135 | Method for the synthesis of irinotecan | US15023827 | 2014-11-24 | US09765083B2 | 2017-09-19 | Alexander Zabudkin; Viktor Matvienko |
| The present invention relates to a method for the synthesis of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. iriniotecan), comprising: (a) preparing 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptotecin; and (b) selectively ethylating the compound of step (a) at the 7-position, thus resulting in the preparation of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin. The present invention is further directed to the use of 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. 7-des-ethyl-irinotecan) as intermediate in a method for the synthesis of irinotecan as described. | ||||||
| 136 | Organometallic complexes which emit in the red to green spectral region and their use in OLEDs | US13863407 | 2013-04-16 | US09522895B2 | 2016-12-20 | Herbert Friedrich Boerner; Hans-Peter Loebl; Josef Salbeck; Elena Popova |
| A triphenylene derivative useful for the production of organic light emitting diodes. | ||||||
| 137 | Remedy for diabetes | US14261953 | 2014-04-25 | US09440980B2 | 2016-09-13 | Naoyuki Fukuchi; Satoru Okamoto; Wataru Miyanaga; Sen Takeshita; Masaru Takayanagi; Yumiko Fukuda; Takao Ikenoue; Naoyuki Yamada; Naoko Arashida |
| A method of screening a compound having a hypoglycemic effect (hereinafter referred to as “hypoglycemic compound”), a remedy for diabetes which contains a compound having a novel function mechanism, etc. More specifically speaking, a method of screening a hypoglycemic compound capable of binding to the β subunit of a trimeric GTP-binding protein, a remedy for diabetes comprising a hypoglycemic compound, which is characterized by being capable of binding to the β subunit of a trimeric GTP-binding protein, as the active ingredient, etc. | ||||||
| 138 | Peripherally acting opioid compounds | US14598678 | 2015-01-16 | US09415045B2 | 2016-08-16 | Laura Cook Blumberg; Derrick Arnelle |
| The invention relates to a compound of Formula I, II, III, IV or a pharmaceutically acceptable ester or prodrug thereof: | ||||||
| 139 | Heteroarylcyanine dyes with sulfonic acid substituents | US14085616 | 2013-11-20 | US09315864B2 | 2016-04-19 | Stephen Yue; Gene Shen; Wei-Chuan Sun |
| Heteroaryl cyanine dyes bearing sulfonic acid substituents are of use in various assays, including single molecule nucleic acid sequencing. Exemplary heteroaryl cyanines dyes include or more reactive functional group, which is of use to covalently conjugate the cyanine dye to a carrier molecule. An exemplary carrier molecule is an analyte molecule or other molecule of interest, for example, a nucleotide oligophosphate. | ||||||
| 140 | Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A) | US14097808 | 2013-12-05 | US09200016B2 | 2015-12-01 | Bertrand Leblond; Thierry Taverne; Cedric Chauvignac; Eric Beausoleil; Anne-Sophie Casagrande; Laurent Desire; Matthew P. Pando; John E. Donello; Rong Yang |
| The invention relates to compounds of the formula or a pharmaceutically acceptable salt thereof, wherein R′, R1 through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases. | ||||||
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