| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 161 | Highly selective sigma receptor ligands | US12673486 | 2008-08-18 | US08809381B2 | 2014-08-19 | Christopher R. McCurdy; Christophe Mesangeau; Sanju Narayanan; Rae Reiko Matsumoto; Jacques Henri Poupaert |
| A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula I in which R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle such as, for example, radicals of optionally substituted piperidines, optionally substituted piperazines, optionally substituted tetrahydropyridines, optionally substituted azepanes, tertiary amines (cyclic or acyclic), isoindoline-1,3-dione, or optionally substituted tetrahydroisoquinolones (aromatically substituted): R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR. R groups can be either H, aryls, alkyls, or cycloalkyls; “n” can be 1 to 5 carbons in length and stereoisomers, functional analogs, and pharmaceutically acceptable salts thereof and wherein the moiety bridging R1 and N can be optionally substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C3-C5 cycloalkyl group, aromatic and heterocyclic group. | ||||||
| 162 | Cephalotaxus esters, methods of synthesis, and uses thereof | US12920227 | 2009-03-03 | US08466142B2 | 2013-06-18 | David Gin; Jeremy Wilmot; Hakim Djaballah |
| The present invention provides novel cephalotaxus esters, syntheses thereof, and intermediates thereto. The invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of using said compounds or compositions in the treatment of proliferative diseases (e.g., benign neoplasm, cancer, inflammatory disease, autoimmune disease, diabetic retinopathy) and infectious disease. The invention further provides methods of using said compounds or compositions in the treatment of multidrug resistant cancer. | ||||||
| 163 | Modulators of aldehyde dehydrogenase and methods of use thereof | US12581704 | 2009-10-19 | US08389522B2 | 2013-03-05 | Daria Mochly-Rosen; Che-Hong Chen; Wenjin Yang |
| The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition. | ||||||
| 164 | Heat shock protein 90 inhibitors | US12570804 | 2009-09-30 | US08188306B2 | 2012-05-29 | Brian S. J. Blagg; Gang Shen |
| Novel compounds useful for inhibiting the 90kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol. | ||||||
| 165 | Ionic liquids | US12128893 | 2008-05-29 | US08088917B2 | 2012-01-03 | Stewart Forsyth; Kenneth R. Seddon; Keith Whiston; Sudhir Aki |
| The invention relates to an ionic liquid composition and a method for preparing the ionic liquid. The ionic liquid comprises a cation containing the Formula I, as herein disclosed, and wherein: n is 2, R1 is selected from the group consisting of: H, C1-C12 alkyl, aryl or together with R2 may form a heterocyclic ring, and R2 is selected from the group consisting of: H, C1-C12 alkyl, aryl or together with R1 may form a heterocyclic ring, and R3 is selected from the group consisting of hydrogen and C1-C12 alkyl, and wherein R1 and R2 are not simultaneously selected from hydrogen. | ||||||
| 166 | Imidazole compounds | US12796858 | 2010-06-09 | US08017600B2 | 2011-09-13 | Daniel J. Buzard; James P. Edwards; David E. Kindrachuk; Jennifer D. Venable |
| Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions. | ||||||
| 167 | Derivatives of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)alkyl]phosphonic acid and methods of making them | US11758459 | 2007-06-05 | US07879826B2 | 2011-02-01 | Reinhardt Bernhard Baudy |
| Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided: wherein: A is alkylenyl of 1 to 4 carbon atoms, or alkenylenyl of 2 to 4 carbon atoms; R1 and R2 are, independently, hydrogen or a C5 to C7 aryl optionally substituted with 1 to 2 substituents, independently, selected from the group consisting of —C(O)R3, halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy, with the proviso that at least one of R1 and R2 is not hydrogen; R3 is, independently, hydrogen, —OR4, alkyl, aryl, or heteroaryl; R4 is hydrogen, alkyl, aryl, or heteroaryl; R5 and R6 are, independently, hydrogen, alkyl, hydroxyl, alkoxy, or C5 to C7 aryl; wherein any R3 to R6 group having an aryl or heteroaryl moiety can optionally be substituted on the aryl or heteroaryl moiety with 1 to about 5 substituents, independently, selected from the group consisting of halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy. Methods of making these compounds as well as methods using the compounds for treating a variety of conditions are also disclosed. | ||||||
| 168 | Derivatives of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)alkyl] phosphonic acid and methods of use thereof | US11757006 | 2007-06-01 | US07879825B2 | 2011-02-01 | Reinhardt B. Baudy; John A. Butera |
| Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided where at least one of R2 or R3 is not hydrogen. The compounds of the present invention are N-methyl-D-aspartate (NMDA) receptor antagonists and are useful in treating a variety of conditions present in a mammal that benefit from inhibiting the NMDA receptor. | ||||||
| 169 | Compounds and compositions as protein kinase inhibitors | US12187289 | 2008-08-06 | US07713958B2 | 2010-05-11 | Yongqin Wan; Nathanael S. Gray |
| The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases and disorders associated with kinase activity, particularly diseases associated with the activity of CDK1, CDK2, CDK4, CDK5, GSK3β, Bcr-abl, Flt-3, c-Kit, PDGFRβ, Src, Mek1 and CK1. | ||||||
| 170 | 2,5-disubstituted 3-mercaptopentanoic acid | US10517713 | 2003-06-10 | US07572817B2 | 2009-08-11 | Magnus Polla |
| The present invention concerns compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases where inhibition of carboxypeptidase U is beneficial. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above. | ||||||
| 171 | 1,1-dioxo-thiomorpholinyl indolyl methanone derivatives | US11605005 | 2006-11-28 | US07538101B2 | 2009-05-26 | Matthias Nettekoven; Jean-Marc Plancher; Hans Richter; Olivier Roche; Rosa Maria Rodriguez Sarmiento; Sven Taylor |
| The present invention relates to compounds of formula I wherein R1, R2 and G are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors. | ||||||
| 172 | Phenylpiperazine cycloalkanol derivatives and methods of their use | US10963458 | 2004-10-12 | US07531543B2 | 2009-05-12 | Paige Erin Mahaney; Eugene John Trybulski; Lori Krim Gavrin; An Thien Vu |
| The present invention is directed to phenylpiperazine cycloalkanol derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof. | ||||||
| 173 | Carboxamide Spirolactam Cgrp Receptor Antagonists | US11660798 | 2005-09-09 | US20070293470A1 | 2007-12-20 | Theresa Williams; Christopher Burgey; Thomas Tucker; Craig Stump; Ian Bell |
| The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved. | ||||||
| 174 | Tuberculosis treatment using pleuromutilin derivatives | US11818094 | 2007-06-13 | US20070270404A1 | 2007-11-22 | Gerd Ascher; Friedrich Stauffer; Heinz Berner; Rosemarie Mang |
| A method of preventing or treating diseases caused by Mycobacterium, comprising administering to a subject in need of such treatment an effective amount of a pleuromutilin. | ||||||
| 175 | Triazole Derivative or Salt Thereof | US11663089 | 2005-09-14 | US20070259854A1 | 2007-11-08 | Takeshi Murakami; Tomoaki Kawano; Ryota Shiraki; Hirofumi Ishii; Seiji Yoshimura; Takehiko Ohkawa; Mitsuru Hosaka; Hiroki Fukudome; Yutaka Inoki |
| [Problem] There is provided a compound which can be used for therapy of diseases in which 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) participates, in particular diabetes, insulin resistance. [Means for Solution] It has been found that a triazole derivative wherein the triazole ring is substituted with a trisubstituted methyl group in the 2-position or a pharmaceutically acceptable salt thereof has a strong 11β-HSD1 inhibitory activity. Moreover, the triazole derivative of the invention exhibits an excellent blood-glucose level-lowering action and hence can be used for therapy of diabetes, insulin resistance. | ||||||
| 176 | Novel Cyclic Amino Benzoic Acid Derivative | US11659854 | 2005-08-11 | US20070249580A1 | 2007-10-25 | Masahiro Nomura; Yasuo Takano; Kazuhiro Yumoto; Takehiro Shinozaki; Shigeki Isogai; Koji Murakami |
| The present invention relates to cyclic amino benzoic acid derivatives which are effective in therapy of lipid metabolism abnormality, diabetes and the like as a human peroxisome proliferators-activated receptor (PPAR) agonist, in particular, as an agonist against human PPARα isoform, and addition salts thereof, and pharmaceutical compositions containing these compounds. A cyclic amino benzoic acid derivative represented by the general formula (1) [wherein a ring Ar represents an aryl group which may have substituent, or the like; Y represents a C1-C4 alkylene, C2-C4 alkenylene, C2-C4 alkynylene, or the like; Z represents an oxygen atom, sulfur atom or —(CH2)n— (n represents 0, 1 or 2); X represents a hydrogen atom, halogen atom, lower alkyl group which may be substituted with a halogen atom, or the like; R represents a hydrogen atom or lower alkyl group, and —COOR substitutes for an ortho position or metha position of binding position of ring W] or a pharmaceutically acceptable salt thereof. | ||||||
| 177 | Derivatives of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)alkyl]phosphonic acid and methods of making them | US11244599 | 2005-10-06 | US07268123B2 | 2007-09-11 | Reinhardt Bernhard Baudy |
| Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided: wherein: A is alkylenyl of 1 to 4 carbon atoms, or alkenylenyl of 2 to 4 carbon atoms; R1 and R2 are, independently, hydrogen or a C5 to C7 aryl optionally substituted with 1 to 2 substituents, independently, selected from the group consisting of —C(O)R3, halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy, with the proviso that at least one of R1 and R2 is not hydrogen; R3 is, independently, hydrogen, —OR4, alkyl, aryl, or heteroaryl; R4 is hydrogen, alkyl, aryl, or heteroaryl; R5 and R6 are, independently, hydrogen, alkyl, hydroxyl, alkoxy, or C5 to C7 aryl; wherein any R3 to R6 group having an aryl or heteroaryl moiety can optionally be substituted on the aryl or heteroaryl moiety with 1 to about 5 substituents, independently, selected from the group consisting of halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy. Methods of making these compounds as well as methods using the compounds for treating a variety of conditions are also disclosed. | ||||||
| 178 | Substituted quinoline CCR5 receptor antagonists | US10607530 | 2003-06-26 | US07220856B2 | 2007-05-22 | Laura Dunning; Stefan Jaroch; Monica J. Kochanny; Wheeseong Lee; Xiongdong Lian; Meina Liang; Shou-Fu Lu; James Onuffer; Gary Phillips; Guo-Ping Wei; Bin Ye |
| The present invention relates to CCR5 receptor antagonists of formulae (1a) or (1b): enantiomers, diastereomers, salts and solvates thereof wherein R1, R2, R3, R4, R5, and R7 are as defined herein. The invention further includes a method of CCR5-mediated disorders employing such compounds. | ||||||
| 179 | Heat shock protein 90 inhibitors | US10976082 | 2004-10-27 | US07208630B2 | 2007-04-24 | Brian Blagg; Gang Shen; Randell C. Clevenger |
| Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol. | ||||||
| 180 | Farnesyl transferase inhibiting benzoheterocyclic derivatives | US10432292 | 2001-11-15 | US07153958B2 | 2006-12-26 | Patrick René Angibaud; Marc Gaston Venet; Virginie Sophie Poncelet |
| This invention comprises the novel compounds of formula (I) wherein r, s, t, X, Z, R1, R2, R3, R4, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine. | ||||||
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