| 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 | Glucosylceramide synthase inhibitors | US14030725 | 2013-09-18 | US09139580B2 | 2015-09-22 | Elyse Bourque; Bradford Hirth; Renato Sklerj; Elina Makino; Fazeela Morshed; Lingyun Li; Paul Mason; John P. Leonard; James Lillie; Hanlan Liu; Mary A. Cromwell; Bing Wang; Thomas O'Shea |
| The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer. | ||||||
| 182 | Compounds | US14097693 | 2013-12-05 | US09090606B2 | 2015-07-28 | Elisabetta Armani; Gabriele Amari; Mauro Riccaboni; Charles Baker-Glenn |
| Compounds of formula (I) defined herein are both inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of a disease of the respiratory tract characterized by airway obstruction. | ||||||
| 183 | 2,5-methano- and 2,5-ethano-tetrahydrobenzazepine derivatives and use thereof to block reuptake of norepinephrine, dopamine, and serotonin | US13211678 | 2011-08-17 | US09045468B2 | 2015-06-02 | Peter R. Guzzo; Shuang Liu; Kristen N. Ryan; Bruce F. Molino; Russell DeOrazio; Richard E. Olson; John E. Macor |
| The compounds of the present invention are represented by the following 2,5-methano- and 2,5-ethano-tetrahydrobenzazepine derivatives having formula (I): where the carbon atom designated * is in the R or S configuration when n is 1 and the substituents X and R1-R7 are as defined herein. | ||||||
| 184 | Highly pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione and methods of preparing same | US13788271 | 2013-03-07 | US09000005B2 | 2015-04-07 | Yoshitaka Nakamura; Jo Ooyama |
| The present invention relates to highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. The present invention also relates to methods for preparing highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. | ||||||
| 185 | Anti-viral compounds | US12964027 | 2010-12-09 | US08921514B2 | 2014-12-30 | David A. DeGoey; Warren M. Kati; Charles W. Hutchins; Pamela L. Donner; Allan C. Krueger; John T. Randolph; Christopher E. Motter; Lissa T. Nelson; Sachin V. Patel; Mark A. Matulenko; Ryan G. Keddy; Tammie K. Jinkerson; Yi Gao; Dachun Liu; John K. Pratt; Todd W. Rockway; Clarence J. Maring; Douglas K. Hutchinson; Charles A. Flentge; Rolf Wagner; Michael D. Tufano; David A. Betebenner; Kathy Sarris; Kevin R. Woller; Seble H. Wagaw; Jean C. Califano; Wenke Li; Daniel D. Caspi; Mary E. Bellizzi; William A. Carroll |
| Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection. | ||||||
| 186 | Process for the preparation of cis-2-methylspiro (1,3-oxathiolane 5-3′) quinuclidine | US12796308 | 2010-06-08 | US08450487B2 | 2013-05-28 | Ravishanker Kovi; Jayaraman Kannapan; Talluri Buhshaiah Chowdari; Chirag Vasantlal Shah |
| Methods are provided for making pharmaceutical-grade cis-2-methylspiro(1,3-oxathiolane-5,3′)quinuclidine and pharmaceutically acceptable salts thereof by isomerizing racemic 2-methylspiro(1,3-oxathiolane-5,3′)quinuclidine to cis-2-methylspiro(1,3-oxathiolane-5,3′)quinuclidine and subsequent purification of the C-MSOQ by salt formation with inexpensive and commercially available material such as sulfuric acid. Purification methods are disclosed which employ an organic solvent/water system and recrystallization with an organic solvent such as acetone. | ||||||
| 187 | 1,3-Dioxanes and Their Uses | US13526110 | 2012-06-18 | US20120252836A1 | 2012-10-04 | Alexandra Santana Sorensen; Jean-Phillippe Meyer; Peteris Alberts; Mainkar Prathama |
| The present invention relates to compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer. | ||||||
| 188 | Aminomethyl azaadamantane derivatives and methods of use thereof | US12052093 | 2008-03-20 | US08168791B2 | 2012-05-01 | Lei Shi; Marc J. C. Scanio; William H. Bunnelle |
| The invention relates to compounds that are substituted aminomethyl azaadamantane derivatives, compositions comprising such compounds, and methods of using such compounds and compositions. | ||||||
| 189 | Indole derivatives as CRTH2 receptor antagonists | US11990378 | 2006-08-07 | US07696222B2 | 2010-04-13 | Zhaoyin Wang |
| Compounds according to formula (I) wherein the radicals R1, R2 and R3 are as herein defined, and wherein Ar represents an aryl group or heteroaryl group, preferably phenyl, n is 1 or 2, and the radical X represents a group selected from —C(Ra)(Rb)—, —C(Ra)(Rb)—C(Ra)(Rb)—, —C(Ra)═C(Ra)—, OC(Ra)(Rb)— or SC(Ra)(Rb)—. These compounds and their pharmaceutical acceptable salts are used in pharmaceutical compositions as prostaglandine D2 receptor antagonists useful in the treatment of CRTH2-mediated diseases such as respiratory, inflammatory or allergic conditions among others. | ||||||
| 190 | Imaging agents and methods of imaging alpha7-nicotinic cholinergic receptor | US12321951 | 2009-01-26 | US20100034741A1 | 2010-02-11 | Martin G. Pomper; John L. Musachio; Hong Fan; Robert F. Dannals; Catherine Foss; Eifion Phillips; John Gordon; Dennis McCarthy; Richard Keith; Mark Smith; Richard Heys; Peter N. Dorff |
| The present invention relates to radiolabelled compounds particularly 1-azabicyclo[2.2.2]octane compounds (i.e., quinuclidine compounds) which are labeled with one or more radioisotopes and which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors which express the α7-nicotinic cholinergic receptor. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled compounds of the invention, particularly tissues, organs, or tumors which express α7-nicotinic cholinergic receptor to which the compounds of the invention have an affinity. | ||||||
| 191 | Nicotinic Acetylcholine Receptor Modulators | US11934583 | 2007-11-02 | US20090118326A1 | 2009-05-07 | Faming Jiang; Taline Khroyan; Cris M. Olsen; Willma E. Polgar; Lawrence R. Toll; Nurulain T. Zaveri |
| The disclosure provides compounds capable of selectively or non-selectively modulating nicotinic acetylcholine receptors. The compounds, compositions, and methods described herein are useful, for example, in treating patients suffering from various medical conditions including pain, chemical addictions, Parkinson's disease, Alzheimer's disease, and neurodegenerative disorders. In one embodiment, the compounds comprise a 7- to 11-membered azabicyclo ring. | ||||||
| 192 | Aminomethyl Azaadamantane Derivatives and Methods of Use Thereof | US12052093 | 2008-03-20 | US20080262023A1 | 2008-10-23 | Lei Shi; Marc J.C. Scanio; William H. Bunnelle |
| The invention relates to compounds that are substituted aminomethyl azaadamantane derivatives, compositions comprising such compounds, and methods of using such compounds and compositions. | ||||||
| 193 | Arylalkylamine Vanadium (V) Salts for the Treatment and/or Prevention of Diabetes Mellitus | US11571439 | 2005-07-01 | US20080227809A1 | 2008-09-18 | Miriam Royo Exposito; Luc Marti Clauzel; Anna Abella Marti; Silvia Garcia Vicente; Xavier Testar Ymbert; Antonio Zorzano Olarte; Manuel Palacin Prieto; Fernando Albericio Palomera; Francesc Yraola Font; Alec Mian |
| This invention provides compounds and pharmaceutical compositions thereof for treating human type 1 and type 2 diabetes, particularly insulin-resistant diabetes. | ||||||
| 194 | Compounds Having Antitumor Activity | US10585972 | 2005-02-08 | US20080227683A1 | 2008-09-18 | Gianfranco Peluso; Menotti Calvani |
| Disclosed is the use of compounds of formula (I) wherein X, Y and Z are as defined in the description of the invention, for the preparation of an antitumor medicament, optionally in combination with different biologically active substances. | ||||||
| 195 | Mutilin-Derivative Substituted at Position 12 | US11794312 | 2005-12-21 | US20080221330A1 | 2008-09-11 | Masanori Takadoi; Yasumichi Fukuda; Taro Sato; Osamu Nagae; Ryuta Kishi; Hideyuki Fukuda |
| A position 12-substituted mutilin derivative, a novel mutilin analogue, is provided that exhibits strong antimicrobial activity against abroad spectrum of Gram-positive or Gram-negative bacteria, including various drug-resistant bacteria, as well as intermediates for the production of such mutilin derivatives.Specifically, a mutilin derivative or an acid-addition salt thereof is provided that is represented by the following chemical formula (1): (wherein R1 is a hydrogen atom, a formyl group, a substituted or unsubstituted lower alkyl group, an aralkyl group whose aromatic ring may be optionally substituted, a heteroaralkyl group whose aromatic ring may be optionally substituted or a lower alkyloxycarbonyl group; and R2 is a hydrogen atom, a lower alkyl group or an aralkyl group whose aromatic ring may be optionally substituted) (R1 is neither an ethyl group nor a vinyl group). | ||||||
| 196 | 3-QUINUCLIDINYL AMINO-SUBSTITUTED BIARYL DERIVATIVES | US11749779 | 2007-05-17 | US20070275975A1 | 2007-11-29 | Jianguo Ji; Tao Li; Ying Wang |
| Compounds of formula (I) wherein A is N or N+—O−; n is 0, 1, or 2; Y is O, S, —NH—, and —N-alkyl-; Ar1 is both 6-membered aromatic rings; Ar2 is 5- or 6-membered aromatic rings with a —NR8R9 group, as defined herein. The compounds are useful in treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formula (I) and methods for using such compounds and compositions. | ||||||
| 197 | Substituted N-cycloexylimidazolinones, process for their preparation and their use as medicaments | US11042713 | 2005-01-25 | US07241787B2 | 2007-07-10 | Lothar Schwink; Thomas Boehme; Matthias Gossel; Siegfried Stengelin |
| The invention relates to substituted N-cyclohexylheterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to processes for their preparation and to their use as medicaments.Compounds of the formula I, in which the radicals have the stated meanings, and the physiologically tolerated salts thereof, and process for their preparation are described. The compounds bring about for example a weight reduction in mammals and are suitable for example for the prevention and treatment of obesity and diabetes. | ||||||
| 198 | Chemokine receptor antagonists and methods of use thereof | US10487168 | 2002-11-13 | US07186729B2 | 2007-03-06 | Jay R. Luly; Yoshisuke Nakasato; Etsuo Ohshima; Geraldine C. B. Harriman; Kenneth G. Carson; Shomir Ghosh; Amy M. Elder; Karen M. Mattia |
| 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: formula (1) or physiologically acceptable salt thereof | ||||||
| 199 | Acylated spiropiperidine derivatives as melanocortin-4 receptor agonists | US10548350 | 2004-03-31 | US20060183904A1 | 2006-08-17 | Liangqin Guo; Shuwen He; Tianying Jian; Jian Liu; Yingjie Lai; Ravi Nargund; Iyassu Sebhat; Feroze Ujjainwalla; Zhixiong Ye; Jonathan Young |
| Certain novel N-acylated spiropiperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction. | ||||||
| 200 | N-aryl diazaspiracyclic compounds and methods of preparation and use thereof | US11173944 | 2005-07-01 | US20050272739A1 | 2005-12-08 | Balwinder Bhatti; Craig Miller; Jeffrey Schmitt |
| Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl diazaspirocyclic compounds, bridged analogs of N-heteroaryl diazaspirocyclic compounds, or prodrugs or metabolites of these compounds. The aryl group can be a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g., side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastro-intestinal tract, and significant effects upon skeletal muscle). | ||||||
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