| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 141 | Substituted imidazoquinoline derivatives as kinase inhibitors | US13810431 | 2011-07-15 | US09062046B2 | 2015-06-23 | Sanjay Kumar; Rajiv Sharma; Robert Zahler; Bichismita Sahu; Veena R. Agarwal; Nishigandha Naik |
| The present invention relates to substituted imidazo[4,5-c]quinoline derivatives, the compounds of formula (I), wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, processes for their preparation, pharmaceutical compositions comprising compounds of formula (I), and their use in the treatment of diseases or disorders mediated by one or more kinases, particularly proliferative diseases or disorders such as cancer. These compounds can also be used in the treatment of inflammatory diseases and angiogenesis related disorders. | ||||||
| 142 | Nicotinic acetylcholine receptor agonists | US13583420 | 2011-03-18 | US09018227B2 | 2015-04-28 | Richard W. Fitch; Thomas F. Spande; H. Martin Garraffo; Herman J. C. Yeh; John W. Daly |
| The invention provides novel nicotinic acetylcholine receptor agonists, for example, phantasmidine and derivatives thereof, for example a compound of formula (I). Also disclosed are methods of treating disorders responsive to nicotinic acetylcholine receptor agonists such as Alzheimer's disease, schizophrenia, Myasthenia Gravis, Tourette's syndrome, Parkinson's disease, epilepsy, pain, and cognitive dysfunction by treatment with the nicotinic acetylcholine for agonists. | ||||||
| 143 | One pot process for producing 6-hydroxyl nal-opiate | US13762431 | 2013-02-08 | US09012468B2 | 2015-04-21 | Peter X. Wang; Tao Jiang |
| The present invention provides processes for preparing nal-opiates without the isolation of intermediates. In general, the process provides for alkylation and reduction in the same pot to give the nal-opiate. | ||||||
| 144 | Benzothiophene compound | US14298208 | 2014-06-06 | US08981119B2 | 2015-03-17 | Tsukasa Ishihara; Kazuhiro Ikegai; Ikumi Kuriwaki; Hiroyuki Hisamichi; Nobuaki Takeshita; Ryuichi Takezawa |
| The present invention is directed to compounds of Formula I: wherein R1, R2, R3, R4, R5, X and n are described herein. These compounds and their pharmaceutically acceptable salts thereof are useful as IK1 channel activators. | ||||||
| 145 | Fused ring compound for use as mineralocorticoid receptor antagonist | US13817462 | 2011-08-18 | US08946279B2 | 2015-02-03 | Zhenhua Huang; Jinyuan Wang; Dedong Zhang |
| The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of X, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4, Cy and n are as presented in the description. | ||||||
| 146 | Methods for improving cognitive function | US13327226 | 2011-12-15 | US08946206B2 | 2015-02-03 | Craig C. Garner; H. Craig Heller; Damien Colas; Daniel Z. Wetmore |
| Provided herein are methods, drug formulations, and dosing regimens for improving cognitive function in a normal or cognitively impaired subject. For instance, methods provided herein comprise administering a GABAA receptor antagonist so that peak concentration of the GABAA receptor antagonist occurs when the subject is asleep. | ||||||
| 147 | Preparation of low impurity opiates in a continuous flow reactor | US13582334 | 2011-03-21 | US08921557B2 | 2014-12-30 | Beat Weber; Stefan Sahli |
| The present invention relates to a novel process for preparing opiates or salts thereof. More particularly, the present invention relates to oxidizing the starting material in a continuous flow reactor, followed by either an isolation of the intermediate, or a direct reduction reaction. | ||||||
| 148 | Imidazo[1,2-a]pyridine derivative | US13661601 | 2012-10-26 | US08822688B2 | 2014-09-02 | Kiyohiro Samizu; Naoyuki Masuda; Kazuhiko Iikubo; Yohei Koganemaru; Noriyuki Kawano; Junya Ohmori; Yasuyuki Mitani; Keni Ni |
| [Problem]To provide a compound useful as medicine having PDE4B inhibitory activity, in particular, as an active ingredient of a composition for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like.[Measures for Solution]The present inventors examined compounds having PDE4B inhibitory activity and found that a tricyclic or tetracyclic imidazo[1,2-a]pyridine derivative or salts thereof had a superior PDE4B inhibitory activity, thereby completing the present invention. The imidazo[1,2-a]pyridine derivative can be used as an agent for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like. | ||||||
| 149 | Pyrazoloquinolines | US13807954 | 2011-06-24 | US08802712B2 | 2014-08-12 | Thomas Fuchss; Werner Mederski; Frank Zenke |
| The invention relates to compounds of the formulae (I), (II) and (III), and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formula (II) or (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of its salts | ||||||
| 150 | Substituted 6,7-dialkoxy-3-isoquinolinol derivatives as inhibitors of phosphodiesterase 10 (PDE10A) | US13399351 | 2012-02-17 | US08772316B2 | 2014-07-08 | Bertrand Leblond; John E. Donello; Cédric Chauvignac; Thierry Taverne; Eric Beausoleil; Anne-Sophie Casagrande; Laurent Désiré; Matthew P. Pando; Rong Yang |
| The invention relates to compounds of the formula 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. | ||||||
| 151 | Pharmacological treatment of cognitive impairment | US11752188 | 2007-05-22 | US08729067B2 | 2014-05-20 | Craig C. Garner; Fabian J. Fernandez |
| Methods for treating an individual to improve cognitive function are provided. In the subject methods, an effective amount of a noncompetitive GABAA ionophore blocker is administered to the individual, resulting in an improvement in cognitive function of the host. The subject methods find use in a variety of different applications. | ||||||
| 152 | Treatment with opioid antagonists and mTOR inhibitors | US12933784 | 2009-03-20 | US08685995B2 | 2014-04-01 | Jonathan Moss; Patrick A. Singleton |
| Embodiments of the invention provide methods of treating a disorder or disease characterized by cellular proliferation and migration by co-administering a synergistically effective amount of an mTOR inhibitor and a μ-opioid receptor antagonist. | ||||||
| 153 | Macrocyclic derivatives for the treatment of diseases | US13786106 | 2013-03-05 | US08680111B2 | 2014-03-25 | Simon Bailey; Benjamin Joseph Burke; Michael Raymond Collins; Jingrong Jean Cui; Judith Gail Deal; Robert Louis Hoffman; Qinhua Huang; Ted William Johnson; Robert Steven Kania; John Charles Kath; Phuong Thi Quy Le; Michele Ann McTigue; Cynthia Louise Palmer; Paul Francis Richardson; Neal William Sach |
| The invention relates to compounds of formula (Φ) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer. | ||||||
| 154 | Lyotropic liquid crystal systems based on aromatic tetracarboxylic bisbenzoimidazole derivatives and methods for making | US13203412 | 2010-02-24 | US08674103B2 | 2014-03-18 | Robert Ramirez; Shijun Zheng; Zongcheng Jiang; Shuangxi Wang; Michiharu Yamamoto |
| Compounds derived from aromatic tetracarboxyl bisbenzoimidazoles are disclosed. These compounds are capable of forming liquid crystal systems that can produce optically isotropic or anisotropic films with desirable optical properties. Formulae (I) or (II), or a salt thereof; wherein y is an integer in the range from 0 to about 4. | ||||||
| 155 | Photoluminescent metal complexes for protein staining | US12274979 | 2008-11-20 | US08664396B2 | 2014-03-04 | Tom Berkelman |
| A method of staining a poly(amino acid) by contacting a poly(amino acid) with an overall neutral or overall cationic complex of at least one of transition metal ion, and a plurality of donor ligands each of which is fully coordinated to the transition metal ion and is either a nitrogen donor ligand or a cyclometalated donor ligand, such that at least one of the donor ligands is a cyclometalated donor ligand. Nitrogen donor ligands will contain heteroaryl ring systems having from 10 to 40 ring atoms, wherein each nitrogen donor ligand is substituted with from 0 to 4 R1 groups. Cyclometalated donor ligands will likewise contain heteroaryl ring systems having from 10 to 40 ring atoms, such that at least one ring atom is N, wherein each cyclometalated donor ligand is substituted with from 0 to 4 R1 groups. R1, R2, R3 and R4 groups are defined herein. | ||||||
| 156 | Chemokine receptor antagonists and methods of use thereof | US13245436 | 2011-09-26 | US08653096B2 | 2014-02-18 | 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: or physiologically acceptable salt thereof. | ||||||
| 157 | Abuse deterrent and anti-dose dumping pharmaceutical salts useful for the treatment of attention deficit/hyperactivity disorder | US13444123 | 2012-04-11 | US08653065B1 | 2014-02-18 | Clifford Riley King; Stephen G. D'Ambrosio; David W. Bristol |
| A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic. | ||||||
| 158 | Modulators of 5-HT receptors and methods of use thereof | US12909319 | 2010-10-21 | US08546377B2 | 2013-10-01 | Ying Wang; Jason T. Brewer; Irini Akritopoulou-Zanze; Stevan W. Djuric; Frauke Pohlki; Wilfried Braje; Ana-Lucia Relo |
| The present application relates to 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,4]benzodiazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,5]benzodiazepine, 2,3,4,4a,5,6,7,11b-octahydro-1H-pyrido[3,4-d][2]benzazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1]benzazepine, 1,2,3,4,4a,5-hexahydro-7H-pyrazino[1,2-a][4,1]benzoxazepine, and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[2,1-d][1,5]benzoxazepine, and 5,6,7,7a,8,9,10,11-octahydropyrazino[1,2-d]pyrido[3,2-b][1,4]diazepine derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X1, X2, X3, X4, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds. | ||||||
| 159 | Modulators of 5-HT receptors and methods of use thereof | US12765034 | 2010-04-22 | US08518933B2 | 2013-08-27 | Ying Wang; Jason T. Brewer; Irini Akritopoulou-Zanze; Stevan W. Djuric; Bhadra Shelat; Frauke Pohlki; Wilfried Braje; Ana-Lucia Relo |
| The present application relates to 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2 -a][1,4]benzodiazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,5]benzodiazepine, 2,3,4,4a,5,6,7,11b-octahydro-1H-pyrido[3,4-d][2]benzazepine, 1,2,3,4,4a,5,6,7 -octahydropyrazino[1,2-a][1]benzazepine, 1,2,3,4,4a,5-hexahydro-7H-pyrazino[1,2 -a][4,1]benzoxazepine, and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[2,1-d][1,5]benzoxazepine, and 5,6,7,7a,8,9,10,11-octahydropyrazino[1,2-d]pyrido[3,2-b][1,4]diazepine derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X1, X2, X3, X4, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds. | ||||||
| 160 | Method for treatment of neurologic dysfunction | US12657052 | 2010-01-12 | US08440685B1 | 2013-05-14 | Elaine A. DeLack |
| A method for treatment of the symptoms of neurologic dysfunctions, including major depression, an autism spectrum disorder (ASD), and schizophrenia. The patient is administered an amount of a compound that increases the catalytic activity of MAO-A. The effective compound is preferably reserpine, administered in a dosage of less than about 0.03 mg per day. The reserpine may be administered topically or transdermally at a dosage in the range from about 0.002 mg per day to about 0.02 mg per day. | ||||||
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