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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 Carboxylic acid amides, the preparation thereof and their use as medicaments US13866255 2013-04-19 US08791103B2 2014-07-29 Henning Priepke; Kai Gerlach; Roland Pfau; Norbert Hauel; Iris Kauffmann-Hefner; Georg Dahmann; Herbert Nar; Sandra Handschuh; Wolfgang Wienen; Annette Schuler-Metz
The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
162 Potentiation of cancer chemotherapy by 7-(2, 5-dihydro-4-imidazo [1, 2-A] pyridine-3-yl-2,5-Dioxo-1H-pyrrol-3-yl)-9-fluoro-1,2,3,4 tetrahydro-2-(1-piperidinyl-carbonyl)-pyrrolo [3,2,1-jk] [1,4] benzodiazepine US12664664 2008-06-20 US08318713B2 2012-11-27 Marcio Chedid; Thomas Albert Engler
A method for treating gastric cancer, ovarian cancer, non-small cell lung cancer, or colorectal cancer in a patient is described, as well as pharmaceutical compositions comprising 7-(2,5-dihydro-4-imidazo[1,2-a]pyridine-3-yl-2,5-dioxo-IH-pyrrol-3-yl)-9-fluoro-1,2,3,4-tetrahydro-2-(1-piperidinyl-carbonyl)-pyrrolo[3,2,1-jk][1,4]benzodiazepine, useful for the method and a process for preparing said compositions.
163 Cell migration modulating compounds US12064535 2006-08-23 US08242108B2 2012-08-14 Ana Maria Schor; Seth Lawrence Schor; Rodolfo Marquez; David George Norman
The described invention relates to compounds which modulate cell migration, and find use in, for example, wound healing, cancer progression and angiogenesis.
164 Combination product comprising an antagonist or inverse agonist of histamine receptor H3 and an antipsychotic and antidepressant agent, and use thereof for the preparation of a medicament that prevents the adverse effects of psychotropic drugs US10562396 2004-06-25 US08106041B2 2012-01-31 Jean-Charles Schwartz; Jeanne-Marie Lecomte
Medicament comprising, in a pharmaceutically acceptable vehicle, an anti-psychotic or an antidepressant (A), which, on its own, has an undesirable effect of a gain in body weight or sedation, and an antagonist and/or inverse agonist (B) of the histamine H3 receptor, the antagonist and/or inverse agonist of the histamine H3 receptor being present in a therapeutically effective amount for ensuring at least one of the following three effects: suppression or at least limitation of the undesirable effect of weight gain, suppression or limitation of the undesirable effect on alertness, epilepsy/convulsions, increase in the precognitive effect of the treatment. Use of such an antagonist or inverse agonist for the preparation of a medicament which is to ensure at least one of the said three effects in a patient treated by such an antipsychotic or antidepressant.
165 Methods for treating anxiety related disorders US11910967 2006-04-07 US08012958B2 2011-09-06 Sanjay Sabnani; Donald Wesson
The present invention relates to methods of and compositions for treating and relieving symptoms and disease associated with indications caused by a physiological drive to alleviate a sensation of anxiety. In one treatment method, methods of, and compositions for, modulating the expression of certain GABAA receptor subunits are used to treat anxiety-related disorders and depressive disorders associated with physiological tolerance to endogenous neurosteroids.
166 Methods of modulating tubulin deacetylast activity US12029333 2008-02-11 US07884081B2 2011-02-08 Eric M. Verdin; Brian J. North; Scott M. Ulrich
The present invention provides methods for identifying agents that modulate a level or an activity of tubulin deacetylase polypeptide, as well as agents identified by the methods. The invention further provides methods of modulating tubulin deacetylase activity in a cell. The invention further provides methods of modulating cellular proliferation by modulating the activity of tubulin deacetylase.
167 Aspartyl protease inhibitors US11451541 2006-06-12 US07868000B2 2011-01-11 Zhaoning Zhu; Brian McKittrick; Andrew Stamford; William J. Greenlee; Xiaoxiang Liu; Mihirbaran Mandal; Johannes H. Voigt; Corey O. Strickland
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein j, k, U, W, R, R1, R2, R3, R4, R6, R7 and R7a are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
168 Pyrrole derivatives as antimycobacterial compounds US12137170 2008-06-11 US07763602B2 2010-07-27 Sudershan Kumar Arora; Neelima Sinha; Sanjay Jain; Ram Shankar Upadhayaya; Gourhari Jana; Shankar Ajay; Rakesh Kumar Sinha
Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).
169 Pharmaceutical composition of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine and uses thereof US10728261 2003-12-03 US07745431B2 2010-06-29 Herbert W. Harris; Robert F. Kucharik; Steven M. Leventer
Pharmaceutical compositions comprising 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine; or a pharmaceutically acceptable salt thereof. The compositions are used for treating, preventing or delaying the onset of disorders mediated by LTB4, TXA2 or adenosine.
170 HIV-1 mutations selected for by β-2′,3′-didehydro-2′,3′-dideoxy-5-fluorocytidine US11542044 2006-10-03 US07635690B2 2009-12-22 Raymond F. Schinazi; Jennifer L. Hammond; John W. Mellors; Dennis C. Liotta
The present invention discloses a method for treating HIV that includes administering β-D-D4FC or its pharmaceutically acceptable salt or prodrug to a human in need of therapy in combination or alternation with a drug that induces a mutation in HIV-1 at a location other than the 70(K to N), 90 or the 172 codons of the reverse transcriptase region. Also disclosed is a method for using β-D-D4FC as “salvage therapy” to patients which exhibit drug resistance to other anti-HIV agents. β-D-D4FC can be used generally as salvage therapy for any patient which exhibits resistance to a drug that induces a mutation at other than the 70(K to N), 90 or the 172 codons.
171 Pharmaceutical compositions for the treatment of diseases related to neurotrophines US10518689 2003-06-18 US07625892B2 2009-12-01 Antonio Guarna; Federico Cozzolino; Maria Torcia; Enrico Garaci
The present invention refers to pharmaceutical preparations including as active compounds 3-aza-bicyclo[3.2.1]octane derivatives of general formula (I) and/or their dimers of general formula (II) and (III) acting as agonists of human neurotrophines. Therefore, such compounds of formula (I), (II) and (III) are useful for treatment of diseases in which the neurotrophine functions are involved in defect, particularly of Nerve Growth Factor (NGF), such as neurodegenerative diseases of central nervous system (CNS), acquired immunodeficiency due to a reduced NGF biodisponibility, or morbous conditions in which the stimulus of neoangiogenesis process is convenient.
172 Modified pyrimidine glucocorticoid receptor modulators US11174096 2005-06-29 US07576076B2 2009-08-18 Robin D. Clark; Nicolas C. Ray; Karen Williams; Peter H. Crackett; Gwen Hickin; David A. Clark
The present invention provides a compound having the formula: wherein, n and m are 1; X1 and X2 are O; R1 is a member selected from unsubstituted phenyl and substituted phenyl; R2 is a member selected from hydrogen, —CN, —OR2A, -L2A—C(O)R2B, -L2B—S(O)2R2C; R3 is a member selected from unsubstituted benzyl and substituted benzyl; R4 is a member selected from hydrogen and substituted or unsubstituted alkyl, wherein if R4 is methyl, then -L1-R1 is not benzyl or —C(O)—O—CH2—CH3; and L1 is a bond; and compositions and methods of using the compounds as glucocorticoid receptor modulators.
173 Methods and Compositions For Repelling Arthropods US11953343 2007-12-10 US20080188456A1 2008-08-07 Ulrich R. Bernier; Kenneth Posey; Daniel L. Kline; Donald Barnard; Kamal Chauhan
A method for repelling arthropods involving treating an object or area with an arthropod repelling effective amount of at least one compound having the formula wherein X is O, S, NH, N-NH2, N-CH3 or CH2, R′ is H or alkyl, R″ is alkyl, n is 0, 1, 2, 3 or 4, and mixtures thereof, optionally including a carrier material or canier. The compound is preferably selected from homopiperazine, 1-methylhomopiperazine, 1-methylpyrrolidine, (R)-(−)-2-methylpiperazine, (S)-(+)-2-methylpiperazine, 2-methylpiperazine, 1-methylpiperazine, pyrrolidine, 1-methylpiperidine, piperidine, 1-ethylpiperazine, 1-methylimidazolidine, 1-methylthiomorpholine, 1,4-dimethylpiperazine, homopiperidine, imidazolidine, 4-methylpiperidine, thiomorpholine, 1-amino-4-methylpiperazine, 4-methylmorpholine, azocane, 2,6-dimethylpiperazine, 2,5-dimethylpiperazine, piperazine, 1-methlyhomopiperidine, or mixtures thereof.
174 Pyridyl derivatives and their use as therapeutic agents US10566857 2004-07-29 US20060293308A1 2006-12-28 Melwyn Abreo; Daniel Harvey; Mikhail Kondratenko; Wenbao Li; Rajender Kamboj; Vishnumurthy Rodumuru; Michael Winther; Heinz Gschwend; Nagasres Chakka; Shifeng Liu; Serguei Sviridov; Shaoyi Sun
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): wherein W, V, x, y, R1, R2, R3, R4, R5, R6, R7, R7a, R8, R8a, R9, R9a, R10 and R10a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
175 Insecticidal tricyclic derivatives US10528740 2003-09-12 US20060111342A1 2006-05-25 Joseph Argentine; Franz Schuler; John Dixson; Scott Crawford; Daniel Cohen; Elizabeth Rowley; Saroj Sehgel
It has now been found that certain tricyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula I: wherein R1 through R8, inclusively, and X and Y are fully described. Compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to the locus where insects are present or are expected to be present.
176 Pesticidal dibenzo(hetero)azepine derivatives US10539643 2003-12-18 US20060069083A1 2006-03-30 Gerd Steiner; Livio Tedeschi; Thomas Schmidt; Ernst Baumann; Wolfgang Deyn; Markus Kordes; Michael Hofmann; Michael Puhl; Norbert Gotz; Michael Rack; Liliana Rapado; Jacobus Kramer; Gavin Heffernan; Deborah Culbertson; Michael Treacy; Hassan Oloumi-Sadeghi; Cecille Ebuenga; Toni Bucci
Use of compounds of formula (I): wherein X is S, O, S═O, SO2, NRa, or CRbRc; R1, R2 are halogen, OH, SH, NH2, CN, NO2, alkyl, alkoxy, alkylamino, dialkylamino, alkylthio, alkenyl, alkenyloxy, alkenylamino, alkenylthio, alkynyl, alkynyloxy, alkynylamino, alkynylthio, alkylsulfonyl, alkylsulfoxyl, alkenylsulfonyl, alkynylsulfoxyl, formyl, alkylcarbonyl, hydroxycarbonyl, alkoxycarbonyl, carbonyloxy, alkylcarbonyloxy, phenyloxy, alkylcarbonylamino, C(O)NRdRe, or (SO2)NRdRe, or C(═NORf)-Gp-Rf′, or a mono- or bicyclic 5- to 10-membered aromatic or heteroaromatic ringsystem, optionally substituted, which is unfused or fused to the aromatic group to which it is bonded and which, when unfused, is bonded directly or through an O, S, alkyl, or alkoxy linkage, or cycloalkyl, wherein the carbon atoms in these groups may be substituted. R3, R4 are each-independently H, alkyl, haloalkyl, alkylamino, alkoxy, cycloalkyl, wherein the carbon atoms in these groups may be substituted, or R3 and R4 together with the nitrogen atom to which they are attached form a saturated or partially saturated mono- or bicyclic 5- to 10-membered ringsystem or 5-membered hetaryl, phenyl or benzyl, wherein the rings are optionally substituted, or R3 and R4 together form the chains —(CH2)2N+(O—)(CH2)2— or —(CH2)3N+(O−)(CH2)2—; and Ra, Rb, Rc, Rd, Re′ Rf, Rf′ G, and p are as defined in the description; m is 0, 1, 2, 3 or 4; n is 0, 1, 2, 3 or 4; or the enantiomers or diastereomers, salts or esters thereof for combatting insects, arachnids, or nematodes, methods for the control of these pests and of protecting growing plants from attack or infestation by these pests by applying a pesticidally effective amount of compounds of formula I, compounds of formula I, processes for preparing them, and compositions comprising them.
177 Benzamide compounds for cancer imaging and therapy US468907 1995-06-06 US5993777A 1999-11-30 Christy S. John; Jesse Baumgold; John G. McAfee; Terry Moody; Wayne Bowen
The present invention relates to a class of compounds having affinity for certain cancer cells, e.g. lung carcinomas, colon carcinomas, renal carcinomas, prostate carcinomas, breast carcinomas, malignant melanomas, gliomas, neuroblastomas and pheochromocytomas. The compounds of the present invention can also bind with high specificity to cell surface sigma receptors and can therefore be used for diagnostic imaging of any tissue having an abundance of cells with sigma receptors. The present invention provides such compounds as agents for diagnostic imaging and for detecting and treating tumors containing the cancer cells described above.
178 2-substituted phenyl-benzimidazole antibacterial agents US924558 1997-09-05 US5942532A 1999-08-24 Kwasi Adomako Ohemeng; Van Nhatton Nguyen
The invention relates to benzimidazole antibacterial compounds of the Formula I: ##STR1## as described herein, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.
179 1-(3-aminoindazol-5-yl)-3-phenylmethyl-cyclic ureas useful as HIV protease inhibitors US966491 1997-11-07 US5932570A 1999-08-03 James David Rodgers; Robert Frank Kaltenbach, III
The present invention relates to compounds of formulae I and II: ##STR1## or pharmaceutically acceptable salt forms or prodrugs thereof, which are useful as inhibitors of HIV protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
180 Psychoactive substance disorders US748294 1996-11-13 US5817657A 1998-10-06 Charles M. Beasley, Jr.; Jiban Kumar Chakrabarti; Terrence Michael Hotten; David Edward Tupper
2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-�2,3-b!�1,5!benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders relating to the use of psychoactive substances. The compound has the following structure: ##STR1##