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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
181 VITAMIN D RECEPTOR MODULATORS PCT/US2004/037182 2004-11-16 WO2005051893A2 2005-06-09 BUNEL, Emilio, Enrique; GAJEWSKI, Robert, Peter; JONES, Charles, David; LU, Jianliang; NAGPAL, Sunil; MA, Tianwei; YEE, Ying, Kwong

The present invention relates to novel, non-secosteroidal, hydroxyl substituted, carbon- linked diaryl compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1?,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.

182 AMINEDIOLS FOR THE TREATMENT OF ALZHEIMER'S DISEASE PCT/US2002/018845 2002-06-13 WO2002100818A2 2002-12-19 SCHOSTAREZ, Heinrich, Josef; CHRUSCIEL, Robert, Alan

The present invention relates to compounds of formula useful in treating Alzheimer's disease and other similar disease. These compounds include inhibitors of the betasecretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

183 AMINO(OXO)ACETIC ACID PROTEIN TYROSINE PHOSPHATASE INHIBITORS PCT/US2001/026906 2001-08-29 WO02018323A2 2002-03-07
Compound of formula (I) or therapeutically acceptable salts thereof, are protein tyrosine kinase PTP1B inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of diseases using the compounds are disclosed.
184 COMPOUNDS AND METHODS TO TREAT ALZHEIMER'S DISEASE PCT/US2001/009501 2001-03-23 WO01070672A2 2001-09-27
The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases.
185 AMINE DERIVATIVES FOR THE TREATMENT OF APOPTOSIS PCT/EP2001/001579 2001-02-13 WO01060798A1 2001-08-23
The present invention is related to substituted amine derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such amine derivatives of formula (I). Said substituted amine derivatives are efficient modulators, in particular inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel substituted amine derivatives as well as methods of their preparation.
186 HSV PRIMASE INHIBITORS PCT/CA0000324 2000-03-23 WO0058270A2 2000-10-05 SIMONEAU BRUNO; LIUZZI MICHELE; MENTRUP ANTON
The invention provides compounds of formula (1) that are active against the HSV primase enzyme: wherein R1 is hydroxy or amino; R2 is hydrogen, halo, (C1-4)alkyl or (C1-4)alkoxy; R3 is hydrogen, halo, (C1-4)alkyl, (C1-4)alkoxy, amino or azido; R4 has the same significance as R2; R5 is hydrogen or (C1-4)alkyl; and R is (C1-7)alkyl, (C3-6)cycloalkyl, {phenyl(C1-7)alkyl}, {phenyl(C1-7)alkoxy}, {{(monocyclic heterocyclo)-{(C1-7)alkoxy}}, CH(W)C(O){O-(C1-4)alkyl} wherein W is hydrogen or (C1-7)alkyl, or (A) wherein Y is hydrogen or (C1-7)alkyl, and Z is (C1-7)alkyl, (C3-6) cycloalkyl, {(C3-6)cycloalkyl}-{(C1-7)alkyl}, phenyl(C1-7)alkyl or {{(monocyclic heterocyclo)-{(C1-7)alkyl}}, or Y and Z together with the nitrogen atom to which they are attached represent, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl or 1-(4-methylpiperazinyl); with the provisos that (1) when R is CH(W)C(O)-{O-(C1-4)alkyl} as defined herein, then R5 is hydrogen; and (2) at least one of R2, R3 and R4 is other than hydrogen.
187 AROMATIC AMINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND AGENTS CONTAINING THE SAME PCT/JP1999/005755 1999-10-19 WO00023420A1 2000-04-27
Compounds represented by formula (I), or salts thereof; a process for the preparation thereof; and somatostatin receptor regulators containing the compounds or salts: wherein A is an optionally substituted aromatic ring; B is an optionally substituted cyclic hydrocarbon group; R<1> is hydrogen, optionally substituted hydrocarbyl, an optionally substituted heterocyclic group, or acyl; R<2> is optionally substituted amino; D is a free valency or a divalent group; E is -CO-, -CON(R)-, -COO-, -N(R)CON(R)-, -N(R)SO2-, -N(R)-, -O-, -S-, -SO- or -SO2-; G is a free valency or a divalent group; L is a free valency, an optionally substituted divalent hydrocarbon group which may be interrupted by -O- or -S-, or the like; X is oxygen, optionally oxidized sulfur, optionally substituted nitrogen, or an optionally substituted divalent hydrocarbon group; Y is two hydrogen atoms, oxygen, or sulfur; and the dotted line indicates that R<2> and an atom on ring B may together form a ring.
188 FUNGICIDAL COMPOSITIONS AND METHODS, AND COMPOUNDS AND METHODS FOR THE PREPARATION THEREOF PCT/US1998/025624 1998-12-03 WO99027783A1 1999-06-10
Fungicidal compositions and methods comprising acylated aminosalicylamides (AASA) described herein. Novel cyclic amines and 3-nitrosalicylamides, and their use as pesticides and in the preparation of the antifungal AASA compounds are also disclosed.
189 BINUCLEAR NON-HEME IRON CATALYSTS PCT/US1998/017610 1998-08-21 WO99010357A1 1999-03-04
The subject invention provides a binuclear metal complex having structure (I) wherein M1, and M2 are independently selected from the group consisting of Fe, Co, Mn and Ru; wherein m and n are independently +2 or +3; wherein R1, R2, R3, R4, R5 and R6 are independently a linear C1-C6 alkyl, C5-C6 cycloalkyl, phenyl, etc.; wherein (i) R1 and R2, (ii) R3 and R4, or (iii) R5 and R6 independently and optionally are linked covalently and together with the respective adjoining C atom comprise a spirocyclic ring; wherein i, j and k are integers such that 2
190 RETINOID-LIKE COMPOUNDS PCT/US1998/006214 1998-03-30 WO98047861A1 1998-10-29
The present invention relates to a compound of formula (I) wherein X is -CONH- or -NHCO-, or a nontoxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof. The compounds of the present invention exhibit retinoid-like properties and are thus useful as antiinflammatory agents for chronic skin inflammatory diseases such as psoriasis and atopic dermatitis, as agents for the treatment of rheumatic diseases such as rheumatoid arthritis, as antitumor agents for the treatment of various tumors, and as agents for the treatment of non-malignant proliferative skin conditions.
191 METHOD OF PREPARING AMINO CARBOXYLIC ACIDS PCT/US1998/002882 1998-02-12 WO98035930A1 1998-08-20
Process for the preparation of an N-acyl amino carboxylic acid by means of a carboxymethylation reaction. In this reaction, a reaction mixture is formed which contains a base pair, carbon monoxide, hydrogen and an aldehyde with the base pair conprising a carbamoyl compound and a carboxymethylation catalyst precursor. In a preferred embodiment, the carbamoyl compound and aldehyde are selected to yield an N-acyl amino carboxylic acid which is readily converted to N-(phosphonomethyl)glycine, or a salt or ester thereof.
192 N-acylethanolamide derivatives and uses thereof US17116414 2020-12-09 US11547681B2 2023-01-10 Andrew D. Levin
The present disclosure provides certain N-Acylethanolamide derivatives, and uses relating thereto.
193 Ethyl benzyl quaternary amines of amido amines for improved antifungal properties US14969920 2015-12-15 US09802908B2 2017-10-31 Thomas P. Daly
Ethyl benzyl quaternaries having superior anti-fungal properties versus their benzyl quaternary analogs. The ethylbenzyl amidoamine quaternaries of the present invention are easily produced without significant waste and with minimal capital, while possessing improved antimicrobial properties.
194 Amides, use of amides as solvents for organic compounds, compositions and emulsions containing amides, and method for treating a plant US14549990 2014-11-21 US09169195B2 2015-10-27 Adrianus Marinus Groenewegen; Kornelis Overkempe; Peter Westbye
The present invention relates in general to the use of amides of the following general formula (I) wherein R1 is a linear or branched hydrocarbyl group containing 9 to 14 carbon atoms; R2 is selected from the group consisting of methyl, ethyl and benzyl; and R3 is selected from the group consisting of hydrogen, methyl and ethyl, as solvents for organic agriculturally active ingredients, compositions comprising organic agriculturally active ingredients and such amides, methods for treating a plant utilizing such compositions, as well as some of the amides as such and methods for their production.
195 Amides useful as inhibitors of voltage-gated sodium channels US13747716 2013-01-23 US08865771B2 2014-10-21 Weichuan Caroline Chen; Paul Krenitsky; Andreas Termin; Dean Wilson
The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
196 Therapeutic peptides US13505625 2010-11-02 US08809280B2 2014-08-19 Morten Strom; Terkel Hansen; Martina Havelkova; Veronika Torfoss
The present invention provides a peptide, peptidomimetic or amino acid derivative having a net positive charge of at least +2 and incorporating a disubstituted β amino acid, each of the substituting groups in the β amino acid, which may be the same or different, comprises at least (7) non-hydrogen atoms, is lipophilic and has at least one cyclic group, one or more cyclic groups within a substituting group may be linked or fused to one or more cyclic groups within the other substituting group and where cyclic groups are fused in this way the combined total number of non-hydrogen atoms for the two substituting groups is at least (12), for use as a cytolytic therapeutic agent; as well as non therapeutic uses of these molecules and certain defined novel compounds from within this definition.
197 Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof US13752664 2013-01-29 US08772542B2 2014-07-08 Heng Cheng; Sanjeev Gangwar; Qiang Cong
Antiproliferative compounds having a structure represented by formula (II), where n, R1, R2, R3, R4, and R5 are as defined herein, can be used to treat tumors, optionally when conjugated to a ligand such as an antibody:
198 Process for the Manufacture of N-acylbiphenyl alanine US14163526 2014-01-24 US20140142320A1 2014-05-22 Guoliang Zhu; Desogn Shi; Junhui Wei; Fengfeng Tao
The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors.
199 Cationic amphiphiles with mannose-mimicking head-groups and a process for the preparation thereof US13812703 2011-09-14 US08703824B2 2014-04-22 Ramishetti Srinivas; Arup Garu; Sachin B. Agawane; Arabinda Chaudhuri
The present invention discloses novel cationic amphiphiles containing mannose-mimicking shikimic and quinic acid head-groups and a process for preparing cationic amphiphiles with mannose-mimicking polar head-groups such as, shikimic and quinic acids. The findings described herein also demonstrate that compounds of the present invention can target model DNA vaccines to antigen presenting cells (APCs) such as macrophages and dendritic cells (DCs), via mannose receptors expressed on the cell surface of APCs. The cationic amphiphiles disclosed herein show enhanced cellular and humoral immune response compared to their mannosyl counterpart in dendritic cell (DC, the most professional APC) based genetic immunization in mice. Cationic amphiphiles with mannose-mimicking quinic and shikimic acid head-groups described in the present invention are likely to find future applications in the field of genetic immunization.
200 Curable overcoat compositions US12100672 2008-04-10 US08697194B2 2014-04-15 Peter G. Odell; Jennifer L. Belelie; Michelle N. Chretien; Gordon Sisler; Christopher A. Wagner
A substantially colorless radiation overcoat composition suitable for overcoating ink-based images and xerographic-based images. The overcoat composition comprises at least one gellant, at least one monomer, at least one substantially non-yellowing photoinitiator, optionally a curable wax, and optionally a surfactant.
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