| 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 | EXCITATORY AMINO ACID RECEPTOR MODULATORS | PCT/US2001/010832 | 2001-05-24 | WO01092213A2 | 2001-12-06 | |
| Compounds of the formula (I) in which: R<1> is (CH2)nY; n is 1 or 2; Y is NHSO2R<2> or X<1>-W-X<2>-R<3>; X<1> is O or NH; W is C=O, C=S, C=NH, or SO2; X<2> is O or NH, provided that X<1> and X<2> are not both O; R<2> is C1-10 alkyl; C2-10 alkenyl; C2-10 alkynyl; aryl; aryl-C1-10 alkyl; aryl-C2-10 alkenyl; aryl-C2-10 alkynyl; C3-8 cycloalkyl or C3-8-cycloalkyl-C1-10 alkyl; and R<3> is hydrogen, C1-10 alkyl; C2-10 alkenyl; C2-10 alkynyl; aryl; aryl-C1-10 alkyl; aryl-C2-10 alkenyl; aryl-C2-10 alkynyl; C3-8 cycloalkyl; or C3-8-cycloalkyl-C1-10 alkyl; or a salt or ester thereof, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous system. | ||||||
| 162 | GELLING OR COAGULATING AGENTS FOR LIQUID ORGANIC MEDIA | PCT/JP2000/001234 | 2000-03-02 | WO00053576A1 | 2000-09-14 | |
| Novel N< alpha >-alkyl- or alkenylcarbamoyl-N< omega >-acylamino acid esters represented by general formula (1); (wherein R<1> is linear or branched C7-C21 alkyl or alkenyl; R<2> is linear, branched or cyclic C1-C22 alkyl or alkenyl; R<3> is linear, branched or cyclic C8-C22 alkyl or alkenyl; and n is an integer of 2 to 4). These esters can gel or coagulate a wide variety of liquid organic media by the addition thereof even in a small amount to give gels excellent in long-term and ordinary-temperature stability, and can be synthesized by an easy and simple process, thus being useful as excellent gelling or coagulating agents. | ||||||
| 163 | PSMA-binding agents and uses thereof | US17237850 | 2021-04-22 | US12070513B2 | 2024-08-27 | Martin G. Pomper; Ronnie Charles Mease; Ying Chen |
| Prostate-specific membrane antigen (PSMA) binding compounds having radioisotope substituents are described, as well as chemical precursors thereof. Compounds include pyridine containing compounds, compounds having phenylhydrazine structures, and acylated lysine compounds. The compounds allow ready incorporation of radionuclides for single photon emission computed tomography (SPECT) and positron emission tomography (PET) for imaging, for example, prostate cancer cells and angiogenesis. | ||||||
| 164 | NAMPT MODULATORS | US17923167 | 2021-05-05 | US20230348369A1 | 2023-11-02 | Antonio ROMERO; Aroop CHANDRA; Christopher EVANS; Minxing SHEN |
| Provided are compounds of Formula (II): or a pharmaceutically acceptable salt thereof, wherein R1, n, and Y1 are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (II), or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula (II), or a pharmaceutically acceptable salt thereof. | ||||||
| 165 | Urea group containing anti-sagging rheology control agents | US16955430 | 2018-12-20 | US11702385B2 | 2023-07-18 | Christiane Knappke-Bongartz; René Nagelsdiek; Sylvia Bühne; Agnetha Klein; Berthold Jacobs |
| The present invention relates to a urea group containing product comprising one or more species of formula (I) R1—X—(C═O)—[NH—R2—NH—(C═O)—NH—R3—NH—(C═O)]n—NH—R2—NH—(C═O)—X—R1 (I), 5 wherein R1 is independently selected from organic groups having (4) to (200) carbon atoms, X is O or NR4, wherein R4 is a hydrogen atom or an aliphatic or aromatic group having (1) to (30) carbon atoms, R2 is independently selected from hydrocarbyl groups having (4) to (40) carbon atoms, R3 is independently selected from hydrocarbyl groups having (2) to (40) carbon atoms, and wherein on average (76) to (100) mol % of all R3 groups contained in the one or more species of formula (I) are hydrocarbyl groups having (2) or (3) carbon atoms, and n is an integer of (2) to (150). The invention further relates to a method of manufacturing such urea group containing products, liquid compositions containing the same and the use of such liquid compositions as rheology control additives. Furthermore, the invention relates to a process for rheology adjustment adding such liquid composition to semi-finished or final products. The invention also relates to an article coated with the liquid composition. | ||||||
| 166 | UREA GROUP CONTAINING ANTI-SAGGING RHEOLOGY CONTROL AGENTS | US16955430 | 2018-12-20 | US20210070697A1 | 2021-03-11 | Christiane Knappke-Bongartz; René Nagelsdiek; Sylvia Bühne; Agnetha Klein; Berthold Jacobs |
| The present invention relates to a urea group containing product comprising one or more species of formula (I) R1—X—(C═O)—[NH—R2—NH—(C═O)—NH—R3—NH—(C═O)]n—NH—R2—NH—(C═O)—X—R1 (I), 5 wherein R1 is independently selected from organic groups having (4) to (200) carbon atoms, X is O or NR4, wherein R4 is a hydrogen atom or an aliphatic or aromatic group having (1) to (30) carbon atoms, R2 is independently selected from hydrocarbyl groups having (4) to (40) carbon atoms, R3 is independently selected from hydrocarbyl groups having (2) to (40) carbon atoms, and wherein on average (76) to (100) mol % of all R3 groups contained in the one or more species of formula (I) are hydrocarbyl groups having (2) or (3) carbon atoms, and n is an integer of (2) to (150). The invention further relates to a method of manufacturing such urea group containing products, liquid compositions containing the same and the use of such liquid compositions as rheology control additives. Furthermore, the invention relates to a process for rheology adjustment adding such liquid composition to semi-finished or final products. The invention also relates to an article coated with the liquid composition. | ||||||
| 167 | PSMA-binding agents and uses thereof | US15864236 | 2018-01-08 | US10500292B2 | 2019-12-10 | Martin G. Pomper; Ronnie Charles Mease; Ying Chen |
| Prostate-specific membrane antigen (PSMA) binding compounds having radioisotope substituents are described, as well as chemical precursors thereof. Compounds include pyridine containing compounds, compounds having phenylhydrazine structures, and acylated lysine compounds. The compounds allow ready incorporation of radionuclides for single photon emission computed tomography (SPECT) and positron emission tomography (PET) for imaging, for example, prostate cancer cells and angiogenesis. | ||||||
| 168 | PSMA-binding agents and uses thereof | US14987032 | 2016-01-04 | US09861713B2 | 2018-01-09 | Martin G. Pomper; Ronnie Charles Mease; Ying Chen |
| Prostate-specific membrane antigen (PSMA) binding compounds having radioisotope substituents are described, as well as chemical precursors thereof. Compounds include pyridine containing compounds, compounds having phenylhydrazine structures, and acylated lysine compounds. The compounds allow ready incorporation of radionuclides for single photon emission computed tomography (SPECT) and positron emission tomography (PET) for imaging, for example, prostate cancer cells and angiogenesis. | ||||||
| 169 | ALPHA HELIX MIMETIC COMPOSITIONS FOR TREATING CANCER AND OTHER CBP/CATENIN-MEDIATED DISEASES AND CONDITIONS | US14843951 | 2015-09-02 | US20150376204A1 | 2015-12-31 | Hiroyuki Kouji; Yuji Kogami; Takenao Odagami |
| Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed. | ||||||
| 170 | Alpha helix mimetic compositions for treating cancer and other CBP/catenin-mediated diseases and conditions | US14247105 | 2014-04-07 | US09126981B2 | 2015-09-08 | Hiroyuki Kouji; Yuji Kogami; Takenao Odagami |
| Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed. | ||||||
| 171 | PSMA-BINDING AGENTS AND USES THEREOF | US14211683 | 2014-03-14 | US20140369931A1 | 2014-12-18 | MARTIN G. POMPER; RONNIE CHARLES MEASE; YING CHEN |
| Prostate-specific membrane antigen (PSMA) binding compounds having radioisotope substituents are described, as well as chemical precursors thereof. Compounds include pyridine containing compounds, compounds having phenylhydrazine structures, and acylated lysine compounds. The compounds allow ready incorporation of radionuclides for single photon emission computed tomography (SPECT) and positron emission tomography (PET) for imaging, for example, prostate cancer cells and angiogenesis. | ||||||
| 172 | Cysteine protease inhibitors | US13704441 | 2011-06-16 | US08859505B2 | 2014-10-14 | Susana Ayesa; Urszula Grabowska; Ellen Hewitt; Daniel Jonsson; Bjorn Klasson; Pia Kahnberg; Stina Lundgren; Jan Tejbrant; Daniel Wiktelius |
| Compounds of the formula I wherein R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a C5-C10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; or R3 is a C2-C4alkyl chain with at least 2 chloro or 3 fluoro substituents; or R3 is C3-C7cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C1-C4alkyl, halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylamino, C1-C6dialkylamino or; R4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R4 is Het, carbocyclyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S. | ||||||
| 173 | N-((3-BENZYL)-2,2-(BIS-PHENYL)-PROPAN-1-AMINE DERIVATIVES AS CETP INHIBITORS FOR THE TREATMENT OF ATHEROSCLEROSIS AND CARDIOVASCULAR DISEASES | US13717871 | 2012-12-18 | US20130184279A1 | 2013-07-18 | Mark E. Salvati; James A. Johnson; Ningning Xu |
| Compounds of formula Ia and Ib wherein A, B, C, R1 and R14 are described herein. | ||||||
| 174 | Small molecule inhibitors of ghrelin O-acyltransferase | US13226471 | 2011-09-06 | US08329745B2 | 2012-12-11 | Patrcik G. Harran; Michael S. Brown; Joseph L. Goldstein; Jing Yang; Tong-Jin Zhao |
| Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules of the general formula: Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition. | ||||||
| 175 | N-Acylthiourea and N-Acylurea Inhibitors of the Hedgehog Protein Signalling Pathway | US12988975 | 2009-04-16 | US20110275663A1 | 2011-11-10 | Martial Ruat; Hélène Faure; Elisabeth Traiffort; Angèle Schoenfelder; André Mann; Maurizio Taddei; Antonio Solinas; Fabrizio Manetti |
| The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or acylurea derivatives as such, to their use as a medicinal product, and to pharmaceutical compositions containing them. | ||||||
| 176 | Small molecule inhibitors of ghrelin O-acyltransferase | US12571538 | 2009-10-01 | US08013015B2 | 2011-09-06 | Patrcik G. Harran; Michael S. Brown; Joseph L. Goldstein; Jing Yang; Tong-Jin Zhao |
| Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules. Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition. | ||||||
| 177 | Histone Deacetylase Inhibitors and Methods of Use Thereof | US12911145 | 2010-10-25 | US20110098504A1 | 2011-04-28 | Alan P. Kozikowski; Anatoly Dritschilo; Mira Jung; Pavel A. Petukhov; Bin Chen |
| The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention. | ||||||
| 178 | 4-Aminomethyl-1-aryl-cyclohexylamine compounds | US11125359 | 2005-05-10 | US20050245593A1 | 2005-11-03 | Bernd Sundermann; Hans Schick; Claudia Hinze |
| The invention concerns 4-aminomethyl-1-aryl-cyclohexylamine compounds, methods for producing same, pharmaceutical formulations containing said compounds and the use of 4-aminomethyyl-1-aryl-cyclohexylamine compounds for producing medicines and in related methods of treatment. | ||||||
| 179 | Fluorine-containing diols and use thereof | US79902901 | 2001-03-06 | US6384174B2 | 2002-05-07 | HANADA KAZUYUKI; KIMURA KAZUYA |
| Fluorine-containing diols represented by the following formula are provided:wherein Rf represents a perfluoroalkyl or perfluoroalkenyl group having 1 to 20 carbon atoms; X represents a substituted or unsubstituted alkylene group having 1 to 10 carbon atoms, a substituted or unsubstituted alkenylene group represented by -CH=CH-(CH2)n- in which n is from 1 to 10, orin which n is from 0 to 6; Y represents a direct bond, -O-, -NH-, or -R0-NH- in which R0 is an alkylene group having 1 to 6 carbon atoms; Z represents a direct bond or -N(R')R- in which R is an alkylene group having 1 to 20 carbon atoms and R' is a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R1 and R2 divalent organic groups; and R3 represents a residual group of diisocyanate. These diols are useful for polyurethanes. | ||||||
| 180 | Amino acid derivatives, medicaments containing said compounds and methods of producing them | US77629 | 1998-05-29 | US5962530A | 1999-10-05 | Wolfhard Engel; Wolfgang Eberlein; Klaus Rudolf; Henri Doods; Heike-Andrea Wieland; Klaus-Dieter Willim |
| The invention relates to new amino acid derivatives of general formula ##STR1## wherein R, U, V, Y, n, m and R.sup.1 to R.sup.3 are defined as in claim 1, their tautomers, diastereomers, enantiomers, mixtures thereof and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly selective NPY-antagonistic properties, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them. | ||||||
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