| 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 | THE PREPARATION AND USE OF ORTHO-SULFONAMIDO BICYCLIC HETEROARYL HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASE AND TACE INHIBITORS | PCT/US1998/007380 | 1998-04-14 | WO99018076A1 | 1999-04-15 | |
| This invention provides, low molecular weight, non-peptide inhibitors of matrix metalloproteinases and TNF- alpha converting enzyme (TACE, tumor necrosis factor- alpha converting enzyme) of formula (B) wherein (B) is (1), (2), or (3); P and Q are (4) or (5), provided that when P is (4), Q is (5), and vice versa; T, U, W, and X are each, independently, carbon or nitrogen, provided that when T or U is carbon, either may be optionally substituted with R<1>; Y is carbon, nitrogen, oxygen or sulfur, provided that at least one of T, U, W, X, and Y is not carbon, and further provided that no more than 2 of T, U, W, and X are nitrogen; (6) is a phenyl ring or is a heteroaryl ring of ring 5-6 atoms which may contain 0-2 heteroatoms selected from nitrogen, oxygen, and sulfur, in addition to any heteroatoms defined by W or X; wherein the phenyl or heteroaryl ring may be optionally mono-, di-, or tri- substituted with R<1>; Z is a phenyl, naphthyl, heteroaryl, or heteroaryl fused to phenyl, wherein the heteroaryl moiety contains of 5-6 ring atoms and 1-3 heteroatoms selected from nitrogen, oxygen, or sulfur; wherein the phenyl, naphthyl, heteroaryl, or phenyl fused heteroaryl moieties may be optionally mono-, di-, or tri-substituted with R<1>; R<1> is hydrogen, halogen, alkyl of 1-8 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, cyclocalkyl of 3-6 carbon atoms, -(CH2)nZ, -OR<2>, -CN, -COR<2>, perfluoroalkyl of 1-4 carbon atoms, -CONR<2>R<3>, -S(O)xR<2>-OPO(OR<2>)OR<3>, -PO(OR<2>)R<3>, -OC(O)NR<2>R3, -COOR<2>, -CONR<2>R<3>, -SO3H, -NR<2>R<3>, -NR<2>COR<3>, -NR<2>COOR<3>, -SO2NR<2>R<3>, -NR<2>CONR<2>R<3>, -NR<2>C(=NR<3>)NR<2>R<3>, -SO2NHCOR<4>, -CONHSO2R<4>, -tetrazol-5-yl, -SO2NHCN, -SO2NHCONR<2>R<3>, or Z; V is a saturated or partially unsaturated heterocycloalkyl ring of 5-7 ring atoms having 1-3 heteroatoms selected from N, O, or S, which may be optionally mono-, or di-substituted with R<2>; R<2> and R<3> are each, independently, hydrogen, alkyl of 1-8 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, cycloalkyl of 3-6 carbon atoms; perfluoroalkyl of 1-4 carbon atoms, Z or V; R<4> is alkyl of 1-8 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, cycloalkyl of 3-6 carbon atoms; perfluoroalkyl of 1-4 carbon atoms, Z or V; R<5> is hydrogen, alkyl of 1-8 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, Z, or V; n = 1-6; x = 0-2 or a pharmaceutically acceptable salt thereof. | ||||||
| 182 | FUSED 1,2,4-THIADIAZINE DERIVATIVES, THEIR PREPARATION AND USE | PCT/DK1998/000288 | 1998-06-30 | WO99003861A1 | 1999-01-28 | |
| 1,2,4-Thiadiazine and 1,4-thiazine derivates represented by formula (I) wherein A, B, D, R<1>, R<2>, R<3> and R<4> are defined in the description, compositions thereof and methods for preparing the compounds are described. The compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. | ||||||
| 183 | NOVEL COMPOUNDS | PCT/SE1998/000935 | 1998-05-18 | WO98054190A1 | 1998-12-03 | |
| A compound of formula (I), wherein R, R<1>, R<2> and R<3> have the meanings given in the description. Compound (I) is useful in the (prophylactic) treatment of autoimmune, inflammatory, proliferative and hyperproliferative diseases and immunologically-mediated diseases including rejection of transplanted organs or tissues and Acquired Immunodeficiency Syndrome (AIDS). | ||||||
| 184 | INHIBITORS OF PROTEIN ISOPRENYL TRANSFERASES | PCT/US1998/009298 | 1998-05-07 | WO98050031A1 | 1998-11-12 | |
| Compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2-, and (i) heterocyclic -L2-; R2 is selected from (a) Formula (Ia), (b) -C(O)NH-CH(R14)-C(O)OR15, (c) Formula (Ib), (d) -C(O)NH-CH(R14)-C(O)NHSO2R16, (e) -C(O)NH-CH(R14)-tetrazolyl, (f) -C(O)NH-heterocyclic, and (g) -C(O)NH-CH(R14)-C(O)NR17R18; R3 is heterocyclic, aryl, substituted or unsubstituted cycloalkyl; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylalkyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) -L4-N(R5)-L5-, (b) -L4-O-L5-, (c) -L4-S(O)n-L5-, (d) -L4-L6-C(W)-N(R5)-L5-, (e) -L4-L6-S(O)m-N(R5)-L5-, (f) -L4-N(R5)-C(W)-L7-L5-, (g) -L4-N(R5)-S(O)p-L7-L5-, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, and (j) optionally substituted alkynylene are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases. | ||||||
| 185 | METHODS FOR TREATING FIBROSIS USING PKM2 ACTIVATORS | PCT/US2021/022009 | 2021-03-11 | WO2021183830A1 | 2021-09-16 | LIU, Zhi-Ren; SATYANARAYANA, Ganesh |
A method of treating a patient suffering from disease that is caused by organ/tissue fibrosis includes the administration of a PKM2 activator. The PKM2 activator can reduce LOX protein expression and activate PKM2. |
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| 186 | SUBSTITUTED PYRIMIDINEDIONE COMPOUNDS AND USES THEREOF | PCT/CN2020/105014 | 2020-07-28 | WO2021018105A1 | 2021-02-04 | JIN, Chuanfei; ZHONG, Wenhe |
Provided are substituted pyrimidinedione compounds and uses thereof, as well as pharmaceutical compositions containing such compounds, which can be used as gonadotropin releasing hormone receptor antagonists. Provided are a method for preparing such compounds and pharmaceutical compositions and their uses in the prevention or treatment of sex hormone dependent diseases including but not limited to prostate cancer, endometriosis, hysteromyoma, precocious puberty and other diseases. |
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| 187 | ACILHIDRAZONAS PARA EL TRATAMIENTO DE ENFERMEDADES NEUROLÓGICAS | PCT/ES2019/070649 | 2019-09-27 | WO2020065119A1 | 2020-04-02 | PÉREZ FERNÁNDEZ, Ruth; CANAL MARTÍN, Andrea; SANCHEZ BARRENA, María José; MANSILLA APARICIO, Alicia |
La presente invención se refiere a un grupo de compuestos con un núcleo estructural de acilhidrazona que presentan capacidad moduladora de la interacción entre las proteínas NCS-1 y Ric8a, implicadas en el proceso de regulación del número de sinapsis y la probabilidad de liberación de neurotransmisores.Estos compuestos, por tanto, son útiles para el tratamiento de enfermedades neurológicas en las que está afectado el número de sinapsis, tales como enfermedad de Alzheimer, enfermedad de Huntington o enfermedad de Parkinson. |
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| 188 | MATERIALIEN FÜR ORGANISCHE ELEKTROLUMINESZENZVORRICHTUNGEN | PCT/EP2015/001456 | 2015-07-15 | WO2016023608A1 | 2016-02-18 | PARHAM, Amir Hossain; EBERLE, Thomas; JATSCH, Anja; GROSSMANN, Tobias; KROEBER, Jonas Valentin; ANEMIAN, Rémi Manouk |
Die vorliegende Erfindung betrifft elektronenarme Heteroaromaten, welche mit Dibenzofuran- bzw. Dibenzothiophenderivaten und mit Carbazolen bzw. Aminen substituiert sind, insbesondere für die Verwendung als Triplettmatrixmaterialien in organischen Elektrolumineszenzvorrichtungen. Die Erfindung betrifft ferner ein Verfahren zur Herstellung der erfindungsgemäßen Verbindungen sowie elektronische Vorrichtungen enthaltend diese Verbindungen. |
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| 189 | METHODS AND COMPOSITIONS FOR INHIBITING HUMAN COPPER TRAFFICKING PROTEINS ATOX1 AND CCS | PCT/US2014/012793 | 2014-01-23 | WO2014116859A1 | 2014-07-31 | HE, Chuan |
Compositions and methods concern organic molecules that bind to human Atox1 and CCS at the copper trafficking interface of these proteins. This binding suppresses copper trafficking, which leads to inhibition of cancer cell proliferation and tumor growth. In addition to serving as an effective treatment of cancer, these organic molecules inhibit cellular copper uptake and can be used as treatment of disorders of copper metabolism such as Wilson's disease, which is characterized by copper overload, as well as wound healing. |
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| 190 | 醌型噻吩有机光电材料、其制备方法和应用 | PCT/CN2010/070436 | 2010-01-30 | WO2011091608A1 | 2011-08-04 | 周明杰; 黄杰; 刘辉 |
| 191 | 一种d-生物素的制备方法 | PCT/CN2010/072977 | 2010-05-20 | WO2010133169A1 | 2010-11-25 | 潘亚金; 皮士卿; 丁文珍; 顾立新; 魏昂锋; 何益民 |
| 192 | HYDROXYQUINOLIN-2(1H)-ONES AND DERIVATIVES THEREOF | PCT/IB2009/054925 | 2009-11-05 | WO2010058314A1 | 2010-05-27 | DUPLANTIER, Allen Jacob; GAN, Xinmin; HU, Lain-Yen; LU, Jiemin; SHEEHAN, Susan Mary Kult |
This invention relates to known and novel hydroxyquinolin-2(1H)-ones and derivatives thereof which are useful for the treatment of cognitive-related disorders and neuropathic pain disorders in a mammal, e.g., a human. The invention also relates to pharmaceutical compositions containing such compounds. |
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| 193 | PRODRUG DERIVATIVES OF ACIDS USING ALCOHOLS WITH HOMOTOPIC HYDROXY GROUPS AND METHODS FOR THEIR PREPARATION AND USE | PCT/US2007066782 | 2007-04-17 | WO2007127639A3 | 2008-06-12 | DELONG MITCHELL A; MCFADDEN JILL M; ROYALTY SUSAN M; TOONE ERIC J; YINGLING JEFFREY D |
| This invention relates to novel homotopic prodrugs and medicaments and methods for their preparation, testing and use. In one embodiment, the homotopic prodrug has the general formula (I) wherein (II) is a biologically-active moiety comprising a carboxylic acid functional group, and Rb is a homotopically-symmetrical alcohol bonded to the biologically-active moiety through the carboxylic acid functional group to form an ester linkage, as well as optical isomers, enantiomers, pharmaceutically acceptable salts, biohydrolyzable amides, esters, and imides thereof and combinations thereof. | ||||||
| 194 | 1-OXO-3-(1H-INDOLE)-3-IL-1,2,3,4-TETRAHYDROISOXYNOLINES, METHODS FOR THE PRODUCTION THEREOF, COMBINATORIC LIBRARY AND FOCUSED LIBRARY | PCT/RU2007000116 | 2007-03-12 | WO2007105989A3 | 2007-11-22 | IVASHCHENKO ALEXANDER VASILIEV; KRAVCHENKO DMITRI VLADIMIROVIC; LOSEVA MARINA VASILIEVNA; OKUN ILYA MATUSOVICH; TKACHENKO SERGEY YEVGENIEVICH; KHVAT ALEXANDER VIKTOROVICH |
| The invention relates to novel 1-oxo-3-(1h-indole)-3-il-1,2,3,4-tetrahydroisoxynolines and to the cis- and trans-isomers thereof exhibiting protein kinase inhibiting properties, to methods for the production thereof and to combinatoric and focused libraries for separating leader compounds. 1-oxo-3-(1h-indole)-3-il-1,2,3,4-tetrahydroisoxynolines correspond to general formulas 1 and 2, wherein R1, R2 and R4, independently from each other are, a cyclic system substituent selected from hydrogen and alkyl, R3 is an aminogroup substituent selected from alkyl, cycloalkyl or alkyl, possibly substituted with an aryl, heteroaryl, heterocyclyl, alkoxy, amine, alkylamine and dialkylamine group, R5 and R6 are, independently from each other, an amino group substituent selected from hydrogen, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl or alkyl, possibly substituted with aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, amino, alkylamine, dialkylamine, aryl alkylamine, or R5 and R6 forms, together with a nitrogen atom with which they are bound, a possibly substituted azaheterocycle. A method for obtaining compounds of general formula 1 consists in interacting corresponding indole-3-ilmethylenamines and homophtalic anhydrides in an organic solvent medium. A method for obtaining compounds of general formula 2 consists in treating the compounds of formula 1 with thionyl chloride or with 1,1'-carbonyldiimidazole in such a way that the respective derivatives are obtain and interact with respective amines of general formula 6 in the organic solvent medium. | ||||||
| 195 | 1-ОКСО-3-(1Н-ИНДОЛ-3-ИЛ)-1,2,3,4-ТЕТРАГИДРОИЗОХИНОЛИНЫ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ, КОМБИНАТОРНАЯ БИБЛИОТЕКА И ФОКУСИРОВАННАЯ БИБЛИОТЕКА | PCT/RU2007/000116 | 2007-03-12 | WO2007105989A2 | 2007-09-20 | ИВАЩЕНКО Александр Васильевич; КРАВЧЕНКО Дмитрий Владимирович; ЛОСЕВА Марина Васильевна; ОКУНЬ Илья Матусович; ТКАЧЕНКО Сергей Евгеньевич; ХВАТ Александр Викторович |
Изобретение относится к новым 1-оксо-3-(1Н-индол-3-ил)-1,2,3,4-тетрагидроизохинолинам и их цис-и транс-изомерам, обладающим свойствами ингибиторов протеинкиназы, способам их получения, а также комбинаторной и фокусированной библиотекам для выделения соединений лидеров. 1-Оксо-3-(1Н-индол-3-ил)-1,2,3,4-тетрагидроизохинолины соответствуют общим формулам 1 и 2 : где: R1, R2 и R4 независимо друг от друга представляют собой заместитель циклической системы, выбранный из водорода, алкила; R3 представляет собой заместитель аминогруппы, выбранный из алкила, циклоалкила или алкила, возможно замещенного арилом, гетероарилом, гетероциклилом, алкокси, амино, алкиламино, диалкиламино группой, R5 и R6 независимо друг от друга представляют собой заместитель аминогруппы, выбранный из водорода, арила, гетероарила, гетероциклила, циклоалкила, циклоалкенилом, алкокси, амино, алкиламино, диалкиламино, арилалкиламино, или R5 и R6 вместе с атомом азота, с которым они связаны, образуют возможно замещенный азагетероцикл. Способ получения соединений общей формулы 1 заключается во взаимодействии соответствующих индол-3-илметиленаминов и гомофталевых ангидридов в среде органического растворителя. Способ получения соединений общей формулы 2 заключается в обработке соединений 1 тионилхлоридом или 1,1' –карбонилдиимидазолом, с получением соответствующих производных, и взаимодействии последних с соответствующими аминами общей формулы 6 в среде органического растворителя. |
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| 196 | 可抑制细胞释放肿瘤坏死因子的5H-噻吩[3, 4-c]吡咯-4, 6-二酮衍生物 | PCT/CN2006/002413 | 2006-09-15 | WO2007036138A1 | 2007-04-05 | 张和胜 |
| The invention relates to 5H-thieno[3,4-c]pyrrole-4,6-dione derivatives represented by formula (`), its various pharmaceutically acceptable salts, its preparation and its use as active ingredient in the medicament which can inhibit release of tumor necrosis factor (TNF) in organism: (`) in which R1 represents H, C1-6 alkyl, OR4, OC(O)R5, NO2, NHC(O)R6, NR7R8; R2 represents H, halogen, C1-6 alkyl; R3 represents H, methyl, isopropyl, allyl, benzyl, CH2CO2(C1-6 alkyl), CH2(CH2)nR9; in which R4, R5, R6, R7 and R8 represent H, C1-6 alkyl; R9 represents H, C1-6 alkyl, OH, OC1-6 alkyl, NH2, NHC1-6 alkyl, N(C1-6 alkyl)2, CO2(C1-6 alkyl); n is 1, 2, 3, 4. | ||||||
| 197 | NOVEL INHIBITORS OF CHYMASE | PCT/US2005/001659 | 2005-01-18 | WO2005073214A2 | 2005-08-11 | HAWKINS, Michael, J.; GRECO, Michael, N.; POWELL, Eugene; DE GARAVILLA, Lawrence; MARYANOFF, Bruce, E. |
The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders. |
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| 198 | SUBSTITUIERTE THIOPHENE | PCT/EP2004/014335 | 2004-12-16 | WO2005063734A2 | 2005-07-14 | THEDE, Kai; WUNBERG, Tobias; LOWINGER, Timothy; KOLETZKI, Diana; URBAN, Andreas; BAUMEISTER, Judith; HENNINGER, Kerstin |
Die Erfindung betrifft substituierte Thiophene und Verfahren zu ihrer Herstellung, ihre Verwendung zur Behandlung und/oder Prophylaxe von Krankheiten sowie ihre Verwendung zur Herstellung von Arzneimitteln zur Behandlung und/oder Prophylaxe von Krankheiten, insbesondere zur Verwendung als antivirale Mittel, insbesondere gegen Hepatitis C Viren. |
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| 199 | PROCESS FOR THE ASYMMETRIC HYDROGENATION OF BETA-AMINO KETONES | PCT/EP2004/009690 | 2004-08-31 | WO2005021527A2 | 2005-03-10 | METTLER, Hans-Peter |
The invention relates to a process for the preparation of enantiomerically enriched or enantiomerically pure (S)- or (R-N-monosubstituted ß-amino alcohols of formula (I) and their addition salts of proton acids, X represents S or O, and R represent C1-6-alkyl, C3-8-cycloalkyl, aryl or aralkyl. |
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| 200 | MODULATION OF PEROXISOME PROLIFERATOR ACTIVATED RECEPTORS ACTIVITY | PCT/EP0311710 | 2003-10-22 | WO2004037248A3 | 2004-06-03 | HUCK JACQUES; SALADIN REGIS; SIERRA MICHAEL; KLOTZ EVELYNE |
| The present invention relates to compounds, compositions and methods useful for modulating nuclear receptors activity in cells, and for treating and/or preventing various diseases and conditions mediated by said nuclear receptors, including metabolic or cell proliferative disorders. According to particular aspects, the present invention relates to compounds, compositions and methods useful for modulating activities of the Peroxisome Proliferator Activated Receptors (PPARs) and for treating and/or preventing various diseases and conditions mediated by said nuclear receptors. More specifically, it relates to Peroxisome Proliferator Activated Receptor-gamma (PPAR-gamma) ligands, which are useful in the modulation of blood glucose levels and in the increase of insulin sensitivity in patients in need thereof. The properties of the compounds and compositions of the invention make these PPAR ligands particularly useful in the treatment of those diseases and conditions including diabetes, atherosclerosis, hyperglycemia, dyslipidemia, obesity, syndrome X, insulin resistance, hypertension, neuropathy, microvascular diseases (e.g. retinopathy, nephropathy), macrovascular diseases (e.g. myocardial infarction, stroke, heart failure) in mammals. | ||||||
