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公开(公告)号：US4407823A
公开(公告)日：1983-10-04
申请号：US91272
申请日：1979-11-05
IPC分类号： A61K31/19 , A61K31/215 , A61P29/00 , C07C1/22 , C07C45/46 , C07C49/792 , C07C49/813 , C07C51/00 , C07C51/08 , C07C51/09 , C07C51/15 , C07C51/347 , C07C51/36 , C07C51/367 , C07C51/377 , C07C51/38 , C07C51/41 , C07C57/46 , C07C57/62 , C07C59/76 , C07C59/86 , C07C61/29 , C07C61/40 , C07C62/36 , C07C62/38 , C07C67/00 , C07C69/753 , C07C201/00 , C07C205/56 , C07C205/61 , C07C229/42 , C07C233/11 , C07C235/78 , C07C237/20 , C07C253/00 , C07C255/33 , C07C259/06 , C07D257/04 , C07D263/10 , C07D263/12 , C07C65/20
CPC分类号： C07D263/10 , C07C1/22 , C07C45/46 , C07C49/792 , C07C49/813 , C07C51/08 , C07C51/36 , C07C51/367 , C07C51/377 , C07C51/38 , C07C51/412 , C07C57/46 , C07C57/62 , C07C59/86 , C07C61/40 , C07C62/36 , C07C62/38 , C07D263/12 , C07C2101/08 , C07C2101/14 , Y10S514/886
摘要： Phenylacetic acid derivatives of the formula ##STR1## wherein n is an integer of 2 to 5; ##STR2## R.sub.1 is hydrogen, halogen, trifluoromethyl, nitro or amino; R.sub.2 and R.sub.3 each independently is hydrogen or lower alkyl; or together form an ethylene group;X.sub.1 represents two hydrogen atoms or an oxo group; andY.sub.1 is cyano, hydroxyamidocarbonyl, carbamoyl, 5-tetrazolyl or carboxyl;and for derivatives wherein Y is carboxyl, salts thereof with physiologically compatible bases, esters thereof from physiologically acceptable alcohols and amides thereof from physiologically acceptable amines have valuable pharmacological activity, e.g., as antiinflammatory agents.
摘要翻译： 其中n为2〜5的整数的下式的苯乙酸衍生物： R1是氢，卤素，三氟甲基，硝基或氨基; R2和R3各自独立地为氢或低级烷基; 或一起形成亚乙基; X1表示2个氢原子或氧代基; Y1是氰基，羟基酰氨基羰基，氨基甲酰基，5-四唑基或羧基; 对于其中Y为羧基的衍生物，其与生理上相容的碱的盐，其生理学上可接受的醇的酯及其生理学上可接受的胺的酰胺具有有价值的药理活性，例如作为抗炎剂。
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公开(公告)号：US4356188A
公开(公告)日：1982-10-26
申请号：US173171
申请日：1980-07-28
IPC分类号： A61K31/165 , A61K31/185 , A61K31/19 , A61K31/215 , A61P1/04 , A61P25/04 , A61P29/00 , C07C51/00 , C07C57/40 , C07C57/50 , C07C59/76 , C07C59/84 , C07C59/86 , C07C67/00 , C07C69/616 , C07C69/734 , C07C233/11 , C07C235/78
CPC分类号： C07C59/86 , C07C57/40 , C07C59/84 , Y10S514/825 , Y10S514/916
摘要： This invention relates to 1-naphthyl-acetic acid derivatives having the general formula: ##STR1## in which: R.sub.1 is hydrogen atom or a straight- or branched-chain C.sub.1-6 alkyl group,R.sub.2 is a straight- or branched-chain alkyl group having 1-12 carbon atoms,R.sub.3 is a hydroxy group, a C.sub.1-6 straight- or branched-chain alkoxy group, and their pharmaceutically acceptable salts.Said compounds have anti-inflammatory, anti-pyretic and analgesic activities and are free from ulcerogenic activity under the administration conditions.
摘要翻译： 本发明涉及具有以下通式的1-萘基 - 乙酸衍生物：其中：R 1是氢原子或直链或支链C 1-6烷基，R 2是直链或支链的 具有1-12个碳原子的链烷基，R3是羟基，C1-6直链或支链烷氧基，以及它们的药学上可接受的盐。 所述化合物具有抗炎，抗热解和止痛活性，并且在给药条件下不含溃疡活性。
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公开(公告)号：US4057573A
公开(公告)日：1977-11-08
申请号：US548956
申请日：1975-02-11
申请人： Georges Haas , Alberto Rossi
发明人： Georges Haas , Alberto Rossi
IPC分类号： C07D295/18 , A61K31/165 , A61K31/19 , A61K31/215 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61P25/04 , A61P29/00 , C07C51/00 , C07C59/54 , C07C59/76 , C07C59/90 , C07C61/28 , C07C62/38 , C07C67/00 , C07C69/017 , C07C69/738 , C07C69/757 , C07C231/00 , C07C231/02 , C07C231/06 , C07C231/12 , C07C233/34 , C07C235/40 , C07C235/78 , C07C235/82 , C07D307/54 , C07D333/24 , C07C69/76
CPC分类号： C07C59/54
摘要： Compounds of the general formula I ##STR1## wherein one of the two radicals R.sub.1 and R.sub.2 denotes the acyl radical of a carboxylic acid of aromatic character and the other denotes hydrogen or optionally esterified or etherified hydroxyl, R.sub.3 denotes hydrogen, alkyl or hydroxyalkyl, R.sub.4 denotes optionally esterified or amidised carboxyl, m denotes 1 or 2 and n denotes 0 or 1, in the free form or in the form of their salts are useful as antiphlogistics, mild analgesics, antipyretics and as anti-rheumatic agents.
摘要翻译： 通式I（I）的化合物，其中两个基团R 1和R 2中的一个表示芳族特征的羧酸的酰基，另一个表示氢或任选酯化或醚化的羟基，R 3表示氢，烷基或 羟烷基，R 4表示任选酯化或酰胺化的羧基，m表示1或2，n表示0或1，以游离形式或其盐的形式可用作消炎剂，温和止痛剂，解热剂和抗风湿剂。
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公开(公告)号：US20240360068A1
公开(公告)日：2024-10-31
申请号：US18770018
申请日：2024-07-11
申请人： Francis Johnson , Lorne Golub
发明人： Francis Johnson , Lorne Golub
IPC分类号： C07C69/738 , C07C49/255 , C07C225/22 , C07C235/78 , C07C235/80 , C07C237/20 , C07D213/50 , C12N9/64
CPC分类号： C07C69/738 , C07C49/255 , C07C225/22 , C07C235/78 , C07C235/80 , C07C237/20 , C07D213/50 , C12N9/6491 , C12Y304/24
摘要： This invention provides a compound having the structure
wherein α, β, X, Y, and R1-R11 are defined herein. This invention also provides a pharmaceutical composition comprising the above compounds, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NFκ-B activation in a population of cells.-
65.发明公开公开(公告)号：US20240317832A1
公开(公告)日：2024-09-26
申请号：US18578487
申请日：2021-07-29
发明人： Jinwei YANG , Chenghao YE , Gang XIA , Pengchao HUO , Wen DING , Longfei CHEN , Lin JIAO , Hao HUANG , Xin HENG , Jingjing ZHU , Yuebin YING , Xuejun LIANG
IPC分类号： C07K14/61 , A61K38/00 , A61K47/60 , C07C235/20 , C07C235/78 , C07C237/12 , C07C271/22 , C07C271/54 , C07K1/00
CPC分类号： C07K14/61 , A61K47/60 , C07C235/20 , C07C235/78 , C07C237/12 , C07C271/22 , C07C271/54 , C07K1/006 , A61K38/00
摘要： An unnatural amino acid may have a structure as shown in formula (1) or may be an enantiomer thereof:
Such unnatural amino acid may be used, e.g., in recombinant proteins. A recombinant protein may contain such unnatural amino acid and a protein conjugate prepared from the recombinant protein. The unnatural amino acid can be simple and convenient to prepare, safe in nature, difficult to inactivate when inserted into a protein, and may have a high binding rate with a coupling moiety, and the obtained conjugate is higher in stability. The unnatural amino acid is applicable to numerous fields, especially in preparation of a recombinant protein or a recombinant protein conjugate.-
公开(公告)号：US11958808B2
公开(公告)日：2024-04-16
申请号：US17419448
申请日：2019-12-26
发明人： Jing Zhang
IPC分类号： C07D211/16 , C07C235/78 , C07D203/18
CPC分类号： C07D211/16 , C07C235/78 , C07D203/18 , C07B2200/13
摘要： An acetylsalicylic acid derivative and an application thereof. The present disclosure relates to the field of chemical pharmaceuticals, and in particular, to a compound shown in formula (I) or pharmaceutically acceptable salts thereof.
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公开(公告)号：US20240018110A1
公开(公告)日：2024-01-18
申请号：US18267987
申请日：2021-12-16
申请人： THE UNIVERSITY OF BRITISH COLUMBIA , PROVINCIAL HEALTH SERVICES AUTHORITY , ALPHA-9 THERANOSTICS INC.
发明人： François BÉNARD , Kuo-Shyan LIN , Chengcheng ZHANG , David PERRIN , Aron ROXIN , Zhengxing ZHANG , Antoine DOUCHEZ , Pargol DANESHMANDKASHANI , Samson LAI
IPC分类号： C07D257/02 , C07C235/78 , A61K51/04
CPC分类号： C07D257/02 , C07C235/78 , A61K51/0482 , A61K2123/00 , C07B2200/07 , A61K2121/00 , C07B2200/05
摘要： The present invention relates to radiolabelled compounds for in vivo imaging or treatment of diseases or conditions characterized by expression of prostate-specific membrane antigen.
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公开(公告)号：US11453640B2
公开(公告)日：2022-09-27
申请号：US16981654
申请日：2019-03-21
发明人： Ali Shilatifard , Kaiwei Liang , Edwin R. Smith , Gary E. Schiltz , Rama K. Mishra , Kristen Stoltz
IPC分类号： C07C235/74 , A61P35/00 , C07C235/78 , C07D213/40 , C07D213/75 , C07D231/14 , C07D239/36 , C07D239/42 , C07D241/20 , C07D257/06 , C07D261/18 , C07D271/07 , C07D277/46
摘要： Disclosed are compounds which may be utilized to inhibit transcription by RNA Polymerase II (Pol II), and in particular to disrupt the Super Elongation Complex (SEC). The compounds may be utilized in pharmaceutical compositions and methods for treating diseases and disorders associated with the biological activity of SEC, and in particular, diseases and disorders that are associated with high levels of expression of genes whose expression is SEC-dependent and that promote, support, or otherwise are required for the disease or disorder such as cancers.
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公开(公告)号：US11304914B2
公开(公告)日：2022-04-19
申请号：US16919044
申请日：2020-07-01
IPC分类号： C07C235/78 , C07C215/28 , C07C215/30 , C07C231/12 , C07C215/08 , A61K31/122 , C07B57/00 , A61K31/164
摘要： Disclosed herein are polymorphic and amorphous forms of anhydrate, hydrate, and solvates of (R)-2-hydroxy-2-methyl-4-(2,4,5-trimethyl-3,6-dioxocyclohexa-1,4-dienyl)butanamide and methods of using such compositions for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging. Further disclosed are methods of making such polymorphic and amorphous forms.
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公开(公告)号：US20210179542A1
公开(公告)日：2021-06-17
申请号：US17249171
申请日：2021-02-22
IPC分类号： C07C235/80 , A61P21/00 , A61P25/00 , A61P25/16 , A61P27/00 , C07C235/32 , C07C235/78 , C07C317/28 , C07D207/27 , C07D211/46 , C07D213/40 , C07D233/61 , C07D295/13 , C07D295/192 , C07D265/30 , C07D311/66 , C07D207/26 , C07D213/50 , C07D295/116 , C07D295/185
摘要： Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.
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