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101. 发明授权

US4044129A 4-Pyridine carbonyl phenyl 1,2,4 triazoles 失效
标题翻译： 4-吡啶羰基苯基1,2,4-三唑
公开(公告)号：US4044129A
公开(公告)日：1977-08-23
申请号：US592889
申请日：1975-07-03
申请人： Yutaka Kuwada , Kanji Meguro , Hideaki Natsugari , Yoshiaki Sato , Hiroyuki Tawada
发明人： Yutaka Kuwada , Kanji Meguro , Hideaki Natsugari , Yoshiaki Sato , Hiroyuki Tawada
IPC分类号： C07D401/04 , A61K31/44 , A61K31/4427 , A61K31/535 , A61P21/02 , A61P25/00 , A61P25/08 , A61P25/20 , C07D213/50 , C07D249/08 , C07D401/10 , C07D413/14
CPC分类号： C07D249/08 , C07D213/50
摘要： A novel triazole derivative of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different, represent alkyl group or aralkyl group and one of R.sup.1 and R.sup.2 may be hydrogen atom, or R.sup.1 and R.sup.2 form a heterocyclic ring together with the nitrogen atom adjacent thereto; R.sup.3 represents hydrogen atom or a hydrocarbon residue; R.sup.4 represents hydrogen atom or a lower alkyl group; Py represents a pyridyl group; and the ring A is either unsubstituted or substituted by halogen atom, nitro, alkyl, alkoxy or trifluoromethyl group, and pharmaceutically acceptable acid addition salts thereof are found to be useful as medicine in human and animal therapy, as these compounds act on the central nervous as for example, muscle relaxants, anticonvulsants, sedatives, minor tranquilizers, etc.
摘要翻译：通式（I）的新的三唑衍生物：（I）其中R 1和R 2可以相同或不同，表示烷基或芳烷基，R 1和R 2之一可以是氢原子或R 1 R2与邻近的氮原子一起形成杂环; R3表示氢原子或烃残基; R4代表氢原子或低级烷基; Py代表吡啶基; 发现环A是未取代的或被卤素原子取代的硝基，烷基，烷氧基或三氟甲基，其药学上可接受的酸加成盐可用作人和动物治疗中的药物，因为这些化合物作用于中枢神经例如，肌肉松弛剂，抗惊厥药，镇静剂，小镇静剂等

102. 发明授权

US3846443A 1H-IMIDAZO{8 1,2a{9 {8 1,4{9 BENZO-DIAZEPINE-1,2(3H)-DIONES 失效
标题翻译： 1H-1MIDAZO {8,12a {9 {8 1,4 {9苯并二氮杂-1,2（3H） - 酮
公开(公告)号：US3846443A
公开(公告)日：1974-11-05
申请号：US36461673
申请日：1973-05-29
申请人： UPJOHN CO
发明人： MOFFETT R
IPC分类号： A23K1/16 , A61K31/55 , A61P21/02 , A61P25/08 , A61P25/20 , C07D487/04 , C07D57/02
CPC分类号： C07D487/04
摘要： This invention relates to 1H-imidazo(1,2-a)(1,4)-benzodiazepine1,2(3H)-diones of the formula WHEREIN R is selected from the group consisting of hydrogen, lower alkyl of 1 through 4 carbon atoms and lower alkenyl of 3 through 4 carbon atoms; R1 is selected from the group consisting of hydrogen and lower alkyl of 1 through 3 carbon atoms; R2 is selected from the group consisting of 2-pyridyl, 3-pyridyl, 4pyridyl, 2-pyrimidyl, furyl, pyrryl, thienyl, lower alkyl of 1 through 3 carbon atoms, lower alkenyl of 2 through 4 carbon atoms, cycloalkyl of 5 through 7 carbon atoms, cycloalkenyl of 5 through 7 carbon atoms and WHEREIN R5 and R6 are selected from the group consisting of hydrogen, lower alkyl of 1 through 3 carbon atoms, halogen, nitro, cyano, trifluoromethyl, lower alkoxy of 1 through 3 carbon atoms, lower alkylthio of 1 through 3 carbon atoms, lower alkylsulfinyl of 1 through 3 carbon atoms, lower alkylsulfonyl of 1 through 3 carbon atoms, lower alkanoylamino having lower alkyl moieties of 1 through 3 carbon atoms and lower dialkylamino having lower alkyl moieties of 1 through 3 carbon atoms; R3 and R4 have the same meaning as R5 and R6, above; and a pharmacologically acceptable acid addition salt thereof. The new products of Formula 1 are useful as sedatives, hypnotics, tranquilizers, muscle relaxants and anti-convulsants in mammals and birds.
摘要翻译：本发明涉及式WHEREIN R的1H-咪唑并[1,2-a] [1,4]苯并二氮杂-1,2（3H） - 二酮，其选自氢，1至4的低级烷基碳原子和3至4个碳原子的低级烯基; R1选自氢和1至3个碳原子的低级烷基; R2选自2-吡啶基，3-吡啶基，4-吡啶基，2-嘧啶基，呋喃基，吡啶基，噻吩基，1至3个碳原子的低级烷基，2至4个碳原子的低级链烯基， 5至7个碳原子，5至7个碳原子的环烯基和WHEREIN R5和R6选自氢，1至3个碳原子的低级烷基，卤素，硝基，氰基，三氟甲基，1至3的低级烷氧基碳原子数1〜3个碳原子的低级烷硫基，1〜3个碳原子的低级烷基亚磺酰基，1〜3个碳原子的低级烷基磺酰基，1〜3个碳原子的低级烷基部分的低级烷酰基氨基， 1至3个碳原子; R3和R4具有与上述R5和R6相同的含义; 及其药理学上可接受的酸加成盐。式1的新产品可用作哺乳动物和鸟类中的镇静剂，催眠药，镇定剂，肌肉松弛剂和抗惊厥药。

103. 发明申请

US20220072014A1 PHARMACEUTICAL COMPOSITION WHICH COMPRISES THE COMBINATION OF A SELECTIVE INHIBITOR OF CYCLOOXYGENASE 2 AND A CARBAMATE DERIVED FROM GUAIFENESIN FOR TREATING PAIN, INFLAMMATION AND MUSCULAR CONTRACTION 有权
公开(公告)号：US20220072014A1
公开(公告)日：2022-03-10
申请号：US17291169
申请日：2019-11-01
申请人： Federico Amezcua Amezcua , Carlos Amezcua Amezcua
发明人： Patricia del Carmen Garcia Armenta , Jose Alonso Chavez Garcia
IPC分类号： A61K31/635 , A61K31/27 , A61K31/415 , A61P21/02
摘要： The present invention refers to a pharmaceutical combination comprising the synergic combination of a selective cyclooxygenase-2 inhibitor, such as the active principle celecoxib and pharmaceutically acceptable salts thereof, and a guaifenesin-derived carbamate such as the active principle methocarbamol and pharmaceutically acceptable salts thereof, formulated with pharmaceutically acceptable excipients and/or carriers and/or additives, in a single dosing unit to be administered orally, dermally or transdermally or topically, indicated for the treatment of pain, inflammation and muscular contractions; said combination triggers a triple effect: analgesic, anti-inflammatory and muscle relaxant, being better tolerated and with less adverse effects in patients with pain, inflammation and muscular contractions.

104. 发明授权

US11161828B2 Class of bisquaternary ammonium compound as well as the preparative method and the use thereof 有权
公开(公告)号：US11161828B2
公开(公告)日：2021-11-02
申请号：US17044158
申请日：2019-07-24
申请人： WEST CHINA HOSPITAL, SICHUAN UNIVERSITY
发明人： Jun Yang , Jin Liu , Weiyi Zhang , Wensheng Zhang , Cheng Zhou , Bowen Ke , Lei Tang
IPC分类号： C07D295/15 , A61P21/02
摘要： A two-quaternary ammonium compound has a structural formula of formula (I). L1 is a C1 to C8 alkylene group; L2 is a C1 to C8 alkylene group; Z1 is nitro group or a halogen or methoxy group; Z2 is nitro group or a halogen or methoxy group; Z3 is nitro group or a halogen or methoxy group; R═H or a C1 to C6 alkyl group; a, b, and c are independently an integer from 0-5; and M is a pharmaceutically acceptable anion, such as a bromine ion, chlorine ion, sulfonate radical, etc. A stereoisomer or mixture of stereoisomers, or a pharmaceutically acceptable salt or solvate or eutectic of the compound of formula (I) forms a composition with a pharmaceutically acceptable carrier, or forms a compounded prescription with other active components, and the composition or compounded prescription may be used in the preparation of a muscle relaxant.

105. 发明授权

US11129900B2 Cytophilic peptide-fused high-density lipoprotein, and delivery of drug to posterior segment of eye by ocular installation of said fusion 有权
公开(公告)号：US11129900B2
公开(公告)日：2021-09-28
申请号：US15539276
申请日：2015-12-25
申请人： KYOTO UNIVERSITY , NOSTA AG
发明人： Kenji Suda , Tatsuya Murakami , Nagahisa Yoshimura , Norimoto Gotoh
IPC分类号： A61K47/64 , A61K47/69 , C07K14/775 , A61P21/02 , A61K45/00 , A61K47/42 , C07K19/00 , C07K7/06 , C07K7/08 , A61P9/10 , A61P27/02 , A61P27/06 , A61P27/12 , A61P27/10 , A61K9/00 , A61K47/24 , A61K31/506
摘要： The purpose of the present invention is to provide a novel system for the delivery of a drug to a posterior segment of the eye. The present invention relates to: a cytophilic peptide-fused high-density lipoprotein (cHDL) which can be used as a carrier for the delivery of a drug to a posterior segment of the eye; a method for producing the cytophilic peptide-fused high-density lipoprotein; a system of the delivery of a drug to a posterior segment of the eye, a pharmaceutical composition, and a system of the delivery of a drug to a posterior segment of the eye, each of which utilizes the cytophilic peptide-fused high-density lipoprotein; and a method for diagnosing, preventing or treating posterior ocular disease.

106. 发明申请

US20210155598A1 CLASS OF BISQUATERNARY AMMONIUM COMPOUND AS WELL AS THE PREPARATIVE METHOD AND THE USE THEREOF 有权
公开(公告)号：US20210155598A1
公开(公告)日：2021-05-27
申请号：US17044158
申请日：2019-07-24
申请人： WEST CHINA HOSPITAL, SICHUAN UNIVERSITY
发明人： Jun YANG , Jin LIU , Weiyi ZHANG , Wensheng ZHANG , Cheng ZHOU , Bowen KE , Lei TANG
IPC分类号： C07D295/15 , A61P21/02
摘要： A two-quaternary ammonium compound has a structural formula of formula (I). L1 is a C1 to C8 alkylene group; L2 is a C1 to C8 alkylene group; Z1 is nitro group or a halogen or methoxy group; Z2 is nitro group or a halogen or methoxy group; Z3 is nitro group or a halogen or methoxy group; R═H or a C1 to C6 alkyl group; a, b, and c are independently an integer from 0-5; and M is a pharmaceutically acceptable anion, such as a bromine ion, chlorine ion, sulfonate radical, etc. A stereoisomer or mixture of stereoisomers, or a pharmaceutically acceptable salt or solvate or eutectic of the compound of formula (I) forms a composition with a pharmaceutically acceptable carrier, or forms a compounded prescription with other active components, and the composition or compounded prescription may be used in the preparation of a muscle relaxant.

107. 发明授权

US10669239B2 Tetrahydronaphthyl urea derivative 审中-公开
公开(公告)号：US10669239B2
公开(公告)日：2020-06-02
申请号：US16514835
申请日：2019-07-17
申请人： MOCHIDA PHARMACEUTICAL CO., LTD.
发明人： Fumihiko Saitoh , Hiroshi Nagasue
IPC分类号： C07D213/75 , C07D401/04 , C07D405/04 , C07D413/06 , C07D417/04 , A61P25/04 , A61K31/4418 , A61K31/506 , A61K31/4439 , A61K31/444 , C07D213/84 , A61K31/4433 , C07D405/14 , C07D213/81 , C07D413/12 , A61K45/06 , A61P37/00 , A61P1/02 , A61P7/00 , A61P13/08 , A61P21/00 , A61P25/20 , A61P25/28 , A61P31/00 , A61P43/00 , A61P1/16 , A61P9/00 , A61P9/06 , A61P11/06 , A61P37/06 , A61P1/18 , A61P3/04 , A61P3/06 , A61P11/04 , A61P17/00 , A61P19/02 , A61P29/02 , A61P31/18 , A61P35/02 , A61P3/10 , A61P9/12 , A61P13/02 , A61P13/10 , A61P13/12 , A61P21/02 , A61P25/24 , A61P1/00 , A61P11/00 , A61P15/00 , A61P25/00 , A61P25/08 , A61P25/16 , A61P29/00 , A61P1/04 , A61P5/14 , A61P11/02 , A61P19/10 , A61P35/00 , A61K45/00 , C07C213/10 , C07C215/44 , C07C271/24
摘要： The present invention aims to provide a compound having a TrkA inhibitory action, a pharmaceutically acceptable salt thereof, or a solvate thereof, a pharmaceutical composition containing the same as an active ingredient, and a preventive and/or therapeutic agent for medicinal use, in particular for a disease in which TrkA in involved (pain, cancers, inflammation/inflammatory diseases, allergic diseases, skin diseases, neurodegenerative diseases, infectious diseases, Sjogren's syndrome, endometriosis, renal diseases, osteoporosis, and the like). Specifically, the present invention provides a compound or an optical isomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof, or the like, the compound

108. 发明申请

US20190282674A1 USE OF HYALURONIDASE FOR TREATMENT OF MUSCLE STIFFNESS 审中-公开
公开(公告)号：US20190282674A1
公开(公告)日：2019-09-19
申请号：US16429272
申请日：2019-06-03
申请人： New York University
发明人： Preeti RAGHAVAN , Antonio STECCO
IPC分类号： A61K38/47 , A61P21/02 , A61K9/00 , A61K47/02
摘要： Provided are methods and kits for reducing the severity of muscle stiffness. The method comprises delivering to one or more specific locations in the deep fascia of an affected muscle a composition comprising a therapeutically effective amount of hyaluronidase.

109. 发明申请

US20190177370A1 PEPTIDE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, OR PRODRUG THEREOF 审中-公开
公开(公告)号：US20190177370A1
公开(公告)日：2019-06-13
申请号：US16324495
申请日：2017-08-08
申请人： TOKYO UNIVERSITY OF PHARMACY & LIFE SCIENCES
发明人： Yoshio HAYASHI , Kentaro TAKAYAMA , Yoichi NEGISHI
IPC分类号： C07K7/08 , A61P21/02 , A61P21/04 , A61K47/66
摘要： Provided is a peptide having a short chain length, for example, having the number of amino acid residues of 20 or less and having a high myostatin inhibitory activity. The present invention is a peptide comprising an amino acid sequence represented by Formula (1) in the specification and having the number of amino acid residues of 20 or less.

110. 发明授权

US10307467B2 Use of hyaluronidase for treatment of muscle stiffness 有权
公开(公告)号：US10307467B2
公开(公告)日：2019-06-04
申请号：US15325938
申请日：2015-07-16
申请人： New York University
发明人： Preeti Raghavan , Antonio Stecco
IPC分类号： A61K38/47 , A61K47/02 , A61K9/00 , A61P21/02
摘要： Provided are methods and kits for reducing the severity of muscle stiffness. The method comprises delivering to one or more specific locations in the deep fascia of an affected muscle a composition comprising a therapeutically effective amount of hyaluronidase.

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