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81. 发明申请

WO00037452A1 SULPHONYLOXAZOLAMINES AS THERAPEUTIC ACTIVE INGREDIENTS 审中-公开
标题翻译： Sulfonyloxazolamines AS治疗物质
公开(公告)号：WO00037452A1
公开(公告)日：2000-06-29
申请号：PCT/EP1999/009335
申请日：1999-12-01
IPC分类号： A61K31/421 , A61K31/454 , A61K31/5377 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , C07D263/48 , A61K31/42
CPC分类号： C07D263/48
摘要： The present invention relates to sulphonyloxazolamines of general formula (I), wherein R , R represent independently from each other H, A, -(CH2)n-Ar or alkenyl with 2-6 C atoms, R and R together also represent a mononuclear saturated heterocycle with 1-2 N, O and/or S atoms, Z is H, A, CF3, NO2, Hal, OH, OA, NH2, NHA or NA2, A represents alkyl with 1-6 C atoms, Ar is Z-monosubstituted or Z-disubstituted phenyl, Hal is F, Cl, Br or I, n is 1 or 2 or the physiologically acceptable salts or solvates thereof. Said sulphonyloxazolamines are used as therapeutic active ingredients. The invention also relates to the use of sulphonyloxazolamines as therapeutic active ingredients and/or to the production of pharmaceutical preparations to combat diseases of the central nervous system. The invention further relates to a pharmaceutical preparation and the production thereof.
摘要翻译：本发明涉及sulfonyloxazolamines通式（I）其中R <1>，R <2>各自独立地是H，A， - （CH 2）N-Ar或碳原子数2〜6的链烯基，R <1> 且R <2>一起还具有1-2个N，O和/或S原子的单核饱和杂环，Z为H，CF 3，NO 2，哈尔，OH，OA，NH 2，NHA或NA2，一个是具有烷基 1〜6个C原子，Ar是单或二取代由Z是苯基，哈尔是F，Cl，Br或I中，n，bedeulen 1或2，或它们的生理学上可接受的盐或溶剂化物作为治疗剂，使用sulfonyloxazolamines作为治疗剂的并 /或用于制备药物制剂的打击中枢神经系统中，药物制剂和它们的生产的疾病。

82. 发明申请

WO99046232A1 CARBOXYLIC ACID DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT 审中-公开
标题翻译：羧酸衍生物和含有其作为活性成分的药物
公开(公告)号：WO99046232A1
公开(公告)日：1999-09-16
申请号：PCT/JP1999/001134
申请日：1999-03-09
IPC分类号： A61K31/00 , A61K31/421 , C07C59/66 , C07C59/68 , C07C59/72 , C07C323/52 , C07D213/30 , C07D213/65 , C07D263/32 , C07D263/34 , C07D263/48 , C07D277/24 , C07D317/54 , C07D413/04 , C07D413/10 , C07D417/04 , C07D417/10 , C07C62/34 , A61K31/19 , A61K31/215 , A61K31/36 , A61K31/42 , A61K31/425 , A61K31/44 , C07C69/734 , C07D417/12
CPC分类号： C07D213/30 , A61K31/00 , C07C59/66 , C07C59/68 , C07C59/72 , C07C323/52 , C07D213/65 , C07D263/32 , C07D263/34 , C07D263/48 , C07D277/24 , C07D317/54 , C07D413/04 , C07D413/10 , C07D417/04 , C07D417/10
摘要： Compounds represented by general formula (I), nontoxic salts thereof or hydrates of the same; and peroxisome proliferator-activated receptor regulating agents containing the same as the active ingredient, wherein each symbol is as defined in the specification. Because of having an effect of regulating PPAR receptor, the compounds of the general formula (I) are useful as hypoglycemic agents, lipid-lowering agents, preventives and/or remedies for diseases associating metabolic errors (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, arteriosclerosis, hypertension, circulatory diseases, overeating, ischemic heart diseases, etc., HDL cholesterol-elevating agents, LDL cholesterol and/or VLDL cholesterol-lowering agents and drugs for relieving risk factors of diabetes or syndrome X.
摘要翻译：由通式（I）表示的化合物，其无毒盐或其水合物; 和含有与活性成分相同的过氧化物酶体增殖物激活受体调节剂，其中每个符号如说明书中所定义。由于具有调节PPAR受体的作用，通式（I）的化合物可用作降血糖剂，降脂剂，预防剂和/或与代谢异常相关的疾病（糖尿病，肥胖症，综合征X，高胆固醇血症，高脂蛋白血症等），高脂血症，动脉硬化，高血压，循环系统疾病，暴饮暴食，缺血性心脏病等，HDL胆固醇升高剂，LDL胆固醇和/或VLDL胆固醇降低剂以及用于缓解糖尿病或综合征危险因素的药物 X。

83. 发明申请

WO1998000408A1 N-PHENYLIMINO HETEROCYCLIC DERIVATIVES AND THEIR USE AS HERBICIDES 审中-公开
标题翻译： N-苯基咪唑杂环衍生物及其作为除草剂的用途
公开(公告)号：WO1998000408A1
公开(公告)日：1998-01-08
申请号：PCT/EP1997003420
申请日：1997-07-01
申请人： NOVARTIS AG , KRISTINSSON, Haukur , REMPFLER, Hermann , NUSSBAUMER, Hans
发明人： NOVARTIS AG
IPC分类号： C07D263/48
CPC分类号： C07D253/06 , A01N43/50 , A01N43/707 , A01N43/76 , A01N47/18 , A01N47/22 , A01N47/36 , C07C261/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D263/28 , C07D263/48 , C07D317/46 , C07D403/12 , C07D405/04 , C07D405/12 , C07D413/04 , C07D413/12
摘要： Compounds of the formula (I), in which -A- is a group (A1), (A2) or (A3) where the bonding of -A- to the nitrogen atom takes place via the carbon atom; R1 is halogen, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy, C1-C4alkylthio, C1-C4haloalkylthio, cyano or nitro; R2 is hydrogen, halogen, C1-C4alkyl or C1-C4haloalkyl; or R2 in position 2 of the phenyl ring and R1 together form a -OCF2O-group; R4 is C1-C6alkyl, C3-C6alkenyl, C3-C6alkynyl or C3-C6cycloalkyl, it being possible for these alkyl, alkenyl and alkynyl radicals to be substituted by halogen, C1-C3alkyl, C1-C3alkoxy, C1-C3alkylthio, C3-C6cycloalkyl, C3-C6cycloalkoxy, cyano, aryl, aryloxy or a saturated heterocyclic ring which contains 2-6 carbon atoms and nitrogen, oxygen and/or sulfur atoms, or R4 is C1-C7alkylaminosulfonyl, di-C1-C7alkylaminosulfonyl, C1-C7alkylsufonyl or C1-C7alkylsulfinyl, it being possible for these alkylaminosulfonyl, dialkylaminosulfonyl, alkylsulfonyl and alkylsulfinyl radicals to be substituted by halogen, C1-C3alkoxy, C1-C3alkylthio, C3-C6cycloalkyl, C3-C6cycloalkoxy, cyano, aryl, aryloxy or a saturated heterocyclic ring which contains 2-6 carbon atoms and nitrogen, oxygen and/or sulfur atoms, or R4 is cyano, arylsulfonyl, sulfamoyl or a -C(X)R7 or -C(X)NHR9 group; and agronomically suitable salts of compounds of the formula (I), are suitable as herbicides.
摘要翻译：式（I）化合物，其中-A-是通过碳原子发生-A-至氮原子键合的基团（A1），（A2）或（A3）; R1是卤素，C1-C4烷基，C1-C4卤代烷基，C1-C4烷氧基，C1-C4卤代烷氧基，C1-C4烷硫基，C1-C4卤代烷硫基，氰基或硝基; R2是氢，卤素，C1-C4烷基或C1-C4卤代烷基; 或R2位于苯环的2位，R1一起形成-OCF 2 O - 基; R 4是C 1 -C 6烷基，C 3 -C 6烯基，C 3 -C 6炔基或C 3 -C 6环烷基，这些烷基，烯基和炔基可被卤素，C 1 -C 3烷基，C 1 -C 3烷氧基，C 1 -C 3烷硫基，C 3 -C 6环烷基 C 3 -C 6环烷氧基，氰基，芳基，芳氧基或含有2-6个碳原子和氮，氧和/或硫原子的饱和杂环，或R 4是C 1 -C 7烷基氨基磺酰基，二-C 1 -C 7烷基氨基磺酰基，C 1 -C 7烷基磺酰基或C 1 -C 7烷基磺酰基 C 7烷基亚磺酰基，这些烷基氨基磺酰基，二烷基氨基磺酰基，烷基磺酰基和烷基亚磺酰基可以被卤素，C 1 -C 3烷氧基，C 1 -C 3烷硫基，C 3 -C 6环烷基，C 3 -C 6环烷氧基，氰基，芳基，芳氧基或饱和杂环取代， 2-6个碳原子和氮，氧和/或硫原子，或R4是氰基，芳基磺酰基，氨磺酰基或-C（X）R7或-C（X）NHR9基团; 和式（I）化合物的农学上合适的盐适合作为除草剂。

84. 发明申请

WO1995010509A1 4-IMINOOXAZOLIDIN-2-ONE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND HERBICIDE CONTAINING THE SAME AS ACTIVE INGREDIENT 审中-公开
标题翻译： 4-IMINOOXAZOLIDIN-2-ONE衍生物，其制备方法和含有它们的除草剂作为活性成分
公开(公告)号：WO1995010509A1
公开(公告)日：1995-04-20
申请号：PCT/JP1994001683
申请日：1994-10-07
申请人： SAGAMI CHEMICAL RESEARCH CENTER , KAKEN PHARMACEUTICAL CO., LTD. , HIRAI, Kenji , MATSUKAWA, Tomoko , YANO, Tomoyuki , MASUDA, Katsuyuki , YOSHII, Tomoko , MOURI, Takehito , UGAI, Sadayuki , YAMADA, Osamu
发明人： SAGAMI CHEMICAL RESEARCH CENTER , KAKEN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D263/48
CPC分类号： C07D263/48 , A01N43/76
摘要： A 4-iminooxazolidin-2-one derivative represented by general formula (1) (wherein X represents hydrogen or halogen; X represents hydrogen, halogen or alkyloxy; and X represents hydrogen, halogen, alkyloxy, cycloalkyloxy or alkynyloxy); a process for producing the above compound by the reaction of an aryl isocyanate represented by general formula (2) with methacrolein cyanohydrin in the presence of a base; a herbicide containing the above compound as the active ingredient; and a process for producing an oxazolidinedione derivative useful as a herbicide by hydrolyzing the above compound.
摘要翻译：由通式（1）表示的4-亚氨基恶唑烷-2-酮衍生物（其中X 1表示氢或卤素; X 2表示氢，卤素或烷氧基; X 3表示氢，卤素，烷氧基，环烷氧基或炔氧基）; 通过在碱存在下通过通式（2）表示的异氰酸酯与异丁烯醛氰醇反应制备上述化合物的方法; 含有上述化合物作为活性成分的除草剂; 以及通过水解上述化合物制备可用作除草剂的恶唑烷二酮衍生物的方法。

85. 发明申请

WO1992005163A1 5-TRIFLUOROACYLAMINO-2-ARYL OXAZOLES 审中-公开
标题翻译： 5-三氟乙酰胺-2-亚胺氧化物
公开(公告)号：WO1992005163A1
公开(公告)日：1992-04-02
申请号：PCT/US1991005172
申请日：1991-07-29
申请人： PFIZER INC. , CLARK, David, A. , HOWARD, Harry, R.
发明人： PFIZER INC.
IPC分类号： C07D263/48
CPC分类号： C07D403/04 , C07D263/48 , C07D403/12 , C07D417/12
摘要： A series of novel 5-trifluoroacylamino-2-aryl oxazoles and their pharmaceutically acceptable base addition salts are disclosed. These compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Methods for preparing these compounds from known starting materials are provided.
摘要翻译：公开了一系列新的5-三氟酰基氨基-2-芳基恶唑及其药学上可接受的碱加成盐。这些化合物可用于治疗某些慢性糖尿病并发症的醛糖还原酶抑制剂。提供了从已知原料制备这些化合物的方法。

86. 发明申请

WO2019209962A1 COMPOUNDS AND USES THEREOF 审中-公开
公开(公告)号：WO2019209962A1
公开(公告)日：2019-10-31
申请号：PCT/US2019/028928
申请日：2019-04-24
申请人： YUMANITY THERAPEUTICS, INC.
发明人： WRONA, Iwona , TIVITMAHAISOON, Parcharee , TARDIFF, Daniel , PANDYA, Bhaumik , OZBOYA, Kerem , LUCAS, Matthew , BOURDONNEC, Bertrand Le
IPC分类号： A61K31/422 , A61P35/00 , C07D263/48
摘要： The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.

87. 发明申请

WO2018101793A9 아미드 유도체 화합물, 이의 입체이성질체, 또는 이의 약학적으로 허용 가능한 염, 및 이를 포함하는 피부 노화 억제, 주름 개선, 또는 피부 상처 치료용 약학적 또는 화장료 조성물 审中-公开
公开(公告)号：WO2018101793A9
公开(公告)日：2018-06-07
申请号：PCT/KR2017/014019
申请日：2017-12-01
申请人： 서울대학교 산학협력단 , 가천대학교 산학협력단
发明人： 김상희 , 김선여
IPC分类号： A61K31/4402 , A61K31/4168 , A61K31/505 , A61K8/49 , A61Q19/08 , C07D241/20 , C07D263/48
摘要： 일 양상에 따른 아미드 유도체 화합물, 이의 입체이성질체, 유도체, 용매화물, 또는 이의 약학적으로 허용 가능한 염, 및 이의 용도를 제공한다. 이에 따르면, Sirt1의 발현을 증가시키는 효과가 우수하고, Sirt1의 활성화에 의한 피부 상처 치유 효과 및 피부 노화 억제 효과가 우수하므로, 피부 상처, 피부 노화 억제 또는 주름 개선용 약학 조성물로 유용하게 사용될 수 있다. 또한, 자외선 조사에 의해 유도된 피부 섬유아세포에서 MMP-1의 분비량 감소 및 프로콜라겐 타입 I의 분비량 증가, 및 Sirt1 분비량 및 활성 증가에 의해 항노화 또는 피부 주름을 개선하는데 유용하게 사용될 수 있다.

88. 发明申请

WO2017160922A1 ANALGESIC COMPOUNDS 审中-公开
公开(公告)号：WO2017160922A1
公开(公告)日：2017-09-21
申请号：PCT/US2017/022430
申请日：2017-03-15
申请人： KALYRA PHARMACEUTICALS, INC.
发明人： BUNKER, Kevin, Duane , SLEE, Deborah, Helen , HOPKINS, Chad, Daniel , PINCHMAN, Joseph, Robert , KAHRAMAN, Mehmet , HUANG, Peter, Qinhua
IPC分类号： A61K31/136 , A61K31/137 , A61K31/165 , A61K31/167 , A61P25/06 , A61P29/00 , A61K31/421 , A61K31/426 , A61K31/4245 , A61K31/433 , A61K31/415 , A61K31/44 , A61K31/505 , C07D277/28 , C07D285/135 , C07D285/12 , C07D271/113 , C07D277/40 , C07D239/42 , C07D213/73 , C07D263/48 , C07D231/12 , C07D213/38 , C07D285/08 , C07D277/32 , C07C211/52 , C07C211/29 , C07C233/13 , C07C233/15 , C07C233/07 , C07C233/25
摘要： Disclosed herein are compounds of Formula (I), methods of synthesizing compounds of Formula (I), and methods of using compounds of Formula (I) as an analgesic.

89. 发明申请

WO2017051353A1 MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE 审中-公开
标题翻译： INDOLEAMINE 2,3-DIOXYGENASE的调节剂
公开(公告)号：WO2017051353A1
公开(公告)日：2017-03-30
申请号：PCT/IB2016/055674
申请日：2016-09-22
申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED
发明人： CHONG, Pek Yoke , DE LA ROSA, Martha , DICKSON, Hamilton , KAZMIERSKI, Wieslaw Mieczyslaw , SAMANO, Vicente , TAI, Vincent Wing-Fai
IPC分类号： C07D403/12 , C07D235/30 , C07D413/12 , C07D417/12 , C07D263/48 , C07D263/58 , C07D277/80 , C07D285/08 , A61K31/41 , A61K31/433
CPC分类号： C07D235/30 , C07D263/48 , C07D263/58 , C07D277/80 , C07D285/08 , C07D403/12 , C07D413/12 , C07D417/12
摘要： Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of HIV; including the prevention of the progression of AIDS and general immunosuppression.
摘要翻译：提供其化合物及其药学上可接受的盐，其药物组合物，其制备方法及其用于预防和/或治疗HIV的方法; 包括预防艾滋病的进展和一般的免疫抑制。

90. 发明申请

WO2017013265A1 METABOLICALLY ROBUST ANALOGS OF CYP-EICOSANOIDS FOR THE TREATMENT OF CARDIAC DISEASE 审中-公开
标题翻译：用于治疗心脏病的CYP-EICOSANOID的代表性的稳定模拟
公开(公告)号：WO2017013265A1
公开(公告)日：2017-01-26
申请号：PCT/EP2016/067601
申请日：2016-07-22
申请人： OMEICOS THERAPEUTICS GMBH , BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , MAX DELBRÜCK-CENTRUM FÜR MOLEKULARE MEDIZIN
发明人： FISCHER, Robert , KONKEL, Anne , WESSER, Tim , WESTPHAL, Philipp , SCHUNK, Wolf-Hagen , WESTPHAL, Christina , FALCK, John Russel
IPC分类号： C07C275/20 , C07D309/14 , C07C311/17 , C07C311/51 , C07D249/08 , C07D257/04 , A61K31/16 , A61K31/395 , A61P9/00 , C07C233/56 , C07D263/48 , C07D295/192 , C07D307/68 , A61K31/17 , A61K31/18
CPC分类号： C07C233/56 , C07C275/20 , C07C311/17 , C07C311/51 , C07D249/12 , C07D257/04 , C07D263/48 , C07D295/192 , C07D307/60 , C07D309/14
摘要： The present invention relates to compounds according to general formula (I) which are metabolically robust analogues of bioactive lipid mediators derived from omega-3 polyunsaturated fatty acids (n-3 PUFAs).The present invention further relates to compositions containing one or more of these compounds and to the use of these compounds or compositions for the treatment or prevention of cardiovascular diseases.
摘要翻译：本发明涉及根据通式（I）的化合物，其是衍生自ω-3多不饱和脂肪酸（n-3 PUFA）的生物活性脂质介质的代谢强度类似物。本发明还涉及含有这些中的一种或多种的组合物化合物和这些化合物或组合物用于治疗或预防心血管疾病的用途。

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