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2. 发明授权

EP2632908B1 SULFONAMIDES AS HIV PROTEASE INHIBITORS 有权
标题翻译：磺酰胺艾滋病毒抗原蛋白酶
公开(公告)号：EP2632908B1
公开(公告)日：2016-05-25
申请号：EP11835401.8
申请日：2011-10-27
申请人： Merck Canada Inc.
发明人： MORADEI, Oscar, M. , CRANE, Sheldon , MCKAY, Daniel, J. , LEBRUN, Marie-Eve , TRUONG, Vouy Linh
IPC分类号： C07D277/62 , A61K31/27 , A61K31/415 , A61K31/421 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/505 , A61K31/506 , A61P31/18 , C07C311/29 , C07C311/41 , C07C317/40 , C07C323/49 , C07D231/12 , C07D261/08 , C07D417/12 , C07D417/14
CPC分类号： C07C311/18 , A61K31/428 , A61K31/4439 , A61K31/506 , A61K31/63 , A61K31/635 , A61K45/06 , C07C311/29 , C07C311/41 , C07C317/40 , C07C323/49 , C07C2601/02 , C07D213/75 , C07D231/12 , C07D239/26 , C07D261/08 , C07D277/62 , C07D277/64 , C07D417/12 , C07D417/14

3. 发明公开

EP2254861A1 THE 1,3-DISUBSTITUTED UREAS, METHOD OF RE ARATION AND UTILISATION THEREOF 审中-公开
标题翻译： 1,3-二取代的脲，方法和应用
公开(公告)号：EP2254861A1
公开(公告)日：2010-12-01
申请号：EP08855483.7
申请日：2008-11-21
申请人： Hameln-rds, A.s.
发明人： KAKALIK, Ivan , VALACHOVIC, Pavol , SCHMIDTOVA, Ludmila
IPC分类号： C07C323/44 , C07C323/49 , C07D213/75 , A61K31/17 , A61K31/44 , A61P9/10 , A61P3/06
CPC分类号： C07D213/75 , C07C323/44 , C07C323/49 , C07C323/62 , C07D213/64 , C07D213/65 , C07D213/68 , C07D215/36 , C07D239/38 , C07D241/18 , C07D241/44 , C07D251/38 , C07D401/12
摘要： The invention relates to 1,3-disubstituted ureas of general formula (I) where X is CH group or nitrogen, II1 is alkyl carbonyl, carbonyl or carbamoyl, and R2 is di fferent substituted phenyl, pyridyl. pyrazyl, pyrimidyl, quinolinyl and quinoxalinyl, and the method of preparing thereof which consist in treating aromatic amines with isocyanates in inert solvents at 20 to 12O0C. The obtained 1,3-disubstituted ureas are inhibitors of the activity of the acyl co¬ enzyme A: cholesterol acykransferase (ACAT) enzyme, and may be used to inhibit cholesterol esterification and absorption in hypercholesterolemia.

4. 发明公开

EP2114874A2 PROCEDE DE PREPARATION DE SULFANYLAMIDES ET SULFINAMIDINES FLUORES ET LEURS UTILISATIONS 审中-公开
标题翻译：用于制备氟化SULPHANYLAMIDEN和方法及其用途SULPHINAMIDINEN AND
公开(公告)号：EP2114874A2
公开(公告)日：2009-11-11
申请号：EP08761839.3
申请日：2008-02-04
申请人： Aventis Pharma S.A. , CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
发明人： BACQUE, Eric , EL-AHMAD, Youssef , BILLARD, Thierry , LANGLOIS, Bernard , FERRY, Aurélien
IPC分类号： C07C311/48 , C07C313/20 , C07C313/32 , C07C319/14 , C07C321/18 , C07C321/22 , C07C323/12 , C07C323/49 , C07C381/00 , C07C381/06 , C07D231/38 , C07D233/74 , C07D263/36 , C07D295/26
CPC分类号： C07C381/00 , C07C311/48 , C07C313/20 , C07C313/32 , C07C319/14 , C07C323/49 , C07C381/06 , C07D231/38 , C07D233/74 , C07D263/36 , C07D295/26 , C07C321/18 , C07C321/22 , C07C323/12
摘要： The invention relates to a method for preparing polyfluorinated sulphanylamides of formula (I) and polyfluorinated sulphinamidines of formula (II), wherein R1-R4 are defined as in the claims, and for preparing the precursors of same.

5. 发明公开

EP1544193A4 SULFONAMIDE DERIVATIVES, INSECTICIDES FOR AGRICULTURAL AND HORTICULTURAL USE, AND USAGE THEREOF 审中-公开
标题翻译：磺胺类药物，杀虫剂FOR USE在农业和园艺，其使用
公开(公告)号：EP1544193A4
公开(公告)日：2007-05-23
申请号：EP03792848
申请日：2003-08-26
申请人： NIHON NOHYAKU CO LTD
发明人： YAMAGUCHI MINORU , NAKAO HAYAMI , GOTO MAKOTO , MORIMOTO MASAYUKI , FUJIOKA SHINSUKE , TOHNISHI MASANORI
IPC分类号： C07D213/75 , A01N41/06 , A01N43/40 , A01N47/02 , C07C311/32 , C07C311/46 , C07C311/48 , C07C317/28 , C07C323/49 , C07D279/12 , C07C311/49 , C07C311/50 , C07D213/42
CPC分类号： C07D213/75 , A01N41/06 , A01N43/40 , A01N47/02 , C07C311/32 , C07C311/48 , C07C317/28 , C07C323/49 , C07D279/12
摘要： Sulfonamide derivatives represented by the general formula (1) or salts thereof; insecticides for agricultural and horticultural use containing the same as the active ingredient; and usage thereof: (1) [wherein A is optionally substituted C1-C6 alkylene, C3-C6 alkenylene, or the like; R1 is H, optionally substituted C1-C6 alkyl, C3-C6 alkenyl, C3-C6 cycloalkyl, or the like; R2, R3, and R4 are each H, C1-C6 alkyl, C3-C6 alkenyl, or the like, or R2 and A or R2 and R1 may form a three- to eight-membered ring which may be interrupted by one to three atoms selected from among O, S, and N; Q is C or N; X and Y are each halogeno, CN, NO2, C1-C6 alkyl, C2-C6 alkenyl, or the like; m is 0 to 2; n is 0 to 3; and two adjacent Xs or Ys on the aromatic ring may be united to form a fused ring]. The compounds exhibit excellent insecticidal activity against pest insects resistant to existing pesticides even when applied in dosages lower than those of similar pesticides.

7. 发明公开

EP0626369A4 BENZENESULFONAMIDE DERIVATIVE. 失效
标题翻译：苯并呋喃衍生物。
公开(公告)号：EP0626369A4
公开(公告)日：1994-08-29
申请号：EP92923185
申请日：1992-11-05
申请人： KYOWA HAKKO KOGYO KK
发明人： KINOSHITA IWAO , TAKAI HARUKI , KOSAKA NOBUO , SUGAWARA KATSURA , ISHII AKIO , ISHIDA HIROYUKI , GOMI KATSUSHIGE
IPC分类号： C07D211/06 , A61K31/18 , C07C311/29 , C07C323/49 , C07D211/10 , C07D211/58 , C07D211/96 , C07D241/04 , C07D277/46 , C07D277/48 , C07D277/52 , C07D295/22 , C07D295/26
CPC分类号： C07C323/49 , C07C311/29 , C07C2601/14 , C07C2601/18 , C07C2603/74 , C07D211/58 , C07D277/46 , C07D295/26
摘要： A benzenesulfonamide derivative represented by general formula (I), which is useful for treating osteoporosis, or a pharmacologically acceptable salt thereof, wherein R?1 and R2¿ may be the same or different from each other and each represents hydrogen or lower alkanoyl; and R?3 and R4¿ may be the same or different from each other and each represents hydrogen, lower alkyl, alicyclic alkyl, (un)substituted polycyclic alkyl, substituted aryl or (un)substituted heterocycle, or alternatively R?3 and R4¿ are combined together with the adjacent nitrogen atom to represent (un)substituted alicyclic heterocycle.
摘要翻译：可用于治疗骨质疏松症的通式（I）表示的苯磺酰胺衍生物或其药理学上可接受的盐，其中R 1和R 2可以彼此相同或不同，并且各自表示氢或低级烷; R 3和R 4可以彼此相同或不同，各自表示氢，低级烷基，脂环族烷基，（取代的）多环烷基，取代的芳基或（取代的）取代的杂环， 3>和R 4与相邻的氮原子一起组合以代表（未）取代的脂环族杂环。

8. 发明公开

EP0481919A2 Heteroatom containing perfluoroalkyl terminated neopentyl sulfates and salts thereof 失效转让
标题翻译：新戊酰硫酸盐终端物，ein Heteroatom enthaltenden全氟烷基葡聚糖和deeth盐。
公开(公告)号：EP0481919A2
公开(公告)日：1992-04-22
申请号：EP91810771.5
申请日：1991-10-01
申请人： CIBA-GEIGY AG
发明人： Karydas, Athanasios , Loh, Yung
IPC分类号： C07C323/12 , C07C323/25 , C07C317/18 , C07C305/10 , C07C311/09 , C07C323/41 , D21H17/11 , D21H17/09 , C07C323/49 , D06M13/265 , D06M13/144 , D06M13/408 , D21H13/16 , D06M13/438 , D06M13/402
CPC分类号： C07C323/25 , C07C305/06 , C07C305/10 , C07C317/18 , C07C317/28 , C07C323/12 , C07C323/41 , C07C323/49 , D06M13/144 , D06M13/265 , D06M13/408 , D21H17/09 , D21H17/11
摘要： The present invention relates to perfluoroalkyl substituted sulfates and salts thereof of the formulas

(R f X CH₂) x C(CH₂OH) y (CH₂OSO₃-M+) z (I)

or

(R f E X CH₂) x C(CH₂OH) y (CH₂OSO₃-M+) z (II)

which are prepared by sulfation of perfluoroalkyl substituted alcohols of the formulas

(R f X CH₂) x C(CH₂OH) q (III)

or

(R f E X CH₂) x C(CH₂OH) q (IV)

wherein
R f is a straight or branched chain perfluoroalkyl of 1 to 18 carbon atoms or said perfluoroalkyl substituted by perfluoroalkyl of 2 to 6 carbon atoms, or mixtures thereof,
E is branched or straight chain alkylene of 1 to 10 carbon atoms or said alkylene interrupted by one to three groups selected from the group consisting of -NR-, -O-, -S-, -SO₂-, -COO-, -OOC-, -CONR-, -NRCO-, -SO₂NR- and -NRSO₂ or terminated at the R f end with -CONR- or -SO₂NR-, where R f is attached to the carbon or sulfur atom, and
for formula II, X is -S-, -O-, SO₂-, or -NR-, and
for formula I, X is -CONR- or -SO₂NR-, where R f is attached to the carbon or sulfur atom, and where R is independently hydrogen, alkyl of 1 to 6 carbon atoms or hydroxyalkyl of 2 to 6 carbon atoms;
x is 1,2 or 3; y is 0, 1 or 2; z is 1, 2 or 3; q is 1,2 or 3; x+y+z=4 and
x+q=4;
M is independently hydrogen, an alkali metal or organoammonium ion.
摘要翻译：本发明涉及式（Rf X CH2）xC（CH2OH）y（CH2OSO3-M +）z（I）或（RfE X CH2）xC（CH2OH）y（CH2OSO3-M +）z的全氟烷基取代的硫酸盐及其盐（II），其通过式（Rf X CH 2）x C（CH 2 OH）q（III）或（R f E X CH 2）x C（CH 2 OH）q（IV）的全氟烷基取代的醇的硫酸化制备，其中R f是直链或支链 1至18个碳原子的全氟烷基或被2至6个碳原子的全氟烷基取代的所述全氟烷基，或其混合物，E是1-10个碳原子的支链或直链亚烷基或所述亚烷基被一至三个选自由-NR - ， - O - ， - S - ， - SO 2 - ， - COO - ， - OC - ， - CONR - ， - NRCO - ， - SO 2 NR-和-NRSO 2组成，或者在Rf端用-CONR- 或-SO 2 NR-，其中R f连接到碳或硫原子上，对于式II，X是-S-，-O-，SO2-或-NR-，对于式I，X是-CONR-或 -SO 2 NR-，其中R f连接到碳或硫原子上，其中R是茚基 1至6个碳原子的烷基或2至6个碳原子的羟基烷基; x为1,2或3; y为0,1或2; z为1,2或3; q为1,2或3; x + y + z = 4，x + q = 4; M独立地是氢，碱金属或有机铵离子。

9. 发明授权

EP3321252B1 NOVEL COMPOUND THAT SPECIFICALLY BINDS TO AMPA RECEPTOR 有权
公开(公告)号：EP3321252B1
公开(公告)日：2020-10-21
申请号：EP16821400.5
申请日：2016-07-05
申请人： Public University Corporation Yokohama City University
发明人： TAKAHASHI Takuya , MIYAZAKI Tomoyuki , SUHARA Tetsuya , HIGUCHI Makoto , CHO Meiei
IPC分类号： C07C323/49 , A61K51/04 , C07C319/20 , C07F7/22 , C07B59/00 , A61K47/50

10. 发明授权

EP1742908B1 NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 有权转让
标题翻译：抑制剂NICHT-NUKLEOSID-INHIBITOREN DER REVERSEN TRANSKRIPTASE
公开(公告)号：EP1742908B1
公开(公告)日：2009-11-11
申请号：EP05742851.8
申请日：2005-04-15
申请人： F.HOFFMANN-LA ROCHE AG
发明人： DUNN, James, Patrick , HIRSCHFELD, Donald, Roy , SILVA, Tania , VORA, Harit
IPC分类号： C07C235/38 , A61K31/167 , A61P31/18 , C07C235/78 , C07C255/54 , C07C255/57 , C07C311/08 , C07C311/46 , C07C311/51 , C07C317/32 , C07C317/40 , C07C317/44 , C07C323/49 , C07C323/62 , C07D207/32
CPC分类号： C07C311/46 , C07C311/08 , C07C311/51 , C07C317/32 , C07C317/40 , C07C317/44 , C07C323/49 , C07C323/62 , C07C2601/14 , C07D207/325 , C07D213/75 , C07D213/82 , C07D213/84 , C07D295/108 , C07D295/13 , C07D295/135 , C07D295/26 , C07D307/79
摘要： The present invention provides compounds for treating or preventing an HIV infection, or treating AIDS or ARC comprising administering a compound according to formula (I) where Ar, R1-R5, R11c and X1 are as defined herein.
摘要翻译：本发明提供用于治疗或预防HIV感染或治疗AIDS或ARC的化合物，其包括给予式（I）化合物，其中Ar，R 1 -R 5，R 11c和X 1，如本文所定义。

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