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1. 发明申请

US20220362257A1 THERAMUTEIN MODULATORS 有权
公开(公告)号：US20220362257A1
公开(公告)日：2022-11-17
申请号：US17857492
申请日：2022-07-05
申请人： HMI Medical Innovations, LLC
发明人： Gerard M. Housey
IPC分类号： A61K31/5377 , C07D213/81 , C07D213/87 , C07D215/50 , C07D231/14 , C07D239/42 , C07D239/84 , C07D253/065 , C07D401/12 , C07D405/12 , C07D409/12 , G01N33/574 , C07D239/48 , C07C243/38 , C07D213/77 , C07D213/86 , C07D215/38 , C07D253/075 , C07D403/12 , G01N33/573 , A61K31/47 , A61K31/4709 , A61K31/505 , A61K31/506 , A61K31/53 , G01N33/50 , A61K31/166 , A61K31/175 , A61K31/195 , A61K31/27 , A61K31/415 , A61K31/4196 , A61K31/44 , A61K31/4436 , A61K31/444 , A61K31/495 , A61K31/517
摘要： This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.

2. 发明申请

US20210008077A1 THERAMUTEIN MODULATORS 有权
公开(公告)号：US20210008077A1
公开(公告)日：2021-01-14
申请号：US17038457
申请日：2020-09-30
申请人： HMI Medical Innovations, LLC
发明人： Gerard M. Housey
IPC分类号： A61K31/5377 , C07D213/81 , C07D213/87 , C07D215/50 , C07D231/14 , C07D239/42 , C07D239/84 , C07D253/065 , C07D401/12 , C07D405/12 , C07D409/12 , G01N33/574 , C07D239/48 , C07C243/38 , C07D213/77 , C07D213/86 , C07D215/38 , C07D253/075 , C07D403/12 , G01N33/573 , A61K31/47 , A61K31/4709 , A61K31/505 , A61K31/506 , A61K31/53 , G01N33/50 , A61K31/166 , A61K31/175 , A61K31/195 , A61K31/27 , A61K31/415 , A61K31/4196 , A61K31/44 , A61K31/4436 , A61K31/444 , A61K31/495 , A61K31/517
摘要： This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.

3. 发明申请

US20180021346A1 NOVEL GLP-1 RECEPTOR MODULATORS 审中-公开
公开(公告)号：US20180021346A1
公开(公告)日：2018-01-25
申请号：US15711858
申请日：2017-09-21
申请人： Celgene International II SÀRL
发明人： Marcus F. Boehm , Esther Martinborough , Manisha Moorjani , Junko Tamiya , Liming Huang , Adam R. Yeager , Enugurthi Brahmachary , Thomas Fowler , Andrew Novak , Premji Meghani , Michael Knaggs , Daniel Glynn , Mark Mills
IPC分类号： A61K31/551 , C07D417/12 , C07D413/12 , C07D413/04 , C07D409/14 , C07D409/12 , C07D407/12 , C07D405/12 , C07D403/12 , C07D403/10 , C07D403/04 , C07D401/12 , C07D401/06 , C07D401/04 , C07D295/135 , C07D295/084 , C07D285/12 , C07D285/08 , C07D277/30 , C07D271/107 , C07D271/06 , C07D263/32 , C07D253/065 , C07D253/06 , C07D243/08 , C07D241/12 , C07D241/08 , C07D239/74 , C07D239/34 , C07D471/04 , C07D237/08 , C07D231/12 , C07D215/14 , C07D213/55 , C07D211/98 , C07D211/22 , C07D207/08 , A61K38/26 , A61K31/53 , A61K31/506 , A61K31/505 , A61K31/501 , A61K31/50 , A61K31/4965 , A61K31/497 , A61K31/495 , A61K31/4725 , A61K31/4709 , A61K31/4545 , A61K31/454 , A61K31/4468 , A61K31/4439 , A61K31/445 , A61K31/44 , A61K31/433 , A61K31/4245 , A61K31/426 , A61K31/421 , A61K31/4178 , C07D495/04 , A61K31/402 , C07D239/26
CPC分类号： A61K31/551 , A61K31/402 , A61K31/4178 , A61K31/421 , A61K31/4245 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/4439 , A61K31/445 , A61K31/4468 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/4965 , A61K31/497 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/53 , A61K38/26 , C07D207/08 , C07D211/22 , C07D211/98 , C07D213/55 , C07D215/14 , C07D231/12 , C07D237/08 , C07D239/26 , C07D239/34 , C07D239/74 , C07D241/08 , C07D241/12 , C07D243/08 , C07D253/06 , C07D253/065 , C07D263/32 , C07D271/06 , C07D271/107 , C07D277/30 , C07D285/08 , C07D285/12 , C07D295/084 , C07D295/135 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04
摘要： Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.

4. 发明授权

US09795613B2 GLP-1 receptor modulators 有权
公开(公告)号：US09795613B2
公开(公告)日：2017-10-24
申请号：US14965777
申请日：2015-12-10
申请人： Celgene International II SÀRL
发明人： Marcus F. Boehm , Esther Martinborough , Manisha Moorjani , Junko Tamiya , Liming Huang , Adam R. Yeager , Enugurthi Brahmachary , Thomas Fowler , Andrew Novak , Premji Meghani , Michael Knaggs , Daniel Glynn , Mark Mills
IPC分类号： C07D403/10 , A61K31/506 , A61K31/551 , C07D403/12 , C07D215/14 , C07D231/12 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D237/08 , C07D239/26 , C07D407/12 , C07D409/12 , C07D409/14 , C07D239/74 , C07D413/04 , C07D413/12 , C07D241/12 , C07D417/12 , C07D471/04 , C07D253/06 , C07D207/08 , C07D271/06 , C07D495/04 , C07D295/084 , C07D295/135 , C07D213/55 , A61K31/402 , A61K31/4178 , A61K31/421 , A61K31/4245 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/4439 , A61K31/445 , A61K31/4468 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/4965 , A61K31/497 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/53 , A61K38/26 , C07D211/22 , C07D211/98 , C07D239/34 , C07D241/08 , C07D243/08 , C07D253/065 , C07D263/32 , C07D271/107 , C07D277/30 , C07D285/08 , C07D285/12 , C07D405/12
CPC分类号： A61K31/551 , A61K31/402 , A61K31/4178 , A61K31/421 , A61K31/4245 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/4439 , A61K31/445 , A61K31/4468 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/4965 , A61K31/497 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/53 , A61K38/26 , C07D207/08 , C07D211/22 , C07D211/98 , C07D213/55 , C07D215/14 , C07D231/12 , C07D237/08 , C07D239/26 , C07D239/34 , C07D239/74 , C07D241/08 , C07D241/12 , C07D243/08 , C07D253/06 , C07D253/065 , C07D263/32 , C07D271/06 , C07D271/107 , C07D277/30 , C07D285/08 , C07D285/12 , C07D295/084 , C07D295/135 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04
摘要： Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.

5. 发明授权

US08795389B2 Non metal tanning 有权
标题翻译：非金属鞣制
公开(公告)号：US08795389B2
公开(公告)日：2014-08-05
申请号：US13879172
申请日：2011-10-05
申请人： Claus Reineking , Roberta Gamarino , Licia Trimarco , Maurizio Quaglierini , Markus Gisler , Rainer Nusser
发明人： Claus Reineking , Roberta Gamarino , Licia Trimarco , Maurizio Quaglierini , Markus Gisler , Rainer Nusser
IPC分类号： C14C3/26 , C14C3/00 , C14C3/02 , C14C3/04 , C14C3/08 , C07D253/00 , C07D253/065 , C07D253/07 , C07D253/075
CPC分类号： C14C3/00 , C07D251/44 , C07D253/00 , C07D253/065 , C07D253/07 , C07D253/075 , C14C3/02 , C14C3/04 , C14C3/08 , C14C3/26 , C14C3/28
摘要： Tanned leather, skin or pelt is produced by non-metal tanning, comprising the step of tanning a bated hide, skin or pelt with a tanning agent (A), the tanning agent (A) being at least one compound of a formula (I), wherein X signifies fluorine or chlorine, and/or (+NR3)0-1, wherein R is a substituted or unsubstituted C1 to C6 alkyl group, a substituted or unsubstituted C6 to C10 aryl or a C5 to C6heteroaryl group, R1 signifies hydrogen, C1-8-alkyl or an alkyleneoxy radical of a formula (Ia), -(—C2-3 alkylene-O—)q—H (Ia), R2 signifies hydrogen or hydroxyl, m, signifies 1, 2 or 3, q is of from 1 to 10, M signifies hydrogen or an alkali metal cation or an ammonium cation, being a protonated tertiary amine or a quaternary ammonium cation, in a tanning bath having a pH of from 6 to 10 at the beginning of tanning step.
摘要翻译：鞣制的皮革，皮肤或毛皮是通过非金属鞣制制成的，包括用鞣剂（A）鞣制皮肤，皮肤或皮肤的步骤，鞣剂（A）是至少一种式（I ），其中X表示氟或氯，和/或（+ NR3）0-1，其中R是取代或未取代的C1至C6烷基，取代或未取代的C6至C10芳基或C5至C6杂芳基，R1表示氢，C1-8烷基或式（Ia）的亚烷基氧基， - （ - C2-3亚烷基-O-）q-H（Ia），R2表示氢或羟基，m表示1,2或3 q为1〜10，M表示在鞣制开始时pH为6〜10的鞣制浴中的氢或碱金属阳离子或铵阳离子，为质子化叔胺或季铵阳离子步。

6. 发明申请

US20120289403A1 Fluorinated Oxa or Thia Heteroarylalkylsulfide Derivatives for Combating Invertebrate Pests 有权
标题翻译：氟化Oxa或Thia杂芳基烷基硫化物用于防治无脊椎动物害虫的衍生物
公开(公告)号：US20120289403A1
公开(公告)日：2012-11-15
申请号：US13510197
申请日：2010-11-11
申请人： Sebastian Soergel , Ralph Paulini , Steffen Gross , Carsten Beyer , Matthias Pohlman , Henricus Maria Martinus Bastiaans , Michael Rack , Deborah L. Culbertson , Douglas D. Anspaugh , Sarah Thompson , Vincent Salgado
发明人： Sebastian Soergel , Ralph Paulini , Steffen Gross , Carsten Beyer , Matthias Pohlman , Henricus Maria Martinus Bastiaans , Michael Rack , Deborah L. Culbertson , Douglas D. Anspaugh , Sarah Thompson , Vincent Salgado
IPC分类号： A01N43/40 , A01N43/707 , A01N43/54 , A01N43/824 , A01N43/653 , C07D253/065 , C07D239/30 , C07D239/26 , C07D401/06 , C07D211/94 , C07D285/12 , C07D249/08 , C07D231/12 , A01P7/04 , A01N43/56
CPC分类号： C07D285/12 , A01N43/08 , A01N43/10 , A01N43/22 , A01N43/40 , A01N43/46 , A01N43/50 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/62 , A01N43/647 , A01N43/66 , A01N43/713 , A01N43/72 , A01N43/78 , A01N43/80 , A01N43/82 , C07D207/325 , C07D209/10 , C07D209/12 , C07D213/32 , C07D213/34 , C07D233/66 , C07D235/12 , C07D237/08 , C07D239/20 , C07D249/08 , C07D251/16 , C07D257/04 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/26 , C07D307/38 , C07D307/40 , C07D307/79 , C07D307/80 , C07D333/18 , C07D333/54 , C07D333/56
摘要： The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.
摘要翻译：本发明涉及用于对抗或控制无脊椎动物害虫，特别是节肢动物害虫和线虫的对映异构体或其兽医学上可接受的盐的烷基硫醚衍生物化合物。本发明还涉及通过使用这些化合物和植物繁殖材料以及包含所述化合物的农业和兽用组合物来控制无脊椎害虫的方法。其中U，R1，R2，R3U，X，n和p如说明书中所定义。

7. 发明申请

US20090264433A1 Compounds, Compositions and Methods Comprising Triazine Derivatives 审中-公开
标题翻译：包含三嗪衍生物的化合物，组合物和方法
公开(公告)号：US20090264433A1
公开(公告)日：2009-10-22
申请号：US12426498
申请日：2009-04-20
申请人： Michael Geoffrey Neil Russell , Joanne Peach , Jacqueline Anne Macritchie , Sebastian Bruckner , Kevin James Doyle
发明人： Michael Geoffrey Neil Russell , Joanne Peach , Jacqueline Anne Macritchie , Sebastian Bruckner , Kevin James Doyle
IPC分类号： A61K31/53 , C07D253/065 , C12N5/06 , A61P1/12
CPC分类号： C07D253/065 , C07D253/07 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or encompassed by formulas I-II) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
摘要翻译：本发明涉及用于治疗动物疾病的组合物和方法，该疾病通过对有需要的哺乳动物施用有效量的本文定义的化合物来对功能性囊性纤维化跨膜传导调节因子（CFTR）多肽的抑制作出反应包括表1所示或由式I-II所包括的化合物或其组合物，从而治疗疾病。本发明特别涉及一种治疗腹泻和多囊肾病的方法。

8. 发明申请

US20080299055A1 Monomer 5, 6-Diphenyl-1.2.4-Traizinic Derivatives and the Use Thereof 有权
标题翻译：单体5,6-二苯基-1.2.4-特异性衍生物及其用途
公开(公告)号：US20080299055A1
公开(公告)日：2008-12-04
申请号：US11579341
申请日：2005-05-04
申请人： Jerome Rey , Pascal Bordat , Roger Tarroux
发明人： Jerome Rey , Pascal Bordat , Roger Tarroux
IPC分类号： A61K8/49 , C07D253/065 , C07D253/07 , A61Q17/04
CPC分类号： C07D253/065 , A61K8/4966 , A61Q17/04 , C07D253/07
摘要： The invention relates to the use of 5,6-diphenyl-1,2,4-triazinic compounds of general formula (I), wherein cycle penetrating bonds display an ortho, meta or para indifferent substitution position, identical or different R1 and R2 represent a hydrogen, fluoride, chloride or bromine atom, C1 to C12 linear or branched alkyl, C1 A C18 linear or branched hydroxy, alkoxy poly(ethoxy)-alkoxy with a C1 to C4 alkyl fragment and an ethoxy number ranging from 1 to 4, amino or mono or di-alkylamino with a C1 to C4 alkyl fragment group, R3 represents a chlorine atom, a hydroxy, amino, a phenyl possibly 1 to 3 times substituted by a hydroxy radical situated at least in a para or phenyl position possibly 1 to 3 times substituted in an ortho, meta or para position by a C1 to C12 alkoxy or cyano or alkymino group with a C1 to C7 alkyl fragment in the form of active sun filters or light-protective agents and to cosmetic composition containing said compounds.
摘要翻译：本发明涉及通式（I）的5,6-二苯基-1,2,4-三嗪化合物的用途，其中循环穿透键显示相邻或不同的取代位置，相同或不同的R 1和R 2表示 C 1 -C 12直链或支链烷基，C 1 -C 18直链或支链羟基，具有C1至C4烷基片段的烷氧基聚（乙氧基） - 烷氧基和1至4的乙氧基，氨基或一或二烷基氨基与C 1至C 4烷基片基，R 3表示氯原子，羟基，氨基，可被1至3倍被至少位于对位或苯基位置的羟基取代的苯基，可能为1 以C1-C12烷氧基或氰基或烷基氨基取代邻位，间位或对位至活性阳离子过滤器或光保护剂形式的C 1至C 7烷基片段，并含有所述化合物的化妆品组合物。

9. 发明授权

US06969716B2 5-phenyl[1,2,4]triazines as ligands for GABA-A α2/α3 receptors for treating anxiety or depression 失效
标题翻译： 5-苯基[1,2,4]三嗪作为用于治疗焦虑或抑郁症的GABA-Aα2/α3受体的配体
公开(公告)号：US06969716B2
公开(公告)日：2005-11-29
申请号：US10769070
申请日：2004-01-30
申请人： Wesley Peter Blackaby , Simon Charles Goodacre , David James Hallett , Andrew Jennings , Richard Thomas Lewis , Leslie Joseph Street , Kevin Wilson
发明人： Wesley Peter Blackaby , Simon Charles Goodacre , David James Hallett , Andrew Jennings , Richard Thomas Lewis , Leslie Joseph Street , Kevin Wilson
IPC分类号： A61K31/53 , C07D253/065 , A61P25/22
CPC分类号： A61K31/53
摘要： The present invention provides a compound of formula I, or an N-oxide thereof or a pharmaceutically acceptable salt thereof: wherein X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy;X2 represents hydrogen or halogen;Z represents hydrogen, halogen, cyano, cyanomethyl, trifluoromethyl, nitro, hydroxy, hydroxy(C1-6)alkyl, C1-6 alkoxy, C1-6 alkoxy(C1-6)alkyl, trifluoromethoxy, trifluoromethylthio, trifluoromethanesulfinyl, formyl, C2-6 alkoxycarbonyl, oxopyrrolidinyl, or an optionally substituted aryl, heteroaryl or heteroaryl(C1-6)alkoxy group; andR1 represents aryl or heteroaryl, either of which groups may be optionally substituted;pharmaceutical compositions comprising it, its use in therapy and methods of treatment of anxiety and/or depression using it.
摘要翻译：本发明提供式I化合物或其N-氧化物或其药学上可接受的盐：其中X 1表示氢，卤素，C 1-6烷基，三氟甲基或C 1-6烷氧基; X 2表示氢或卤素; Z表示氢，卤素，氰基，氰基甲基，三氟甲基，硝基，羟基，羟基（C 1-6 - ）烷基，C 1-6烷氧基，C 1 C 1-6烷氧基（C 1-6）烷基，三氟甲氧基，三氟甲硫基，三氟甲磺酰基，甲酰基，C 2-6烷氧基羰基，氧代吡咯烷基或任选取代的芳基，杂芳基或杂芳基（C 1-6 - ）烷氧基; 且R 1表示芳基或杂芳基，其中任一个可以任选被取代; 包含它的药物组合物，其在治疗中的用途以及使用其治疗焦虑和/或抑郁症的方法。

10. 发明授权

US06867207B2 IL-5 inhibiting 6-azauracil derivatives 失效
标题翻译： IL-5抑制6-氮尿嘧啶衍生物
公开(公告)号：US06867207B2
公开(公告)日：2005-03-15
申请号：US09891888
申请日：2001-06-26
申请人： Jean Fernand Armand Lacrampe , Eddy Jean Edgard Freyne , Marc Gaston Venet , Gustaaf Maria Boeckx
发明人： Jean Fernand Armand Lacrampe , Eddy Jean Edgard Freyne , Marc Gaston Venet , Gustaaf Maria Boeckx
IPC分类号： A61P37/08 , C07D401/10 , C07D403/10 , C07D403/12 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D253/065 , A61K31/53 , A61K17/00
CPC分类号： C07D401/10 , C07D403/10 , C07D403/12 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14
摘要： The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, p and q are 0, 1, 2, 3 or 4 and q is also 5; X is O, S, NR3 or a direct bond; R1 is hydrogen, hydroxy, halo, optionally substituted amino, optionally substituted C1-6alkyl, C1-6alkyloxy, C3-7cycloalkyl or aryl; R2 is aryl, Het1, C3-7cycloalkyl, optionally substituted C1-6alkyl; and if X is O, S or NR3, then R2 may also be a carbonyl or thiocarbonyl linked substituent; R3 is hydrogen or C1-4alkyl; R4 and R5 independently are optionally substituted C1-6alkyl, halo, hydroxy, mercapto, C1-6alkyloxy, C1-6akylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6 or NR7R8; R6 is substituted sulfonyl or sulfinyl; R7 and R8 are hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R9 and R10 are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, carboxyl, C1-4alkyloxycarbonyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, aryl, aryloxy, arylcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3 and C(═O)Het3; R12 and R13 are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl and R6; aryl is optionally substituted phenyl; Het1, Het2 and Het3 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.
摘要翻译：本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐及其立体化学异构形式，p和q分别为0,1,2,3或4，q也为5; X是O，S，NR 3或直接键; R 1是氢，羟基，卤素，任选取代的氨基，任选取代的C 1-6烷基，C 1-6烷氧基，C 3-7环烷基或芳基; R 2是芳基，Het 1，C 3-7环烷基，任选取代的C 1-6烷基; 并且如果X是O，S或NR 3，则R 2也可以是羰基或硫代羰基连接的取代基; R 3是氢或C 1-4烷基; R 4和R 5独立地是任选取代的C 1-6烷基，卤素，羟基，巯基，C 1-6烷氧基，C 1-6烷硫基，C 1-6烷基羰基氧基，芳基，氰基，硝基，Het 3，或NR 7 R 8; R 6是取代的磺酰基或亚磺酰基; R 7和R 8是氢，任选取代的C 1-4烷基，芳基，羰基或硫代羰基连接的取代基，C 3-7环烷基，Het 3和R 6; R 9和R 10各自独立地选自氢，任选取代的C 1-4烷基，苯基，羰基或硫代羰基连接的取代基，C 3-7环烷基，Het 3和R 6; R 11是羟基，巯基，氰基，硝基，卤素，三卤代甲基，C 1-4烷氧基，羧基，C 1-4烷氧基羰基，三卤代C 1-4烷基磺酰氧基，R 6，NR 7 R 8，C（= O） NR 7 R 8，芳基，芳氧基，芳基羰基，C 3-7环烷基，C 3-7环烷氧基，邻苯二甲酰亚胺-2-基，Het 3和C（= O）Het 3; R 12和R 13各自独立地选自氢，任选取代的C 1-4烷基，苯基，羰基或硫代羰基连接的取代基，C 3-7环烷基和R 6; 芳基是任选取代的苯基; Het <1>，Het <

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