专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2009124965A1 PYRROLO[2,3-d]PYRIMIDIN-2-YL-AMINE DERIVATIVES AS PKC-THETA INHIBITORS 审中-公开
标题翻译：吡咯并[<我
公开(公告)号：WO2009124965A1
公开(公告)日：2009-10-15
申请号：PCT/EP2009/054209
申请日：2009-04-08
申请人： N.V. ORGANON , PHARMACOPEIA, LLC , ROUGHTON, Andrew Laird , HO, Koc-Kan , OHLMEYER, Michael , DILLER, David , NEAGU, Irina , KINGSBURY, Celia , CHAN, Jui-Hsiang , LOMMERSE, Johannes, Petrus, Maria , TEERHUIS, Neeltje, Miranda , WIJKMANS, Jacobus Cornelis Henricus Maria , PLATE, Ralf
发明人： ROUGHTON, Andrew Laird , HO, Koc-Kan , OHLMEYER, Michael , DILLER, David , NEAGU, Irina , KINGSBURY, Celia , CHAN, Jui-Hsiang , LOMMERSE, Johannes, Petrus, Maria , TEERHUIS, Neeltje, Miranda , WIJKMANS, Jacobus Cornelis Henricus Maria , PLATE, Ralf
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： The present invention relates to a pyrrolo[2,3-d]pyrimidin-2-yl-amine derivative according to formula (I) wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said pyrrolo[2,3-d]pyrimidine-2-ylamine derivatives and to their use in therapy, for instance in the treatment of PKCθ mediated disorders.
摘要翻译：本发明涉及式（I）的吡咯并[2,3-d]嘧啶-2-基 - 胺衍生物，其中变量如说明书中所定义，或其药学上可接受的盐或溶剂合物。本发明还涉及包含一种或多种所述吡咯并[2,3-d]嘧啶-2-基胺衍生物的药物组合物及其在治疗中的用途，例如用于治疗PKC？介导的疾病。

2. 发明申请

WO2008119918A1 MINERALOCORTICOID RECEPTOR ANTAGONISTS 审中-公开
标题翻译：矿物胆碱受体拮抗剂
公开(公告)号：WO2008119918A1
公开(公告)日：2008-10-09
申请号：PCT/GB2007/001141
申请日：2007-03-29
申请人： N.V. ORGANON , PEETERS, Bernardus, Wijnand, Mathys, Marie , GROEN, Marinus, Bernard , PLATE, Ralf
发明人： PEETERS, Bernardus, Wijnand, Mathys, Marie , GROEN, Marinus, Bernard , PLATE, Ralf
IPC分类号： A61K31/56 , C07J7/00 , A61P5/42
CPC分类号： C07J7/00 , A61K31/56 , Y02P20/582
摘要： Compounds of the formula (I) are provided having a steroid skeleton and substitution characteristics in the A and B rings of the steroid skeleton effective for mineralocorticoid receptor antagonism, and rings C and D of the steroid skeleton having substituents thereon according to formula (I), wherein R 1 is -OH or =O; R 2 is (C 1-3 )alkyl or (C 2- 3 )alkenyl; R 3 is selected from formulas (IIa), (IIb), (IIc).These compounds are useful in the treatment of inter alia aldosteronism, hypokalemia, hypertension, congestive heart failure, heart fibrosis, renal failure and restenosis.
摘要翻译：提供式（I）化合物，其具有类固醇骨架和在类固醇骨架的A环和B环中有效用于盐皮质激素受体拮抗作用的取代特性，并且具有根据式（I）的取代基的类固醇骨架的环C和D，其中R 1是-OH或= O; R 2是（C 1-3-3）烷基或（C 1 -C 3 - 3）链烯基; R III选自式（IIa），（IIb），（IIc）。这些化合物可用于治疗尤其是醛固酮增多症，低钾血症，高血压，充血性心力衰竭，心脏纤维化，肾衰竭和再狭窄。

3. 发明申请

WO2009027482A3 TSH RECEPTOR ANTAGONIZING TETRAHYDROQUINOLINE COMPOUNDS 审中-公开
公开(公告)号：WO2009027482A3
公开(公告)日：2009-03-05
申请号：PCT/EP2008/061325
申请日：2008-08-28
申请人： N.V. ORGANON , KARSTENS, Willem, Frederik, Johan , CONTI, Paolo, Giovanni, Martino , TIMMERS, Cornelis, Marius , PLATE, Ralf , VAN KOPPEN, Christianus, Johannes
发明人： KARSTENS, Willem, Frederik, Johan , CONTI, Paolo, Giovanni, Martino , TIMMERS, Cornelis, Marius , PLATE, Ralf , VAN KOPPEN, Christianus, Johannes
IPC分类号： A61K31/47 , A61P5/08 , C07D215/38
摘要： The present invention relates the use of a compound, a pharmaceutical composition, compounds and a kit for treating or preventing disorders in a mammal responsive to TSH receptor mediated pathways, including disorders such as hyperthyroidism, Graves' disease, Graves Ophthalmopathy, Graves' associated pretibial dermopathy, nodular goitre and thyroid cancer comprising administering to said mammal an effective amount of a tetrahydroquinoline compound of Formula (I) or an pharmaceutically acceptable salt thereof.

4. 发明申请

WO2006084917A1 NON STEROIDAL GLUCOCORTICOID RECEPTOR MODULATORS 审中-公开
标题翻译：非离子葡萄糖激素受体调节剂
公开(公告)号：WO2006084917A1
公开(公告)日：2006-08-17
申请号：PCT/EP2006/050906
申请日：2006-02-14
申请人： AKZO NOBEL N.V. , PLATE, Ralf , ZAMAN, Guido, Jenny, Rudolf , HERMKENS, Pedro, Harold, Han , JANS, Christiaan, Gerardus, Johannes, Maria , BUIJSMAN,, Rogier, Christian , MAN, Adrianus, Petrus, Antonius , CONTI, Paolo, Giovanni, Martino , LUSHER, Scott, James , DOKTER, Willem, Hendrik, Abraham
发明人： PLATE, Ralf , ZAMAN, Guido, Jenny, Rudolf , HERMKENS, Pedro, Harold, Han , JANS, Christiaan, Gerardus, Johannes, Maria , BUIJSMAN,, Rogier, Christian , MAN, Adrianus, Petrus, Antonius , CONTI, Paolo, Giovanni, Martino , LUSHER, Scott, James , DOKTER, Willem, Hendrik, Abraham
IPC分类号： C07D471/04 , A61K31/551 , A61P29/00
CPC分类号： C07D471/04
摘要： The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof. In this formula R 1 is H or (1-4C)alkyl; R 2 is -C(O)R 15 or -S(O)2R 15 ; R 3 is H, (1-4C)alkyl or -OR 16 ; R 4 is H, (1-4C)alkyl or -OR 16 ; R 6 is H or -C(H)NOR 16 ; R 7 is H or halogen, cyano; (1-6C)alkyl, (2-6C)alkenyl or (2- 6C)alkynyl, all three optionally substituted with OH, halogen or NH 2 ;-C(H)NOR 16 , - OR 16 , -C(O)R 16 , or -C(O)OR 16 ; R 8 is H, cyano, halogen, nitro; (1-6C) alkyl, (2- 6C)alkenyl, (2-6C)alkynyl or -O(1-6C)alkyl, all optionally substituted with amino, hydroxyl or halogen; (hetero)aryl, optionally substituted with cyano, halogen, (1- 4C)alkyl, (1-4C)alkoxy, (1-4C)alkoxy(1-4C)alkyl; -C(O)R 18 , -C(O)OR 19 , -C(O)NHR 17 , -NHC(O)R 20 , -C(1-4C)alkylNOR 21 ; -C(H)NOR 16 , or -NHS(O) 2 R 21 ; R 9 is H, halogen, cyano or (1-4C)alkyl optionally substituted with halogen; R 10 is H or (1-4C)alkyl; R 11 is H; R 12 is H, cyano or (1-4C)alkyl; R 13 is H, (1-4C)alkyl, halogen or formyl; R 14 is H, halogen, cyano, (1-4C)alkyl, (2-6C)alkenyl, C(O)R 21 or (hetero)aryl; R 15 is H; (1- 6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl,-O(2-6C)alkyl, -O(2-6C)alkenyl or -O(2- 6C)alkynyl, all optionally substituted with one or more OH, halogen, cyano or (hetero)aryl, (hetero)aryl, optionally substituted with (1-4C)alkyl, halogen, cyano, nitro or amino, NH2, (di)(1-4C)alkylamino, (1-4C)alkyl(1-4C)alkoxyamine, (1- 4C)alkylt hio(1-4C)alkyl or (1-4C)alkoxy(1-4C)alkyl; R 16 is H, (1-6C)alkyl, (2- 6C)alkenyl or (2-6C)alkynyl; R 17 is H, (1-6C)alkyl, optionally substituted with halogen, (1-4C)alkoxy or (hetero)aryl, optionally substituted with halogen, (1-4C)alkyl or (1- 25 4C)alkoxy; (3-6C)cycloalkyl or (hetero)aryl, optio nally substituted with halogen, (1- 4C)alkyl or (1-4C)alkoxy; R 18 is H, NH2, C(O)R 21 or (1-4C)alkyl, optionally substituted with OH, halogen, cyano or -S(1-4C)alkyl; R 19 is H or (1-6C)alkyl, optionally substituted with OH or halogen; R 20 is H, (1-6C)alkyl or (2-6C)alkenyl, both optionally substituted by halogen, O(1-6C)alkyl, (hetero)aryl, optionally substituted with (1- 4C)alkyl or halogen; (3-6C)cycloalkyl; (1-6C)alkoxy; (1-6C)alkenyloxy; or (hetero)aryl, optionally subst ituted with (1-4C)alkyl); NH2, -NH(1-6C)alkyl or -NH(hetero)aryl and R21 is H or (1-6C)alkyl. The present invention also relates to pharmaceutical compositions comprising said compounds and the use of these derivatives to modulate glucocorticoid receptor activity.
摘要翻译：本发明涉及具有通式（I）的化合物或其药学上可接受的盐。在该式中R 1是H或（1-4C）烷基; R 2是-C（O）R 15或-S（O）2 R 15; R 3是H，（1-4C）烷基或-OR 16; R 4是H，（1-4C）烷基或-OR 16; R 6是H或-C（H）NOR 16; R 7是H或卤素，氰基; （1-6C）烷基，（2-6C）烯基或（2- 6C）炔基，全部三个任选被OH，卤素或NH 2 -C（= H）NOR 16取代 -C（O）R 16或-C（O）OR 16;或-C（O）OR 16。 R 8是H，氰基，卤素，硝基; （1-6C）烷基，（2-6C）烯基，（2-6C）炔基或-O（1-6C）烷基，全部任选被氨基，羟基或卤素取代; （1-4C）烷氧基，（1-4C）烷氧基（1-4C）烷基，（1-4C）烷氧基， -C（O）R 18，-C（O）OR 19，-C（O）NHR 17，-NHC（O） R 20，-C（1-4C）烷基-NOR 21; -C（H）NOR 16或-NHS（O）2 R 21; R 9是H，卤素，氰基或任选被卤素取代的（1-4C）烷基; R 10是H或（1-4C）烷基; R 11是H; R 12是H，氰基或（1-4C）烷基; R 13是H，（1-4C）烷基，卤素或甲酰基; R 14是H，卤素，氰基，（1-4C）烷基，（2-6C）烯基，C（O）R 21或（杂）芳基; R 15是H; （1-6C）烷基，（2-6C）烯基，（2-6C）炔基，-O（2-6C）烷基，-O（2-6C）烯基或-O（2-6C）炔基，被一个或多个OH，卤素，氰基或（杂）芳基，（杂）芳基取代，任选被（1-4C）烷基，卤素，氰基，硝基或氨基，NH 2，（二）（1-4C）烷基氨基，（1-4C）烷基（1-4C）烷氧基胺，（1-4C）烷基硫代（1-4C）烷基或（1-4C）烷氧基（1-4C）烷基; R 16是H，（1-6C）烷基，（2- 6C）烯基或（2-6C）炔基; R 17是H，（1-6C）烷基，任选被卤素取代，（1-4C）烷氧基或（杂）芳基，任选被卤素，（1-4C）烷基或（1） 25 4C）烷氧基; （3-6C）环烷基或（卤素）取代的（杂）芳基，（1-4C）烷基或（1-4C）烷氧基; R 18是H，NH 2，C（O）R 21或（1-4C）烷基，任选被OH，卤素，氰基或-S（1-4C））烷基; R 19是H或（1-6C）烷基，任选被OH或卤素取代; R 20是H，（1-6C）烷基或（2-6C）烯基，其任选被卤素取代，O（1-6C）烷基，（杂）芳基，任选被（1 4C）烷基或卤素; （3-6C）环烷基; （1-6C）烷氧基; （1-6C）链烯氧基; 或（杂）芳基，任选被（1-4C）烷基取代）; NH 2，-NH（1-6C）烷基或-NH（杂）芳基，R 21是H或（1-6C）烷基。本发明还涉及包含所述化合物的药物组合物和这些衍生物用于调节糖皮质激素受体活性的用途。

5. 发明申请

WO2007025938A1 NON-STEROIDAL COMPOUNDS USEFUL AS GLUCOCORTICOID RECEPTOR MODULATORS 审中-公开
标题翻译：非甾体化合物作为葡萄糖激素受体调节剂有用
公开(公告)号：WO2007025938A1
公开(公告)日：2007-03-08
申请号：PCT/EP2006/065696
申请日：2006-08-25
申请人： AKZO NOBEL N.V. , PLATE, Ralf , JANS, Christiaan, Gerardus, Johannes, Maria
发明人： PLATE, Ralf , JANS, Christiaan, Gerardus, Johannes, Maria
IPC分类号： C07D471/04 , A61K31/55 , A61P29/00 , A61P5/44
CPC分类号： C07D471/04
摘要： This invention relates to novel amino acid derivatives of formula (I) wherein the R groups have the following meanings: -R 1 is -H or -(1-4C)alkyl; -R 2 is -C(O)R 15 or -S(O) 2 R 15 ; -R 3 is -H, -(1-4C)alkyl or -OR 16 ; -R 4 is -H, -(1-4C)alkyl or -OR 16 ; -R 6 is -H or -C(R 16 )NOR 16 ; -R 7 is -H, -halogen, -cyano; -(1-6C)alkyl, -(2-6C)alkenyl or -(2-6C)alkynyl, all optionally substituted with -amino, -hydroxyl or -halogen; -R 8 is -H, -cyano, -halogen, -nitro; -(1-6C)alkyl, -(2-6C)alkenyl, -(2-6C)alkynyl or -O(l-6C)alkyl, all optionally substituted with -amino, -hydroxyl or -halogen; -(hetero)aryl, optionally substituted with -cyano, -halogen, -(1-4C)alkyl, -(1-4C)alkoxy, -(l-4C)alkoxy(l- 4C)alkyl or -(hetero)aryl; -C(R 16 )NOR 16 ; -C(O)N(R 17 ) 2 ; -C(O)R18, -C(O)OR 19 , -NHC(O)R 20 , or -NHS(O) 2 R 21 ; -R 9 is -H, -halogen, -cyano, or -(1-4C)alkyl, optionally substituted with -halogen; -R 10 is -H or -(1-4C)alkyl; -R 11 is -H; -R 12 is -H, -cyano or - (1-4C)alkyl; -R 13 is -H, -(1-4C)alkyl, -halogen or -formyl; -R 14 is -H, -halogen, -cyano, -(1-4C)a!kyl or -(hetero)aryl; or a pharmaceutically acceptable salt thereof. The compounds of this invention are highly specific for the glucocorticoid receptor and may be used for treating inflammatory diseases.
摘要翻译：本发明涉及式（I）的新型氨基酸衍生物，其中R基具有以下含义：-R 1是-H或 - （1-4C）烷基; -R 2是-C（O）R 15或-S（O）2 R 15; -R 3是-H， - （1-4C）烷基或-OR 16; -R 4是-H， - （1-4C）烷基或-OR 16; -R 6是-H或-C（R 16）NOR 16; -R 7是-H， - 卤素， - 氰基; - （1-6C）烷基， - （2-6C）烯基或 - （2-6C）炔基，全部被氨基，羟基或卤素取代; -R 8是-H， - 氰基， - 卤素， - 硝基; - （1-6C）烷基， - （2-6C）烯基， - （2-6C）炔基或-O（1-6C）烷基，全部任选被 - 氨基， - 羟基或卤素取代; - （1-4）烷氧基， - （1-4C）烷氧基，（1-4C）烷基或 - （杂）芳基， ; -C（R _{16 ）NOR _{16 ; -C（O）N（R _{17 ）_{2 ; -C（O）R 18，-C（O）OR 19，-NHC（O）R 20或-NHS（O）2 - [R _{21 ; -R 9是-H， - 卤素， - 氰基或 - （1-4C）烷基，任选被卤素取代; -R 10是-H或 - （1-4C）烷基; -R 11是-H; -R 12是-H， - 氰基或 - （1-4C）烷基; -R 13是-H， - （1-4C）烷基， - 卤素或 - 甲酰基; -R 14是-H， - 卤素， - 氰基， - （1-4C）烷基或 - （杂）芳基; 或其药学上可接受的盐。本发明化合物对糖皮质激素受体高度特异，可用于治疗炎性疾病。}}}}}

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式