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1. 发明申请

WO0236116A9 TRIPEPTIDYL PEPTIDASE INHIBITORS 审中-公开
标题翻译： TRIPEPTIDYL肽抑制剂
公开(公告)号：WO0236116A9
公开(公告)日：2003-05-30
申请号：PCT/EP0112388
申请日：2001-10-24
申请人： JANSSEN PHARMACEUTICA NV , BRESLIN HENRY JOSEPH , DE WINTER HANS LOUIS JOS , KUKLA MICHAEL JOSEPH
发明人： BRESLIN HENRY JOSEPH , DE WINTER HANS LOUIS JOS , KUKLA MICHAEL JOSEPH
IPC分类号： A61K31/4178 , A61K31/4184 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61P1/00 , A61P3/04 , A61P25/18 , A61P43/00 , C07D233/64 , C07D401/04 , C07D403/04 , C07D403/12 , C07D403/14 , C07D413/04 , C07D417/04 , A61K31/404 , A61K31/422 , A61K31/47
CPC分类号： C07D401/04 , C07D403/04 , C07D403/12 , C07D413/04 , C07D417/04
摘要： The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds. (I) wherein n is an integer (0) or (1); X represents O; S; or -(CR R )m- wherein m is an integer (1) or (2); R and R are each independently from each other hydrogen or C1-4alkyl; R is C1-6alkylcarbonyl optionally substituted with hydroxy; C1-6alkyloxycarbonyl; aminoC1-6alkylcarbonyl wherein the C1-6alkyl group is optionally substituted with C3-6cycloalkyl; mono- and di(C1-4alkyl)aminoC1-6alkylcarbonyl; aminocarbonyl substituted with aryl; C1-6alkylcarbonyloxyC1-6alkylcarbonyl; C1-6alkyloxycarbonylaminoC1-6alkylcarbonyl wherein the amino group is optionally substituted with C1-4alkyl; an amino acid; C1-6alkyl substituted with amino; or arylcarbonyl; R is an optionally substituted (5)-membered heterocycle, or R is optionally substituted benzimidazole; R is a bivalent radical -CH2CH2- optionally substituted with halo or phenylmethyl; or R is a bivalent radical of formula (II).
摘要翻译：本发明涉及新型的式（I）化合物，其是负责灭活内源性神经肽如缩胆囊壶菌（CCKs）的膜三肽基肽酶的抑制剂。本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及用作所述化合物的药物。（I）其中n为整数（0）或（1）; X表示O; S; 或 - （CR 4 R 5）m - ，其中m是整数（1）或（2）; R 4和R 5各自独立地为氢或C 1-4烷基; R 1是任选被羟基取代的C 1-6烷基羰基; C1-6alkyloxycarbonyl; 氨基C 1-6烷基羰基，其中C 1-6烷基任选被C 3-6环烷基取代; 单和二（C 1-4烷基）氨基C 1-6烷基羰基; 被芳基取代的氨基羰基; C1-6alkylcarbonyloxyC1-6alkylcarbonyl; C 1-6烷氧基羰基氨基C 1-6烷基羰基，其中氨基任选被C 1-4烷基取代; 氨基酸; 被氨基取代的C1-6烷基; 或芳基羰基; R 2是任选取代的（5）表示的杂环，或R 2是任选取代的苯并咪唑; R 3是任选被卤素或苯基甲基取代的二价基团-CH 2 CH 2; 或R 3是式（II）的二价基团。

2. 发明申请

WO2006017836A3 2-AMINO-QUINAZOLINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) 审中-公开
标题翻译：用作β-分泌酶（BACE）抑制剂的2-氨基喹唑啉衍生物
公开(公告)号：WO2006017836A3
公开(公告)日：2006-06-29
申请号：PCT/US2005028191
申请日：2005-08-08
申请人： JANSSEN PHARMACEUTICA NV , BAXTER ELLEN , BISCHOFF FRANCOIS PAUL , BOYD ROBERT , BRAEKEN MIRIELLE , COATS STEVEN , HUANG YIFANG , JORDAN ALFONZO , LUO CHI , MERCKEN MARC HUBERT , REYNOLDS CHARLES H , ROSS TINA MORGAN , TOUNGE BRETT A , SCHULZ MARK , DE WINTER HANS LOUIS JOS , PIETERS SERGE MARIA ALOYSIUS , REITZ ALLEN B
发明人： BAXTER ELLEN , BISCHOFF FRANCOIS PAUL , BOYD ROBERT , BRAEKEN MIRIELLE , COATS STEVEN , HUANG YIFANG , JORDAN ALFONZO , LUO CHI , MERCKEN MARC HUBERT , REYNOLDS CHARLES H , ROSS TINA MORGAN , TOUNGE BRETT A , SCHULZ MARK , DE WINTER HANS LOUIS JOS , PIETERS SERGE MARIA ALOYSIUS , REITZ ALLEN B
IPC分类号： C07D239/84 , A61K31/517 , A61P25/28
CPC分类号： C07D239/84 , C07D401/04 , C07D401/06 , C07D403/06 , C07D405/06 , C07D413/06 , C07H15/26
摘要： The present invention is directed to novel 2-amino-3, 4-dihydroquinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of P-secretase, also known as n-site cleaving enzyme and BACE.
摘要翻译：本发明涉及新的2-氨基-3,4-二氢喹唑啉衍生物，含有它们的药物组合物及其在治疗阿尔茨海默病（AD）和相关病症中的用途。本发明的化合物是P-分泌酶的抑制剂，也称为n-位切割酶和BACE。

4. 发明专利

CY1111086T1 ΠΑΡΑΓΩΓΑ 2-ΑΜΙΝΟ-ΚΙΝΑΖΟΛΙΝΗΣ ΧΡΗΣΙΜΑ ΩΣ ΑΝΑΣΤΟΛΕΙΣ ΤΗΣ ΒΗΤΑ-ΣΕΚΡΕΤΑΣΗΣ (BACE) 未知
公开(公告)号：CY1111086T1
公开(公告)日：2015-06-11
申请号：CY111100022
申请日：2011-01-04
申请人： JANSSEN PHARMACEUTICA NV
发明人： BAXTER ELLEN , BISCHOFF FRANCOIS PAUL , BOYD ROBERT , BRAEKEN MIRIELLE , COATS STEVEN , HUANG YIFANG , JORDAN ALFONZO , LUO CHI , MERCKEN MARC HUBERT , REYNOLDS CHARLES H , ROSS TINA MORGAN , TOUNGE BRETT A , SCHULZ MARK , DE WINTER HANS LOUIS JOS , PIETERS SERGE MARIA ALOYSIUS , REITZ ALLEN B
IPC分类号： C07D239/84 , A61K31/517 , A61P25/28
摘要： Ηπαρούσαεφεύρεσηαναφέρεταισεκαινούργιαπαράγωγατου 2-amino-3, 4-dihydroquinazoline, φαρμακευτικέςσυνθέσειςπουτιςπεριέχουνκαιτηχρήσητουςστηνθεραπευτικήαντιμετώπισητηςνόσουτου Alzheimer (AD) καισυγγενώνπαθήσεων. Οιχημικέςενώσειςτηςεφεύρεσηςείναιαναστολείςτης P-secretase, επίσηςγνωστήωςένζυμοδιχοτόμησηςστηθέση-n ήκαι BACE.

5. 发明专利

HU0302770A2 TRIPEPTIDYL PEPTIDASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知
公开(公告)号：HU0302770A2
公开(公告)日：2003-12-29
申请号：HU0302770
申请日：2001-10-24
申请人： JANSSEN PHARMACEUTICA NV
发明人： BRESLIN HENRY JOSEPH , KUKLA MICHAEL JOSEPH , DE WINTER HANS LOUIS JOS
IPC分类号： A61K31/4178 , A61K31/4184 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61P1/00 , A61P3/04 , A61P25/18 , A61P43/00 , C07D233/64 , C07D401/04 , C07D403/04 , C07D403/12 , C07D403/14 , C07D413/04 , C07D417/04 , A61K31/404
摘要： The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs).

10. 发明专利

SI1789398T1 2-AMINO-KINAZOLINSKI DERIVATI, UPORABNI KOT INHIBITORJI B-SEKRETAZE (BACE) 未知
公开(公告)号：SI1789398T1
公开(公告)日：2011-01-31
申请号：SI200531176
申请日：2005-08-08
申请人： JANSSEN PHARMACEUTICA NV
发明人： BISHOFF FRANCOIS PAUL , BRAEKEN MIRIELLE , PIETERS SERGE MARIA ALOYSIUS , MERCKEN MARC HUBERT , DE WINTER HANS LOUIS JOS , BERTHELOT DIEDER JEAN-CLAUDE
IPC分类号： C07D239/00 , A61K31/00 , A61P25/00

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