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1. 发明申请

US20050113373A1 Sulfonyl-Derivatives as novel inhibitors of histone deacetylase 有权
标题翻译：磺酰衍生物作为组蛋白脱乙酰酶的新型抑制剂
公开(公告)号：US20050113373A1
公开(公告)日：2005-05-26
申请号：US10507708
申请日：2003-03-11
申请人： Kristof Van Emelen , Janine Arts , Leo Backx , Hans De Winter , Sven Van Brandt , Marc Verdonck , Lieven Meerpoel , Isabelle Pilatte , Virginie Poncelet , Alexey Dyatkin
发明人： Kristof Van Emelen , Janine Arts , Leo Backx , Hans De Winter , Sven Van Brandt , Marc Verdonck , Lieven Meerpoel , Isabelle Pilatte , Virginie Poncelet , Alexey Dyatkin
IPC分类号： C07D249/12 , A61K31/40 , A61K31/438 , A61K31/4427 , A61K31/445 , A61K31/4545 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/517 , A61K31/52 , A61K31/53 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K45/00 , A61P1/04 , A61P3/10 , A61P5/00 , A61P9/00 , A61P9/02 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/08 , A61P13/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/04 , A61P17/06 , A61P17/10 , A61P17/14 , A61P17/16 , A61P19/02 , A61P19/06 , A61P21/04 , A61P25/00 , A61P25/16 , A61P25/28 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07D20060101 , C07D207/09 , C07D207/14 , C07D207/28 , C07D211/26 , C07D211/58 , C07D213/74 , C07D213/78 , C07D213/82 , C07D215/36 , C07D217/02 , C07D217/04 , C07D233/34 , C07D233/64 , C07D233/84 , C07D233/90 , C07D237/24 , C07D239/42 , C07D239/48 , C07D241/04 , C07D241/24 , C07D241/26 , C07D243/08 , C07D261/10 , C07D295/14 , C07D295/155 , C07D295/20 , C07D295/22 , C07D295/26 , C07D307/68 , C07D307/79 , C07D317/58 , C07D333/34 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/02 , C07D413/04 , C07D413/12 , C07D471/10 , C07D487/08 , C07D513/04 , C12Q1/48 , C07D41/02 , C07D43/02
CPC分类号： C07D413/12 , A61K31/40 , A61K31/402 , A61K31/435 , A61K31/4427 , A61K31/454 , A61K31/4545 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D207/09 , C07D207/14 , C07D207/277 , C07D207/28 , C07D211/14 , C07D211/58 , C07D213/78 , C07D213/81 , C07D213/82 , C07D217/02 , C07D217/04 , C07D217/16 , C07D233/90 , C07D239/42 , C07D241/04 , C07D241/24 , C07D243/08 , C07D261/10 , C07D295/155 , C07D295/22 , C07D295/26 , C07D307/68 , C07D307/79 , C07D333/34 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D471/10 , C07D513/04 , C12Q1/34 , C12Q1/48 , G01N33/573 , G01N2333/91
摘要： This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括新的式（I）化合物，其中n，m，t，R 1，R 2，R 3，R 3，具有组氨酸脱乙酰酶抑制酶活性的含义; 其制剂，含有它们的组合物及其作为药物的用途。

2. 发明申请

US20080108601A1 Sulfonyl-Derivatives as Novel Inhibitors or Histone Deacetylase 有权
标题翻译：磺酰衍生物作为新型抑制剂或组蛋白脱乙酰酶
公开(公告)号：US20080108601A1
公开(公告)日：2008-05-08
申请号：US11926759
申请日：2007-10-29
申请人： Kristof Van Emelen , Janine Arts , Leo-Jacobus Backx , Hans De Winter , Sven Van Brandt , Marc Verdonck , Lieven Meerpoel , Isabelle Pilatte , Virginie Poncelet , Alexey Dyatkin , Jimmy Van heusden
发明人： Kristof Van Emelen , Janine Arts , Leo-Jacobus Backx , Hans De Winter , Sven Van Brandt , Marc Verdonck , Lieven Meerpoel , Isabelle Pilatte , Virginie Poncelet , Alexey Dyatkin , Jimmy Van heusden
IPC分类号： A61K31/551 , A61K31/495 , A61K31/501 , C07D241/04 , C07D403/04 , C12Q1/00 , C07D413/14 , C07D243/08 , A61K31/506 , A61K31/5355
CPC分类号： C07D413/12 , A61K31/40 , A61K31/402 , A61K31/435 , A61K31/4427 , A61K31/454 , A61K31/4545 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D207/09 , C07D207/14 , C07D207/277 , C07D207/28 , C07D211/14 , C07D211/58 , C07D213/78 , C07D213/81 , C07D213/82 , C07D217/02 , C07D217/04 , C07D217/16 , C07D233/90 , C07D239/42 , C07D241/04 , C07D241/24 , C07D243/08 , C07D261/10 , C07D295/155 , C07D295/22 , C07D295/26 , C07D307/68 , C07D307/79 , C07D333/34 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D471/10 , C07D513/04 , C12Q1/34 , C12Q1/48 , G01N33/573 , G01N2333/91
摘要： This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括新的式（I）化合物，其中n，m，t，R 1，R 2，R 3，R 3，具有组氨酸脱乙酰酶抑制酶活性的含义; 其制剂，含有它们的组合物及其作为药物的用途。

3. 发明申请

US20070142393A1 SULFONYL-DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE 有权
标题翻译：磺酰衍生物作为HISTONE脱乙酰壳多糖的新型抑制剂
公开(公告)号：US20070142393A1
公开(公告)日：2007-06-21
申请号：US11668906
申请日：2007-01-30
申请人： Kristof Emelen , Janine Arts , Leo Backx , Hans De Winter , Sven Van Brandt , Marc Verdonck , Lieven Meerpoel , Isabelle Pilatte , Virginie Poncelet , Alexey Dyatkin , Jimmy Van heusden
发明人： Kristof Emelen , Janine Arts , Leo Backx , Hans De Winter , Sven Van Brandt , Marc Verdonck , Lieven Meerpoel , Isabelle Pilatte , Virginie Poncelet , Alexey Dyatkin , Jimmy Van heusden
IPC分类号： A61K31/506 , C07D403/04
CPC分类号： C07D413/12 , A61K31/40 , A61K31/402 , A61K31/435 , A61K31/4427 , A61K31/454 , A61K31/4545 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D207/09 , C07D207/14 , C07D207/277 , C07D207/28 , C07D211/14 , C07D211/58 , C07D213/78 , C07D213/81 , C07D213/82 , C07D217/02 , C07D217/04 , C07D217/16 , C07D233/90 , C07D239/42 , C07D241/04 , C07D241/24 , C07D243/08 , C07D261/10 , C07D295/155 , C07D295/22 , C07D295/26 , C07D307/68 , C07D307/79 , C07D333/34 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D471/10 , C07D513/04 , C12Q1/34 , C12Q1/48 , G01N33/573 , G01N2333/91
摘要： This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括新的式（I）化合物，其中n，m，t，R 1，R 2，R 3，R 3，具有组氨酸脱乙酰酶抑制酶活性的含义; 其制剂，含有它们的组合物及其作为药物的用途。

4. 发明申请

US20050171347A1 Sulfonylamino-derivatives as novel inhibitors of histone deacetylase 有权
标题翻译：磺酰氨基衍生物作为组蛋白脱乙酰酶的新型抑制剂
公开(公告)号：US20050171347A1
公开(公告)日：2005-08-04
申请号：US10507159
申请日：2003-03-11
申请人： Kristof Emelen , Leo Backx , Sven Van Brandt , Patrick Angibaud , Isabelle Noelle Pilatte , Marc Gustaaf Verdonck , Hans De Winter
发明人： Kristof Emelen , Leo Backx , Sven Van Brandt , Patrick Angibaud , Isabelle Noelle Pilatte , Marc Gustaaf Verdonck , Hans De Winter
IPC分类号： C07D239/42 , A61K31/40 , A61K31/4025 , A61K31/438 , A61K31/4427 , A61K31/445 , A61K31/451 , A61K31/4545 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/517 , A61K31/53 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K45/00 , A61P1/04 , A61P1/18 , A61P3/10 , A61P5/00 , A61P9/00 , A61P9/02 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/08 , A61P13/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/04 , A61P17/06 , A61P17/10 , A61P17/14 , A61P17/16 , A61P19/00 , A61P19/02 , A61P19/06 , A61P21/04 , A61P25/00 , A61P25/16 , A61P25/28 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07D207/09 , C07D207/14 , C07D211/26 , C07D211/58 , C07D213/74 , C07D213/78 , C07D217/02 , C07D217/04 , C07D241/04 , C07D249/12 , C07D295/14 , C07D295/155 , C07D295/20 , C07D295/22 , C07D295/26 , C07D307/68 , C07D317/58 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/02 , C07D413/04 , C07D413/12 , C07D471/10 , C12Q1/48 , C07D43/04
CPC分类号： C07D413/12 , A61K31/40 , A61K31/402 , A61K31/435 , A61K31/4427 , A61K31/454 , A61K31/4545 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D207/09 , C07D207/14 , C07D211/14 , C07D211/58 , C07D213/78 , C07D217/02 , C07D217/04 , C07D217/16 , C07D239/42 , C07D295/155 , C07D295/26 , C07D307/68 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/04 , C07D471/04 , C07D471/10 , C07D513/04 , C12Q1/34 , C12Q1/48
摘要： This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括新的式（I）化合物，其中n，m，t，R 1，R 2，R 3，R 3，具有组蛋白脱乙酰酶抑制酶活性的含义，具有定义的含义; 其制剂，含有它们的组合物及其作为药物的用途。

5. 发明申请

US20080108653A1 TRIPEPTIDYL PEPTIDASE INHIBITORS 有权
标题翻译： TRIPEPTIDYL肽抑制剂
公开(公告)号：US20080108653A1
公开(公告)日：2008-05-08
申请号：US11928273
申请日：2007-10-30
申请人： Henry Breslin , Hans De Winter , Michael Kukla
发明人： Henry Breslin , Hans De Winter , Michael Kukla
IPC分类号： A61K31/4725 , A61K31/4178 , A61K31/4184 , C07D401/04 , C07D417/04 , C07D403/04 , A61K31/427 , A61K31/4709
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. wherein n is an integer 0 or 1; X represents O; S; or —(CR4R5)m— wherein m is an integer 1 or 2; R4 and R5 are each independently from each other hydrogen or C1-4alkyl; R1 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; R2 is an optionally substituted 5-membered heterocycle, or R2 is optionally substituted benzimidazole; R3 is a bivalent radical —CH2CH2— optionally substituted with halo or phenylmethyl; or R3 is a bivalent radical of formula
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肿（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。其中n为整数0或1; X表示O; S; 或 - （CR 4）5 其中m是整数1或2; R 4和R 5各自彼此独立地为氢或C 1-4烷基; R 1是任选被羟基取代的C 1-6烷基羰基; C 1-6烷氧基羰基; 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; C 1-6烷基羰基氧基C 1-6烷基羰基; 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C 1-6烷基; 或芳基羰基; R 2是任选取代的5元杂环，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是式的二价基团

6. 发明申请

US20060276509A1 Tripeptidyl peptidase inhibitors 审中-公开
标题翻译：三肽基肽酶抑制剂
公开(公告)号：US20060276509A1
公开(公告)日：2006-12-07
申请号：US11499937
申请日：2006-08-07
申请人： Henry Breslin , Hans De Winter , Michael Kukla
发明人： Henry Breslin , Hans De Winter , Michael Kukla
IPC分类号： A61K31/454 , A61K31/426 , A61K31/427 , A61K31/4245 , A61K31/422 , A61K31/4178 , A61K31/4196 , A61K31/4025 , C07D417/04 , C07D403/04 , C07D413/04
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. wherein n is an integer 0 or 1; X represents O; S; or —(CR4R5)m— wherein m is an integer 1 or 2; R4 and R5 are each independently from each other hydrogen or C1-4alkyl; R1 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; R2 is an optionally substituted 5-membered heterocycle, or R2 is optionally substituted benzimidazole; R3 is a bivalent radical —CH2CH2— optionally substituted with halo or phenylmethyl; or R3 is a bivalent radical of formula
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肿（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。其中n为整数0或1; X表示O; S; 或 - （CR 4）5 其中m是整数1或2; R 4和R 5各自彼此独立地为氢或C 1-4烷基; R 1是任选被羟基取代的C 1-6烷基羰基; C 1-6烷氧基羰基; 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; C 1-6烷基羰基氧基C 1-6烷基羰基; 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C 1-6烷基; 或芳基羰基; R 2是任选取代的5元杂环，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是式的二价基团

7. 发明授权

US07932261B2 Macrocycle derivatives useful as inhibitors of β-secretase (BACE) 有权
标题翻译：可用作分泌抑制剂（BACE）的大分子衍生物
公开(公告)号：US07932261B2
公开(公告)日：2011-04-26
申请号：US11671732
申请日：2007-02-06
申请人： Ellen W. Baxter , François P. Bischoff , Hans De Winter , Chih Yung Ho , Yifang Huang , Michael H. Parker , Allen B. Reitz , Charles H. Reynolds , Eric D. Strobel
发明人： Ellen W. Baxter , François P. Bischoff , Hans De Winter , Chih Yung Ho , Yifang Huang , Michael H. Parker , Allen B. Reitz , Charles H. Reynolds , Eric D. Strobel
IPC分类号： C07D487/04 , A61K31/517
CPC分类号： C07D498/08 , C07D487/08
摘要： The present invention is directed to macrocycle 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 β-secretase, also known as β-site cleaving enzyme and BACE, BACE1, Asp2 and memapsin2.
摘要翻译：本发明涉及大环衍生物，含有它们的药物组合物及其在治疗阿尔茨海默病（AD）和相关疾病中的用途。本发明的化合物是分泌酶抑制剂，也被称为“切割酶”和BACE，BACE1，Asp2和memapsin2。

8. 发明申请

US20060079687A1 Novel 2-amino-quinazoline derivatives useful as inhibitors of beta-secretase (BACE) 有权
标题翻译：可用作β-分泌酶（BACE）抑制剂的新型2-氨基 - 喹唑啉衍生物
公开(公告)号：US20060079687A1
公开(公告)日：2006-04-13
申请号：US11197669
申请日：2005-08-04
申请人： Ellen Baxter , Francois Bischoff , Robert Boyd , Mirielle Braeken , Steve Coats , Yifang Huang , Alfonzo Jordan , Chi Luo , Marc Mercken , Serge Maria Pieters , Allen Reitz , Charles Reynolds , Tina Ross , Brett Tounge , Mark Schulz , Hans De Winter
发明人： Ellen Baxter , Francois Bischoff , Robert Boyd , Mirielle Braeken , Steve Coats , Yifang Huang , Alfonzo Jordan , Chi Luo , Marc Mercken , Serge Maria Pieters , Allen Reitz , Charles Reynolds , Tina Ross , Brett Tounge , Mark Schulz , Hans De Winter
IPC分类号： C07D239/84 , C07D403/02
CPC分类号： C07D413/06 , C07D239/84 , C07D401/06 , C07D403/06 , C07D403/12 , C07D405/06
摘要： The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline 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 β-secretase, also known as β-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β-分泌酶的抑制剂，也称为β-位点切割酶和BACE。

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