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11. 发明申请

US20070259898A1 NOVEL 2-AMINO-3,4-DIHYDRO-PYRIDO[3,4-D]PYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF beta-SECRETASE (BACE) 有权
标题翻译：新型2-氨基-3,4-二氢吡啶并[3,4-D]吡啶衍生物作为β-分泌酶（BACE）的抑制剂有用
公开(公告)号：US20070259898A1
公开(公告)日：2007-11-08
申请号：US11552792
申请日：2006-10-25
申请人： Ellen Baxter , Christopher Creighton , Yifang Huang , Chi Luo , Michael Parker , Allen Reitz , Charles Reynolds , Tina Ross , Eric Strobel , Brett Tounge
发明人： Ellen Baxter , Christopher Creighton , Yifang Huang , Chi Luo , Michael Parker , Allen Reitz , Charles Reynolds , Tina Ross , Eric Strobel , Brett Tounge
IPC分类号： A61K31/519 , A61P25/28 , C07D211/72 , C07D471/04
CPC分类号： C07D213/73 , C07D471/04
摘要： The present invention is directed to novel 2-amino-3,4-dihydro-pyrido[3,4-d]pyrimidine 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：本发明涉及新的2-氨基-3,4-二氢 - 吡啶并[3,4-d]嘧啶衍生物，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β-分泌酶的抑制剂，也称为β-位点切割酶和BACE，BACE1，Asp2和memapsin2。

12. 发明申请

US20070232630A1 MACROCYCLE DERIVATIVES USEFUL AS INHIBITORS OF beta-SECRETASE (BACE) 有权
标题翻译：大分子衍生物作为β-分泌酶（BACE）的抑制剂有用
公开(公告)号：US20070232630A1
公开(公告)日：2007-10-04
申请号：US11671732
申请日：2007-02-06
申请人： Ellen Baxter , Allen Reitz , Michael Parker , Yifang Huang , Chih Ho , Eric Strobel , Charles Reynolds
发明人： Ellen Baxter , Allen Reitz , Michael Parker , Yifang Huang , Chih Ho , Eric Strobel , Charles Reynolds
IPC分类号： A61K31/519 , C07D491/14 , C07D487/14
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β-分泌酶的抑制剂，也称为β-位点切割酶和BACE，BACE1，Asp2和memapsin2。

13. 发明申请

US20110224209A1 4,4-DISUBSTITUTED PIPERIDINE DERIVATIVES USEFUL AS INHIBITORS OF DIPEPTIDYL PEPTIDASE-1 (DPP-1) 有权
标题翻译：作为DIPPTIDYL PEPTIDASE-1（DPP-1）的抑制剂的4,4 - 取代的哌啶衍生物
公开(公告)号：US20110224209A1
公开(公告)日：2011-09-15
申请号：US13043609
申请日：2011-03-09
申请人： Bart L. DeCorte , Renee L. DesJarlais , Yifang Huang , Michael H. Parker , Dennis J. Hlasta
发明人： Bart L. DeCorte , Renee L. DesJarlais , Yifang Huang , Michael H. Parker , Dennis J. Hlasta
IPC分类号： A61K31/4535 , C07D409/06 , C07D409/14 , C07D211/64 , C07D401/06 , C07D417/14 , C07D413/14 , C07D401/14 , A61K31/4545 , A61K31/451 , A61K31/454 , A61K31/445 , A61K31/5377 , A61K31/4725 , A61K31/506 , A61P29/00 , A61P11/06 , A61P11/00 , A61P1/00 , A61P9/00
CPC分类号： C07D409/14 , C12N5/0606
摘要： The present invention is directed to 4,4-di-substituted piperidine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.
摘要翻译：本发明涉及4,4-二取代哌啶衍生物，含有它们的药物组合物及其用于治疗由DPP-1调节的病症和状况的用途。

14. 发明授权

US08686152B2 4,4-disubstituted piperidine derivatives useful as inhibitors of dipeptidyl peptidase-1 (DPP-1) 有权
标题翻译：可用作二肽基肽酶-1（DPP-1）抑制剂的4,4-二取代哌啶衍生物
公开(公告)号：US08686152B2
公开(公告)日：2014-04-01
申请号：US13043609
申请日：2011-03-09
申请人： Bart L. DeCorte , Renee L. DesJarlais , Yifang Huang , Michael H. Parker , Dennis J. Hlasta
发明人： Bart L. DeCorte , Renee L. DesJarlais , Yifang Huang , Michael H. Parker , Dennis J. Hlasta
IPC分类号： C07D409/06 , C07D405/06 , A61K31/4525 , A61K31/4535
CPC分类号： C07D409/14 , C12N5/0606
摘要： The present invention is directed to 4,4-di-substituted piperidine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.
摘要翻译：本发明涉及4,4-二取代哌啶衍生物，含有它们的药物组合物及其用于治疗由DPP-1调节的病症和状况的用途。

15. 发明申请

US20070014751A1 Novel spiro-quinuclidinyl derivatives for the treatment of central nervous system disorders 审中-公开
标题翻译：用于治疗中枢神经系统疾病的新型螺 - 奎宁环衍生物
公开(公告)号：US20070014751A1
公开(公告)日：2007-01-18
申请号：US11443929
申请日：2006-05-31
申请人： Yifang Huang , Michael Parker , Allen Reitz
发明人： Yifang Huang , Michael Parker , Allen Reitz
IPC分类号： A61K31/74
CPC分类号： C07D498/20 , C07D471/20
摘要： The present invention is directed to novel spiro-quinuclidinyl derivatives, pharmaceutical compositions containing them and their use in the treatment of central nervous system disorders.
摘要翻译：本发明涉及新的螺 - 奎宁环衍生物，含有它们的药物组合物及其在治疗中枢神经系统疾病中的用途。

16. 发明授权

US5801247A Process for the enantioselective synthesis of hydroxypyrrolidines from amino acids and products thereof 失效
标题翻译：从氨基酸及其产物对映选择性合成羟基吡咯烷的方法
公开(公告)号：US5801247A
公开(公告)日：1998-09-01
申请号：US787994
申请日：1997-01-23
申请人： David R. Dalton , Yifang Huang
发明人： David R. Dalton , Yifang Huang
IPC分类号： C07D207/12 , C07D207/26 , C07D207/273 , C07D263/10 , C07D263/14
CPC分类号： C07D207/273 , C07D207/12 , C07D263/10
摘要： The present invention relates to processes for the enantioselective synthesis of hydroxypyrrolidines from amino acids. An amino methyl ester is used as the starting material. The ester is reacted with a benziminoethyl ether to produce an oxazoline or thiazoline. Specifically, L-serine methyl ester is used to produce 4-(carbomethoxy)-2-phenyl-.increment..sup.2 -oxazoline, and cysteine is used to produce the corresponding thiazoline. The oxazoline (or thiazoline) can be reduced to an aldehyde by treatment with a slight excess of DIBAL-H. The oxazoline is quenched with alcohol and reacted with (carbomethoxymethylene)triphenylphosphorane, to produce (S)-(+)-methyl (E)- and (S)-(-)-methyl (Z)-3-(4,5-dihydro-2-phenyl-4-oxazolyl)-2-propenoate. The double bond is hydroxylated to yield the diol esters. The resulting diol is then treated with aqueous acid to hydrolyze the oxazoline and recyclize to produce 3,4-dihydroxy-5-hydroxymethylpyrrolidone benzoate. This is treated with an excess of borane in tetrahydrofuran to yield (2-hydroxymethyl) 3,4-dihydroxypyrrolidine. The intermediate compounds are useful both in the present process and as final products themselves. The total yield of the mixture of isomers, as well as their ratio, can be varied.
摘要翻译：本发明涉及从氨基酸对映选择性合成羟基吡咯烷的方法。使用氨基甲酯作为原料。酯与苯甲亚乙基醚反应生成恶唑啉或噻唑啉。具体地说，使用L-丝氨酸甲酯来制备4-（甲酯基）-2-苯基-2H-恶唑啉，半胱氨酸用于制备相应的噻唑啉。恶唑啉（或噻唑啉）可以通过用稍微过量的DIBAL-H处理而还原成醛。恶唑啉用醇淬灭并与（甲酯基亚甲基）三苯基正膦反应生成（S） - （+） - 甲基（E） - 和（S） - （ - ） - 甲基（Z）-3- 二氢-2-苯基-4-恶唑基）-2-丙烯酸甲酯。羟基化双键得到二醇酯。然后将所得二醇用酸水溶液处理以水解恶唑啉并再循环以产生3,4-二羟基-5-羟甲基吡咯烷酮苯甲酸酯。在四氢呋喃中用过量的硼烷处理，得到（2-羟甲基）3,4-二羟基吡咯烷。中间体化合物在本方法中可用作最终产物本身。异构体混合物的总产率及其比例可以变化。

17. 发明申请

US20070004715A1 Novel spiro-quinuclidinyl derivatives for the treatment of central nervous system disorders 审中-公开
公开(公告)号：US20070004715A1
公开(公告)日：2007-01-04
申请号：US11443928
申请日：2006-05-31
申请人： Yifang Huang , Michael Parker , Allen Reitz
发明人： Yifang Huang , Michael Parker , Allen Reitz
IPC分类号： A61K31/538 , C07D491/04
CPC分类号： C07D491/04
摘要： The present invention is directed to novel spiro-quinuclidinyl derivatives, pharmaceutical compositions containing them and their use in the treatment of central nervous system disorders.

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