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1. 发明申请

US20050165047A1 Crystalline fumarate salts of 1-azabicyclo[2.2.2]oct substituted furo[2,3-c]pyridinyl carboxamide and compositions and preparations thereof 审中-公开
标题翻译： 1-氮杂双环[2.2.2]辛烷基取代的呋喃并[2,3-c]吡啶甲酰胺的结晶富马酸盐及其组合物和制剂
公开(公告)号：US20050165047A1
公开(公告)日：2005-07-28
申请号：US10962071
申请日：2004-10-08
申请人： Jon Selbo , Donn Wishka , Bradley Hewitt , David Rappath , Ahmad Sheikh
发明人： Jon Selbo , Donn Wishka , Bradley Hewitt , David Rappath , Ahmad Sheikh
IPC分类号： A61K31/4545 , A61P25/00 , C07D519/00 , C07D491/02 , A61K31/4745
CPC分类号： C07D519/00
摘要： The invention provides fumarate salts of N-[1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, compositions, racemic mixtures, or pure enantiomers thereof, and preparation thereof. The fumarate salts are useful to treat diseases or conditions in which α7 nAChR is known to be involved.
摘要翻译：本发明提供N- [1-氮杂双环[2.2.2]辛-3-基]呋喃并[2,3-c]吡啶-5-甲酰胺的组合物，外消旋混合物或其纯对映异构体的富马酸盐及其制备方法。富马酸盐可用于治疗已知α7nAChR涉及的疾病或病症。

2. 发明授权

US07767850B2 S-[2-[(1-iminoethy)amino]ethyl]-2-methyl-L-cysteine maleate hydrochloride crystalline salt 有权
标题翻译： S- [2 - [（1-亚氨基）氨基]乙基] -2-甲基-L-半胱氨酸马来酸盐盐酸盐结晶盐
公开(公告)号：US07767850B2
公开(公告)日：2010-08-03
申请号：US12315744
申请日：2008-12-05
申请人： Lyle Brostrom , Ann Czyzewski , Vahid Zia , Ahmad Sheikh
发明人： Lyle Brostrom , Ann Czyzewski , Vahid Zia , Ahmad Sheikh
IPC分类号： C07C323/25
CPC分类号： C07C323/59 , C07B2200/07 , C07B2200/13 , C07C319/28
摘要： A novel mixed salt of S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine is disclosed. The novel mixed salt, S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine maleate hydrochloride, may be produced to form crystals that may be arranged as generally orderly packed agglomerates, which are particularly useful in making pharmaceutical compositions. Such pharmaceutical compositions are also described, as well as methods to make crystalline S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine maleate hydrochloride, and methods of treating conditions characterized by an overexpression on nitric oxide from the inducible isoform of nitric oxide synthase using the S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine maleate hydrochloride.
摘要翻译：公开了S- [2 - [（1-亚氨基乙基）氨基]乙基] -2-甲基-L-半胱氨酸的新型混合盐。可以制备新的混合盐S- [2 - [（1-亚氨基乙基）氨基]乙基] -2-甲基-L-半胱氨酸马来酸盐盐酸盐，以形成可以排列成通常有序包装的附聚物的晶体，可用于制备药物组合物。还描述了这样的药物组合物，以及制备结晶S- [2 - [（1-亚氨基乙基）氨基]乙基] -2-甲基-L-半胱氨酸马来酸盐酸盐盐酸盐的方法和以过表达为特征的病症的方法使用S- [2 - [（1-亚氨基乙基）氨基]乙基] -2-甲基-L-半胱氨酸马来酸盐酸盐从一氧化氮合酶的诱导型同种型的一氧化氮。

3. 发明申请

US20120196792A1 MACROCYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS 有权
公开(公告)号：US20120196792A1
公开(公告)日：2012-08-02
申请号：US13439551
申请日：2012-04-04
申请人： Yiyin Ku , Keith F. McDaniel , Hui-Ju Chen , Jason P. Shanley , Dale J. Kempf , David J. Grampovnik , Ying Sun , Dong Liu , Yonghua Gai , Yat Sun Or , Seble H. Wagaw , Ken Engstrom , Tim Grieme , Ahmad Sheikh , Jianzhang Mei
发明人： Yiyin Ku , Keith F. McDaniel , Hui-Ju Chen , Jason P. Shanley , Dale J. Kempf , David J. Grampovnik , Ying Sun , Dong Liu , Yonghua Gai , Yat Sun Or , Seble H. Wagaw , Ken Engstrom , Tim Grieme , Ahmad Sheikh , Jianzhang Mei
IPC分类号： A61K38/12 , A61P31/12 , C07K5/12
CPC分类号： C07K1/113 , C07D487/04
摘要： The present invention relates to novel macrocyclic compounds and methods of treating a hepatitis C infection in a subject in need of such therapy with said macrocyclic compounds. The present invention further relates to pharmaceutical compositions comprising the compounds of the present invention, or pharmaceutically acceptable salts, esters, or prodrugs thereof, in combination with a pharmaceutically acceptable carrier or excipient.

4. 发明申请

US20100144608A1 Macrocyclic hepatitis C serine protease inhibitors 有权
标题翻译：大环丙型肝炎丝氨酸蛋白酶抑制剂
公开(公告)号：US20100144608A1
公开(公告)日：2010-06-10
申请号：US12584716
申请日：2009-09-10
申请人： Yiyin Ku , Keith F. McDaniel , Hui-Ju Chen , Jason P. Shanley , Dale J. Kempf , David J. Grampovnik , Ying Sun , Dong Liu , Yonghua Gai , Yat Sun Or , Seble H. Wagaw , Ken Engstrom , Tim Grieme , Ahmad Sheikh , Jianzhang Mei
发明人： Yiyin Ku , Keith F. McDaniel , Hui-Ju Chen , Jason P. Shanley , Dale J. Kempf , David J. Grampovnik , Ying Sun , Dong Liu , Yonghua Gai , Yat Sun Or , Seble H. Wagaw , Ken Engstrom , Tim Grieme , Ahmad Sheikh , Jianzhang Mei
IPC分类号： A61K38/12 , C07D487/04 , A61P31/12
CPC分类号： C07K1/113 , C07D487/04
摘要： The present invention relates to novel macrocyclic compounds and methods of treating a hepatitis C infection in a subject in need of such therapy with said macrocyclic compounds. The present invention further relates to pharmaceutical compositions comprising the compounds of the present invention, or pharmaceutically acceptable salts, esters, or prodrugs thereof, in combination with a pharmaceutically acceptable carrier or excipient.
摘要翻译：本发明涉及新的大环化合物和在需要用所述大环化合物进行这种治疗的受试者中治疗丙型肝炎感染的方法。本发明还涉及包含本发明化合物或其药学上可接受的盐，酯或前药与药学上可接受的载体或赋形剂组合的药物组合物。

5. 发明申请

US20080064703A1 Fused bicycloheterocycle substituted quinuclidine derivatives 有权
标题翻译：稠合双环杂环取代的奎宁环衍生物
公开(公告)号：US20080064703A1
公开(公告)日：2008-03-13
申请号：US11789949
申请日：2007-04-26
申请人： Eric Stoner , Alan Christesen , Ahmad Sheikh , Xiu Wang , Agnes Pal , David Murphey , Jianguo Ji , Devalina Law , Daozhong Zou
发明人： Eric Stoner , Alan Christesen , Ahmad Sheikh , Xiu Wang , Agnes Pal , David Murphey , Jianguo Ji , Devalina Law , Daozhong Zou
IPC分类号： A61K31/501 , A61P25/34 , C07D401/14
CPC分类号： C07D453/02
摘要： Compounds of formula (II): known as: 5-{6-[(3R)-1-azabicyclo[2.2.2]oct-3-yloxy]pyridazin-3-yl}-1-H-indole salt with (2R, 3R)-2,3-dihydroxybutanedioic acid (1:1).
摘要翻译：式（II）化合物：称为5- {6 - [（3R）-1-氮杂双环[2.2.2]辛-3-基氧基]哒嗪-3-基} -1H-吲哚盐与（2R ，3R）-2,3-二羟基丁二酸（1:1）。

6. 发明申请

US20070185034A1 CRYSTALLINE FORM OF A DRUG 有权
标题翻译：药物的结晶形式
公开(公告)号：US20070185034A1
公开(公告)日：2007-08-09
申请号：US11615234
申请日：2006-12-22
申请人： John Tolle , Ahmad Sheikh
发明人： John Tolle , Ahmad Sheikh
IPC分类号： A61K38/10 , C07K7/08
CPC分类号： C07K7/06 , A61K38/00
摘要： Ac-Sar-Gly-Val-D-allo-Ile-Thr-Nva-Ile-Arg-ProNHCH2CH3 Crystalline Form 1, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.
摘要翻译： Ac-Sar-Gly-Val-D-allo-Ile-Thr-Nva-Ile-Arg-ProNHCH 2 CH 3结晶形式1，制备方法，组合物公开了其含有疾病的治疗方法和抑制不良生理事件。

7. 发明申请

US20090215891A1 S-[2-[(1-lminoethy)Amino]Ethyl]-2-Methyl-L-Cysteine Maleate Hydrochloride Crystalline Salt 有权
标题翻译： S- [2 - [（1,1-二乙基）氨基]乙基] -2-甲基-L-半胱氨酸马来酸盐盐酸盐结晶盐
公开(公告)号：US20090215891A1
公开(公告)日：2009-08-27
申请号：US12315744
申请日：2008-12-05
申请人： Lyle Brostrom , Ann Czyzewski , Vahid Zia , Ahmad Sheikh
发明人： Lyle Brostrom , Ann Czyzewski , Vahid Zia , Ahmad Sheikh
IPC分类号： C07C321/02 , A61K31/221
CPC分类号： C07C323/59 , C07B2200/07 , C07B2200/13 , C07C319/28
摘要： A novel mixed salt of S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine is disclosed. The novel mixed salt, S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine maleate hydrochloride, may be produced to form crystals that may be arranged as generally orderly packed agglomerates, which are particularly useful in making pharmaceutical compositions. Such pharmaceutical compositions are also described, as well as methods to make crystalline S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine maleate hydrochloride, and methods of treating conditions characterized by an overexpression on nitric oxide from the inducible isoform of nitric oxide synthase using the S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine maleate hydrochloride.
摘要翻译：公开了S- [2 - [（1-亚氨基乙基）氨基]乙基] -2-甲基-L-半胱氨酸的新型混合盐。可以制备新的混合盐S- [2 - [（1-亚氨基乙基）氨基]乙基] -2-甲基-L-半胱氨酸马来酸盐盐酸盐，以形成可以排列成通常有序包装的附聚物的晶体，可用于制备药物组合物。还描述了这样的药物组合物，以及制备结晶S- [2 - [（1-亚氨基乙基）氨基]乙基] -2-甲基-L-半胱氨酸马来酸盐酸盐盐酸盐的方法和以过表达为特征的病症的方法使用S- [2 - [（1-亚氨基乙基）氨基]乙基] -2-甲基-L-半胱氨酸马来酸盐酸盐从一氧化氮合酶的诱导型同种型的一氧化氮。

8. 发明申请

US20050038120A1 S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine maleate hydrochloride crystalline salt 审中-公开
标题翻译： S- [2 - [（1-亚氨基乙基）氨基]乙基] -2-甲基-L-半胱氨酸马来酸盐盐酸盐结晶盐
公开(公告)号：US20050038120A1
公开(公告)日：2005-02-17
申请号：US10797462
申请日：2004-03-10
申请人： Lyle Brostrom , Ann Czyzewski , Vahid Zia , Ahmad Sheikh
发明人： Lyle Brostrom , Ann Czyzewski , Vahid Zia , Ahmad Sheikh
IPC分类号： A61K31/198 , A61P29/00 , C07C319/28 , C07C323/39 , C07C323/59
CPC分类号： C07C323/59 , C07B2200/07 , C07B2200/13 , C07C319/28
摘要： A novel mixed salt of S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine is disclosed. The novel mixed salt, S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine maleate hydrochloride, may be produced to form crystals that may be arranged as generally orderly packed agglomerates, which are particularly useful in making pharmaceutical compositions. Such pharmaceutical compositions are also described, as well as methods to make crystalline S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine maleate hydrochloride, and methods of treating conditions characterized by an overexpression on nitric oxide from the inducible isoform of nitric oxide synthase using the S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine maleate hydrochloride.
摘要翻译：公开了S- [2 - [（1-亚氨基乙基）氨基]乙基] -2-甲基-L-半胱氨酸的新型混合盐。可以制备新的混合盐S- [2 - [（1-亚氨基乙基）氨基]乙基] -2-甲基-L-半胱氨酸马来酸盐盐酸盐，以形成可以排列成通常有序包装的附聚物的晶体，可用于制备药物组合物。还描述了这样的药物组合物，以及制备结晶S- [2 - [（1-亚氨基乙基）氨基]乙基] -2-甲基-L-半胱氨酸马来酸盐酸盐盐酸盐的方法和以过表达为特征的病症的方法使用S- [2 - [（1-亚氨基乙基）氨基]乙基] -2-甲基-L-半胱氨酸马来酸盐酸盐从一氧化氮合酶的诱导型同种型的一氧化氮。

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