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51. 发明授权

US06326380B1 Thrombin receptor antagonists 有权
标题翻译：凝血酶受体拮抗剂
公开(公告)号：US06326380B1
公开(公告)日：2001-12-04
申请号：US09545720
申请日：2000-04-07
申请人： Samuel Chackalamannil , Theodros Asberom , Yan Xia , Dario Doller , Martin C. Clasby , Michael F. Czarniecki
发明人： Samuel Chackalamannil , Theodros Asberom , Yan Xia , Dario Doller , Martin C. Clasby , Michael F. Czarniecki
IPC分类号： A61K3147
CPC分类号： C07D405/06 , C07D405/14 , C07D409/14 , C07D413/06 , C07D417/06 , C07D471/04 , C07D491/04 , C07D493/10
摘要： Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the single dotted line represents an optional double bond; the double dotted line represents an optional single bond; n is 0-2; Q is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is —(CH2)n3—, wherein n3 is 0-5, —CH2—O—, —CH2S—, —CH2—NR6—, —C(O)NR6—, —NR6C(O)—, optionally substituted alkenyl or optionally substituted alkynyl; X is —O— or —NR6— when the double dotted line represents a single bond, or X is —OH or —NHR20 when the bond is absent; Y is ═O, ═S, (H, H), (H, OH) or (H, C1-C6 alkoxy) when the double dotted line represents a single bond, or when the bond is absent, Y is ═O, (H, H), (H, OH), (H, SH) or (H, C1-C6 alkoxy); R15 is absent when the double dotted line represents a single bond and is H, —NR18R19, or —OR17 when the bond is absent; or Y is or and R15 is H or C1-C6 alkyl; are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds.
摘要翻译：式2的杂环取代的三环或其药学上可接受的盐，其中：单点线表示任选的双键;双点划线表示任选的单键; n为0-2; Q为任选取代的环烷基，杂环烷基，芳基或杂芳基; Het是任选取代的单，双或三环杂芳族基团; B是 - （CH 2）n3-，其中n3是0-5，-CH2-O-，-CH2S-，-CH2-NR6-， -C（O）NR 6 - ，-NR 6 C（O） - ，任选取代的烯基或任选取代的炔基;当双点划线表示单键时，X为-O-或-NR6-，或X为-OH或-NHR20 当双键虚线表示单键时，当不存在键时，Y为= O，= S，（H，H），（H，OH）或（H，C 1 -C 6烷氧基），Y为= O，（H，H），（H，OH），（H，SH）或（H，C1-C6烷氧基）;当双点表示单键且为H时， NR18R19或-OR17，当该键不存在时; 或Y为或R 15为H或C 1 -C 6烷基;以及含有它们的药物组合物和治疗与血栓形成，动脉粥样硬化，再狭窄，高血压，心绞痛，心律失常，心力衰竭和癌症相关的疾病的方法通过施用所述化合物。

52. 发明授权

US5106979A Method for the synthesis of huperzine A and analogs thereof and compounds useful therein 失效
标题翻译：合成石杉碱甲及其类似物的方法及其中有用的化合物
公开(公告)号：US5106979A
公开(公告)日：1992-04-21
申请号：US499122
申请日：1990-03-23
申请人： Alan P. Kozikowski , Yan Xia
发明人： Alan P. Kozikowski , Yan Xia
IPC分类号： C07D215/48 , C07D221/22
CPC分类号： C07D221/22 , C07D215/48
摘要： The present invention relates to a method for the synthesis of certain bridged fused ring pyridines. Such bridged fused ring pyridines can be converted to huperzine A and analogs of huperzine A. The present invention also covers such bridged fused ring pyridines, compounds utilized for the preparation of the bridged fused ring pyridines and analogs of huperzine A.
摘要翻译：本发明涉及合成某些桥连稠环吡啶的方法。这种桥连稠环吡啶可以转化为石杉碱甲和石杉碱甲类似物。本发明还涵盖了这种桥连稠环吡啶，用于制备桥连稠环吡啶的化合物和石杉碱甲的类似物。

53. 发明申请

US20170323462A1 METHOD AND APPARATUS FOR THE RECONSTRUCTION OF MEDICAL IMAGE DATA USING FILTERED BACKPROJECTION 审中-公开
公开(公告)号：US20170323462A1
公开(公告)日：2017-11-09
申请号：US15589321
申请日：2017-05-08
申请人： Sebastian Bauer , Andreas Maier , Yan Xia
发明人： Sebastian Bauer , Andreas Maier , Yan Xia
IPC分类号： G06T11/00
CPC分类号： G06T11/006 , G06T2211/421 , G06T2211/432
摘要： A system and method are provided for the reconstruction of medical image data using filtered backprojection with the use of a wavelet transformation. A filter function is applied to at least one part of an object using projection data captured with a detection device prior to backprojection.

54. 发明申请

US20150286750A1 MODEL DRIVEN CONNECTION APPROXIMATION FOR MECHANICAL, ELECTRICAL AND PLUMBING DRAWINGS 审中-公开
标题翻译：机械，电气和配件图的驱动连接近似模型
公开(公告)号：US20150286750A1
公开(公告)日：2015-10-08
申请号：US14407196
申请日：2012-06-25
申请人： Henry Chen , Geng Jian Du , Xiaoli Wang , Yan Xia , Liana Maria Kiff
发明人： Henry Chen , Geng Jian Du , Xiaoli Wang , Yan Xia , Liana Maria Kiff
IPC分类号： G06F17/50
CPC分类号： G06F17/5004 , G06F17/509 , G06F2217/34 , G06K9/00476 , G06T7/001 , G06T2207/10004 , G06T2207/30108 , G06T2207/30176
摘要： A system displays a raster-based or a vector-based formatted drawing on a user interface. A user selects a device on the drawing. The selected device is classified on a template. The drawing is searched for the classified template. Three-dimensional characteristics are imbued to the selected device. Connection types among different types of devices on the drawing are received into the system. A search is performed for all connection instances throughout the drawing using the received connection types. An object oriented and three-dimensionally, spatially referenced view of the drawing is generated on a user interface.
摘要翻译：系统在用户界面上显示基于栅格或基于矢量的格式化图形。用户选择图纸上的设备。所选设备分为模板。搜索图纸的分类模板。所选设备的三维特征。图形中不同类型设备之间的连接类型被接收到系统中。使用接收到的连接类型，对整个绘图中的所有连接实例执行搜索。在用户界面上生成绘图的面向对象和三维空间参考视图。

55. 发明申请

US20110059958A1 MORPHOLINONE COMPOUNDS AS FACTOR IXA INHIBITORS 有权
公开(公告)号：US20110059958A1
公开(公告)日：2011-03-10
申请号：US12744736
申请日：2009-12-03
申请人： Hidemitsu Nishida , Fumihiko Saitoh , Tomokazu Hirabayashi , Samuel Chackalamannil , Tin-Yau Chan , Mariappan V. Chelliah , Martin C. Clasby , Michael Dwyer , William J. Greenlee , Yan Xia
发明人： Hidemitsu Nishida , Fumihiko Saitoh , Tomokazu Hirabayashi , Samuel Chackalamannil , Tin-Yau Chan , Mariappan V. Chelliah , Martin C. Clasby , Michael Dwyer , William J. Greenlee , Yan Xia
IPC分类号： A61K31/5377 , C07D413/12 , A61P7/02 , A61P9/10 , A61P9/12 , C07D265/32 , C07D413/10
CPC分类号： C07D401/12 , C07D265/30 , C07D265/32 , C07D267/10 , C07D279/06 , C07D413/12 , C07D413/14 , C07D417/04
摘要： The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt or a solvate thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.

56. 发明申请

US20100152138A1 CYCLIC AMINE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT 有权
标题翻译：具有苯甲酸替代物的循环胺BACE-1抑制剂
公开(公告)号：US20100152138A1
公开(公告)日：2010-06-17
申请号：US12641952
申请日：2009-12-18
申请人： Jared N. Cumming , Ulrich Iserloh , Andrew Stamford , Corey Strickland , Johannes H. Voigt , Yusheng Wu , Ying Huang , Yan Xia , Samuel Chackalamannil , Tao Guo , Douglas W. Hobbs , Thuy X.H. Le , Jeffrey F. Lowrie , Kurt W. Saionz , Suresh D. Babu
发明人： Jared N. Cumming , Ulrich Iserloh , Andrew Stamford , Corey Strickland , Johannes H. Voigt , Yusheng Wu , Ying Huang , Yan Xia , Samuel Chackalamannil , Tao Guo , Douglas W. Hobbs , Thuy X.H. Le , Jeffrey F. Lowrie , Kurt W. Saionz , Suresh D. Babu
IPC分类号： A61K31/4015 , C07D207/12 , C07D217/24 , C07D413/12 , C07D243/08 , A61K31/47 , A61K31/675 , A61K31/397 , A61K31/5377 , A61K31/551 , A61P25/28
CPC分类号： C07D243/08 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/26 , C07D209/52 , C07D211/26 , C07D211/46 , C07D217/18 , C07D233/32 , C07D241/04 , C07D241/08 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/12 , C07D403/14 , C07D409/06 , C07D409/12 , C07D413/06
摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification.Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease.Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
摘要翻译：公开了下式的化合物或其药学上可接受的盐或溶剂化物，其中R1是R是-C（O）-N（R27）（R28），或其余的变量如说明书中所定义。还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经变性疾病如阿尔茨海默病的方法。还公开了治疗认知或神经变性疾病的药物组合物和方法，其包含式I化合物与除式I以外的分泌抑制剂抑制剂，HMG-CoA还原酶抑制剂，γ-分泌酶抑制剂，非 - 甾族抗炎药，N-甲基-D-天冬氨酸受体拮抗剂，胆碱酯酶抑制剂或抗淀粉样蛋白抗体。

57. 发明申请

US20080090830A1 Bicyclic And Tricyclic Derivatives As Thrombin Receptor Antagonists 有权
标题翻译：双环和三环衍生物作为凝血酶受体拮抗剂
公开(公告)号：US20080090830A1
公开(公告)日：2008-04-17
申请号：US11865793
申请日：2007-10-02
申请人： Samuel Chackalamannil , Mariappan Chelliah , Yuguang Wang , Yan Xia
发明人： Samuel Chackalamannil , Mariappan Chelliah , Yuguang Wang , Yan Xia
IPC分类号： A61K31/4427 , A61K31/435 , A61K31/443 , A61K31/4439 , A61K31/502 , A61P1/00 , A61P11/00 , A61P15/00 , A61P17/00 , A61P35/00 , A61P9/00 , C07D221/06 , C07D401/06 , C07D413/02 , C07D487/00
CPC分类号： C07D401/06 , C07D417/06
摘要： Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bonds the dotted line is optionally a bond or no bonds resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failures and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
摘要翻译：异构体或外消旋混合物的下式的杂环取代三环或其药学上可接受的盐或溶剂合物，其中表示可选的双键，虚线可选地是一个键或没有导致双键或单键的键，如允许通过化合价要求，其中E，A，GM，Het，B，X，R 3，R 10，R 11，本文定义了SUP 32和33 SS，其余取代基如说明书中所定义，以及含有它们的药物组合物和治疗与血栓形成有关的疾病的方法，动脉粥样硬化，再狭窄，高血压，心绞痛，心律失常，心脏衰竭和癌症。还要求与其它心血管药物联合治疗。

58. 发明授权

US07304078B2 Thrombin receptor antagonists 有权
标题翻译：凝血酶受体拮抗剂
公开(公告)号：US07304078B2
公开(公告)日：2007-12-04
申请号：US10412982
申请日：2003-04-14
申请人： Samuel Chackalamannil , William J. Greenlee , Yuguang Wang , Wenxue Wu , Enrico P. Veltri , Yan Xia
发明人： Samuel Chackalamannil , William J. Greenlee , Yuguang Wang , Wenxue Wu , Enrico P. Veltri , Yan Xia
IPC分类号： A61K31/443 , C07D405/02
CPC分类号： C07D405/06 , C07D405/14 , C07D417/14
摘要： Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond; represents an optional double bond; n is 0–2; Q is cycloalkyl, optionally substituted by R13 and R14; R13 and R14 are independently selected from (C1–C6)alkyl, (C3–C8)cycloalkyl, —OH, (C1–C6)alkoxy, R27-aryl(C1–C6)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, halogen and haloalkyl; or R13 and R14 together form a spirocyclic or a heterospirocyclic ring of 3–6 atoms; Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
摘要翻译：式中的杂环取代三环

59. 发明申请

US20070244163A1 Fused Ring Thrombin Receptor Antagonists 有权
标题翻译：融合环凝血酶受体拮抗剂
公开(公告)号：US20070244163A1
公开(公告)日：2007-10-18
申请号：US11734057
申请日：2007-04-11
申请人： Yan Xia , Mariappan V. Chelliah , Samuel Chackalamannil
发明人： Yan Xia , Mariappan V. Chelliah , Samuel Chackalamannil
IPC分类号： A61K31/4439 , C07D491/02
CPC分类号： C07D405/06 , C07D498/04
摘要： Fused-ring, heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, and wherein An, En, Mn, Gn, Jn, R3, n7, R8, R9, R10, R11, R32, R33, X, Y, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
摘要翻译：熔融环，具有下式的杂环取代的三环或所述化合物的药学上可接受的盐或溶剂合物，异构体或外消旋混合物，其中表示可选的双键，并且其中A N，N， M，N，N，N，N，N，N，N，N， R 8，R 9，R 10，R 11，R 32，R 12，本文中定义了R32，X，Y，B和Het，其余取代基如说明书中所定义，以及含有它们的药物组合物和通过施用所述化合物治疗与血栓形成，动脉粥样硬化，再狭窄，高血压，心绞痛，心律失常，心力衰竭和癌症相关的疾病。还要求与其它心血管药物联合治疗。

60. 发明申请

US20060223808A1 Spirocyclic thrombin receptor antagonists 有权
标题翻译：螺环状凝血酶受体拮抗剂
公开(公告)号：US20060223808A1
公开(公告)日：2006-10-05
申请号：US11392324
申请日：2006-03-29
申请人： Samuel Chackalamannil , Mariappan Chelliah , Yan Xia
发明人： Samuel Chackalamannil , Mariappan Chelliah , Yan Xia
IPC分类号： A61K31/4747 , A61K31/502 , C07D413/02
CPC分类号： C07D263/52 , C07D413/08
摘要： Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein An, En, Mn, Un, Gn, Jn, Kn, R9, R10, R11, R32, R33, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
摘要翻译：异构体或外消旋混合物的下式的杂环取代三环或其药学上可接受的盐或溶剂化物，其中表示可选的双键，虚线是可选的键或无键，导致双重债券或单一债券，如价格要求所允许的，并且其中A N，N，N，N， N，N，N，N，R 9，R 10，在本文中定义，其余取代基如本说明书中所定义，其中R 11，R 32，R 32和/ ，以及含有它们的药物组合物和治疗与血栓形成，动脉粥样硬化，再狭窄，高血压，心绞痛，心律失常，心力衰竭，和癌症。还要求与其它心血管药物联合治疗。

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