公开(公告)号：US07713999B2

公开(公告)日：2010-05-11

申请号：US11733635

申请日：2007-04-10

申请人： Samuel Chackalamannil ,  Martin C. Clasby ,  William J. Greenlee ,  Yuguang Wang ,  Yan Xia ,  Enrico P. Veltri ,  Mariappan V. Chelliah

发明人： Samuel Chackalamannil ,  Martin C. Clasby ,  William J. Greenlee ,  Yuguang Wang ,  Yan Xia ,  Enrico P. Veltri ,  Mariappan V. Chelliah

IPC分类号： A61K31/443 ,  C07D307/78

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： 具有下式的杂环取代的三环或其药学上可接受的盐，其中：虚线表示任选的单键; 表示可选的双键，n为0-2; Q是环烷基，任选被R 13和R 14取代; R 13和R 14独立地选自（C 1 -C 6）烷基，（C 3 -C 8）环烷基，-OH，（C 1 -C 6）烷氧基，R 27 - 芳基（C 1 -C 6）烷基，杂芳基，杂芳基烷基，杂环基，杂环基烷基，卤素 和卤代烷基; 或R 13和R 14一起形成3-6个原子的螺环或异环环，Het是单或双环任选取代的杂芳基; 和B是键，亚烷基或任选取代的亚烯基或亚炔基，其中剩余的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，动脉粥样硬化，再狭窄有关的疾病的方法， 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。

公开(公告)号：US20080234236A1

公开(公告)日：2008-09-25

申请号：US12051504

申请日：2008-03-19

申请人： Enrico P. Veltri ,  John T. Strony ,  Madhu Chintala

发明人： Enrico P. Veltri ,  John T. Strony ,  Madhu Chintala

IPC分类号： A61K31/443 ,  A61K31/5377 ,  A61K31/4365 ,  A61K31/60

CPC分类号： A61K31/443

摘要： Disclosed are methods of preventing adverse clinical events in a patient undergoing a percutaneous coronary intervention procedure or a peripheral percutaneous interventional procedure comprising administering a therapeutically effective amount of a thrombin receptor antagonist, such as SCH 530348, to the patient. Administration of a loading dose of about 40 mg of SCH 530348 in as little as one hour prior to the procedure can result in therapeutically effective levels of platelet aggregation.

摘要翻译： 公开了防止经历经皮冠状动脉介入手术或周边经皮介入手术的患者的不利临床事件的方法，包括向患者施用治疗有效量的凝血酶受体拮抗剂，例如SCH 530348。 在手术前至少1小时施用约40mg SCH 530348的负荷剂量可导致治疗有效的血小板聚集水平。

公开(公告)号：US20090149480A1

公开(公告)日：2009-06-11

申请号：US12364305

申请日：2009-02-02

申请人： Cynthia Cuffie-Jackson ,  Enrico P. Veltri

发明人： Cynthia Cuffie-Jackson ,  Enrico P. Veltri

IPC分类号： A61K31/522

CPC分类号： A61K31/422 ,  A61K31/522 ,  A61K45/06 ,  A61K2300/00

摘要： The uses of PDE V inhibitors in methods for the treatment of congestive heart failure and other physiological disorders, as a monotherapy and in combination with other active agents are disclosed. Such PDE V inhibitors include those having the formula (I), with the variables defined herein: For example, a representative compound useful in the methods of the invention is:

摘要翻译： 公开了PDE V抑制剂在治疗充血性心力衰竭和其它生理障碍的方法中作为单一疗法并与其它活性剂组合的用途。 这样的PDE V抑制剂包括具有式（I）的那些，具有本文定义的变量：例如，可用于本发明方法的代表性化合物是：

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

公开(公告)号：US07071181B2

公开(公告)日：2006-07-04

申请号：US10247099

申请日：2002-09-19

申请人： Harry R. Davis ,  Teddy Kosoglou ,  Gilles J. Picard ,  Rudyard J. Ress ,  John T. Strony ,  Enrico P. Veltri

发明人： Harry R. Davis ,  Teddy Kosoglou ,  Gilles J. Picard ,  Rudyard J. Ress ,  John T. Strony ,  Enrico P. Veltri

IPC分类号： A61K31/397 ,  A61K31/7052

CPC分类号： A61K31/397 ,  A61K31/7052

摘要： The present invention provides methods of treating diabetes and associated conditions by administering a composition including at least one sterol or 5α-stanol absorption inhibitor or compositions or therapeutic combinations including: (a) at least one antidiabetic medication; and (b) at least one sterol or 5α-stanol absorption inhibitor.

摘要翻译： 本发明提供了通过施用包含至少一种甾醇或5α-甾烷醇吸收抑制剂的组合物或组合物或治疗组合来治疗糖尿病和相关病症的方法，包括：（a）至少一种抗糖尿病药物; 和（b）至少一种甾醇或5α-甾烷醇吸收抑制剂。

公开(公告)号：US20090062239A1

公开(公告)日：2009-03-05

申请号：US12261844

申请日：2008-10-30

申请人： Enrico P. Veltri ,  John T. Strony ,  Gail Berman

发明人： Enrico P. Veltri ,  John T. Strony ,  Gail Berman

IPC分类号： A61K31/443 ,  A61P9/00 ,  A61K31/444 ,  A61K31/60 ,  A61K31/4365

CPC分类号： A61K31/443 ,  A61K31/4365 ,  A61K31/444 ,  A61K31/60

摘要： Disclosed herein are methods of preventing, inhibiting, or ameliorating complications associated with cardiopulmonary bypass surgery by the use of a thrombin receptor antagonist compound. Among the thrombin receptor antagonist compounds useful in these methods are those of Formulas I and II, described herein. Examples of such thrombin receptor antagonists include:

摘要翻译： 本文公开了通过使用凝血酶受体拮抗剂化合物来预防，抑制或改善与心肺分流手术相关的并发症的方法。 在这些方法中有用的凝血酶受体拮抗剂化合物是本文所述的式I和II的化合物。 这种凝血酶受体拮抗剂的实例包括：

公开(公告)号：US07442712B2

公开(公告)日：2008-10-28

申请号：US11137283

申请日：2005-05-25

申请人： Mariappan V. Chelliah ,  Samuel Chackalamannil ,  Yan Xia ,  Martin C. Clasby ,  William J. Greenlee ,  Yuguang Wang ,  Enrico P. Veltri ,  Wenxue Wu ,  Michael P. Graziano ,  Teddy Kosoglou ,  Madhu Chintala

发明人： Mariappan V. Chelliah ,  Samuel Chackalamannil ,  Yan Xia ,  Martin C. Clasby ,  William J. Greenlee ,  Yuguang Wang ,  Enrico P. Veltri ,  Wenxue Wu ,  Michael P. Graziano ,  Teddy Kosoglou ,  Madhu Chintala

IPC分类号： A61K31/44 ,  C07D409/00

CPC分类号： C07D493/04 ,  C07D405/06

摘要： A compound represented by the structural formula and pharmaceutically acceptable salts and solvents thereof is disclosed, wherein: the single-dashed line between the ring carbons to which R10 and R34 are attached represents either a single bond or a double bond; the double-dashed line between X and the carbon to which Y is attached represents either a single bond or an absent bond; X is —O— or —NR6— when the double-dashed line represents a single bond; X is H, —OH or —NHR20 when the double-dashed line represents an absent bond; and other parameters are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing said compounds and their uses as thrombin receptor antagonists and binders to cannabinoid receptors.

摘要翻译： 公开了由结构式表示的化合物及其药学上可接受的盐和溶剂，其中：R 10和R 34之间的环碳之间的单点划线是 附表示单键或双键; X与Y所连接的碳之间的双点划线表示单键或不存在键; 当双点划线表示单键时，X是-O-或-NR 6 - 当双点划线表示不存在的键时，X是H，-OH或-NHR 20; 和其他参数如本文所定义。 还公开了含有所述化合物及其作为凝血酶受体拮抗剂和大麻素受体的结合物的药物组合物和组合。

公开(公告)号：US20120028976A1

公开(公告)日：2012-02-02

申请号：US13129725

申请日：2009-11-16

申请人： Larisa Reyderman ,  Teddy Kosoglou ,  Enrico P. Veltri

发明人： Larisa Reyderman ,  Teddy Kosoglou ,  Enrico P. Veltri

IPC分类号： A61K31/443 ,  A61K31/5377 ,  A61P9/00 ,  A61K31/444

CPC分类号： A61K31/443 ,  A61K31/5377

摘要： Dosing regimens based on the pharmacokinetic characteristics of a thrombin receptor antagonist are disclosed. In some embodiments, the dosing regimens result in mean plasma concentrations. Also disclosed are methods of treating acute coronary syndrome and peripheral arterial disease, and of effecting secondary prevention, by orally administering thrombin receptor antagonists according to such dosing regimens.

摘要翻译： 公开了基于凝血酶受体拮抗剂的药代动力学特征的给药方案。 在一些实施方案中，给药方案导致平均血浆浓度。 还公开了通过根据这种给药方案口服施用凝血酶受体拮抗剂来治疗急性冠状动脉综合征和外周动脉疾病以及进行二次预防的方法。

公开(公告)号：US20080152712A1

公开(公告)日：2008-06-26

申请号：US11860165

申请日：2007-09-24

申请人： David Monteith ,  Enrico P. Veltri ,  Srinivas Duggirala ,  Michael Angelo Falvo ,  John R. Erbey ,  Kung-I Feng ,  Anastasia Pavlovsky ,  Suliman Chawdry

发明人： David Monteith ,  Enrico P. Veltri ,  Srinivas Duggirala ,  Michael Angelo Falvo ,  John R. Erbey ,  Kung-I Feng ,  Anastasia Pavlovsky ,  Suliman Chawdry

IPC分类号： A61K9/00 ,  A61K31/443 ,  A61P9/00

CPC分类号： A61K31/4402 ,  A61K9/0056 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2063 ,  A61K9/2095 ,  A61K31/5377

摘要： Disclosed is a lyophilized rapidly disintegrating solid dosage form, one embodiment of which comprises a thrombin receptor antagonist such as, or a pharmaceutically acceptable salt or hydrate thereof, a polymer such as gelatin, and a matrix forming agent such as mannitol. Systems for effectively buffering the pre-lyophilized suspension are taught, along with methods of treating patients at risk for acute coronary syndrome by administering such a rapidly disintegrating solid dosage form.

摘要翻译： 公开了一种冻干的快速崩解固体剂型，其一个实施方案包括凝血酶受体拮抗剂或其药学上可接受的盐或水合物，诸如明胶的聚合物和基质形成剂如甘露糖醇。 教导了用于有效缓冲预冻干悬浮液的系统，以及通过施用这种快速崩解固体剂型治疗患有急性冠状动脉综合征风险的患者的方法。

公开(公告)号：US07053080B2

公开(公告)日：2006-05-30

申请号：US10247397

申请日：2002-09-19

申请人： Harry R. Davis ,  Rudyard J. Ress ,  John T. Strony ,  Enrico P. Veltri

发明人： Harry R. Davis ,  Rudyard J. Ress ,  John T. Strony ,  Enrico P. Veltri

IPC分类号： A61K31/00 ,  A61K31/7028 ,  A61K31/397 ,  C07H17/00

CPC分类号： A61K31/397 ,  A61K31/70 ,  A61K31/7052 ,  A61K45/06 ,  C07H15/26 ,  A61K2300/00

摘要： The present invention provides methods for the treatment of obesity using sterol or 5α-stanol absorption inhibitors and compositions and therapeutic combinations including sterol or 5α-stanol absorption inhibitors and at least one obesity control medication.