公开(公告)号：US08222411B2

公开(公告)日：2012-07-17

申请号：US12066769

申请日：2006-09-15

Applicant: Jun Feng ,  Stephen L. Gwaltney ,  Jeffrey A. Stafford ,  Zhiyuan Zhang ,  Paul R. Brodfuahrer ,  Bruce Elder ,  Paul Isbester ,  Richard S. Fornicola ,  Philip B. Kisanga ,  Bingidimi I. Mobele ,  Grant J. Palmer ,  Maxwell M. Reeve ,  Jonathon S. Salsbury ,  Luckner Ulysse ,  Sripathy Venkatraman

Inventor： Jun Feng ,  Stephen L. Gwaltney ,  Jeffrey A. Stafford ,  Zhiyuan Zhang ,  Paul R. Brodfuahrer ,  Bruce Elder ,  Paul Isbester ,  Richard S. Fornicola ,  Philip B. Kisanga ,  Bingidimi I. Mobele ,  Grant J. Palmer ,  Maxwell M. Reeve ,  Jonathon S. Salsbury ,  Luckner Ulysse ,  Sripathy Venkatraman

IPC: C07D239/02

CPC classification number: C07D239/553 ,  C07D239/545 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14

Abstract: Methods of making compounds of the formula (I) wherein the variables are as defined herein. Also, methods of making compounds that may be used to inhibit dipeptidyl peptidase.

Abstract translation: 制备式（I）化合物的方法，其中变量如本文所定义。 另外，制备可用于抑制二肽基肽酶的化合物的方法。

公开(公告)号：US07795428B2

公开(公告)日：2010-09-14

申请号：US11835295

申请日：2007-08-07

Applicant: Jun Feng ,  Stephen L. Gwaltney ,  Jeffrey Alan Stafford ,  Zhiyuan Zhang ,  Bruce Elder ,  Paul Isbester ,  Grant Palmer ,  Jonathan S. Salsbury ,  Luckner Ulysse

Inventor： Jun Feng ,  Stephen L. Gwaltney ,  Jeffrey Alan Stafford ,  Zhiyuan Zhang ,  Bruce Elder ,  Paul Isbester ,  Grant Palmer ,  Jonathan S. Salsbury ,  Luckner Ulysse

IPC: C07D401/04 ,  A61K31/506 ,  A61P3/10 ,  A61P19/02 ,  A61P35/00

CPC classification number: C07D403/04 ,  C07D239/545 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14

Abstract: Compounds are provided for use with DPP-IV of the formula: Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

Abstract translation: 化合物被提供用于下式的DPP-IV：还提供包含这些化合物的药物组合物，试剂盒和制品; 用于制备化合物的方法和中间体; 以及使用所述化合物的方法。

公开(公告)号：US20090270442A1

公开(公告)日：2009-10-29

申请号：US12422877

申请日：2009-04-13

Applicant: Lauren Graham ,  Paul Isbester ,  Olga V. Lapina ,  Bingidimi I. Mobele ,  Grant J. Palmer ,  Karl Reineke ,  Jonathon S. Salsbury ,  Luckner Ulysse

Inventor： Lauren Graham ,  Paul Isbester ,  Olga V. Lapina ,  Bingidimi I. Mobele ,  Grant J. Palmer ,  Karl Reineke ,  Jonathon S. Salsbury ,  Luckner Ulysse

IPC: A61K31/437 ,  C07D471/04 ,  A61P35/00 ,  A61P25/28 ,  A61P25/00 ,  A61P19/00

CPC classification number: C07D471/04

Abstract: Polymorphic forms of the hydrochloride salt of 5-(3-(ethylsulfonyl)phenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9h-pyrido[2,3-b]indole-7-carboxamide (referred to herein as Compound 1) which has the formula: and compositions thereof, wherein the Compound 1 is present in one or more polymorphic forms. Also provided are novel methods for the preparation of the polymorphs of Compound 1, and kits and articles of manufacture of the compositions, and methods of using the compositions to treat various diseases.

Abstract translation: 5-（3-（乙基磺酰基）苯基）-3,8-二甲基-N-（1-甲基哌啶-4-基）-9H-吡啶并[2,3-b]吲哚-7-基的盐酸盐的多晶型形式 甲酰胺（本文称为化合物1），其具有下式：及其组合物，其中化合物1以一种或多种多晶型形式存在。 还提供了用于制备化合物1的多晶型物的新方法，以及组合物的试剂盒和制品，以及使用该组合物治疗各种疾病的方法。

公开(公告)号：US20080009542A1

公开(公告)日：2008-01-10

申请号：US11773892

申请日：2007-07-05

Applicant: Elisabeth Brot ,  Daniel Keefe ,  Brian Haney ,  Nigel Metcalfe ,  Grant Palmer ,  Paul Isbester

Inventor： Elisabeth Brot ,  Daniel Keefe ,  Brian Haney ,  Nigel Metcalfe ,  Grant Palmer ,  Paul Isbester

IPC: A61K31/39 ,  A61P25/00 ,  C07D497/00

CPC classification number: C07D327/08

Abstract: Provided herein is a new form of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathin 10,10-dioxide, which demonstrates higher stability relative to other forms of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin-10,10-dioxide. In particular, this new form affords less dosage critical administration of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathin 10,10-dioxide relative to other forms. The new solid form of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin-10,10-dioxide has been determined and is provided herein. This new solid form of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin-10,10-dioxide can be characterized by any of a number of its properties, including, but not limited to, melting point, differential scanning calorimetry, infrared spectroscopic spectrum or portions thereof, solubility, methods and conditions under which this form is prepared, and/or precipitated from solution, and, when in crystalline form, the crystalline form can be characterized according to the diffraction pattern or portions thereof

Abstract translation: 本文提供了一种新形式的3-氟-7-（2,2,2-三氟乙氧基）吩恶嗪素10,10-二氧化物，其相对于其它形式的3-氟-7-（2,2,2' - 三氟乙氧基）苯氧硫蛋白-10,10-二氧化物。 特别地，相对于其它形式，这种新形式对3-氟-7-（2,2,2-三氟乙氧基）吩恶嗪素10,10-二氧化物的剂量临界施用较少。 已经确定了新的固体形式的3-氟-7-（2,2,2-三氟乙氧基）苯氧硫杂质-10,10-二氧化物，并在此提供。 这种新的固体形式的3-氟-7-（2,2,2-三氟乙氧基）苯氧硫杂-10,10-二氧化物可用其许多特性来表征，包括但不限于熔点差 扫描量热法，红外光谱或其部分，溶解度，制备这种形式的方法和条件和/或从溶液中沉淀出来，并且当以结晶形式时，可以根据衍射图案或其部分来表征结晶形式

公开(公告)号：US20120184568A1

公开(公告)日：2012-07-19

申请号：US13347423

申请日：2012-01-10

Applicant: Pingda Ren ,  Michael Martin ,  Paul Isbester ,  Benjamin S. Lane ,  Jason Kropp

Inventor： Pingda Ren ,  Michael Martin ,  Paul Isbester ,  Benjamin S. Lane ,  Jason Kropp

IPC: A61K31/52 ,  A61P35/00 ,  A61P29/00 ,  C07D475/06

CPC classification number: C07D473/34

Abstract: Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.

Abstract translation: 本文描述了调节激酶活性的化合物的多晶型物质，包括PI3激酶活性，以及​​化合物，药物组合物和治疗与激酶活性（包括P13激酶活性）相关的疾病和病症的方法。 本文还提供了制备化合物，多晶型物及其药物组合物的方法。

公开(公告)号：US20080108808A1

公开(公告)日：2008-05-08

申请号：US11929673

申请日：2007-10-30

Applicant: Jun Feng ,  Stephen Gwaltney ,  Jeffrey Stafford ,  Zhiyuan Zhang ,  Bruce Elder ,  Paul Isbester ,  Grant Palmer ,  Jonathon Salsbury ,  Luckner Ulysse

Inventor： Jun Feng ,  Stephen Gwaltney ,  Jeffrey Stafford ,  Zhiyuan Zhang ,  Bruce Elder ,  Paul Isbester ,  Grant Palmer ,  Jonathon Salsbury ,  Luckner Ulysse

IPC: C07D401/04 ,  C07D401/14 ,  C07D403/04

CPC classification number: C07D403/04 ,  C07D239/545 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14

Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C═NR9; and each L, X, R1, R2, and R3 are as defined herein.

Abstract translation: 提供化合物，药物，试剂盒和方法用于DPP-IV和其它S9蛋白酶，其包含包含以下的化合物：其中M为N或CR 4; Q 1和Q 2各自独立地选自CO，SO，SO 2和C-NR 9 并且每个L，X，R 1，R 2和R 3 3如本文所定义。

公开(公告)号：US20080108807A1

公开(公告)日：2008-05-08

申请号：US11929482

申请日：2007-10-30

Applicant: Jun Feng ,  Stephen Gwaltney ,  Jeffrey Stafford ,  Zhiyuan Zhang ,  Bruce Elder ,  Paul Isbester ,  Grant Palmer ,  Jonathon Salsbury ,  Luckner Ulysse

Inventor： Jun Feng ,  Stephen Gwaltney ,  Jeffrey Stafford ,  Zhiyuan Zhang ,  Bruce Elder ,  Paul Isbester ,  Grant Palmer ,  Jonathon Salsbury ,  Luckner Ulysse

IPC: C07D401/04 ,  C07D401/14 ,  C07D403/04

CPC classification number: C07D403/04 ,  C07D239/545 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14

Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C═NR9; and each L, X, R1, R2, and R3 are as defined herein.

公开(公告)号：US20080003283A1

公开(公告)日：2008-01-03

申请号：US11835295

申请日：2007-08-07

Applicant: Jun Feng ,  Stephen Gwaltney ,  Jeffrey Stafford ,  Zhiyuan Zhang ,  Bruce Elder ,  Paul Isbester ,  Grant Palmer ,  Jonathan Salsbury ,  Luckner Ulysse

Inventor： Jun Feng ,  Stephen Gwaltney ,  Jeffrey Stafford ,  Zhiyuan Zhang ,  Bruce Elder ,  Paul Isbester ,  Grant Palmer ,  Jonathan Salsbury ,  Luckner Ulysse

IPC: A61K31/506 ,  A61K9/20 ,  A61P13/12 ,  A61P19/00 ,  A61P3/10 ,  A61P35/00 ,  A61P37/00 ,  C07D239/08 ,  C12N9/99

CPC classification number: C07D403/04 ,  C07D239/545 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14

Abstract: Compounds are provided for use with DPP-IV of the formula: Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

Abstract translation: 化合物被提供用于下式的DPP-IV：还提供包含这些化合物的药物组合物，试剂盒和制品; 用于制备化合物的方法和中间体; 以及使用所述化合物的方法。

公开(公告)号：US20050261271A1

公开(公告)日：2005-11-24

申请号：US11080992

申请日：2005-03-15

Applicant: Jun Feng ,  Stephen Gwaltney ,  Jeffrey Stafford ,  Zhiyuan Zhang ,  Bruce Elder ,  Paul Isbester ,  Grant Palmer ,  Jonathon Salsbury ,  Luckner Ulysse

Inventor： Jun Feng ,  Stephen Gwaltney ,  Jeffrey Stafford ,  Zhiyuan Zhang ,  Bruce Elder ,  Paul Isbester ,  Grant Palmer ,  Jonathon Salsbury ,  Luckner Ulysse

IPC: C07D239/54 ,  A61K9/08 ,  A61K9/20 ,  A61K31/506 ,  A61K31/513 ,  A61K31/53 ,  A61K31/55 ,  A61P3/10 ,  A61P13/12 ,  A61P17/06 ,  A61P19/02 ,  A61P25/00 ,  A61P29/00 ,  A61P31/18 ,  A61P35/00 ,  A61P37/02 ,  A61P37/06 ,  A61P39/02 ,  A61P43/00 ,  C07D239/545 ,  C07D239/553 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D43/02

CPC classification number: C07D403/04 ,  C07D239/545 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14

Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C═NR9; and each L, X, R1, R2, and R3 are as defined herein.

Abstract translation: 提供化合物，药物，试剂盒和方法用于DPP-IV和其它S9蛋白酶，其包含包含以下的化合物：其中M为N或CR 4; Q 1和Q 2各自独立地选自CO，SO，SO 2和C-NR 9 并且每个L，X，R 1，R 2和R 3 3如本文所定义。

公开(公告)号：US08809349B2

公开(公告)日：2014-08-19

申请号：US13347423

申请日：2012-01-10

Applicant: Pingda Ren ,  Michael Martin ,  Paul Isbester ,  Benjamin S. Lane ,  Jason Kropp

Inventor： Pingda Ren ,  Michael Martin ,  Paul Isbester ,  Benjamin S. Lane ,  Jason Kropp

IPC: C07D473/34 ,  A61K31/52 ,  A61P35/00

CPC classification number: C07D473/34

Abstract: Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.

Abstract translation: 本文描述了调节激酶活性的化合物的多晶型物质，包括PI3激酶活性，以及​​化合物，药物组合物和治疗与激酶活性（包括P13激酶活性）相关的疾病和病症的方法。 本文还提供了制备化合物，多晶型物及其药物组合物的方法。