公开(公告)号：US08946269B2

公开(公告)日：2015-02-03

申请号：US13223023

申请日：2011-08-31

Applicant: Vincent R. Capodanno ,  Liam Corcoran ,  Michael McNevin ,  Itzia Zoraida Arroyo ,  Robert M. Wenslow ,  Richard G. Ball ,  Eric L. Margelefsky ,  Timothy K. Maher ,  Anjali Pandey

Inventor： Vincent R. Capodanno ,  Liam Corcoran ,  Michael McNevin ,  Itzia Zoraida Arroyo ,  Robert M. Wenslow ,  Richard G. Ball ,  Eric L. Margelefsky ,  Timothy K. Maher ,  Anjali Pandey

IPC: A61K31/44 ,  C07D213/75

CPC classification number: A61K31/44 ,  C07D213/75

Abstract: Provided herein are crystalline forms of a maleate salt of betrixaban, compositions and methods of preparation or use thereof.

Abstract translation: 本文提供的是betrixaban的马来酸盐的结晶形式，组合物及其制备方法或用途。

公开(公告)号：US20110237634A1

公开(公告)日：2011-09-29

申请号：US13133516

申请日：2009-12-07

Applicant: Joseph E. Lynch ,  Yuri Y. Bereznitski ,  Frederick T. Mattrey ,  John L. Leazer, JR. ,  Russell R. Ferlita ,  Jinchu Liu ,  Jungjun Yin ,  Robert M. Wenslow, JR.

Inventor： Joseph E. Lynch ,  Yuri Y. Bereznitski ,  Frederick T. Mattrey ,  John L. Leazer, JR. ,  Russell R. Ferlita ,  Jinchu Liu ,  Jungjun Yin ,  Robert M. Wenslow, JR.

IPC: A61K31/4196 ,  C07D249/08 ,  A61P3/10 ,  A61P3/06 ,  A61P3/04 ,  A61P9/12 ,  A61P25/00

CPC classification number: C07D249/08

Abstract: Novel crystalline salts of 3-[4-(3-ethanesulfonyl-propyl)-bicyclo[2.2.2]oct-1-yl]-4-methyl-5-(2-trifluoromethyl-phenyl)-4H-1,2,4-triazole are potent inhibitors of 11β-hydroxysteroid dehydrogenase Type 1 and are useful for the treatment of conditions associated with Metabolic Syndrome as well as cognitive impairment. The invention also relates to pharmaceutical compositions containing these novel salts, processes to prepare these salts and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes, hyperglycemia, obesity, dyslipidemia, hypertension, and cognitive impairment.

Abstract translation: 3- [4-（3-乙磺酰基 - 丙基） - 二环[2.2.2]辛-1-基] -4-甲基-5-（2-三氟甲基 - 苯基）-4H-1,2的新型结晶盐， 4-三唑是11型的有效抑制剂 - 1类羟基类固醇脱氢酶，可用于治疗与代谢综合征相关的病症以及认知障碍。 本发明还涉及含有这些新型盐的药物组合物，制备这些盐的方法及其药物组合物及其用于治疗2型糖尿病，高血糖症，肥胖症，血脂异常，高血压和认知障碍的用途。

公开(公告)号：US20090221592A1

公开(公告)日：2009-09-03

申请号：US11988197

申请日：2006-07-21

Applicant: Martha E. Ellison ,  Andrey V. Peresypkin ,  Robert M. Wenslow

Inventor： Martha E. Ellison ,  Andrey V. Peresypkin ,  Robert M. Wenslow

IPC: A61K31/4985 ,  C07D487/04 ,  A61P3/10

CPC classification number: C07D487/04

Abstract: The dodecylsulfate salt of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine is a potent inhibitor of dipeptidyl peptidase-IV and is useful for the treatment of Type 2 diabetes. The invention also relates to a crystalline anhydrate of the dodecylsulfate salt as well as a process for its preparation, pharmaceutical compositions containing this novel form and methods of use for the treatment of Type 2 diabetes, hyperglycemia, insulin resistance, and obesity.

Abstract translation: （2R）-4-氧代-4- [3-（三氟甲基）-5,6-二氢[1,2,4]三唑并[4,3-a]吡嗪-7（8H） - 基]的十二烷基硫酸盐 -1-（2,4,5-三氟苯基）丁-2-胺是二肽基肽酶-IV的有效抑制剂，可用于治疗2型糖尿病。 本发明还涉及十二烷基硫酸盐的结晶无水物及其制备方法，含有这种新型形式的药物组合物和用于治疗2型糖尿病，高血糖症，胰岛素抵抗和肥胖症的方法。

公开(公告)号：USRE40794E1

公开(公告)日：2009-06-23

申请号：US11999720

申请日：2002-09-20

Applicant: Karel M. J. Brands ,  Raymond Cvetovich ,  Louis S. Crocker ,  Michael D. Ward ,  Amar J. Mahajan ,  Robert M. Wenslow ,  John M. Williams ,  Daniel R. Sidler ,  Charles Orella ,  Elizabeth S. Fisher ,  Ronald Jobson

Inventor： Karel M. J. Brands ,  Raymond Cvetovich ,  Louis S. Crocker ,  Michael D. Ward ,  Amar J. Mahajan ,  Robert M. Wenslow ,  John M. Williams ,  Daniel R. Sidler ,  Charles Orella ,  Elizabeth S. Fisher ,  Ronald Jobson

IPC: C07D477/20

CPC classification number: C07D477/20

Abstract: A process for preparing a crystalline, carbapenem monosodium salt of formula IIa: characterized by the steps a) adding about 10 to 30% of an organic solvent to an aqueous solution of the carbapenem, b) cooling the resulting solution to less than −5° C., c) adjusting the pH using a solution containing an acid in an organic solvent to give the appropriate pH for crystallization, and d) crystallizing the compound by adding methanol, and a C2-5 alcohol at between −5 and −25° C.

Abstract translation: 制备式IIa的结晶碳青霉烯单钠盐的方法，其特征在于以下步骤：a）向碳青霉烯的水溶液中加入约10至30％的有机溶剂，b）将所得溶液冷却至小于-5℃ c）c）使用在有机溶剂中含有酸的溶液调节pH以得到适当的结晶pH，和d）通过加入甲醇和C2-5醇在-5至-25℃之间使该化合物结晶 C。

公开(公告)号：US20090131465A1

公开(公告)日：2009-05-21

申请号：US12290062

申请日：2008-10-27

Applicant: Alex M. Chen ,  Jennifer R. Foley ,  John Limanto ,  Robert M. Wenslow ,  Karen C. Thompson ,  Andrey V. Peresypkin

Inventor： Alex M. Chen ,  Jennifer R. Foley ,  John Limanto ,  Robert M. Wenslow ,  Karen C. Thompson ,  Andrey V. Peresypkin

IPC: A61K31/438 ,  C07D401/06 ,  A61P3/04 ,  A61P3/10 ,  A61P15/10

CPC classification number: C07D401/06

Abstract: The present invention relates to a process for producing crystalline N-[1-((3R)-1′-{[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-yl]carbonyl}-6-chloro-5-methyl-2,3-dihydrospiro[indene-1,4′-piperidine]-3-yl)-1-methylethyl]acetamide, and novel salts, solvates, hydrates and polymorphs thereof.

Abstract translation: 本发明涉及N- [1 - （（3R）-1' - {[（3S，4R）-1-叔丁基-4-（2,4-二氟苯基）吡咯烷-3-基） 吡啶-4-基]羰基} -6-氯-5-甲基-2,3-二氢螺[茚-1,4'-哌啶] -3-基）-1-甲基乙基]乙酰胺及其新的盐，溶剂合物，水合物及其多晶型物 。

公开(公告)号：US09242917B2

公开(公告)日：2016-01-26

申请号：US14239389

申请日：2012-08-16

Applicant: Gregory L Beutner ,  Robert M Wenslow, Jr. ,  Eric J Choi ,  Clinton Scott Shultz ,  Jeremy Scott ,  Juan D Arredondo ,  Laura Artino

Inventor： Gregory L Beutner ,  Robert M Wenslow, Jr. ,  Eric J Choi ,  Clinton Scott Shultz ,  Jeremy Scott ,  Juan D Arredondo ,  Laura Artino

IPC: C07K5/08 ,  C07C35/04 ,  C07K5/083 ,  C07D403/12 ,  C07D498/16 ,  C07K5/12 ,  C07C67/14 ,  C07C69/013 ,  C07C69/12 ,  C07C269/04 ,  C07C271/34 ,  A61K38/00

CPC classification number: C07C35/04 ,  A61K38/00 ,  C07C67/14 ,  C07C69/013 ,  C07C69/12 ,  C07C269/04 ,  C07C271/34 ,  C07D403/12 ,  C07D498/16 ,  C07K5/0808 ,  C07K5/126

Abstract: The present invention relates to different forms of a HCV inhibitory compound.

Abstract translation: 本发明涉及不同形式的HCV抑制化合物。

公开(公告)号：US08129413B2

公开(公告)日：2012-03-06

申请号：US11921824

申请日：2006-06-23

Applicant: Ralph Calabria ,  Yu Cheng ,  Russell R. Ferlita ,  Ashkan Kamali ,  Jerry A. Murry ,  David Mathre ,  Andrey V. Peresypkin ,  Karen Thompson ,  Jian Wang ,  Robert M. Wenslow

Inventor： Ralph Calabria ,  Yu Cheng ,  Russell R. Ferlita ,  Ashkan Kamali ,  Jerry A. Murry ,  David Mathre ,  Andrey V. Peresypkin ,  Karen Thompson ,  Jian Wang ,  Robert M. Wenslow

IPC: A61K31/454 ,  C07D401/06

CPC classification number: C07D401/06

Abstract: The present invention relates to a process for producing N-{(1S)-1-[2-(1-{[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]carbonyl}piperidin-4-yl)-5-chlorophenyl]ethyl}acetamide, and novel crystalline salts, hydrates, solvates, and polymorphic forms thereof.

Abstract translation: 本发明涉及生产N - {（1S）-1- [2-（1 - {[（3S，4R）-1-叔丁基-4-（2,4-二氟苯基）吡咯烷-3 - 基]羰基}哌啶-4-基）-5-氯苯基]乙基}乙酰胺，以及新的结晶盐，水合物，溶剂合物及其多晶型物。

公开(公告)号：US07145002B2

公开(公告)日：2006-12-05

申请号：US10485319

申请日：2002-09-20

Applicant: Karel M. J. Brands ,  Raymond Cvetovich ,  Louis S. Crocker ,  Michael D. Ward ,  Amar J. Mahajan ,  Robert M. Wenslow ,  John M. Williams ,  Daniel R. Sidler ,  Charles Orella ,  Elizabeth S. Fisher ,  Ronald Jobson

Inventor： Karel M. J. Brands ,  Raymond Cvetovich ,  Louis S. Crocker ,  Michael D. Ward ,  Amar J. Mahajan ,  Robert M. Wenslow ,  John M. Williams ,  Daniel R. Sidler ,  Charles Orella ,  Elizabeth S. Fisher ,  Ronald Jobson

IPC: C07D477/20

CPC classification number: C07D477/20

Abstract: A process for preparing a crystalline, carbapenem monosodium salt of formula IIa: characterized by the steps a) adding about 10 to 30% of an organic solvent to an aqueous solution of the carbapenem, b) cooling the resulting solution to less than −5° C., c) adjusting the pH using a solution containing an acid in an organic solvent to give the appropriate pH for crystallization, and d) crystallizing the compound by adding methanol, and a C2-5 alcohol at between −5 and −25° C.

Abstract translation: 制备式IIa的结晶碳青霉烯单钠盐的方法，其特征在于以下步骤：a）向碳青霉烯的水溶液中加入约10至30％的有机溶剂，b）将所得溶液冷却至小于-5℃ c）c）使用在有机溶剂中含有酸的溶液调节pH以得到适当的结晶pH，和d）通过加入甲醇和C 2-5醇来使化合物结晶 在-5和-25℃之间

公开(公告)号：US20120095019A1

公开(公告)日：2012-04-19

申请号：US13223038

申请日：2011-08-31

Applicant: Uma Sinha ,  George A. Mansoor ,  Anne Hermanowski Vosatka ,  Vincent R. Capodanno ,  Robert M. Wenslow ,  Richard G. Ball ,  Eric L. Margelefsky ,  Timothy K. Maher ,  Itzia Zoraida Arroyo ,  Brett Lauring ,  Liam Corcoran ,  William Denney ,  Michael McNevin ,  Anjali Pandey

Inventor： Uma Sinha ,  George A. Mansoor ,  Anne Hermanowski Vosatka ,  Vincent R. Capodanno ,  Robert M. Wenslow ,  Richard G. Ball ,  Eric L. Margelefsky ,  Timothy K. Maher ,  Itzia Zoraida Arroyo ,  Brett Lauring ,  Liam Corcoran ,  William Denney ,  Michael McNevin ,  Anjali Pandey

IPC: A61K31/44 ,  A61P7/02 ,  A61K31/496

CPC classification number: A61K31/277 ,  A61K31/343 ,  A61K31/435 ,  A61K31/44 ,  A61K31/496 ,  A61K45/06 ,  A61K2300/00

Abstract: This invention is directed to methods of inhibiting coagulation or treating thrombosis using a factor Xa inhibitor and a P-glycoprotein (Pgp) inhibitor. The invention is also directed to formulations used in the methods.

Abstract translation: 本发明涉及使用因子Xa抑制剂和P-糖蛋白（Pgp）抑制剂来抑制凝血或治疗血栓形成的方法。 本发明还涉及用于该方法的制剂。

公开(公告)号：US20120071519A1

公开(公告)日：2012-03-22

申请号：US13223023

申请日：2011-08-31

Applicant: Vincent R. Capodanno ,  Liam Corcoran ,  Michael McNevin ,  Itzia Zoraida Arroyo ,  Robert M. Wenslow ,  Richard G. Ball ,  Eric L. Margelefsky ,  Timothy K. Maher ,  Anjali Pandey

Inventor： Vincent R. Capodanno ,  Liam Corcoran ,  Michael McNevin ,  Itzia Zoraida Arroyo ,  Robert M. Wenslow ,  Richard G. Ball ,  Eric L. Margelefsky ,  Timothy K. Maher ,  Anjali Pandey

IPC: A61K31/44 ,  A61P7/02 ,  A61P9/10 ,  C07D213/75

CPC classification number: A61K31/44 ,  C07D213/75

Abstract: Provided herein are crystalline forms of a maleate salt of betrixaban, compositions and methods of preparation or use thereof.

Abstract translation: 本文提供的是betrixaban的马来酸盐的结晶形式，组合物及其制备方法或用途。