公开(公告)号：US08829197B2

公开(公告)日：2014-09-09

申请号：US13042193

申请日：2011-03-07

Applicant: Amy E. Tapper ,  Hugh Y. Rienhoff, Jr. ,  Stephan D. Parent ,  Patricia Andres ,  Jason A. Hanko ,  Huamin Zhang

Inventor： Amy E. Tapper ,  Hugh Y. Rienhoff, Jr. ,  Stephan D. Parent ,  Patricia Andres ,  Jason A. Hanko ,  Huamin Zhang

IPC: C07D277/10

CPC classification number: C07D277/12 ,  C07D277/10

Abstract: Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.

Abstract translation: 本文公开了脱氮代硫代聚醚（DADFT-PE）类似物的新盐和多晶型物，以及包含它们的药物组合物及其作为用于治疗疾病的金属螯合剂的应用。 还提供了人或动物受试者中铁和其他金属的螯合方法用于治疗金属过载和毒性。

公开(公告)号：US20100137383A1

公开(公告)日：2010-06-03

申请号：US12502559

申请日：2009-07-14

Applicant: Amy E. Tapper ,  Hugh Y. Rienhoff, JR. ,  Stephan D. Parent ,  Patricia Andres ,  Jason A. Hanko ,  Huamin Zhang

Inventor： Amy E. Tapper ,  Hugh Y. Rienhoff, JR. ,  Stephan D. Parent ,  Patricia Andres ,  Jason A. Hanko ,  Huamin Zhang

IPC: A61K31/426 ,  C07D277/12 ,  A61P43/00 ,  A61P7/06

CPC classification number: C07D277/12 ,  C07D277/10

Abstract: Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.

Abstract translation: 本文公开了脱氮代硫代聚醚（DADFT-PE）类似物的新盐和多晶型物，以及包含它们的药物组合物及其作为用于治疗疾病的金属螯合剂的应用。 还提供了人或动物受试者中铁和其他金属的螯合方法用于治疗金属过载和毒性。

公开(公告)号：US07692038B2

公开(公告)日：2010-04-06

申请号：US11951801

申请日：2007-12-06

Applicant: Eric Hagen ,  Jason A. Hanko ,  Stuart Dimock

Inventor： Eric Hagen ,  Jason A. Hanko ,  Stuart Dimock

IPC: C07C229/00

CPC classification number: C07C237/22 ,  C07B2200/13

Abstract: The present invention relates to crystalline forms of (3S)-3-[N—(N′-(2-tert-butylphenyl)oxamyl)alaninyl]amino-5-(2′,3′,5′,6′-tetrafluorophenoxy)-4-oxopentanoic acid (see formula I). The invention further relates to pharmaceutical compositions comprising such crystalline forms and to the use of said pharmaceutical compositions and said crystalline forms in the treatment of various conditions, particularly in the treatment of liver fibrosis.

Abstract translation: 本发明涉及（3S）-3- [N-（N' - （2-叔丁基苯基）氧戊酰基）乙酰基]氨基-5-（2'，3'，5'，6'-四氟苯氧基 ）-4-氧代戊酸（参见式I）。 本发明还涉及包含这种结晶形式的药物组合物以及所述药物组合物和所述结晶形式在治疗各种病症，特别是用于治疗肝纤维化中的用途。

公开(公告)号：US08846731B2

公开(公告)日：2014-09-30

申请号：US13267285

申请日：2011-10-06

Applicant: Amy E. Tapper ,  Hugh Y. Rienhoff, Jr. ,  Stephan D. Parent ,  Patricia Andres ,  Jason A. Hanko ,  Huamin Zhang

Inventor： Amy E. Tapper ,  Hugh Y. Rienhoff, Jr. ,  Stephan D. Parent ,  Patricia Andres ,  Jason A. Hanko ,  Huamin Zhang

IPC: A61K31/426 ,  C07D277/10 ,  C07D277/12

CPC classification number: C07D277/12 ,  C07D277/10

Abstract: Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogs, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.

Abstract translation: 本文公开了脱氮代硫代聚醚（DADFT-PE）类似物的新盐和多晶型物，以及包含它们的药物组合物及其作为用于治疗疾病的金属螯合剂的应用。 还提供了人或动物受试者中铁和其他金属的螯合方法用于治疗金属过载和毒性。

公开(公告)号：US20120202857A1

公开(公告)日：2012-08-09

申请号：US13198287

申请日：2011-08-04

Applicant: Amy E. Tapper ,  Hugh Y. Rienhoff, JR. ,  Stephan D. Parent ,  Patricia Andres ,  Jason A. Hanko ,  Huamin Zhang

Inventor： Amy E. Tapper ,  Hugh Y. Rienhoff, JR. ,  Stephan D. Parent ,  Patricia Andres ,  Jason A. Hanko ,  Huamin Zhang

IPC: A61K31/426 ,  A61P7/06 ,  A61P31/14 ,  A61P3/10 ,  A61P1/16 ,  A61P39/04 ,  A61P35/02

CPC classification number: C07D277/12 ,  C07D277/10

Abstract: Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.

公开(公告)号：US20110281911A1

公开(公告)日：2011-11-17

申请号：US13057542

申请日：2009-08-03

Applicant: Isabel Kalofonos ,  G. Patrick Stahly ,  William Martin-Doyle ,  Dimitris Kalofonos ,  Jeffrey S. Stults ,  Jason A. Hanko ,  Jeffrey P. Kiplinger

Inventor： Isabel Kalofonos ,  G. Patrick Stahly ,  William Martin-Doyle ,  Dimitris Kalofonos ,  Jeffrey S. Stults ,  Jason A. Hanko ,  Jeffrey P. Kiplinger

IPC: A61K31/4453 ,  A61P21/00 ,  A61P25/00 ,  A61P29/00 ,  A61P25/14 ,  C07D295/108 ,  A61P21/02

CPC classification number: C07D295/108

Abstract: The invention relates to substantially enantiopure crystalline salt forms of (2RS)-I-(4-Ethylphenyl)-2-methyl-3-piperidin-1-ylpropan-1-one. The preparation and characterization of the substantially enantiopure crystalline salt forms according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the substantially enantiopure crystalline salt forms, which are useful to treat and/or prevent various conditions such as pathological muscle contracture, myotome conditions, and spastic paralysis or spasticity caused by various neurologic conditions, and are also useful for the treatment and/or prevention of various types of pain and pathological muscle tension.

Abstract translation: 本发明涉及（2RS）-1-（4-乙基苯基）-2-甲基-3-哌啶-1-基丙-1-酮的基本对映体纯的结晶盐形式。 描述了根据本发明的各种实施方案的基本对映体纯的结晶盐形式的制备和表征。 本发明还涉及含有基本上对映体纯的结晶盐形式的药物组合物，其可用于治疗和/或预防各种病症如病理性肌肉挛缩，肌肉破裂症状，以及由各种神经病症引起的痉挛性麻痹或痉挛状态，并且也是有用的 用于治疗和/或预防各种类型的疼痛和病理性肌肉紧张。

公开(公告)号：US08003684B2

公开(公告)日：2011-08-23

申请号：US11709299

申请日：2007-02-21

Applicant: Jason A. Hanko

Inventor： Jason A. Hanko

IPC: A61K31/381

CPC classification number: C07D333/58 ,  A61K31/381 ,  C07D333/50

Abstract: Crystalline forms of (+)-R-zileuton, which may be used in pharmaceutical applications, are disclosed. Particular single crystalline forms of (+)-R-zileuton are characterized by a variety of properties and physical measurements. As well, methods of producing crystalline (+)-R-zileuton, and using it to inhibit 5-lipoxygenase activity in subjects to treat a number of diseases, are also discussed.

Abstract translation: 公开了可用于药物应用的（+） - R-Zileuton的结晶形式。 （+） - R-Zileuton的特殊单晶形式的特征在于各种性质和物理测量。 此外，还讨论了生产结晶（+） - R-Zileuton，并用于抑制受试者中的5-脂氧合酶活性以治疗许多疾病的方法。

公开(公告)号：US20110160257A1

公开(公告)日：2011-06-30

申请号：US13042193

申请日：2011-03-07

Applicant: Amy E. Tapper ,  Hugh Y. Rienhoff, JR. ,  Stephan D. Parent ,  Patricia Andres ,  Jason A. Hanko ,  Huamin Zhang

Inventor： Amy E. Tapper ,  Hugh Y. Rienhoff, JR. ,  Stephan D. Parent ,  Patricia Andres ,  Jason A. Hanko ,  Huamin Zhang

IPC: A61K31/426 ,  C07D277/12 ,  A61P3/00 ,  A61P43/00 ,  A61P7/00

CPC classification number: C07D277/12 ,  C07D277/10

Abstract: Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.

Abstract translation: 本文公开了脱氮代硫代聚醚（DADFT-PE）类似物的新盐和多晶型物，以及包含它们的药物组合物及其作为用于治疗疾病的金属螯合剂的应用。 还提供了人或动物受试者中铁和其他金属的螯合方法用于治疗金属过载和毒性。

公开(公告)号：US08710087B2

公开(公告)日：2014-04-29

申请号：US13198287

申请日：2011-08-04

Applicant: Amy E. Tapper ,  Hugh Y. Rienhoff, Jr. ,  Stephan D. Parent ,  Patricia Andres ,  Jason A. Hanko ,  Huamin Zhang

Inventor： Amy E. Tapper ,  Hugh Y. Rienhoff, Jr. ,  Stephan D. Parent ,  Patricia Andres ,  Jason A. Hanko ,  Huamin Zhang

IPC: A61K31/426

CPC classification number: C07D277/12 ,  C07D277/10

Abstract: Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.

公开(公告)号：US08203019B2

公开(公告)日：2012-06-19

申请号：US11408609

申请日：2006-04-20

Applicant: Edward D. Daugs ,  Eric J. Hagen ,  Jason A. Hanko ,  David H. Louks

Inventor： Edward D. Daugs ,  Eric J. Hagen ,  Jason A. Hanko ,  David H. Louks

IPC: C07C69/76 ,  C07C69/63 ,  C07C67/02 ,  A61K31/235 ,  A61K31/22

CPC classification number: C07C233/18 ,  A61K9/0053 ,  A61K31/216 ,  C07B2200/07 ,  C07B2200/13 ,  C07C235/78

Abstract: The present invention provides crystalline solid and amorphous forms of (−)-halofenate. The crystalline solid forms may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of conditions associated with blood lipid deposition in a mammal, particularly those diseases related to Type 2 diabetes and hyperlipidemia. The invention also relates to a method for preventing or treating Type 2 diabetes and hyperlipidemia in a mammal comprising the step of administering a therapeutically effective amount of crystalline solid and amorphous forms of (−)-halofenate.

Abstract translation: 本发明提供（ - ） - 卤代苯甲酸酯的结晶固体和无定形形式。 结晶固体形式可以用于各种药物组合物中，并且对于预防和/或治疗与哺乳动物血脂沉积相关的病症，特别是涉及2型糖尿病和高脂血症的疾病特别有效。 本发明还涉及一种用于预防或治疗哺乳动物的2型糖尿病和高脂血症的方法，其包括施用治疗有效量的（ - ） - 氟酸盐的结晶固体和无定形形式的步骤。