公开(公告)号：US08906926B2

公开(公告)日：2014-12-09

申请号：US13649430

申请日：2012-10-11

Applicant: Kelly Sullivan Kraft

Inventor： Kelly Sullivan Kraft

IPC: A61K31/495 ,  A61K38/28 ,  C07D241/08 ,  A61K38/00

CPC classification number: A61K31/495 ,  A61K9/0073 ,  A61K9/1617 ,  A61K9/1694 ,  A61K38/00 ,  A61K38/26 ,  A61K38/28 ,  A61K2121/00 ,  C07D241/08

Abstract: Disclosed are drug delivery systems for the delivery of small molecule and macromolecular drugs. More particularly, disclosed are substituted analogs of 3,6-di(alkyl-4 aminobutyl)-2,5-diketopiperazine (which may also be referred to DKP), their use in the formulation of both small molecule and macromolecular drugs including therapeutic, prophylactic and diagnostic agents, stabilizing agents and systems for their delivery.

Abstract translation: 公开了用于递送小分子和大分子药物的药物递送系统。 更具体地，公开了3,6-二（烷基-4-氨基丁基）-2,5-二酮哌嗪（其也可以称为DKP）的取代的类似物，它们在小分子和大分子药物的制剂中的用途，包括治疗， 预防和诊断剂，稳定剂和用于其递送的系统。

公开(公告)号：US20130289278A1

公开(公告)日：2013-10-31

申请号：US13834106

申请日：2013-03-15

Applicant: Kelly Sullivan Kraft ,  John J. Freeman ,  Paul Serwinski ,  Vinnie Pavia ,  Otto Phanstiel, IV ,  Navneet Kaur

Inventor： Kelly Sullivan Kraft ,  John J. Freeman ,  Paul Serwinski ,  Vinnie Pavia ,  Otto Phanstiel, IV ,  Navneet Kaur

IPC: C07D241/08 ,  C07C67/39 ,  C07C201/12

CPC classification number: C07D241/08 ,  C07C67/30 ,  C07C67/39 ,  C07C201/12 ,  C07C69/60 ,  C07C205/43

Abstract: Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4-nitrophenyl, diphenylphosphoryl azide, pivaloyl chloride, chlorosulfonyl isocyanate, p-nitrophenol, MEF, trifluoroacetyl and chlorine, for example, ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl-diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput.

公开(公告)号：US20130053309A1

公开(公告)日：2013-02-28

申请号：US13649430

申请日：2012-10-11

Applicant: Kelly Sullivan Kraft

Inventor： Kelly Sullivan Kraft

IPC: A61K38/28 ,  A61P3/10

CPC classification number: A61K31/495 ,  A61K9/0073 ,  A61K9/1617 ,  A61K9/1694 ,  A61K38/00 ,  A61K38/26 ,  A61K38/28 ,  A61K2121/00 ,  C07D241/08

Abstract: Disclosed are drug delivery systems for the delivery of small molecule and macromolecular drugs. More particularly, disclosed are substituted analogs of 3,6-di(alkyl-4 aminobutyl)-2,5-diketopiperazine (which may also be referred to DKP), their use in the formulation of both small molecule and macromolecular drugs including therapeutic, prophylactic and diagnostic agents, stabilizing agents and systems for their delivery.

公开(公告)号：US08314106B2

公开(公告)日：2012-11-20

申请号：US12649210

申请日：2009-12-29

Applicant: Kelly Sullivan Kraft

Inventor： Kelly Sullivan Kraft

IPC: A61K31/4965 ,  C07D241/00

CPC classification number: A61K31/495 ,  A61K9/0073 ,  A61K9/1617 ,  A61K9/1694 ,  A61K38/00 ,  A61K38/26 ,  A61K38/28 ,  A61K2121/00 ,  C07D241/08

Abstract: Disclosed are drug delivery systems for the delivery of small molecule and macromolecular drugs. More particularly, disclosed are substituted analogs of 3,6-di(alkyl-4 aminobutyl)-2,5-diketopiperazine (which may also be referred to DKP), their use in the formulation of both small molecule and macromolecular drugs including therapeutic, prophylactic and diagnostic agents, stabilizing agents and systems for their delivery.

Abstract translation: 公开了用于递送小分子和大分子药物的药物递送系统。 更具体地，公开了3,6-二（烷基-4-氨基丁基）-2,5-二酮哌嗪（其也可以称为DKP）的取代的类似物，它们在小分子和大分子药物的制剂中的用途，包括治疗， 预防和诊断剂，稳定剂和用于其递送的系统。

公开(公告)号：US20110158935A1

公开(公告)日：2011-06-30

申请号：US12649210

申请日：2009-12-29

Applicant: Kelly Sullivan Kraft

Inventor： Kelly Sullivan Kraft

IPC: A61K38/28 ,  C07D241/08 ,  A61K38/26 ,  A61K38/23 ,  A61K38/02 ,  A61K31/7088 ,  A61K31/404 ,  A61K31/727 ,  A61K31/352 ,  A61K31/519 ,  A61K31/4985 ,  A61K31/7072 ,  A61K31/708 ,  A61K31/53 ,  A61K38/47 ,  A61P31/18 ,  A61P3/10 ,  A61P15/10 ,  A61K38/12 ,  A61K31/27

CPC classification number: A61K31/495 ,  A61K9/0073 ,  A61K9/1617 ,  A61K9/1694 ,  A61K38/00 ,  A61K38/26 ,  A61K38/28 ,  A61K2121/00 ,  C07D241/08

Abstract: Disclosed are drug delivery systems for the delivery of small molecule and macromolecular drugs. More particularly, disclosed are substituted analogs of 3,6-di(alkyl-4 aminobutyl)-2,5-diketopiperazine (which may also be referred to DKP), their use in the formulation of both small molecule and macromolecular drugs including therapeutic, prophylactic and diagnostic agents, stabilizing agents and systems for their delivery.

Abstract translation: 公开了用于递送小分子和大分子药物的药物递送系统。 更具体地，公开了3,6-二（烷基-4-氨基丁基）-2,5-二酮哌嗪（其也可以称为DKP）的取代的类似物，它们在小分子和大分子药物的制剂中的用途，包括治疗， 预防和诊断剂，稳定剂和用于其递送的系统。