公开(公告)号：US10744105B2

公开(公告)日：2020-08-18

申请号：US16212428

申请日：2018-12-06

Applicant: Emisphere Technologies, Inc.

Inventor： Halina Levchik ,  Shingai Majuru ,  Brahma Singh ,  Jamila Harris

IPC: A61K31/197 ,  A61K45/06 ,  A61K31/198 ,  C07C235/60 ,  A61K9/20 ,  A61J3/02

Abstract: The present invention relates to crystalline polymorphic forms of monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate (“SNAC”), including two hydrates, a methanol solvate, and an ethanol solvate, of SNAC. More specifically, the present invention provide six polymorphic forms of SNAC (hereafter referred to as Forms I-VI). The present invention also provides an amorphous form of SNAC.

公开(公告)号：US20200071263A1

公开(公告)日：2020-03-05

申请号：US16490424

申请日：2007-08-30

Applicant: Emisphere Technologies, Inc.

Inventor： William Elliot Bay ,  Joseph Norman Bernadino ,  George Frederick Klein ,  Yi Ren ,  Pingsheng Zhang

IPC: C07C231/12 ,  C07C231/24

Abstract: Disclosed are improved methods for the synthesis of N-(8-[2-hydroxybenzoyl]-amino) caprylic acid. Certain compounds have been found useful for preventing the formation of a colored impurity when included in an ester hydrolysis reaction. Conducting ester hydrolysis in anaerobic conditions has also been found to minimize the formation of the color impurity. Also disclosed are improved methods for synthesizing the sodium salt of N-(8-[2-hydroxybenzoyl]-amino) caprylic acid.

公开(公告)号：US20170326087A1

公开(公告)日：2017-11-16

申请号：US15668236

申请日：2017-08-03

Applicant: Emisphere Technologies, Inc.

Inventor： Halina Levchik ,  Shingai Majuru ,  Brahma Singh ,  Jamila Harris

IPC: A61K31/197 ,  A61J3/02 ,  A61K9/20

CPC classification number: A61K31/197 ,  A61J3/02 ,  A61K9/2095 ,  A61K31/198 ,  A61K45/06 ,  A61K2300/00 ,  C07C235/60

Abstract: The present invention relates to crystalline polymorphic forms of monosodium N-[8-(2-hydroxybenzoyl)amino] caprylate (“SNAC”), including two hydrates, a methanol solvate, and an ethanol solvate, of SNAC. More specifically, the present invention provide six polymorphic forms of SNAC (hereafter referred to as Forms I-VI). The present invention also provides an amorphous form of SNAC.

公开(公告)号：US20160184251A1

公开(公告)日：2016-06-30

申请号：US15049313

申请日：2016-02-22

Applicant: Emisphere Technologies, Inc.

Inventor： Halina LEVCHIK ,  Shingai MAJURU ,  Brahma SINGH ,  Jamila HARRIS

IPC: A61K31/198 ,  A61K9/20 ,  A61J3/02 ,  A61K45/06

CPC classification number: A61K31/197 ,  A61J3/02 ,  A61K9/2095 ,  A61K31/198 ,  A61K45/06 ,  A61K2300/00 ,  C07C235/60

Abstract: The present invention relates to crystalline polymorphic forms of monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate (“SNAC”), including two hydrates, a methanol solvate, and an ethanol solvate, of SNAC. More specifically, the present invention provide six polymorphic forms of SNAC (hereafter referred to as Forms I-VI). The present invention also provides an amorphous form of SNAC.

Abstract translation: 本发明涉及SNAC的包括两种水合物，甲醇溶剂化物和乙醇溶剂合物的N- [8-（2-羟基苯甲酰基）氨基]辛酸单钠（“SNAC”）的结晶多晶形式。 更具体地说，本发明提供了六种多晶型的SNAC（以下称为形式I-VI）。 本发明还提供了无定形形式的SNAC。

公开(公告)号：US09321719B2

公开(公告)日：2016-04-26

申请号：US14138787

申请日：2013-12-23

Applicant: Emisphere Technologies, Inc.

Inventor： Halina Levchik ,  Shingai Majuru ,  Brahma Singh ,  Jamila Harris

IPC: C07C235/60

CPC classification number: A61K31/197 ,  A61J3/02 ,  A61K9/2095 ,  A61K31/198 ,  A61K45/06 ,  A61K2300/00 ,  C07C235/60

Abstract: The present invention relates to crystalline polymorphic forms of monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate (“SNAC”), including two hydrates, a methanol solvate, and an ethanol solvate, of SNAC. More specifically, the present invention provide six polymorphic forms of SNAC (hereafter referred to as Forms I-VI). The present invention also provides an amorphous form of SNAC.

Abstract translation: 本发明涉及SNAC的包括两种水合物，甲醇溶剂化物和乙醇溶剂合物的N- [8-（2-羟基苯甲酰基）氨基]辛酸单钠（“SNAC”）的结晶多晶形式。 更具体地说，本发明提供了六种多晶型的SNAC（以下称为形式I-VI）。 本发明还提供了无定形形式的SNAC。

公开(公告)号：US20140031287A1

公开(公告)日：2014-01-30

申请号：US13971680

申请日：2013-08-20

Applicant: Emisphere Technologies, Inc.

Inventor： Robert Jason Herr ,  Louis Nickolaus Jungheim ,  John McNeill McGill ,  Kenneth Jeff Thrasher ,  Muralikrishna Valluri

IPC: C07D263/48 ,  A61K31/4164 ,  A61K38/22 ,  A61K38/26

CPC classification number: C07D263/48 ,  A61K31/4164 ,  A61K38/22 ,  A61K38/26 ,  A61K47/22 ,  C07D233/64 ,  C07D249/06 ,  C07D249/08 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D285/12 ,  C07D409/04 ,  C07D413/04

Abstract: The present invention relates to novel compounds, methods, and formulations useful for the oral delivery of a GLP-1 compound or an MC4 agonist peptide.

Abstract translation: 本发明涉及可用于口服递送GLP-1化合物或MC4激动剂肽的新化合物，方法和制剂。

公开(公告)号：US20020155993A1

公开(公告)日：2002-10-24

申请号：US10125836

申请日：2002-04-19

Applicant: Emisphere Technologies, Inc.

Inventor： Sam J. Milstein

IPC: A61K038/18 ,  A61K038/27 ,  A61K031/726 ,  A61K031/70 ,  A61K031/715 ,  A61K031/225 ,  A61K031/495

CPC classification number: A61K9/5031 ,  A61K9/1617 ,  A61K31/35 ,  A61K31/70 ,  A61K38/16 ,  A61K38/21 ,  A61K38/28 ,  C07C229/42 ,  C07C233/55 ,  C07C233/63 ,  C07C233/87 ,  C07C235/38 ,  C07C235/64 ,  C07C235/84 ,  C07C237/22 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2601/18 ,  Y10S977/906 ,  Y10S977/926

Abstract: Compositions useful in the delivery of active agents are provided. These delivery compositions include (a) an active agent; and (b) a carrier of at least one mono-C-substituted or di-C-substituted diketopiperazine. Methods for preparing these compositions and administering these compositions are also provided.

公开(公告)号：US20020127202A1

公开(公告)日：2002-09-12

申请号：US10005511

申请日：2001-11-07

Applicant: Emisphere Technologies, Inc.

Inventor： Andrea Leone-Bay ,  Sam J. Milstein ,  Donald J. Sarrubi ,  Harry Leipold

IPC: A61K038/21 ,  A61K038/28 ,  A61K031/715 ,  A61K038/18 ,  A61K038/20

CPC classification number: C07D209/48 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0056 ,  A61K9/1617 ,  A61K9/4858 ,  A61K31/727 ,  A61K38/212 ,  A61K38/23 ,  A61K38/27 ,  A61K38/29 ,  A61K47/18 ,  A61K47/183 ,  A61K47/20 ,  A61K47/22 ,  A61K47/541 ,  C07C229/42 ,  C07C233/34 ,  C07C233/47 ,  C07C233/48 ,  C07C233/51 ,  C07C233/52 ,  C07C233/54 ,  C07C233/55 ,  C07C233/63 ,  C07C233/69 ,  C07C233/81 ,  C07C233/83 ,  C07C233/84 ,  C07C233/87 ,  C07C235/12 ,  C07C235/24 ,  C07C235/34 ,  C07C235/38 ,  C07C235/52 ,  C07C235/56 ,  C07C235/60 ,  C07C235/64 ,  C07C235/66 ,  C07C235/74 ,  C07C235/82 ,  C07C237/12 ,  C07C237/20 ,  C07C237/36 ,  C07C237/40 ,  C07C237/42 ,  C07C243/38 ,  C07C259/06 ,  C07C271/28 ,  C07C271/54 ,  C07D211/62 ,  C07D213/81 ,  C07D213/82 ,  C07D239/42 ,  C07D241/24 ,  C07D257/04 ,  C07D295/192 ,  C07D311/12 ,  C07D311/24 ,  C07D311/30

Abstract: Modified amino acid compounds useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

公开(公告)号：US20020102286A1

公开(公告)日：2002-08-01

申请号：US10062829

申请日：2002-01-31

Applicant: Emisphere Technologies, Inc.

Inventor： Martin L. Kantor ,  Evgueni Barantsevitch ,  Sam J. Milstein

IPC: A61K007/46

CPC classification number: A61Q13/00 ,  A23L27/72 ,  A61K8/11 ,  A61K2800/412 ,  B01F17/0028 ,  B01F17/005 ,  B01J13/02 ,  B01J13/14 ,  Y10T442/2303

Abstract: This invention provides an encapsulated fragrance in which the fragrance is controlled can be released by exposing the encapsulated fragrance to a solution of a predetermined pH. The invention also contemplates a process for preparing encapsulated fragrances.

Abstract translation: 本发明提供一种包封的香料，其中香料被控制可以通过将包封的香料暴露于预定pH的溶液来释放。 本发明还考虑了一种制备包封香料的方法。

公开(公告)号：US20020001591A1

公开(公告)日：2002-01-03

申请号：US09862013

申请日：2001-05-21

Applicant: Emisphere Technologies, Inc.

Inventor： Noemi B. Santiago ,  Susan Haas ,  Andrea Leone-Bay ,  Sam J. Milstein ,  Evgueni Barantsevitch

IPC: A61K039/00

CPC classification number: A61K9/1617 ,  A61K9/1641 ,  A61K31/16 ,  A61K31/352 ,  A61K31/727 ,  A61K38/212 ,  A61K38/23 ,  A61K38/25 ,  A61K38/27 ,  A61K39/12 ,  A61K39/39 ,  A61K47/183 ,  A61K2039/5252 ,  A61K2039/542 ,  A61K2039/552 ,  A61K2039/55544 ,  A61K2039/55555 ,  C07C229/42 ,  C07C233/55 ,  C07C233/63 ,  C07C233/87 ,  C07C235/38 ,  C07C235/64 ,  C07C235/84 ,  C07C237/22 ,  C07C279/14 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07K1/1077 ,  C07K5/06043 ,  C12N2720/10034

Abstract: The present invention relates to compositions and methods for orally delivering antigens. The antigen and an adjuvant are combined with an acylated amino acid or polyamino acid and, a sulfonated amino acids or polyamino acid, or a salt of the foregoing.

Abstract translation: 本发明涉及用于口服递送抗原的组合物和方法。 将抗原和佐剂与酰化氨基酸或聚氨基酸，磺化氨基酸或聚氨基酸或前述的盐组合。