公开(公告)号：US09833428B2

公开(公告)日：2017-12-05

申请号：US14269055

申请日：2014-05-02

Applicant: LEO Laboratories Limited

Inventor： Marc Barry Brown ,  Michael Crothers ,  Tahir Nazir

IPC: A61K31/25 ,  A61P35/00 ,  A61K31/22 ,  A61K9/00 ,  A61K9/06 ,  A61K47/10 ,  A61K47/12 ,  A61K47/32 ,  A61K31/215 ,  A61K47/38 ,  A61K36/47

CPC classification number: A61K31/22 ,  A61K9/0014 ,  A61K9/06 ,  A61K31/215 ,  A61K36/47 ,  A61K47/10 ,  A61K47/12 ,  A61K47/32 ,  A61K47/38

Abstract: Ingenol angelate is a potent anticancer agent, and can be stabilized by dissolving it in an aprotic solvent in the presence of an acidic buffer.

公开(公告)号：US20170258770A1

公开(公告)日：2017-09-14

申请号：US15529631

申请日：2015-11-27

Applicant: LEO Laboratories Limited

Inventor： Casper Clemmensen ,  Johan Selmer ,  Kim Mark Knudsen

IPC: A61K31/42 ,  A61K9/06 ,  A61K9/00

CPC classification number: A61K31/42 ,  A61K9/0014 ,  A61K9/06 ,  A61K31/41

Abstract: The invention relates to the treatment of actinic keratosis on the full face or 250 cm2 on the chest with ingenol 3-(3,5-diethylisoxazole-4-carboxylate).

公开(公告)号：US09708286B2

公开(公告)日：2017-07-18

申请号：US14748925

申请日：2015-06-24

Applicant: LEO Laboratories Limited

Inventor： Gunnar Grue-Sørensen ,  Xifu Liang ,  Thomas Högberg ,  Kristoffer Månsson ,  Per Vedsø ,  Thomas Vifian

IPC: C07C271/34 ,  C07D333/38 ,  C07C271/36 ,  C07C271/38 ,  C07D249/06 ,  C07D261/18 ,  C07D277/32 ,  C07D295/21 ,  C07D309/08 ,  C07D401/04 ,  C07D471/04 ,  C07D495/04 ,  C07D265/36 ,  C07D271/08 ,  C07D277/587 ,  C07D295/205 ,  C07D307/00 ,  C07D307/94 ,  C07D405/06 ,  C07D513/04 ,  A61K31/365 ,  A61K31/381 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/472 ,  A61K31/502 ,  A61K31/5375 ,  A61K31/538 ,  C07D209/42 ,  C07D217/26 ,  C07D231/14 ,  C07D231/56 ,  C07D237/28 ,  C07D249/04

CPC classification number: C07D261/18 ,  A61K31/365 ,  A61K31/381 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/472 ,  A61K31/502 ,  A61K31/5375 ,  A61K31/538 ,  C07C271/34 ,  C07C271/36 ,  C07C271/38 ,  C07C2603/86 ,  C07D209/08 ,  C07D209/42 ,  C07D213/79 ,  C07D215/50 ,  C07D217/26 ,  C07D231/14 ,  C07D231/56 ,  C07D233/90 ,  C07D237/28 ,  C07D239/28 ,  C07D249/04 ,  C07D249/06 ,  C07D261/20 ,  C07D263/34 ,  C07D265/36 ,  C07D271/08 ,  C07D277/32 ,  C07D277/56 ,  C07D277/587 ,  C07D295/182 ,  C07D295/205 ,  C07D295/21 ,  C07D307/00 ,  C07D307/68 ,  C07D307/94 ,  C07D309/08 ,  C07D333/38 ,  C07D333/40 ,  C07D401/04 ,  C07D405/06 ,  C07D471/04 ,  C07D493/08 ,  C07D495/04 ,  C07D513/04

Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.

公开(公告)号：US20170119719A1

公开(公告)日：2017-05-04

申请号：US15351042

申请日：2016-11-14

Applicant: LEO Laboratories Limited

Inventor： Steven Martin Ogbourne

IPC: A61K31/22 ,  A61K9/00 ,  A61K9/06

CPC classification number: A61K31/22 ,  A61K9/0014 ,  A61K9/06

Abstract: The present invention relates to novel crystalline forms of ingenol ingenol-3-angelate and methods of preparation and use thereof. More specifically, the invention relates to a novel crystalline form and purified forms of the compound of Formula 1 (ingenol-3-mebutate; ingenol-3-angelate; isoform ‘b’; PEP005), which is characterized by, for example, attenuated total reflectance Fourier transform infrared (FTIR-ATR) spectroscopy, single crystal X-Ray crystallography (XRC), X-ray powder diffraction, and, Differential Scanning calorimetry (DSC), and methods of preparation and use thereof.

公开(公告)号：US20160128965A1

公开(公告)日：2016-05-12

申请号：US14738784

申请日：2015-06-12

Applicant: LEO Laboratories Limited

Inventor： Per-Ola Arvidsson ,  Edit Farkas ,  Chinar Sami Saeed ,  Mikkel Krogh-Madsen ,  Andre Huss Eriksson ,  Kresten Skak ,  Karsten Petersson

IPC: A61K31/22 ,  A61K9/00 ,  A61K9/107 ,  A61K9/06

CPC classification number: A61K31/22 ,  A61K9/0014 ,  A61K9/06 ,  A61K9/1075 ,  A61K9/1272 ,  A61K31/60

Abstract: Novel aqueous topical gel compositions comprising ingenol-3-angelate.

公开(公告)号：US20160120835A1

公开(公告)日：2016-05-05

申请号：US14897270

申请日：2014-06-12

Applicant: LEO LABORATORIES LIMITED

Inventor： Edit FARKAS ,  Chinar Sami SAEED ,  Mikkel KROGH-MADSEN ,  Per-Ola ARVIDSSON

IPC: A61K31/22 ,  A61K9/00 ,  A61K9/107

CPC classification number: A61K31/22 ,  A61K9/0014 ,  A61K9/107 ,  A61K31/235

Abstract: The invention provides a topical composition for cutaneous application which is an oil-in-water emulsion comprising (a) an oily phase, (b) an ingenol derivative in dissolved form; (c) an aqueous phase buffered to a p H of below 4.5, (d) at least one surfactant.

Abstract translation: 本发明提供了一种皮肤应用的局部用组合物，其是水包油乳液，其包含（a）油相，（b）溶解形式的茚满醇衍生物; （c）缓冲至pH低于4.5的水相，（d）至少一种表面活性剂。

公开(公告)号：US20150320679A1

公开(公告)日：2015-11-12

申请号：US14652097

申请日：2013-12-11

Applicant: LEO LABORATORIES LIMITED

Inventor： Per-Ola Arvidsson ,  Edit Farkas ,  Chinar Sami Saeed ,  Mikkel Krogh-Madsen ,  Andrea Huss Eriksson ,  Kresten Skak ,  Karsten Petersson

IPC: A61K9/00 ,  A61K9/06 ,  A61K31/22 ,  A61K31/60

CPC classification number: A61K31/22 ,  A61K9/0014 ,  A61K9/06 ,  A61K9/1075 ,  A61K9/1272 ,  A61K31/60

Abstract: Novel aqueous topical gel compositions comprising ingenol-3-angelate.

Abstract translation: 新颖的水性局部凝胶组合物，其包含美尼康3-angelate。

公开(公告)号：US20130251782A1

公开(公告)日：2013-09-26

申请号：US13839975

申请日：2013-03-15

Applicant: LEO LABORATORIES LIMITED

Inventor： Lotte Groth Ladefoged ,  Per-Ola Arvidsson ,  Karsten Petersson

IPC: A61K9/70 ,  A61K31/22

CPC classification number: A61K31/22 ,  A61K9/0014 ,  A61K9/06 ,  A61K9/7023 ,  A61K9/703 ,  A61K47/10 ,  A61K47/12 ,  A61K47/38

Abstract: The present invention relates to formulations of ingenol mebutate and methods of preparation and use thereof. More specifically, the invention relates to formulations of ingenol-3-mebutate applied to the skin with occlusion, and methods for treating or preventing diseases or conditions.

Abstract translation: 本发明涉及内酯醇制剂的制剂及其制备方法和用途。 更具体地，本发明涉及应用于具有闭塞的皮肤的美烯醇-3-甲酸酯的制剂，以及用于治疗或预防疾病或病症的方法。