公开(公告)号：US09249086B2

公开(公告)日：2016-02-02

申请号：US14419125

申请日：2013-08-02

Applicant: Photocure ASA

Inventor： Jon Erik Brænden ,  Colin Barry Charnock ,  Aslak Godal ,  Jo Klaveness ,  Nils Olav Nilsen

IPC: C07C229/24 ,  A61K41/00 ,  C07C229/22

CPC classification number: C07C229/24 ,  A61K41/0061 ,  C07C229/22

Abstract: The invention relates to new derivatives of 5-aminolevulinic acid (5-ALA) and their use as photosensitizing agents. In particular, it relates to compounds of general formula I and their pharmaceutically acceptable salts, to methods for preparing such compounds and their medical and cosmetic use, for example in methods of photodynamic therapy and diagnosis: wherein R1 represents a hydrogen atom or an optionally substituted alkyl or cycloalkyl group; R2, each of which may be the same or different, represents a hydrogen atom or an optionally substituted alkyl group; and X is a linking group.

Abstract translation: 本发明涉及5-氨基乙酰丙酸（5-ALA）的新衍生物及其作为光敏剂的用途。 具体地说，本发明涉及通式Ⅰ化合物及其药学上可接受的盐，制备这些化合物的方法及其医疗和化妆品用途，例如在光动力学治疗和诊断方法中：其中R1表示氢原子或任选取代的 烷基或环烷基; R2各自可以相同或不同，表示氢原子或任选取代的烷基; X是连接基团。

公开(公告)号：US20150231407A1

公开(公告)日：2015-08-20

申请号：US14700501

申请日：2015-04-30

Applicant: PHOTOCURE ASA

Inventor： Bjørn Klem ,  Morten Groseth

IPC: A61N5/06 ,  A61K41/00

CPC classification number: A61N5/062 ,  A61B5/0084 ,  A61K9/0036 ,  A61K31/221 ,  A61K41/0061 ,  A61N5/0603 ,  A61N2005/0608 ,  A61N2005/0611 ,  A61N2005/0626 ,  A61N2005/0645 ,  A61N2005/0652 ,  A61N2005/0658

Abstract: An irradiation device for insertion into an orifice of the body for providing photodynamic therapy or diagnosis comprises: a housing adapted to be fully inserted and secured in the orifice, the housing enclosing an LED lamp system and a power source for powering the LED lamp system wherein the device is independently operational while located within the orifice.

Abstract translation: 用于插入身体的用于提供光动力学治疗或诊断的孔的照射装置包括：适于完全插入并固定在孔中的壳体，壳体包围LED灯系统和为LED灯系统供电的电源，其中， 该装置在位于孔内时独立地工作。

公开(公告)号：WO2012004399A1

公开(公告)日：2012-01-12

申请号：PCT/EP2011/061688

申请日：2011-07-08

Applicant: PHOTOCURE ASA ,  KLEM, Bjørn ,  LANGE, Norbert

Inventor： KLEM, Bjørn ,  LANGE, Norbert

IPC: A61N5/06 ,  A61K9/70 ,  A61K41/00 ,  A61K47/36

CPC classification number: A61K31/197 ,  A61K9/19 ,  A61K9/7007 ,  A61K41/0061 ,  A61K49/0017 ,  A61K49/0036 ,  A61N5/0601 ,  A61N5/062

Abstract: This invention relates to dry pharmaceutical compositions comprising an active ingredient which is 5-aminolevulinic acid (5-ALA) or a precursor or derivative of 5-ALA, or a pharmaceutically acceptable salt thereof. The compositions may be used in the photodynamic treatment (PDT) or photodynamic diagnosis (PDD) of cancer, pre-cancerous conditions and non-cancerous conditions. The invention relates further to irradiation devices comprising dry compositions and the use of such devices in the photodynamic treatment (PDT) or photodynamic diagnosis (PDD) of cancer, pre-cancerous conditions and non-cancerous conditions.

Abstract translation: 本发明涉及包含5-氨基乙酰丙酸（5-ALA）或5-ALA的前体或衍生物的活性成分或其药学上可接受的盐的干燥药物组合物。 组合物可用于癌症，癌前病症和非癌症病症的光动力学治疗（PDT）或光动力学诊断（PDD）。 本发明进一步涉及包含干组合物的照射装置以及在光动力学治疗（PDT）或癌症，癌前病症和非癌症病症的光动力学诊断（PDD）中使用这些装置。

公开(公告)号：WO2009074811A2

公开(公告)日：2009-06-18

申请号：PCT/GB2008/004113

申请日：2008-12-12

Applicant: PHOTOCURE ASA ,  GOLDING, Louise ,  KLAVENESS, Jo ,  STENSRUD, Gry ,  GODAL, Aslak ,  BRAENDEN, Jon, Erik ,  KLEM, Bjørn

Inventor： KLAVENESS, Jo ,  STENSRUD, Gry ,  GODAL, Aslak ,  BRAENDEN, Jon, Erik ,  KLEM, Bjørn

IPC: A61K41/00 ,  A61P35/00 ,  A61K49/00 ,  A61K9/02 ,  A61K9/28 ,  A61K9/48 ,  A61K31/197

CPC classification number: A61K9/02 ,  A61K9/0031 ,  A61K9/0034 ,  A61K9/0075 ,  A61K9/14 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/20 ,  A61K9/2013 ,  A61K9/205 ,  A61K9/2054 ,  A61K9/2077 ,  A61K9/28 ,  A61K9/284 ,  A61K9/2846 ,  A61K9/2866 ,  A61K9/2886 ,  A61K9/48 ,  A61K9/4858 ,  A61K9/4891 ,  A61K9/5042 ,  A61K9/5073 ,  A61K31/197 ,  A61K31/221 ,  A61K41/0057 ,  A61K41/0061 ,  A61K49/00 ,  A61K49/0021

Abstract: The present invention relates to the use of a photosensitiser which is 5-ALA or a precursor or derivative thereof (e.g. an ALA ester), in the manufacture of a pharmaceutical product for use in the photodynamic treatment or diagnosis of cancer, an infection associated with cancer, or in the treatment or diagnosis of a non-cancerous condition, wherein said pharmaceutical product is in the form of a solid. The invention also relates to solid pharmaceutical products for use in such methods, e.g. suppositories, pessaries, tablets, pellets and capsules which comprise 5-ALA or a precursor or derivative thereof (e.g. an ALA ester) and at least one pharmaceutically acceptable carrier or excipient. Such products are particularly suitable for use in the photodynamic treatment or diagnosis of cancerous or non¬ cancerous conditions in the lower part of the gastrointestinal system or in the female reproductive system, e.g. in the treatment or diagnosis of colorectal cancer or cervical cancer.

Abstract translation: 本发明涉及使用5-ALA或其前体或衍生物（例如ALA酯）的光敏剂在制造用于癌症的光动力学治疗或诊断的药物产品中，与 癌症或治疗或诊断非癌症状况，其中所述药物产品为固体形式。 本发明还涉及用于这些方法的固体药物产品，例如。 栓剂，阴道栓剂，片剂，丸剂和胶囊，其包含5-ALA或其前体或衍生物（例如ALA酯）和至少一种药学上可接受的载体或赋形剂。 这些产品特别适用于光动力学治疗或诊断胃肠系统下部或女性生殖系统中的癌性或非癌性病症，例如， 在结直肠癌或宫颈癌的治疗或诊断中。

公开(公告)号：WO2005092838A1

公开(公告)日：2005-10-06

申请号：PCT/GB2005/001236

申请日：2005-03-29

Applicant: PHOTOCURE ASA ,  BRAENDEN, Jon, Erik ,  GODAL, Aslak ,  NILSEN, Nils, Olav ,  KLAVENESS, Jo

Inventor： BRAENDEN, Jon, Erik ,  GODAL, Aslak ,  NILSEN, Nils, Olav ,  KLAVENESS, Jo

IPC: C07C229/22

CPC classification number: A61K41/0061 ,  C07C229/22

Abstract: The present invention provides an acid addition salt of 5-aminolevulinic acid (5-ALA) or of a 5-ALA derivative (e.g. a 5-ALA ester) with an acid which has a pKa of about 5 or less, preferably about 3 or less, with the proviso that the acid is other than hydrochloric acid. Particularly preferred salts are those derived from acids selected from the group comprising sulphonic acid and its derivatives, hydrobromic acid, sulfuric acid, nitric acid and phosphoric acid. The salts in accordance with the invention are particularly suitable for use as photosensitizing agents in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body.

Abstract translation: 本发明提供5-氨基乙酰丙酸（5-ALA）或5-ALA衍生物（例如5-ALA酯）与酸的加成盐，所述酸的pKa为约5或更小，优选约3或 较少，条件是酸不是盐酸。 特别优选的盐是衍生自选自磺酸及其衍生物，氢溴酸，硫酸，硝酸和磷酸的酸的酸。 根据本发明的盐特别适用于诊断和光化学治疗身体的外表面或内表面的病症或异常的光敏剂。

公开(公告)号：WO2003045893A1

公开(公告)日：2003-06-05

申请号：PCT/GB2002/005305

申请日：2002-11-22

Applicant: PHOTOCURE ASA ,  COCKBAIN, Julian ,  KLAVENESS, Jo

Inventor： KLAVENESS, Jo

IPC: C07C69/50

CPC classification number: A61K31/225 ,  A61K31/23 ,  C07C69/34 ,  C07C69/48 ,  C07C69/96

Abstract: The invention provides acyloxymethyl esters of C 6-14 alkane-dicarboxylic acids, or physiologically tolerable salts or esters thereof, for use in medicine as therapeutic or prophylactic agents.

Abstract translation: 本发明提供了用作医药或预防药物的C 6-14烷烃二羧酸或其生理上可耐受的盐或酯的酰氧基甲基酯。

公开(公告)号：WO2017103283A1

公开(公告)日：2017-06-22

申请号：PCT/EP2016/081803

申请日：2016-12-19

Applicant: PHOTOCURE ASA

Inventor： HESTDAL, Kjetil

IPC: A61K41/00 ,  A61P35/00

CPC classification number: A61K41/0061

Abstract: This invention relates to a neoadjuvant therapy for bladder cancer in bladder cancer patients who are scheduled for a cystectomy and methods of carrying out such a neoadjuvant therapy. In particular the invention relates to a composition comprising hexyl 5-ALA ester (HAL) or a pharmaceutically acceptable salt thereof for use in a neoadjuvant therapy for bladder cancer in a bladder cancer patient who is scheduled for a cystectomy, the therapy comprises instilling said composition into the bladder of said patient and exposing the inside of said bladder to light.

Abstract translation: 本发明涉及定于进行膀胱切除术的膀胱癌患者中用于膀胱癌的新辅助疗法和进行这种新辅助疗法的方法。 具体地，本发明涉及包含己基5-ALA酯（HAL）或其药学上可接受的盐的组合物，其用于定于膀胱癌切除术的膀胱癌患者中用于膀胱癌的新辅助疗法，所述疗法包括将所述组合物 进入所述患者的膀胱并使所述膀胱的内部暴露于光下。

公开(公告)号：WO2017103280A9

公开(公告)日：2017-06-22

申请号：PCT/EP2016/081798

申请日：2016-12-19

Applicant: PHOTOCURE ASA

Inventor： HESTDAL, Kjetil

IPC: C07K16/28 ,  A61K39/00

Abstract: This invention relates to an intravesical therapy for bladder cancer.

公开(公告)号：WO2006051269A1

公开(公告)日：2006-05-18

申请号：PCT/GB2005/004253

申请日：2005-11-04

Applicant: PHOTOCURE ASA ,  GOLDING, Louise ,  GODAL, Aslak ,  KLAVENESS, Jo ,  MORRIS, Hilde

Inventor： GODAL, Aslak ,  KLAVENESS, Jo ,  MORRIS, Hilde

IPC: A61K31/197

CPC classification number: A61N5/0616 ,  A61K31/197 ,  A61K41/0061

Abstract: The invention provides use of a photosensitiser, which is a derivative (e.g. an ester) of 5-aminolevulinic acid (5-ALA) or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in the prevention or treatment of acne.

Abstract translation: 本发明提供了在制备用于预防或治疗痤疮的药物中使用光敏剂，其是5-氨基乙酰丙酸（5-ALA）的衍生物（例如酯）或其药学上可接受的盐）。

公开(公告)号：WO0054802A2

公开(公告)日：2000-09-21

申请号：PCT/GB0000903

申请日：2000-03-10

Applicant: PHOTOCURE ASA ,  JONES ELIZABETH LOUISE ,  BERG KRISTIAN ,  TJELLE TORUNN E ,  HOGSET ANDERS ,  PRASMICKAITE LINA

Inventor： BERG KRISTIAN ,  TJELLE TORUNN E ,  HOGSET ANDERS ,  PRASMICKAITE LINA

IPC: A61K47/22 ,  A61K35/12 ,  A61K35/14 ,  A61K39/00 ,  A61P25/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/00 ,  A61P37/02 ,  C12N5/09 ,  A61K41/00 ,  C12N5/00

CPC classification number: A61K39/0011 ,  A61K2039/5152 ,  A61K2039/5156 ,  A61N5/0613 ,  C12N5/0693 ,  C12N13/00 ,  C12N15/85 ,  C12N2501/999

Abstract: The present invention provides a method of expressing an antigenic molecule or a part thereof on the surface of an antigen-presenting cell, said method comprising introducing a molecule into the cell cytosol by photochemical internalisation, wherein said molecule, or a part thereof, is subsequently presented on the surface of said cell. Methods of vaccination comprising this method, together with compositions comprising said cells and uses involving said cells expressing antigenic molecules are also provided.

Abstract translation: 本发明提供了在抗原呈递细胞表面上表达抗原性分子或其一部分的方法，所述方法包括通过光化学内化将分子引入细胞溶质中，其中所述分子或其一部分随后 呈现在所述细胞的表面上。 还提供了包含该方法的疫苗接种方法，以及包含所述细胞的组合物和涉及所述表达抗原性分子的细胞的用途。