公开(公告)号：US08946474B2

公开(公告)日：2015-02-03

申请号：US13806391

申请日：2011-06-24

Applicant: Søren Ebdrup ,  Kim Troensegaard Nielsen ,  Tanja Maria Greve

Inventor： Søren Ebdrup ,  Kim Troensegaard Nielsen ,  Tanja Maria Greve

IPC: C07C53/00 ,  A61K31/075 ,  A61K31/04 ,  C07C217/74 ,  C07C213/10 ,  A61K31/196

CPC classification number: C07C217/74 ,  A61K31/196 ,  C07C213/10 ,  C07C2601/08

Abstract: The present invention relates to the crystalline, polymorphic Form X of the calcimimetic compound {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, to methods of preparation thereof, to methods of characterization thereof by single crystal X-Ray crystallography (XRC), X-Ray Powder diffractometry, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, Solid State NMR spectroscopy and Differential Scanning Calorimetry (DSC), and to its use. The invention also relates to the preparation of Form X by crystallization from a saturated solution of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid in a C1-C6 alkyl alcohol, or alternatively by precipitation from a neutralized saponification reaction mixture following the alkaline hydrolysis of a C1-C6 alkyl ester of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid.

Abstract translation: 本发明涉及拟钙化合物{4 - [（1R，3S）-3 - （（R）-1-萘基-1-乙基氨基） - 环戊基] - 苯氧基} - 乙酸的晶体多晶型X 酸，其制备方法，通过单晶X射线晶体学（XRC），X射线粉末衍射，衰减全反射傅立叶变换红外（ATR-FTIR）光谱，固态NMR光谱和差示扫描的表征方法 量热法（DSC）及其用途。 本发明还涉及通过从饱和的{4 - [（1R，3S）-3 - （（R）-1-萘基-1-基 - 乙基氨基） - 环戊基] - 苯氧基} - 乙酸在C1-C6烷基醇中反应，或者通过碱解水解{4 - [（1R，3S）-3 - （（R） - 1-萘基-1-基 - 乙基氨基） - 环戊基] - 苯氧基} - 乙酸。

公开(公告)号：US08785494B2

公开(公告)日：2014-07-22

申请号：US13322522

申请日：2010-05-26

Applicant: Bjarne Nørremark

Inventor： Bjarne Nørremark

IPC: A61K31/21 ,  A61K31/215 ,  A61K31/195 ,  A61K31/135

CPC classification number: A61K31/195 ,  C07C229/46 ,  C07C2601/08 ,  A61K31/215 ,  A61K31/135 ,  C07C227/18 ,  C07C69/738 ,  C07C67/343

Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating trifluoromethylphenylene cyclopentylene compounds represented in formula (I) and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.

Abstract translation: 本发明涉及将用于治疗的所述化合物，用于治疗的所述化合物，包含所述化合物的药物组合物的式（I）所示的三氟甲基亚苯基亚环戊基化合物及其衍生物的新型钙感受受体（CaSR） 涉及用所述化合物治疗疾病的方法，以及所述化合物在制备药物中的用途。

公开(公告)号：US20140079785A1

公开(公告)日：2014-03-20

申请号：US14006890

申请日：2012-03-23

Applicant: Louise Bastholm Jensen ,  Karsten Petersson

Inventor： Louise Bastholm Jensen ,  Karsten Petersson

IPC: A61K31/593 ,  A61K31/573

CPC classification number: A61K31/593 ,  A61K9/0014 ,  A61K9/5123 ,  A61K31/573 ,  A61K45/06 ,  A61K2300/00

Abstract: A pharmaceutical composition comprises, as a therapeutically active ingredient, a corticosteroid and/or vitamin D derivative incorporated as a solid solution or dispersion in lipid nanoparticles, said lipid nanoparticles being solid at ambient temperature and comprising a first lipid with a melting point above body temperature, the first lipid being a wax selected from the group consisting of esters of C12-24 alcohols and C12-24 fatty acids, glyceryl mono-, di- or triesters of C12-24 fatty acids, C12-24 fatty alcohols, and cholesterol, optionally a second lipid which is an oil at ambient temperature and miscible with the first lipid, and a pharmaceutically acceptable surfactant.

Abstract translation: 药物组合物包含作为治疗活性成分的作为固体溶液或分散体掺入脂质纳米颗粒中的皮质类固醇和/或维生素D衍生物，所述脂质纳米颗粒在环境温度下为固体，并且包含熔点高于体温的第一种脂质 第一种脂质是选自C12-24醇和C12-24脂肪酸的酯的蜡，C12-24脂肪酸的单 - ，二 - 或三酯，C12-24脂肪醇和胆固醇， 任选的第二脂质，其在环境温度下是油，并与第一种脂质混溶，和药学上可接受的表面活性剂。

公开(公告)号：US20140023700A1

公开(公告)日：2014-01-23

申请号：US14000811

申请日：2012-02-21

Applicant: Nina Østergaard Knudsen ,  Thorsten Thormann

Inventor： Nina Østergaard Knudsen ,  Thorsten Thormann

IPC: A61K38/12 ,  A61K31/047 ,  A61K47/48 ,  A61K9/127

CPC classification number: A61K38/12 ,  A61K8/64 ,  A61K9/1271 ,  A61K31/047 ,  A61K38/00 ,  A61K47/48246 ,  A61K47/48815 ,  A61K47/64 ,  A61K47/6911 ,  A61Q19/008 ,  C07K7/06 ,  C07K7/64

Abstract: A cyclic peptide capable of binding specifically to the α2 I domain of a collagen binding integrin receptor may be conjugated to a drug containing particle via a linker moiety. The conjugate may be used to target a therapeutic drug to a cell expressing a collagen binding integrin receptor on its surface.

Abstract translation: 能够特异性结合胶原结合整联蛋白受体的α2I结构域的环肽可通过接头部分与含药物颗粒结合。 缀合物可用于将治疗药物靶向表面上表达胶原结合整联蛋白受体的细胞。

公开(公告)号：US20130039952A1

公开(公告)日：2013-02-14

申请号：US13518214

申请日：2010-12-22

Applicant: Karsten Petersson

Inventor： Karsten Petersson

IPC: A61K9/14 ,  A61P17/00 ,  A61P17/10 ,  C07C401/00 ,  A61K31/7016 ,  A61K31/593 ,  A61P17/06 ,  B82Y5/00

CPC classification number: A61K31/592 ,  A61K9/0014 ,  A61K9/06 ,  A61K9/146 ,  A61K31/593 ,  A61K45/06 ,  C07C35/21 ,  Y10T428/2982

Abstract: Calcipotriol monohydrate nanocrystals prepared by the process disclosed herein may be incorporated in a pharmaceutical composition for use in the prevention or treatment of dermal diseases and conditions.

Abstract translation: 通过本文公开的方法制备的卡泊三醇一水合物纳米晶体可以掺入用于预防或治疗皮肤疾病和病症的药物组合物中。

公开(公告)号：US20130005680A1

公开(公告)日：2013-01-03

申请号：US13518333

申请日：2009-12-22

Applicant: Karsten Petersson

Inventor： Karsten Petersson

IPC: A61K31/593 ,  A61K31/7016 ,  A61P17/10 ,  A61P17/06 ,  A61P17/08 ,  A61K31/592 ,  A61P17/00

CPC classification number: A61K31/592 ,  A61K9/0014 ,  A61K9/113 ,  A61K31/593 ,  A61K31/7016 ,  A61K45/06 ,  A61K47/10 ,  A61K47/14 ,  A61K47/26 ,  A61K47/44 ,  A61K2300/00

Abstract: A topical pharmaceutical composition which is an oil-in-water-oil emulsion comprising a vitamin D derivative or analogue dissolved in a mixture of a non-ionic surfactant and a lower alkanol. The topical pharmaceutical composition may be used in the treatment of dermal conditions, such as psoriasis.

Abstract translation: 一种局部药物组合物，其是包含溶解在非离子表面活性剂和低级链烷醇的混合物中的维生素D衍生物或类似物的水包油乳液。 局部药物组合物可用于治疗皮肤状况，如牛皮癣。

公开(公告)号：US20110257262A1

公开(公告)日：2011-10-20

申请号：US13088910

申请日：2011-04-18

Applicant: Steven Martin OGBOURNE

Inventor： Steven Martin OGBOURNE

IPC: A61K31/22 ,  A61P17/12 ,  A61P35/00 ,  C07C69/56

CPC classification number: C07C67/52 ,  A61K9/0014 ,  A61K9/0034 ,  A61K9/06 ,  C07B2200/13 ,  C07C69/533 ,  C07C2603/86 ,  Y02A50/463

Abstract: The present invention relates to a novel crystalline form of ingenol mebutate, methods of preparation thereof, and to its use. More specifically, the invention relates to the conversion of amorphous ingenol mebutate (ingenol-3-angelate, PEP005) to a crystalline form, which was characterized by single crystal X-Ray crystallography (XRC), attenuated total reflectance Fourier transform infrared (FTIR-ATR) spectroscopy and Differential Scanning calorimetry (DSC).

Abstract translation: 本发明涉及一种新型的烯酸甲酯结晶形式，其制备方法及其用途。 更具体地说，本发明涉及以单结晶X射线晶体学（XRC），衰减全反射傅里叶变换红外（FTIR-3）为特征的无定形内酯酚酸酯（茚满醇-3-当归，PEP005）转化为结晶形式， ATR）光谱和差示扫描量热法（DSC）。

公开(公告)号：US20100317582A1

公开(公告)日：2010-12-16

申请号：US12744137

申请日：2008-11-20

Applicant: Jef Fensholdt ,  Sophie Elisabeth Havez ,  Bjarne Nørremark

Inventor： Jef Fensholdt ,  Sophie Elisabeth Havez ,  Bjarne Nørremark

IPC: A61K38/23 ,  C07C211/30 ,  A61K31/137 ,  C07D295/027 ,  A61K31/5375 ,  C07D271/06 ,  A61K31/4245 ,  A61P25/28 ,  A61P9/10 ,  A61P13/12 ,  A61K31/59

CPC classification number: C07D295/182 ,  C07C211/35 ,  C07C211/36 ,  C07C211/48 ,  C07C215/28 ,  C07C217/52 ,  C07C217/74 ,  C07C233/05 ,  C07C233/41 ,  C07C237/24 ,  C07C237/30 ,  C07C237/32 ,  C07C237/34 ,  C07C237/36 ,  C07C237/40 ,  C07C239/14 ,  C07C255/03 ,  C07C255/32 ,  C07C255/50 ,  C07C257/18 ,  C07C259/10 ,  C07C259/18 ,  C07C271/44 ,  C07C309/15 ,  C07C311/05 ,  C07C311/08 ,  C07C311/37 ,  C07C311/51 ,  C07C317/32 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07D205/04 ,  C07D207/08 ,  C07D207/12 ,  C07D207/16 ,  C07D207/27 ,  C07D209/08 ,  C07D209/12 ,  C07D209/20 ,  C07D211/46 ,  C07D211/60 ,  C07D211/62 ,  C07D213/30 ,  C07D213/38 ,  C07D213/40 ,  C07D213/80 ,  C07D231/12 ,  C07D231/40 ,  C07D233/61 ,  C07D233/90 ,  C07D263/22 ,  C07D271/06 ,  C07D295/088 ,  C07D295/13 ,  C07D295/135 ,  C07D295/192 ,  C07D295/195 ,  C07D295/26 ,  C07D305/08 ,  C07D307/12 ,  C07D307/52 ,  C07D307/68 ,  C07D307/79 ,  C07D309/10 ,  C07D319/18 ,  C07D333/38 ,  C07D333/40 ,  C07D333/58 ,  C07D413/04 ,  C07D413/06 ,  C07D417/06

Abstract: The invention relates to novel cyclic hydrocarbon compounds and derivatives thereof, processes for the preparation thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.

Abstract translation: 本发明涉及新的环烃化合物及其衍生物，其制备方法，用作药物的所述化合物，用于治疗的所述化合物，包含所述化合物的药物组合物，涉及用所述化合物治疗疾病的方法 ，以及所述化合物在制备药物中的用途。

公开(公告)号：US20090131389A1

公开(公告)日：2009-05-21

申请号：US12084231

申请日：2006-10-30

Applicant: Jan Jensen ,  Niels Rastrup Andersen

Inventor： Jan Jensen ,  Niels Rastrup Andersen

IPC: A61K31/575 ,  C07J13/00 ,  A61P31/00

CPC classification number: C07J13/007

Abstract: The present invention relates to processes for the crystallisation and for the preparation and isolation of a novel crystalline form of fusidic acid, to the use of said processes in the manufacture of pharmaceutical formulation or medicament, and to the use of said crystalline fusidic acid form for the treatment of bacterial infections.

Abstract translation: 本发明涉及结晶和制备和分离夫西地酸的新结晶形式的方法，以及所述方法在制备药物制剂或药物中的用途，以及所述结晶夫西地酸形式用于 治疗细菌感染。

公开(公告)号：US20080118930A1

公开(公告)日：2008-05-22

申请号：US11576272

申请日：2005-10-14

Applicant: Ian Chopra ,  O'Neil Alexander

Inventor： Ian Chopra ,  O'Neil Alexander

IPC: G01N33/53

CPC classification number: C12Q1/18

Abstract: A screening method for agents which are capable of reversing resistance to the antibiotic fusidic acid in bacteria that contain the fusB resistance gene or a homologue thereof and that express the FusB fusidic acid resistance protein or a homologue thereof based on the interaction between the fusB resistance protein or a homologue thereof with elongation factor-G (EF-G) protein.

Abstract translation: 一种试剂的筛选方法，其能够在含有fusB抗性基因或其同源物的细菌中抵抗抗生素夫西地酸，并且基于fusB抗性蛋白质之间的相互作用表达FusB阻抗蛋白或其同源物 或其与延伸因子-G（EF-G）蛋白的同系物。