公开(公告)号：US20240285532A1

公开(公告)日：2024-08-29

申请号：US18289738

申请日：2022-05-23

申请人： ACTIVE BIOTECH AB

发明人： Hans Wännman

IPC分类号： A61K9/14 ,  A61K31/4704

CPC分类号： A61K9/14 ,  A61K31/4704

摘要： A plurality of particles of tasquinimod in free base form or as a pharmaceutically acceptable salt, said particles having a D(v, 0.9) of at most 30 pm and a D(v, 0.5) of at most 15 μm. A pharmaceutical composition comprising said particles and preferably one or more pharmaceutically acceptable excipients. A pharmaceutical dosage unit. The particles, composition and dosage unit are useful in the treatment of cancer.

公开(公告)号：US20240180819A1

公开(公告)日：2024-06-06

申请号：US18284284

申请日：2022-03-31

申请人： ACTIVE BIOTECH AB

发明人： Hans Wännman ,  Marie Törngren ,  Helena Eriksson ,  Andreas Buhl

IPC分类号： A61K9/00 ,  A61K31/4704 ,  A61K47/10 ,  A61K47/18 ,  A61K47/26 ,  A61K47/32 ,  A61K47/38 ,  A61P27/02

CPC分类号： A61K9/0048 ,  A61K31/4704 ,  A61K47/10 ,  A61K47/183 ,  A61K47/186 ,  A61K47/26 ,  A61K47/32 ,  A61K47/38 ,  A61P27/02

摘要： A pharmaceutical formulation comprising laquinimod or a pharmaceutically acceptable salt thereof as active ingredient, a pharmaceutically acceptable viscosity agent, a pharmaceutically acceptable tonicity adjusting agent, a pharmaceutically acceptable humectant, a pharmaceutically acceptable antioxidant, and a pharmaceutically acceptable pH regulating agent. The formulation is suitable for the treatment of ocular diseases by ocular administration, preferably topical ocular administration.

公开(公告)号：US10385069B2

公开(公告)日：2019-08-20

申请号：US15545573

申请日：2015-12-04

申请人： Active Biotech AB

发明人： Ulf Wellmar ,  Stephen East ,  Marie Bainbridge ,  Colin MacKinnon ,  James Carr ,  Jonathan Hargrave

IPC分类号： C07D513/04 ,  C07D513/14

摘要： A compound of formula (I) or a pharmaceutically acceptable salt thereof. The compound is useful for use in the treatment of cancer, an inflammatory disorder, an autoimmunity disorder or a neurodegenerative disorder.

公开(公告)号：US10314836B2

公开(公告)日：2019-06-11

申请号：US15947279

申请日：2018-04-06

申请人： Active Biotech AB

发明人： David Liberg ,  Anders Olsson ,  Dmitry Gabrilovich ,  Yuliya Nefedova

IPC分类号： A61K31/47 ,  A61K31/167 ,  C07D215/22

摘要： A compound of formula (I) or a pharmaceutically acceptable salt thereof, for use in the treatment of multiple myeloma.

公开(公告)号：US20140112946A1

公开(公告)日：2014-04-24

申请号：US14125666

申请日：2012-06-22

申请人： ACTIVE BIOTECH AB

发明人： Leif Svensson

IPC分类号： C07D215/56

CPC分类号： C07D215/56 ,  A61K31/4704

摘要： Deuterium-enriched 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[(4-trifluoromethyl)-phenyl]-1,2-dihydroquinoline-3-carboxamide, having a deuterium enrichment in the amide-N methyl group of at least 70%; or a salt thereof with a pharmaceutically acceptable organic or inorganic cation; and a method of preparing said compounds. The compounds are useful in therapy, e.g. for the treatment of a malignant hyperproliferative disorder or an autoimmune disease.

摘要翻译： 富含氘的4-羟基-5-甲氧基-N，1-二甲基-2-氧代-N - [（4-三氟甲基） - 苯基] -1,2-二氢喹啉-3-甲酰胺在酰胺中具有氘浓缩 -N甲基至少70％; 或其盐与药学上可接受的有机或无机阳离子; 以及制备所述化合物的方法。 这些化合物可用于治疗，例如 用于治疗恶性过度增殖性疾病或自身免疫性疾病。

公开(公告)号：US20100166775A1

公开(公告)日：2010-07-01

申请号：US12597735

申请日：2008-04-24

申请人： Per Bjork ,  Fredrik Ivars ,  Tomas Leanderson

发明人： Per Bjork ,  Fredrik Ivars ,  Tomas Leanderson

IPC分类号： A61K39/395 ,  G01N33/566 ,  G01N33/567 ,  G01N33/53 ,  C07K16/18 ,  A61P35/00

CPC分类号： C07K14/52 ,  C07K14/705 ,  C07K16/18 ,  C07K2317/56 ,  C07K2317/76 ,  G01N33/566 ,  G01N33/6842 ,  G01N2333/705 ,  G01N2333/70503 ,  G01N2500/00

摘要： A method of identifying a compound for use in therapy which modulates the interaction of S1OO A9 with a ligand comprising: -determining whether a candidate compound is capable of modulating the interaction of S1OO A9 with RAGE or the interaction of S1OO A9 with a TLR (Toll like receptor), or -determining whether a candidate compound is capable of binding to S100A9 in a manner which disrupts binding of S1OO A9 with RAGE or the binding of S100A9 with a TLR, to thereby identify whether the compound may be used in therapy.

摘要翻译： 鉴定用于调节S100A9与配体的相互作用的化合物的方法，包括： - 确定候选化合物是否能够调节S100A9与RAGE的相互作用或S100A9与TLR的相互作用（Toll 或者以确定S100A9与RAGE的结合或S100A9与TLR的结合的方式确定候选化合物是否能够结合S100A9，从而鉴定该化合物是否可用于治疗。

公开(公告)号：US07615225B2

公开(公告)日：2009-11-10

申请号：US11526437

申请日：2006-09-25

申请人： Goran Forsberg ,  Eva Erlandsson ,  Per Antonsson ,  Bjorn Walse

发明人： Goran Forsberg ,  Eva Erlandsson ,  Per Antonsson ,  Bjorn Walse

IPC分类号： A61K39/395

CPC分类号： C07K14/31 ,  A61K39/00 ,  A61K47/6851 ,  A61K2039/505 ,  C07K14/315 ,  C07K16/30 ,  C07K2319/00 ,  H04L51/063 ,  H04L51/38

摘要： The present invention relates to compositions and methods of use, wherein the composition comprises a conjugate of a bacterial superantigen and an antibody moiety. More particularly, the bacterial superantigen has been modified to decrease seroreactivity with retained superantigen activity.

摘要翻译： 本发明涉及组合物和使用方法，其中组合物包含细菌超抗原和抗体部分的缀合物。 更具体地，细菌超抗原已被修饰以降低具有保留的超抗原活性的血清反应性。

公开(公告)号：US07589208B2

公开(公告)日：2009-09-15

申请号：US11050441

申请日：2005-02-04

申请人： Karl Jansson ,  Tomas Fristedt ,  Hans Wännman ,  Anders Björk

发明人： Karl Jansson ,  Tomas Fristedt ,  Hans Wännman ,  Anders Björk

IPC分类号： C07D215/38

CPC分类号： A61K31/47 ,  A61K9/1617 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/2059 ,  A61K31/4706

摘要： A stable solid pharmaceutical composition consisting essentially of an effective amount of a salt of formula (II) together with an alkaline-reacting component maintaining the pH preferably above 8, or a salt with a divalent metal cation; and at least one pharmaceutical excipient; said salt of formula (II) being essentially stable during storage at room temperature for a period of at least 3 years. A process for stabilizing the salt of formula (II). A crystalline salt of formula (II) and a process for preparing said salt.

摘要翻译： 一种稳定的固体药物组合物，其基本上由有效量的式（II）的盐与保持pH优选高于8的碱反应组分或与二价金属阳离子的盐组成; 和至少一种药物赋形剂; 所述式（II）的盐在室温下储存至少3年的时间基本上是稳定的。 稳定式（II）的盐的方法。 式（II）的结晶盐和制备所述盐的方法。

公开(公告)号：US20080119485A1

公开(公告)日：2008-05-22

申请号：US12018692

申请日：2008-01-23

申请人： Eric WELLNER ,  Helena Sandin

发明人： Eric WELLNER ,  Helena Sandin

IPC分类号： A61K31/496 ,  C07D405/06 ,  C07D403/06 ,  A61P37/00 ,  A61P29/00

CPC分类号： C07D307/85 ,  C07D209/42

摘要： Compounds of formula (I) wherein X is a fluorine or a chlorine atom; the methyl groups located at the 2- and 5-position of the piperazine ring are in trans-configuration to each other; Y is NH or O; R1 is selected from hydrogen, chloro, bromo, nitro, methyl or trifluoromethyl; R2 is selected from hydrogen, halo, methyl, trifluoromethyl, methoxy or trifluoromethoxy; or a pharmaceutically acceptable salt or solvate thereof; The invention also relates to pharmaceutical compositions containing a compound of formula (I) together with a pharmaceutically acceptable carrier. Included are also processes for the preparation of compounds of formula (I), as well as methods for treating mammals suffering from inflammatory, autoimmune, proliferative or hyperproliferative diseases by administering a compound having the formula (I) to said mammal.

摘要翻译： 其中X为氟或氯原子的式（I）化合物; 位于哌嗪环的2-位和5-位的甲基彼此反式构型; Y是NH或O; R 1选自氢，氯，溴，硝基，甲基或三氟甲基; R 2选自氢，卤素，甲基，三氟甲基，甲氧基或三氟甲氧基; 或其药学上可接受的盐或溶剂化物; 本发明还涉及含有式（I）化合物与药学上可接受的载体的药物组合物。 还包括制备式（I）化合物的方法，以及通过向所述哺乳动物施用具有式（I）的化合物来治疗患有炎性，自身免疫性，增殖性或过度增殖性疾病的哺乳动物的方法。

公开(公告)号：US07339059B2

公开(公告)日：2008-03-04

申请号：US10995037

申请日：2004-11-23

申请人： Eric Wellner ,  Helena Sandin

发明人： Eric Wellner ,  Helena Sandin

IPC分类号： C07D405/00

CPC分类号： C07D307/85 ,  C07D209/42

摘要： Compounds of formula (I) wherein X is a fluorine or a chlorine atom; the methyl groups located at the 2- and 5-position of the piperazine ring are in trans-configuration to each other; Y is NH or O; R1 is selected from hydrogen, chloro, bromo, nitro, methyl or trifluoromethyl; R2 is selected from hydrogen, halo, methyl, trifluoromethyl, methoxy or trifluoromethoxy; or a pharmaceutically acceptable salt or solvate thereof; The invention also relates to pharmaceutical compositions containing a compound of formula (I) together with a pharmaceutically acceptable carrier. Included are also processes for the preparation of compounds of formula (I), as well as methods for treating mammals suffering from inflammatory, autoimmune, proliferative or hyperproliferative diseases by administering a compound having the formula (I) to said mammal.

摘要翻译： 其中X为氟或氯原子的式（I）化合物; 位于哌嗪环的2-位和5-位的甲基彼此反式构型; Y是NH或O; R 1选自氢，氯，溴，硝基，甲基或三氟甲基; R 2选自氢，卤素，甲基，三氟甲基，甲氧基或三氟甲氧基; 或其药学上可接受的盐或溶剂化物; 本发明还涉及含有式（I）化合物与药学上可接受的载体的药物组合物。 还包括制备式（I）化合物的方法，以及通过向所述哺乳动物施用具有式（I）的化合物来治疗患有炎性，自身免疫性，增殖性或过度增殖性疾病的哺乳动物的方法。