公开(公告)号：US20050004363A1

公开(公告)日：2005-01-06

申请号：US10484765

申请日：2002-07-18

申请人： Masaya Hashimoto ,  Osamu Okamoto

发明人： Masaya Hashimoto ,  Osamu Okamoto

IPC分类号： A61P1/00 ,  A61P3/04 ,  A61P7/12 ,  A61P11/06 ,  A61P11/08 ,  A61P11/14 ,  A61P15/10 ,  A61P23/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/36 ,  A61P43/00 ,  C07D471/10 ,  C07D487/10

CPC分类号： C07D471/10

摘要： The invention relates to 4-oxoimidazolidine-2-spiropiperidine derivatives represented by a general formula [I] [in which A1, A2, A3, A4 and A5 stand for optionally halogen-substituted methine, or nitrogen atom; R1 and R2 stand for lower alkyl or the like; R3 stands for hydrogen or lower alkyl; R4 and R5 stand for hydrogen, or lower alkyl which is optionally substituted with hydroxy, or the like]or salts thereof. These compounds act as nociceptin receptor agonist, and are useful as analgesic, reliever from tolerance to narcotic analgesic, reliever from dependence on narcotic analgesic, analgesic enhancer, antiobestic, drug for ameliorating brain function, remedy for schizophrenia, drug for treating regressive neurodegenerative diseases, antianxiety agent or antidepressant and remedy for diabetes insipidus and polyuria; and the like.

摘要翻译： 本发明涉及由通式[I]表示的4-氧代咪唑烷-2-螺哌啶衍生物[其中A1，A2，A3，A4和A5代表任选卤素取代的次甲基或氮原子; R 1和R 2代表低级烷基等; R 3代表氢或低级烷基; R 4和R 5代表氢，或任选被羟基取代的低级烷基等或其盐。 这些化合物作为伤害感受肽受体激动剂起作用，可用作镇痛药，缓解麻醉止痛药耐受性，缓解依赖麻醉止痛药，镇痛增强剂，抗胆固醇药，改善脑功能药物，精神分裂症药物治疗，治疗退行性神经退行性疾病药物， 抗焦虑药或抗抑郁药及其治疗尿崩症及多尿症; 等等。

公开(公告)号：US5891878A

公开(公告)日：1999-04-06

申请号：US691338

申请日：1996-08-02

申请人： Steven Colin Beasley ,  John Gary Montana ,  Hazel John Dyke ,  Alan Findlay Haughan ,  Karen Ann Runcie ,  David Thomas Manallack ,  George Martin Buckley ,  Robert James Maxey ,  Hannah Jayne Kendall ,  Andrew Douglas Baxter

发明人： Steven Colin Beasley ,  John Gary Montana ,  Hazel John Dyke ,  Alan Findlay Haughan ,  Karen Ann Runcie ,  David Thomas Manallack ,  George Martin Buckley ,  Robert James Maxey ,  Hannah Jayne Kendall ,  Andrew Douglas Baxter

IPC分类号： C07D215/54 ,  A61K31/00 ,  A61K31/435 ,  A61K31/439 ,  A61K31/444 ,  A61K31/47 ,  A61K31/4709 ,  A61P1/00 ,  A61P1/04 ,  A61P3/00 ,  A61P3/10 ,  A61P7/00 ,  A61P7/12 ,  A61P9/00 ,  A61P11/00 ,  A61P11/06 ,  A61P17/00 ,  A61P19/00 ,  A61P19/02 ,  A61P19/08 ,  A61P25/16 ,  A61P25/28 ,  A61P27/00 ,  A61P27/02 ,  A61P27/16 ,  A61P29/00 ,  A61P31/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/00 ,  A61P37/08 ,  A61P43/00 ,  C07D215/56 ,  C07D401/06 ,  C07D401/14 ,  C07D471/04 ,  C07D491/048 ,  A61K31/50 ,  A61K31/505

CPC分类号： A61K31/47 ,  A61K31/444

摘要： 1-Alkyl-substituted-quinolone-3-carboxamides have therapeutic utility via inhibition of Phosphodiesterase IV esterase and/or Tumour Necrosis Factor activity. The compounds of the invention have the general formula (I): ##STR1## The compounds of the invention encompassed by formula (I) include enantiomers, diastereoisomers and mixtures, including racemic mixtures.

摘要翻译： 1-烷基取代的喹诺酮-3-甲酰胺通过抑制磷酸二酯酶IV酯酶和/或肿瘤坏死因子活性具有治疗效用。 本发明的化合物具有通式（I）：（I）式（I）所包括的本发明化合物包括对映异构体，非对映异构体和混合物，包括外消旋混合物。

公开(公告)号：US11752106B2

公开(公告)日：2023-09-12

申请号：US17475622

申请日：2021-09-15

申请人： Vertex Pharmaceuticals Incorporated

发明人： Eleni Dokou ,  Shahla Jamzad ,  John P. Caesar, Jr. ,  Majed Fawaz ,  Laura Das ,  Chong-Hui Gu ,  Patricia Nell Hurter ,  Meghna Jai Israni ,  Meghan M. Johnston ,  Dragutin Knezic ,  Andrew G. Kuzmission ,  HongRen Wang

IPC分类号： A61K9/20 ,  A61K9/14 ,  A61K9/16 ,  A61K9/48 ,  A61K31/47 ,  A61K47/02 ,  A61K47/12 ,  A61K47/20 ,  A61K47/26 ,  A61K47/38 ,  C07D215/56 ,  A61P1/10 ,  A61P1/16 ,  A61P1/18 ,  A61P3/00 ,  A61P3/06 ,  A61P3/10 ,  A61P3/12 ,  A61P5/00 ,  A61P5/14 ,  A61P5/16 ,  A61P5/18 ,  A61P7/00 ,  A61P7/04 ,  A61P7/10 ,  A61P7/12 ,  A61P9/00 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P13/02 ,  A61P13/12 ,  A61P15/08 ,  A61P15/10 ,  A61P17/00 ,  A61P19/08 ,  A61P19/10 ,  A61P21/00 ,  A61P21/02 ,  A61P21/04 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/20 ,  A61P25/22 ,  A61P25/28 ,  A61P27/02 ,  A61P27/04 ,  A61P29/00 ,  A61P31/10 ,  A61P35/00 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  A61K47/00

CPC分类号： A61K9/205 ,  A61K9/143 ,  A61K9/145 ,  A61K9/146 ,  A61K9/1611 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1652 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2072 ,  A61K9/2077 ,  A61K9/485 ,  A61K9/4808 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/47 ,  A61K47/02 ,  A61K47/12 ,  A61K47/20 ,  A61K47/26 ,  A61K47/38 ,  C07D215/56

摘要： The present invention relates to pharmaceutical compositions containing a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide including formulations of the solid dispersions into powders, granules and mini-tablets, methods for manufacturing and processing the powders, granules and mini-tablets, and methods for treating cystic fibrosis employing the pharmaceutical composition.

公开(公告)号：US20230097398A1

公开(公告)日：2023-03-30

申请号：US17659653

申请日：2022-04-18

申请人： Eloxx Pharmaceuticals Ltd.

发明人： Timor Baasov

IPC分类号： C07H15/224 ,  C07H15/23 ,  A61P21/04 ,  A61P7/04 ,  A61P7/12

摘要： Novel pseudo-disaccharide and pseudo-trisaccharide aminoglycosides, represented by Formulae I or Ia, as defined in the instant specification, designed to exhibit stop codon mutation readthrough activity, are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic diseases and disorders, such as diseases and disorders associated with stop codon mutations.

公开(公告)号：US11492385B2

公开(公告)日：2022-11-08

申请号：US17003921

申请日：2020-08-26

申请人： Merck Sharp & Dohme Corp.

发明人： Anandan Palani ,  Ravi Nargund ,  Paul E. Carrington ,  Tomi Sawyer ,  Qiaolin Deng ,  Antonello Pessi ,  Elisabetta Bianchi ,  Federica Orvieto

IPC分类号： A61K38/00 ,  A61K38/28 ,  A61P3/04 ,  A61P7/12 ,  A61P3/10 ,  C07K14/435 ,  C07K14/605

摘要： Long-acting co-agonists of the glucagon and GLP-1 receptors are described.

公开(公告)号：US11147770B2

公开(公告)日：2021-10-19

申请号：US16299675

申请日：2019-03-12

申请人： Vertex Pharmaceuticals Incorporated

发明人： Eleni Dokou ,  Shahla Jamzad ,  John P. Caesar, Jr. ,  Majed Fawaz ,  Laura Das ,  Chong-Hui Gu ,  Patricia Nell Hurter ,  Meghna Jai Israni ,  Meghan M. Johnston ,  Dragutin Knezic ,  Andrew G. Kuzmission ,  Hongren Wang

IPC分类号： A61K9/20 ,  A61K9/14 ,  A61K47/02 ,  A61K47/12 ,  A61K47/20 ,  A61K47/26 ,  A61K47/38 ,  A61K9/16 ,  C07D215/56 ,  A61K9/48 ,  A61K31/47 ,  A61P3/10 ,  A61P9/00 ,  A61P7/12 ,  A61P7/10 ,  A61P7/04 ,  A61P7/00 ,  A61P5/16 ,  A61P5/18 ,  A61P5/14 ,  A61P5/00 ,  A61P43/00 ,  A61P37/08 ,  A61P37/06 ,  A61P3/06 ,  A61P35/00 ,  A61P31/10 ,  A61P31/12 ,  A61P3/00 ,  A61P29/00 ,  A61P27/04 ,  A61P27/02 ,  A61P25/28 ,  A61P25/22 ,  A61P25/20 ,  A61P25/16 ,  A61P25/14 ,  A61P25/08 ,  A61P25/00 ,  A61P21/04 ,  A61P21/02 ,  A61P21/00 ,  A61P19/10 ,  A61P19/08 ,  A61P17/00 ,  A61P15/10 ,  A61P15/08 ,  A61P13/12 ,  A61P13/02 ,  A61P11/06 ,  A61P11/02 ,  A61P11/00 ,  A61P1/18 ,  A61P1/16 ,  A61P1/10

摘要： The present invention relates to pharmaceutical compositions containing a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide including formulations of the solid dispersions into powders, granules and mini-tablets, methods for manufacturing and processing the powders, granules and mini-tablets, and methods for treating cystic fibrosis employing the pharmaceutical composition.

公开(公告)号：US20190099502A1

公开(公告)日：2019-04-04

申请号：US16086861

申请日：2017-03-23

申请人： INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE) ,  UNIVERSITÉ DE MONTPELLIER

发明人： Benjamin DELPRAT ,  Cécile CRIBAILLET-DELETTRE ,  Claire ANGEBAULT

IPC分类号： A61K48/00 ,  A61P3/10 ,  A61P27/00 ,  A61K9/51 ,  A61P7/12 ,  C12Q1/6883

摘要： The present invention relates to novel therapeutic ways for treating Wolfram Syndrome (WS) by targeting the neuronal calcium sensor 1 (NCS1). The present inventors have demonstrated that WFS1, which loss of function is responsible of the Wolfram Syndrome, forms a complex with the neuronal calcium sensor 1 (NCS1). The inventors have further demonstrated that WFS1 associates with NCS1 to prevent its degradation by the proteasome and that NCS1 regulates VDAC expression and mitochondrial respiratory chain. Thus, present invention provides an agonist of NCS1 for use in the treatment of WS. Such an agonist is e.g. a NCS1-encoding polynucleotide, an inhibitor of the proteasome or of calpains. The inventors have further shown that overexpression of NCS1 in WS cells allows increasing complex II driven respiration. The present invention further relates to a method for predicting the severity of WS by measuring the NCS1 level in a sample obtained from a patient.

公开(公告)号：US10118955B2

公开(公告)日：2018-11-06

申请号：US14539578

申请日：2014-11-12

申请人： The General Hospital Corporation

发明人： Joel F. Habener ,  Tatsuya Yano ,  Eva Tomas Falco

IPC分类号： A61K38/26 ,  A61P3/10 ,  A61P7/12 ,  C07K14/605 ,  C07K14/005 ,  C12N7/00 ,  A61K38/00

摘要： C-Terminal Fragments of Glucagon-Like Peptide-1 (GLP 1), and methods of use thereof, e.g., for the treatment of obesity and obesity-related disorders, e.g., diabetes and the metabolic syndrome.

公开(公告)号：US09868772B2

公开(公告)日：2018-01-16

申请号：US14408813

申请日：2013-06-18

申请人： INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION ,  HOFFMANN-LA ROCHE INC.

发明人： Richard D. Dimarchi ,  David L. Smiley ,  Konrad H. Bleicher ,  Eric A. Kitas

IPC分类号： A61K38/26 ,  A61K38/28 ,  A61K38/00 ,  A61P3/10 ,  A61P7/12 ,  C07K14/605 ,  C07K5/00 ,  C07K7/00 ,  C07K16/00 ,  C07K17/00

CPC分类号： C07K14/605 ,  A61K38/26

摘要： Provided herein are glucagon analogs which exhibit potent activity at the GIP receptor, and, as such are contemplated for use in treating diabetes and obesity. In exemplary embodiments, the glucagon analog of the present disclosures exhibit an EC50 at the GIP receptor which is within the nanomolar or picomolar range.

公开(公告)号：US09764004B2

公开(公告)日：2017-09-19

申请号：US15293324

申请日：2016-10-14

申请人： Eli Lilly and Company

发明人： Jorge Alsina-Fernandez ,  Tamer Coskun

IPC分类号： A61K38/26 ,  A61P3/10 ,  A61P7/12 ,  C07K14/605 ,  C07K14/00

CPC分类号： A61K38/26 ,  A61K45/06 ,  C07K14/001 ,  C07K14/605 ,  A61K2300/00

摘要： The present invention relates to compounds with an extended duration of action at the glucagon receptor as compared to native glucagon. Specifically provided are glucagon receptor agonists with modifications to the structure of native glucagon introduced to selectively agonize the glucagon receptor over an extended period of time.