公开(公告)号：US10968166B2

公开(公告)日：2021-04-06

申请号：US16228657

申请日：2018-12-20

申请人： PTC Therapeutics, Inc.

发明人： Orion D. Jankowski ,  Kieron E. Wesson ,  Paul Mollard ,  William D. Shrader

IPC分类号： C07C235/80 ,  C07C235/32 ,  C07C235/78 ,  C07C317/28 ,  C07D207/27 ,  C07D211/46 ,  C07D213/40 ,  C07D233/61 ,  C07D295/13 ,  C07D295/192 ,  C07D265/30 ,  C07D311/66 ,  C07D207/26 ,  C07D213/50 ,  C07D295/116 ,  C07D295/185 ,  A61P21/00 ,  A61P25/00 ,  A61P25/16 ,  A61P27/00

摘要： Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinoly)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.

公开(公告)号：US10167251B2

公开(公告)日：2019-01-01

申请号：US15374916

申请日：2016-12-09

申请人： BioElectron Technology Corporation

发明人： Orion D. Jankowski ,  Kieron E. Wesson ,  Paul Mollard ,  William D. Shrader

IPC分类号： C07C235/80 ,  C07C235/78 ,  C07C317/28 ,  C07D207/27 ,  C07D211/46 ,  C07D213/40 ,  C07D233/61 ,  C07D295/13 ,  C07D295/192 ,  C07D265/30 ,  C07D311/66 ,  C07D207/26 ,  C07D213/50 ,  C07D295/116 ,  C07D295/185

摘要： Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, an well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.

公开(公告)号：US20180305328A1

公开(公告)日：2018-10-25

申请号：US15766011

申请日：2016-10-07

申请人： Khondrion IP B.V.

发明人： Julien David Beyrath ,  Mina Pellegrini ,  Petrus Maria van Zandvoort ,  Johannes Albertus Maria Smeitink

IPC分类号： C07D311/66 ,  C07D405/12

摘要： The invention relates to novel compounds that are useful for modulating cellular ROS. The compounds are amide-derivatives of 2-hydroxy-2-methyl-4-(3,5,6-trimethyl-1,4-benzoquinon-2-yl)-butanoic acid. The compounds of the invention are formulated into pharmaceutical or cosmetic compositions. The invention further relates to methods wherein the compounds of the invention are used for treating or preventing diseases associated with increased ROS levels mitochondrial disorders and/or conditions associated with mitochondrial dysfunction, including adverse drug effects. The invention also relates to cosmetic methods for treating or delaying further aging of the skin and veterinary applications.

公开(公告)号：US20130289034A1

公开(公告)日：2013-10-31

申请号：US13924363

申请日：2013-06-21

申请人： Edison Pharmaceuticals, Inc.

发明人： Orion D. JANKOWSKI ,  Kieron E. WESSON ,  Paul MOLLARD ,  William D. SHRADER

IPC分类号： C07C235/78 ,  C07D295/192 ,  C07D311/66 ,  C07D213/40 ,  C07D207/27 ,  C07D265/30 ,  C07D211/46 ,  C07D295/13

CPC分类号： C07C235/80 ,  C07C235/78 ,  C07C317/28 ,  C07C2601/02 ,  C07C2601/16 ,  C07D207/26 ,  C07D207/27 ,  C07D211/46 ,  C07D213/40 ,  C07D213/50 ,  C07D233/61 ,  C07D265/30 ,  C07D295/116 ,  C07D295/13 ,  C07D295/185 ,  C07D295/192 ,  C07D311/66

摘要： Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.

公开(公告)号：US20110251407A1

公开(公告)日：2011-10-13

申请号：US13126281

申请日：2009-10-28

申请人： Youichi Kyuuko

发明人： Youichi Kyuuko

IPC分类号： C07D311/66 ,  C07B57/00

CPC分类号： C07D311/66 ,  C07B57/00 ,  C07B2200/07 ,  C07C51/487 ,  C07C53/134

摘要： The present invention is a simple method, in which a specific amount of alkali is added to an enantiomeric mixture of an optically active organic carboxylic acid where enantiomers are present in a non-equimolar ratio, or in which the enantiomeric mixture of an optically active organic carboxylic acid is neutralized with an alkali, and then a specific amount of acid is added thereto, thereby separating an organic carboxylic acid salt in the mother liquor and a crystallized organic carboxylic acid from each other. The method makes it possible to obtain an optically active organic carboxylic acid with improved enantiomeric excess. The present invention provides a simple production method for obtaining an optically active organic carboxylic acid with improved enantiomeric excess from an enantiomeric mixture of an optically active organic carboxylic acid where enantiomers are present in a non-equimolar ratio.

摘要翻译： 本发明是一种简单的方法，其中将特定量的碱加入到对映异构体以非等摩尔比存在的光学活性有机羧酸的对映体混合物中，或其中光学活性有机物的对映体混合物 羧酸用碱中和，然后加入特定量的酸，从而将母液中的有机羧酸盐和结晶的有机羧酸彼此分离。 该方法可以获得具有改善的对映体过量的光学活性有机羧酸。 本发明提供了一种简单的制备方法，用于从对映异构体以非等摩尔比存在的光学活性有机羧酸的对映体混合物中获得具有改进的对映异构体过量的光学活性有机羧酸。

公开(公告)号：US20110021514A1

公开(公告)日：2011-01-27

申请号：US12742425

申请日：2008-11-13

申请人： Matthew Cox ,  Donogh John Roger O'Mahony ,  Maria De Los Angeles Estiarte-Martinez ,  Tadashi Kawashima ,  Satoshi Nagayama ,  Yuji Shishido ,  Hirotaka Tanaka ,  Matthew Alexander James Duncton ,  Andrew Antony Calabrese

发明人： Matthew Cox ,  Donogh John Roger O'Mahony ,  Maria De Los Angeles Estiarte-Martinez ,  Tadashi Kawashima ,  Satoshi Nagayama ,  Yuji Shishido ,  Hirotaka Tanaka ,  Matthew Alexander James Duncton ,  Andrew Antony Calabrese

IPC分类号： A61K31/18 ,  C07D311/66 ,  A61K31/352 ,  C07C311/08 ,  C07D265/36 ,  A61K31/538 ,  C07D215/48 ,  A61K31/47 ,  C07D319/20 ,  A61K31/357 ,  C07D405/04 ,  A61K31/4709 ,  A61P29/00 ,  A61P37/06 ,  A61P13/10 ,  A61P3/00 ,  A61P9/00 ,  A61P35/00 ,  A61P19/00

CPC分类号： C07D215/48 ,  C07C311/08 ,  C07C2602/10 ,  C07D265/36 ,  C07D311/58 ,  C07D311/66 ,  C07D319/20 ,  C07D405/04

摘要： Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.

摘要翻译： 公开了具有下列化学式的化合物：化合物可以制备成药物组合物，并且可以用于预防和治疗哺乳动物包括人的多种病症，包括作为非限制性实例的疼痛 ，炎症，创伤性损伤等。

公开(公告)号：US20050209283A1

公开(公告)日：2005-09-22

申请号：US10775883

申请日：2004-02-09

申请人： Robert Hormann ,  Colin Tice ,  Orestes Chortyk ,  Howard Smith ,  Thomas Meteyer

发明人： Robert Hormann ,  Colin Tice ,  Orestes Chortyk ,  Howard Smith ,  Thomas Meteyer

IPC分类号： C07C243/38 ,  C07D311/58 ,  C07D311/66 ,  C07D319/20 ,  A61K31/455 ,  A61K31/165 ,  A61K31/277

CPC分类号： C07C243/38 ,  C07D213/87 ,  C07D311/58 ,  C07D311/66 ,  C07D319/20 ,  C07F7/1896 ,  C12N9/0069 ,  C12N15/85 ,  C12N2830/002

摘要： The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.

摘要翻译： 本发明涉及用于基于核受体的诱导型基因表达系统的非甾体配体，以及调节外源基因表达的方法，其中蜕皮激素受体复合物包含：DNA结合结构域; 配体结合域; 反式激活域 并且配体与包含以下的DNA构建体接触：外源基因和应答元件; 其中外源基因处于响应元件的控制之下，并且在配体存在下DNA结合结构域与响应元件的结合导致基因的激活或抑制。

公开(公告)号：US06855833B2

公开(公告)日：2005-02-15

申请号：US10296873

申请日：2001-06-01

申请人： James Kanter ,  John J. G. Mullins ,  Robert Scarborough ,  Derek Walker ,  Thomas Hense

发明人： James Kanter ,  John J. G. Mullins ,  Robert Scarborough ,  Derek Walker ,  Thomas Hense

IPC分类号： A61P7/00 ,  C07D311/20 ,  C07D311/22 ,  C07D311/58 ,  C07D311/66

CPC分类号： C07D311/22 ,  C07D311/20 ,  C07D311/58

摘要： Disclosed are processes for producing chromane compounds, preferably chroman-2-yl acetic acid compounds and 6-amino-chroman-2-yl acetic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors.

摘要翻译： 本发明公开了生产色氨酸化合物，优选苯并二氢吡喃-2-基乙酸化合物和6-氨基 - 苯并二氢吡喃-2-基乙酸酯的方法，其为制备血小板聚集抑制剂的中间体和/或本身是有效的血小板聚集抑制剂。

公开(公告)号：US20050009818A1

公开(公告)日：2005-01-13

申请号：US10889350

申请日：2004-07-12

申请人： Edward Pierson ,  Daniel Sohn ,  Markus Haeberlein ,  Timothy Davenport ,  Marc Chapdelaine ,  Carey Horchler ,  John McCauley

发明人： Edward Pierson ,  Daniel Sohn ,  Markus Haeberlein ,  Timothy Davenport ,  Marc Chapdelaine ,  Carey Horchler ,  John McCauley

IPC分类号： C07D215/48 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61P5/00 ,  A61P9/00 ,  A61P15/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D215/50 ,  C07D311/24 ,  C07D311/58 ,  C07D311/66 ,  C07D401/04 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  C07D521/00 ,  C07D417/14 ,  C07D413/14 ,  C07

CPC分类号： C07D231/12 ,  A61K31/495 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  C07D215/50 ,  C07D233/56 ,  C07D249/08 ,  C07D311/24 ,  C07D311/58 ,  C07D401/04 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D417/12

摘要： Provided herein is a compound having the formula (I): Wherein said compounds are useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B and 5HT1D antagonists.

摘要翻译： 本文提供具有式（I）的化合物：其中所述化合物可用于治疗精神障碍，包括但不限于抑郁症，广泛性焦虑症，进食障碍，痴呆症，惊恐障碍和睡眠障碍。 该化合物还可用于治疗胃肠道疾病，心血管调节，运动障碍，内分泌障碍，血管痉挛和性功能障碍。 这些化合物是5HT1B和5HT1D拮抗剂。

公开(公告)号：US5731324A

公开(公告)日：1998-03-24

申请号：US376191

申请日：1995-01-19

申请人： Matthew J. Fisher ,  Anne Marie Happ ,  Joseph A. Jakubowski ,  Michael Dean Kinnick ,  Allen D. Kline ,  Michael John Martinelli ,  John Michael Morin, Jr. ,  Michael Paal ,  Gerd Ruhter ,  Kenneth James Ruterbories ,  Daniel J. Sall ,  Theo Schotten ,  Marshall A. Skelton ,  Wolfgang Stenzel ,  Robert Theodore Vasileff

发明人： Matthew J. Fisher ,  Anne Marie Happ ,  Joseph A. Jakubowski ,  Michael Dean Kinnick ,  Allen D. Kline ,  Michael John Martinelli ,  John Michael Morin, Jr. ,  Michael Paal ,  Gerd Ruhter ,  Kenneth James Ruterbories ,  Daniel J. Sall ,  Theo Schotten ,  Marshall A. Skelton ,  Wolfgang Stenzel ,  Robert Theodore Vasileff

IPC分类号： C07D487/04 ,  A61K31/195 ,  A61K31/215 ,  A61K31/335 ,  A61K31/35 ,  A61K31/352 ,  A61K31/38 ,  A61K31/381 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/47 ,  A61K31/472 ,  A61K31/495 ,  A61P7/02 ,  A61P9/10 ,  C07C257/18 ,  C07C257/20 ,  C07C271/64 ,  C07D211/22 ,  C07D211/32 ,  C07D211/34 ,  C07D213/82 ,  C07D217/04 ,  C07D217/06 ,  C07D217/24 ,  C07D221/00 ,  C07D311/22 ,  C07D311/58 ,  C07D311/66 ,  C07D311/70 ,  C07D319/16 ,  C07D333/38 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D491/052 ,  C07D497/04 ,  G03F7/20 ,  C07D311/02

CPC分类号： C07D211/34 ,  C07C257/18 ,  C07C271/64 ,  C07D211/22 ,  C07D213/82 ,  C07D217/04 ,  C07D217/06 ,  C07D217/24 ,  C07D311/22 ,  C07D311/58 ,  C07D333/38 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07C2102/10

摘要： This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, benzopyran, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.