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公开(公告)号：EP3873893A1
公开(公告)日：2021-09-08
申请号：EP19809243.9
申请日：2019-10-31
发明人： ARASAPPAN, Ashok , BELL, Ian, M. , BRESLIN, Michael, J. , BUNGARD, Christopher James , BURGEY, Christopher, S. , CHOBANIAN, Harry, R. , COX, Jason, M. , GINNETTI, Anthony, T. , GUIADEEN, Deodial Guy , JONES, Kristen, L. G. , LAYTON, Mark, E. , LIU, Hong , LIU, Jian , PERKINS, James, J. , STACHEL, Shawn, J. , SUEN-LAI, Linda, M. , WU, Zhe
IPC分类号： C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D491/04 , C07D495/04 , A61P29/00 , A61K31/4439 , A61K31/444
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2.发明授权
公开(公告)号：EP1755572B1
公开(公告)日：2012-02-15
申请号：EP05756622.6
申请日：2005-06-03
发明人： HANNEY, Barbara , KIM, Yuntae , KROUT, Michael, R. , MEISSNER, Robert, S. , MITCHELL, Helen, J. , MUSSELMAN, Jeffrey , PERKINS, James, J. , WANG, Jiabing
IPC分类号： C07D213/61 , C07C235/06 , C07C233/13 , A61K31/165 , A61P5/26
CPC分类号： C07D295/205 , C07C233/13 , C07C235/34 , C07C255/60 , C07C271/12 , C07C271/22 , C07C2601/02 , C07D213/61 , C07D213/73
摘要： Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzhheiner’s disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.
摘要翻译： 结构式I的化合物是以组织选择性方式的雄激素受体（AR）的调节剂。 这些化合物可用于增强减弱的肌肉紧张度和治疗由雄激素缺乏引起的疾病或可由雄激素给药改善的疾病，包括骨质疏松症，骨质减少症，糖皮质激素诱导的骨质疏松症，牙周病，骨折，骨重建后的骨损伤 手术，肌营养不良，虚弱，衰老皮肤，男性性腺机能减退，女性绝经后症状，动脉粥样硬化，高胆固醇血症，高脂血症，肥胖，再生障碍性贫血和其他造血障碍，炎症性关节炎和关节修复，艾滋病毒消耗，前列腺癌，良性前列腺增生 ），腹部肥胖，代谢综合征，II型糖尿病，癌症恶病质，阿尔茨海默病，肌营养不良症，认知衰退，性功能障碍，睡眠呼吸暂停，抑郁症，卵巢早衰，自身免疫性疾病，单独或与其他活性剂组合。
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3.发明授权N-(4-OXO-3,4-DIHYDROQUINAZOLIN-2-YL)BUTANAMIDES AS ANDROGEN RECEPTOR MODULATORS 有权N-（4-氧代-3,4-二氢喹唑啉-2-基）丁酰胺ALS雄激素受体调节
公开(公告)号：EP1940407B1
公开(公告)日：2010-11-10
申请号：EP06825101.6
申请日：2006-09-22
发明人： HANNEY, Barbara , KIM, Yuntae , MITCHELL, Helen, J. , MUSSELMAN, Jeffrey, D. , PERKINS, James, J.
IPC分类号： A61K31/517 , C07D239/90 , C07D409/12 , A61P15/00 , A61P19/00 , A61P25/00 , A61P35/00 , A61P3/00 , A61P5/00
CPC分类号： C07D403/06 , C07D239/90 , C07D409/12
摘要： The invention relates to substituted N-(4-oxo-3,4-dihydroquinazolin-2-yl)butanamid derivatives which modulate androgen receptors to treat conditions such as: osteoporosis, peridontal disease, bone fracture, frailty, and sarcopenia.
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4.发明授权POLYMORPHS OF ANDROGEN RECEPTOR MODULATOR - (N-3H-IMIDAZO [4 , 5-B] PYRIDIN-2-YL-METHYL) -2-FLUORO-4-METHYL-3-OXO-4-AZA-ANDROST- 1-EN-17 . BETA . -CARBOXAMIDE 有权多聚乙二醇和脱氧核糖核酸酶N-（3H-咪唑并[4,5-B]吡啶-2-基]甲基} -2-氟-4-甲基-3-氧代-4-氮杂-5-丙酸安替罗醌-1 -EN-17 -β-CARBONSÄUREAMID
公开(公告)号：EP1960417B1
公开(公告)日：2012-10-17
申请号：EP06838943.6
申请日：2006-12-04
发明人： TAN, Lushi , MEISSNER, Robert S. , LI, Wenjie , PERKINS, James, J. , COTE, Aaron, S. , STELLABOTT, Joyce , KIANG, Yuan-Hon
CPC分类号： C07J73/005 , C07D471/04
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公开(公告)号：EP1252162B1
公开(公告)日：2012-07-25
申请号：EP01942625.3
申请日：2001-01-16
发明人： DUGGAN, Mark, E. , HALCZENKO, Wasyl , HUTCHINSON, John, H. , LI, Aiwen , MEISSNER, Robert, S. , PERKINS, James, J. , STEELE, Thomas, G. , WANG, Jiabing , PATANE, Michael, A.
IPC分类号： A61K31/444 , A61K31/4166 , A61P19/10 , A61K31/4178 , C07D471/04 , C07D401/14 , C07D405/14 , C07D471/10
CPC分类号： C07D213/73 , A61K45/06 , C07D401/14 , C07D405/14 , C07D471/04 , C07D471/10
摘要： The present invention relates to novel imidazolidinone derivatives thereof, their synthesis, and their use as αν integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3 and/or αvβ5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.
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6.发明授权QUINOLINE CARBOXAMIDE AND QUINOLINE CARBONITRILE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE 有权喹啉羧酰胺和喹啉碳腈衍生物作为mGluR2-阴离子调节剂，组合物和它们的用途
公开(公告)号：EP2775841B1
公开(公告)日：2017-09-13
申请号：EP12846579.6
申请日：2012-10-26
发明人： BUNGARD, Christopher James , CONVERSO, Antonella , DE LEON, Pablo , HANNEY, Barbara , HARTINGH, Timothy John , MANIKOWSKI, Jesse Josef , MANLEY, Peter, J. , MEISSNER, Robert , MENG, Zhaoyang , PERKINS, James, J. , RUDD, Michael, T. , SHU, Youheng
IPC分类号： A61K31/4725 , A61P25/20 , A61P25/28 , A61P25/04 , C07D401/06 , C07D401/14 , C07D215/48
CPC分类号： C07D413/14 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D215/48 , C07D401/04 , C07D401/06 , C07D401/14 , C07D409/04 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D491/10
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7.发明公开QUINOLINE CARBOXAMIDE AND QUINOLINE CARBONITRILE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE 有权喹啉羧酰胺和喹啉碳腈衍生物作为mGluR2-阴离子调节剂，组合物和它们的用途
公开(公告)号：EP2775841A1
公开(公告)日：2014-09-17
申请号：EP12846579.6
申请日：2012-10-26
发明人： BUNGARD, Christopher James , CONVERSO, Antonella , DE LEON, Pablo , HANNEY, Barbara , HARTINGH, Timothy John , MANIKOWSKI, Jesse Josef , MANLEY, Peter, J. , MEISSNER, Robert , MENG, Zhaoyang , PERKINS, James, J. , RUDD, Michael, T. , RUDD, Michael, T. , SHU, Youheng
IPC分类号： A01N43/42
CPC分类号： C07D413/14 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D215/48 , C07D401/04 , C07D401/06 , C07D401/14 , C07D409/04 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D491/10
摘要： The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, R
Q , -L-, R
1 , n, R
2 , and R
3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.摘要翻译： 本发明提供了式（I）的喹啉甲酰胺和喹啉甲腈化合物，其中环A，R Q，-L-，R 1，n，R 2和R 3如本文所定义。 本发明化合物可用作非竞争性mGluR2拮抗剂或mGluR2阴变构调节剂（NAM），并且在涉及mGluR2-NAM受体参与的疾病或病症（例如人）治疗患者（优选人类）的方法中，例如 通过给患者施用治疗有效量的本发明化合物或其药学上可接受的盐作为阿尔茨海默病，认知障碍，精神分裂症和其他情绪障碍，疼痛障碍和睡眠障碍。 本发明还涉及包含本发明化合物或其药学上可接受的盐（任选与一种或多种另外的活性成分组合）和药学上可接受的载体的药物组合物，以及所述化合物和药物组合物 本发明在治疗这些疾病中的用途。
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公开(公告)号：EP1622567B1
公开(公告)日：2013-07-24
申请号：EP04751257.9
申请日：2004-05-03
IPC分类号： A61K31/56
CPC分类号： A61K31/58 , C07J73/005
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9.发明公开2- [1-PHENYL-5-HYDROXY-4a-SUBSTITUTED-HEXAHYDROCYCLOPENTA [F]INDAZOL-5-YL]ETHYL PHENYL DERIVATIVES AS GLUCOCORTICOID RECEPTOR LIGANDS 审中-公开2- [1-苯基-5-羟基-4-取代基 - 六氢环戊二烯并[F]茚满-5-YL]乙基戊二酸盐GLUCOCORTICOIDREZEPTORLIGANDEN
公开(公告)号：EP2493303A1
公开(公告)日：2012-09-05
申请号：EP10827382.2
申请日：2010-10-26
发明人： BUNGARD, Christopher, James , PERKINS, James, J. , MANIKOWSKI, Jesse, J. , DE LEON, Pablo , MEISSNER, Robert, S.
CPC分类号： C07D401/06 , C07D231/54 , C07D401/04
摘要： The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
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公开(公告)号：EP3873468A1
公开(公告)日：2021-09-08
申请号：EP19880139.1
申请日：2019-10-28
发明人： BRESLIN, Michael, J. , BUNGARD, Christopher James , CHOBANIAN, Harry, R. , JONES, Kristen, L. G. , LAYTON, Mark, E. , LIU, Jian , PERKINS, James, J. , SCHUBERT, Jeffrey William , STACHEL, Shawn, J. , SUEN-LAI, Linda, M. , WU, Zhe
IPC分类号： A61K31/4425 , A61K31/167 , A61K31/44 , C07D213/06 , C07D213/20
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