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序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
101 Anti-viral compounds US15434789 2017-02-16 US10028937B2 2018-07-24 Mary E. Bellizzi; David A. Betebenner; Jean-Christophe C. Califano; William A. Carroll; Daniel D. Caspi; David A. DeGoey; Pamela L. Donner; Charles A. Flentge; Yi Gao; Charles W. Hutchins; Douglas K. Hutchinson; Tammie K. Jinkerson; Warren M. Kati; Ryan G. Keddy; Allan C. Krueger; Wenke Li; Dachun Liu; Clarence J. Maring; Mark A. Matulenko; Christopher E. Motter; Lissa T. Nelson; Sachin V. Patel; John K. Pratt; John T. Randolph; Todd W. Rockway; Kathy Sarris; Michael D. Tufano; Seble H. Wagaw; Rolf Wagner; Kevin R. Woller
Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
102 Geminal Substituted Aminobenzisoxazole Compounds as Agonists of Alpha7-Nicotinic Acetylcholine Receptors US15233664 2016-08-10 US20170044155A1 2017-02-16 Raksha Acharya; Duane A. Burnett; Matthew Gregory Bursavich; Andrew Simon Cook; Bryce Alden Harrison; Andrew J. McRiner
The present invention relates to novel geminal substituted aminobenzisoxazole compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of α7-nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.
103 SALT FORMS OF (S)-QUINUCLIDIN-3-YL (2-(2-(4-FLUOROPHENYL)THIAZOL-4-YL)PROPAN-2-YL)CARBAMATE US14776432 2014-03-14 US20160039805A1 2016-02-11 Craig S. SIEGEL; Jin ZHAO
The present invention relates to novel salt forms of (S)-Quinuclidin-3-yl(2-(2-(4-fluorophenyl)thiazol-4-yl)propan-2-yl)carbamate useful as an inhibitor of glucosylceramide synthase (GCS) and for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.
104 Compounds US14097586 2013-12-05 US09199980B2 2015-12-01 Elisabetta Armani; Gabriele Amari; Mauro Riccaboni; Andrea Rizzi; Charles Baker-Glenn; Wesley Blackaby; Herve′ Van de Poel; Ben Whittaker
Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of diseases of the respiratory tract characterized by airway obstruction.
105 Inhibitors of PDE4 enzyme and antagonists of muscarinic M3 receptor US14097397 2013-12-05 US09169245B2 2015-10-27 Elisabetta Armani; Gabriele Amari; Mauro Riccaboni; Charles Baker-Glenn
Compounds of formula (I) described herein are both inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists, and are useful for the prevention and/or treatment of diseases of the respiratory tract characterized by airway obstruction.
106 Glucosylceramide synthase inhibitors US14471958 2014-08-28 US09126993B2 2015-09-08 Elyse Bourque; Bradford Hirth; Renato Sklerj; Elina Makino; Fazeela Morshed; Lingyun Li; Paul Mason; John P. Leonard; James Lillie; Hanlan Liu; Mary A. Cromwell; Bing Wang; Thomas O'Shea
The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.
107 Anti-Viral Compounds US14683910 2015-04-10 US20150218194A1 2015-08-06 Mary E. Bellizzi; David A. Betebenner; Jean C. Califano; Daniel D. Caspi; David A. DeGoey; Pamela L. Donner; Charles A. Flentge; Yi Gao; Charles W. Hutchins; Douglas K. Hutchinson; Tammie K. Jinkerson; Warren M. Kati; Ryan G. Keddy; Allan C. Krueger; Wenke Li; Dachun Liu; Clarence J. Maring; Mark A. Matulenko; Christopher E. Motter; Lissa T. Nelson; Sachin V. Patel; John K. Pratt; John T. Randolph; Todd W. Rockway; Kathy Sarris; Michael D. Tufano; Seble H. Wagaw; Rolf Wagner; Kevin R. Woller
Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
108 Anti-viral compounds US14180886 2014-02-14 US09006387B2 2015-04-14 Rolf Wagner; John K. Pratt; Dachun Liu; Michael D. Tufano; David A. DeGoey; Warren M. Kati; Charles W. Hutchins; Pamela L. Donner; John T. Randolph; Christopher E. Motter; Lissa T. Nelson; Sachin V. Patel; Mark A. Matulenko; Ryan G. Keddy; Tammie K. Jinkerson; Todd W. Rockway; Clarence J. Maring; Douglas K. Hutchinson; Charles A. Flentge; David A. Betebenner; Kathy Sarris; Kevin R. Woller; Seble H. Wagaw; Jean C. Califano; Wenke Li; Daniel D. Caspi; Mary E. Bellizzi; Yi Gao; Allan C. Krueger
Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
109 PROCESS FOR PRODUCTION OF QUINUCLIDINE COMPOUNDS US14471732 2014-08-28 US20140371457A1 2014-12-18 Yutaka KITAGAWA; Masao FUJITA; Kumiko OTAYA
Provided is a production method for a cis-QMF, which has a low environmental burden and is industrially advantageous. Specifically provided is a production method for a cis-type 2-alkylspiro(1,3-oxathiolane-5,3′)quinuclidine hydrochloride, including: reacting a cis-trans isomer mixture of 2-alkylspiro(1,3-oxathiolane-5,3′)quinuclidine with p-nitrobenzoic acid; resolving the resultant product to produce a cis-type 2-alkylspiro(1,3-oxathiolane-5,3′)quinuclidine p-nitrobenzoate; and converting the p-nitrobenzoate into a hydrochloride.
110 ANTI-VIRAL COMPOUNDS US14180886 2014-02-14 US20140315792A1 2014-10-23 Rolf Wagner; John K. Pratt; Dachun Liu; Michael D. Tufano; David A. DeGoey; Warren M. Kati; Charles W. Hutchins; Pamela L. Dooner; John T. Randolph; Christopher E. Motter; Lissa T. Nelson; Sachin V. Patel; Mark A. Matulenko; Ryan G. Keddy; Tammie K. Jinkerson; Todd W. Rockway; Clarence J. Maring; Douglas K. Hutchinson; Charles A. Flentge; David A. Betebenner; Kathy Sarris; Kevin R. Woller; Seble H. Wagaw; Jean C. Califano; Wenke Li; Daniel D. Caspi; Mary E. Bellizzi; Yi Gao; Allan C. Krueger
Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
111 NOVEL COMPOUNDS US14097586 2013-12-05 US20140155427A1 2014-06-05 Elisabetta Armani; Gabriele Amari; Mauro Riccaboni; Andrea Rizzi; Charles Baker-Glenn; Wesley Blackaby; Herve' Van de Poel; Ben Whittaker
Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of diseases of the respiratory tract characterized by airway obstruction.
112 NOVEL COMPOUNDS US14097397 2013-12-05 US20140155373A1 2014-06-05 Elisabetta Armani; Gabriele Amari; Mauro Riccaboni; Charles Baker-Glenn
Compounds of formula (I) described herein are both inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists, and are useful for the prevention and/or treatment of diseases of the respiratory tract characterized by airway obstruction.
113 Compounds for the treatment of hepatitis C US13798286 2013-03-13 US08722688B2 2014-05-13 Kap-Sun Yeung; Kyle E. Parcella; John A. Bender; Brett R. Beno; Katharine A. Grant-Young; Ying Han; Piyasena Hewawasam; John F. Kadow; Andrew Nickel
The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
114 Anti-viral compounds US12813301 2010-06-10 US08691938B2 2014-04-08 David A. DeGoey; Warren M. Kati; Charles W. Hutchins; Pamela L. Donner; Allan C. Krueger; John T. Randolph; Christopher E. Motter; Lissa T. Nelson; Sachin V. Patel; Mark A. Matulenko; Ryan G. Keddy; Tammie K. Jinkerson; Yi Gao; Dachun Liu; John K. Pratt; Todd W. Rockway; Clarence J. Maring; Douglas K. Hutchinson; Charles A. Flentge; Rolf Wagner; Michael D. Tufano; David A. Betebenner; Kathy Sarris; Kevin R. Woller; Seble H. Wagaw; Jean C. Califano; Wenke Li; Daniel D. Caspi; Mary E. Bellizzi
Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
115 INDOLE AND BENZOFURAN FUSED ISOQUINUCLIDENE DERIVATIVES AND PROCESSES FOR PREPARING THEM US13749593 2013-01-24 US20130211074A1 2013-08-15 Robert M. Moriarty
Provided herein are indole and benzofuran fused isoquinuclidene derivatives. Also provided herein are processes, preferably enantioselective processes, for preparing such derivatives including processes for preparing (−) and (+) noribogaine or a salt thereof, in substantially enantiomerically pure forms.
116 COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE US13440981 2012-09-04 US20130095193A1 2013-04-18 Jean-Damien Charrier; David Kay; Somhairle MacCormick; Pierre-Henri Storck; Joanne Pinder; Michael Edward O'Donnell; Ronald Marcellus Alphonsus Knegtel; Stephen Clinton Young; Philip Michael Reaper; Steven John Durrant; Heather Clare Twin; Christopher John Davis
The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I: wherein the variables are as defined herein.
117 PROCESS FOR PRODUCTION OF QUINUCLIDINE COMPOUNDS US13503382 2010-10-21 US20130060036A1 2013-03-07 Yutaka Kitagawa; Masao Fujita; Kumiko Otaya
Provided is a production method for a cis-QMF, which has a low environmental burden and is industrially advantageous. Specifically provided is a production method for a cis-type 2-alkylspiro(1,3-oxathiolane-5,3′)quinuclidine hydrochloride, including: reacting a cis-trans isomer mixture of 2-alkylspiro(1,3-oxathiolane-5,3′)quinuclidine with p-nitrobenzoic acid; resolving the resultant product to produce a cis-type 2-alkylspiro(1,3-oxathiolane-5,3′)quinuclidine p-nitrobenzoate; and converting the p-nitrobenzoate into a hydrochloride.
118 Pyridone/hydroxypyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors US12307424 2007-07-02 US08318941B2 2012-11-27 Jeffrey A. Robl; Shung C. Wu; David S. Yoon
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure formula (I) enantiomers, diastereomers, solvates, salts, tautomers or prodrugs thereof wherein, A, W, X, Y and R1 are defined herein.
119 HSP90 inhibitory carbazole derivatives, compositions containing same and use thereof US12881414 2010-09-14 US08309721B2 2012-11-13 Jean-Marie Ruxer; Victor Certal; Marcel Alasia; Luc Bertin; Herve Minoux; Patrick Mailliet; Frank Halley; Maria Mendez-Perez
The invention relates to the novel substances in Formula (I): wherein Het is a heterocycle optionally substituted by one or a plurality of radicals R1 or R′1; R is selected from the group comprising Formula (A′), (B), (C), (D), or (E), with R1 and/or R′1 selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxyl, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalcoxy, alkylhio, or carboxy that is free or esterified by an alkyl, carboxamide, CO—NH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—S02-alkyl, S(0)2-NHalkyl, or S(02)-N(alkyl)2 radical; all these radicals are optionally substituted; W1, W2, and W3 independently are CH or N; X is 0, S, NR2, C(O), S(O), or S(0)2; Z is optionally substituted H, Hal, -0-R2 or —NH—R2 with R2 being H, alkyl, cycloalkyl, or heterocycloalkyl; and these substances are all isomeric forms and salts thereof, used as drugs.
120 Compounds for the treatment of hepatitis C US13371786 2012-02-13 US08309558B2 2012-11-13 Kap-Sun Yeung; Kyle E. Parcella; John A. Bender; Brett R. Beno; Katharine A. Grant-Young; Ying Han; Piyasena Hewawasam; John F. Kadow; Andrew Nickel
The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
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