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. |