- HALO-SUBSTITUTED PIPERIDINES AS OREXIN RECEPTOR MODULATORS
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The present application relates to certain halo-substituted piperidine compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating substance addiction, panic disorder, anxiety, post-traumatic stress disorder, pain, depression, seasonal affective disorder, an eating disorder, or hypertension.
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Page/Page column 112
(2017/09/05)
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- PYRROLIDINE THROMBIN INHIBITORS
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Compounds of the invention, which may be useful in inhibiting thrombin and associated thrombotic occlusions, have the following structure: (I) or a pharmaceutically acceptable salt thereof, wherein R is a heterocycle or -(CR4R5)1-2NH2 , wherein R4 and R5,
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Page/Page column 25
(2014/03/21)
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- Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability
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Modification of lead compound 1 by reducing lipophilicity in the P3 group produced a series of low molecular weight thrombin inhibitors with excellent potency in functional assays, metabolic stability, and oral bioavailability. These modifications led to
- Morrissette, Matthew M.,Stauffer, Kenneth J.,Williams, Peter D.,Lyle, Terry A.,Vacca, Joseph P.,Krueger, Julie A.,Lewis, S. Dale,Lucas, Bobby J.,Wong, Bradley K.,White, Rebecca B.,Miller-Stein, Cynthia,Lyle, Elizabeth A.,Wallace, Audrey A.,Leonard, Yvonne M.,Welsh, Denise C.,Lynch, Joseph J.,McMasters, Daniel R.
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p. 4161 - 4164
(2007/10/03)
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- THERAPEUTIC USE OF ARYL AMINO ACID DERIVATIVES
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The compounds of formula (I) are useful in the treatment of faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, neuropathic pain, neuropathological disorders and sleep disorders. Processes for the preparation of the final products and intermediates useful in the process are included. Pharmaceutical compositions containing one or more of the compounds are also included.
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Page/Page column 35-36
(2010/02/06)
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- Stereoselective synthesis of a potent thrombin inhibitor by a novel P2-P3 lactone ring opening
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The concise synthesis of a potent thrombin inhibitor was accomplished by a mild lactone aminolysis between an orthogonally protected bis-benzylic amine and a diastereomerically pure lactone. The lactone was synthesized by the condensation of L-proline met
- Nelson, Todd D.,LeBlond, Carl R.,Frantz, Doug E.,Matty, Louis,Mitten, Jeffrey V.,Weaver, Damian G.,Moore, Jeffrey C.,Kim, Jaehon M.,Boyd, Russell,Kim, Pei-Yi,Gbewonyo, Kodzo,Brower, Mark,Sturr, Michael,McLaughlin, Kathleen,McMasters, Daniel R.,Kress, Michael H.,McNamara, James M.,Dolling, Ulf H.
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p. 3620 - 3627
(2007/10/03)
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- Thrombin inhibitors
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Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e.g. 1-(3(S)-Cyclopropyl-2(R)-hydroxybutanoyl)azetidine-2(S)-N-(2-aminomethyl-5-chlorobenzyl)carboxamide, and 1-(3-Cyclopropyl-3-methyl-2(R)-hydroxybutanoyl)azetidine-2(S)-N-(2-aminomethyl-5-chlorobenzyl)carboxamide.
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- Thrombin inhibitors
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Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e.g. 1-(3(S)-Cyclopropyl-2(R)-hydroxybutanoyl)azetidine-2(S)-N-(2-aminomethyl-5-chlorobenzyl)carboxamide, and 1-(3-Cyclopropyl-3-methyl-2(R)-hydroxybutanoyl)azetidine-2(S)-N-(2-aminomethyl-5-chlorobenzyl)carboxamide.
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- Thrombin inhibitors
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Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: wherein R1 is, for example, hydrogen, Cl, or cyano, and R2 is, for example, hydrogen,
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- Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position
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Thrombin inhibitors incorporating o-aminoalkylbenzylamides in the P1 position were designed, synthesized and found to have enhanced potency and selectivity in several different structural classes. X-ray crystallographic analysis of compound 24 bound in the α-thrombin-hirugen complex provides an explanation for these unanticipated results.
- Rittle, Kenneth E.,Barrow, James C.,Cutrona, Kellie J.,Glass, Kristen L.,Krueger, Julie A.,Kuo, Lawrence C.,Lewis, S. Dale,Lucas, Bobby J.,McMasters, Daniel R.,Morrissette, Matthew M.,Nantermet, Philippe G.,Newton, Christina L.,Sanders, William M.,Yan, Youwei,Vacca, Joseph P.,Selnick, Harold G.
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p. 3477 - 3482
(2007/10/03)
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- Thrombin inhibitors
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Compounds of the invention are useful in inhibiting thrombin and treating blood coagulation and cardiovascular disorders and have the following structure: wherein R3 is hydrogen or halogen, and u is N or CH.
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- Thrombin inhibitors
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Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e.g. where R3 is —CH2NH2, —CH2CH2NH2, or —CH2NHC(O)OC(CH3)3.
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- Practical Synthesis of Aryl Triflates under Aqueous Conditions
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A practical and efficient synthesis of aryl triflates under biphasic basic aqueous conditions is described. The current methodology provides entry into these valuable substrates that omits the use of amine bases and allows facile isolation by s
- Frantz, Doug E.,Weaver, Damian G.,Carey, James P.,Kress, Michael H.,Dolling, Ulf H.
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p. 4717 - 4718
(2007/10/03)
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