- Modified benzoxazolone derivative as 18-kDa TSPO ligand
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We have synthesized six new congeners of acetamidobenzoxazolone for Translocator Protein [18 kDa, TSPO] imaging. The best in vitro binding affinity (10.8?±?1.2?nm) for TSPO was found for N-methyl-2-(5-(naphthalen-1-yl)-2-oxobenzo[d]oxazol-3(2H)-yl)-N-phen
- Kumari, Neelam,Chadha, Nidhi,Srivastava, Pooja,Mishra, Lokesh Chandra,Bhagat, Sunita,Mishra, Anil K.,Tiwari, Anjani K.
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p. 511 - 519
(2017/09/13)
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- "TRPV1 VANILLOID RECEPTOR ANTAGONISTS WITH A BICYCLIC PORTION"
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The invention discloses compounds of formula I wherein Y is a group of formula A, B, C, D, or E: and W, Q, n, R1, R2, R3, U1-U5, J and K have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active
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Page/Page column 66; 132
(2011/10/13)
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- TRPV1 vanilloid receptor antagonists with a bicyclic portion
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The invention discloses compounds of formula I wherein Y s selected from a group of formula and W, Q, n, R1, R2, R3, U1-U5 have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1. 1.
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Page/Page column 22
(2011/11/01)
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- 3H-BENZOOXAZOL-2-ONE MODULATORS OF D2 RECEPTOR AND/OR 5-HT1A RECEPTOR
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The present invention relates to new 3H-benzooxazol-2-one modulators of D2 receptors and/or 5-HT1A receptors, pharmaceutical compositions thereof, and methods of use thereof.
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Page/Page column 17
(2010/06/11)
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- SPIROHYDANTOIN ARYL CGRP RECEPTOR ANTAGONISTS
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Compounds of formula (I); (wherein variables A1, A2. A3, A4, A5, A6, A7, B3 E1, E2, E3, E4, E5, G1, G2 and R.6 are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
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Page/Page column 72-73
(2008/06/13)
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- SPIROLACTAM ARYL CGRP RECEPTOR ANTAGONISTS
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Compounds of formula (I): (wherein variables A1, A2, A3, A4, A5, A6, A7, E1, E2, E3, E4, E5, G1, G2, J and K are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
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Page/Page column 89
(2008/06/13)
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- Stable crystalline form of bifeprunox mesylate, dosage forms thereof and methods for using same
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The present disclosure provides novel pharmaceutical compounds and methods for making the same, novel pharmaceutical dosage forms and methods for making the same, and methods for using said compounds and dosage forms to treat and prevent diseases and/or d
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Page/Page column 6
(2008/06/13)
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- Stable crystalline form of bifeprunox mesylate (7-[4-([1,1'-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate)
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The invention relates to a stable polymorphic form of the compound 7-[4-([1,1′-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate (INNM bifeprunox mesylate), a method for the preparation of said polymorphic form and its use in p
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Page/Page column 5
(2010/10/19)
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- STABLE CRYSTALLINE FORM OF BIFEPRUNOX MESYLATE (7-[4-([1,1'-BIPHENYL]-3-YLMETHEYL)-1-PIPERAZINYL]-2(3H)-BENZOXAZOLONE MONOMETHANESULFONATE
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The invention relates to a stable polymorphic form of the compound 7-[4-([1,1'-biphenyl] -3-ylmethyl)-l -piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate (INNM bifeprunox mesylate), a method for the preparation of said polymorphic form and its use in
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Page/Page column 11
(2010/02/10)
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