Other

Merck Sharp + Dohme Corp.

N.v. Organon

Merck Sharp + Dohme B.v.

Msd Oss B.v.

Akzo Nobel

Pharmacopeia Inc.

Ronald Palin

Simon James Anthony Grove

Mingiang Zhang

John Kinnaird Maclean

Koc-Kan Ho

Michael H Ohlmeyer

Nasrin Ansari

Paul David Ratcliffe

Steven G Kultgen

Irina Neagu

Yajing Rong

Craig Jamieson

John Kinnaird Ferguson MacLean

Andrew Laird Roughton

Ashvinkumar Dhirubhai Mistry

John Kinnaird Ferguson Maclean

Colin Alasdair Gray

David Jonathan Bennett

Angus John Morrison

Jonathan Bennett

The invention relates to amino-heteroaryl derivatives having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain. 

Amino-heteroaryl derivatives as HCN blockers

Disclosed is a 6-mercapto-cyclodextrin derivative having general formula (I) wherein m is 0-7 and n is 1-8 and m+n=7 or 8; R is (C)alkylene, optionally substituated with 1-3 OH groups, or (CH)-phenylene-(CH)&#x2014;; o and p are independently 0-4; X is COOH, CONHR, NHCOR, SOOH, PO(OH), O(CH&#x2014;CH&#x2014;O)&#x2014;H, OH or tetrazol-5-yl; Ris H or (C)alkyl; Ris carboxyphenyl; q is 1-3; or pharmaceutically acceptable salts thereof. The 6-mercaptocyclodextrin derivative is highly suitable for use in the reversal of drug-induced neuromuscular block.

6-mercapto-cyclodextrin derivatives:reversal agents for drug-induced neuromuscular block

The present invention relates to isoxazole-3-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders. 

5-phenyl-isoxazole-3-carboxamide derivatives as TRPV1 modulators

The invention relates to (pyrrolidin-2-yl)phenyl derivatives having the general Formula I wherein Ris (C)alkyl, halo(C)alkyl, (C)alkyloxy, or halo(C)alkyloxy; Ris H, (C)alkyl, halo(C)alkyl, (C)alkyloxy, halo(C)alkyloxy or halogen; Ris H, (C)alkyl or halo(C)alkyl; Ris H, (C)alkyl or halo(C)alkyl; Ris H, (C)alkyl or halo-(C)-alkyl; or Rand R, when bonded to the same carbon atom, can together with the carbon atom form a spiro(C)cycloalkyl group, optionally substituted with halogen; Ris H, (C)alkyl, halo(C)alkyl, (C)alkyloxy, halo(C)alkyloxy or halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these (pyrrolidin-2-yl)phenyl derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.

(Pyrrolidin-2-yl)phenyl derivatives

The invention relates to 2-(benzimidazol-1-yl)-acetamide bisaryl derivative having the general Formula I wherein n is 0 or 1; Arrepresents a diradical derived from a 5- or-6-membered aromatic ring, optionally comprising 1-3 heteroatoms selected from N, O and S, said ring being optionally substituted with (C)alkyl, (C)alkyloxy, halogen, CFor cyano; Arrepresents a 6-membered aryl ring, optionally comprising 1-3 nitrogen atoms, said ring being optionally substituted with 1-3 substituents selected from (C)alkyl (optionally substituted with 1 or more halogens), (C)alkyloxy (optionally substituted with 1 or more halogens), di(C)alkylamino, halogen, CFor cyano; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same and to the use of said 2-(benzimidazol-1-yl)-acetamide bisaryl derivatives in the treatment of TRPV1 mediated disorders.

2-(benzimidazol-1-yl)-acetamide bisaryl derivatives

Disclosed is a 6-mercapto-cyclodextrin derivative having general formula (I) wherein m is 0-7 and n is 1-8 and m&plus;n&equals;7 or 8; R is (C )alkylene, optionally substituated with 1-3 OH groups, or (CH ) -phenylene-(CH ) &mdash;; o and p are independently 0-4; X is COOH, CONHR , NHCOR , SO OH, PO(OH) , O(CH &mdash;CH &mdash;O) &mdash;H, OH or tetrazol-5-yl; R is H or (C )alkyl; R is carboxyphenyl; q is 1-3; or pharmaceutically acceptable salts thereof. The 6-mercaptocyclodextrin derivative is highly suitable for use in the reversal of drug-induced neuromuscular block.

6-Mercapto-cyclodextrin derivatives:reversal agents for drug-induced neuromuscular block

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Newhouse, United Kingdom

Ronald Palin