N.v. Organon

Merck Sharp + Dohme B.v.

Msd Oss B.v.

Akzo Nobel N.v.

Pharmacopeia Inc.

David Jonathan Bennett

Jiaqiang Cai

Philip Stephen Jones

Andrew John Cooke

Andrew Stanley Edwards

Koc-Kan Ho

Michael H Ohlmeyer

Nasrin Ansari

Emma Louise Carswell

Michelle Lee Morris

Irina Neagu

Zoran Rankovic

Yajing Rong

Jui-Hsiang Chan

Andrew Roughton

Andrew Cooke

Niall Morton Hamilton

Robert Gilfillan

Andrew Laird Roughton

Olaf Nimz

Mingqiang Zhang

Jonathan Gillespie

Ronald Palin

John Stephen Robinson

Fiona Elizabeth Andrews

Iain Cumming

Xavier Fradera

The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein Ris H or (C)alkyl; Ris halogen or (C)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the S. . . Ssubstites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain. 

1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derivatives

The present invention relates to (1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl derivatives having the general formula (I) to pharmaceutical compositions comprising the same and to the use of these (1,1,1,3,3,3-hexafluoro-2-hydroxy-propan-2-yl)phenyl derivatives in the treatment of atherosclerosis. 

(1, 1, 1,3,3,3-hexafluoro-2 hydroxypropan-2-yl) phenyl derivative, pharmaceutical compositions thereof and their use for the treatment of atherosclerosis

The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein Ris (C)alkyl, (C)cycloalkyl or (C)cycloalkyl(C)alkyl, each of which may be substituted by hydroxy, cyano or halogen; Rrepresents 1 or 2 optional halogens; Ris (C)alkyl, (C)cycloalkyl or (C)cycloalkyl(C)alkyl, each of which may be substituted by one or more halogens; A represents a heteroaryl ring system comprising 1-3 heteroatoms selected from N, O and S, which ring system is 5- or 6-membered when X is C, and 5-membered when X is N; n is 1 or 2; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same, and to the use of a these 1-(4-ureidobenzoyl)piperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism. 

1-(4-ureidobenzoyl)piperazine derivatives

The present invention relates to hexafluoroisopropanol derivatives having the general formula I to pharmaceutical compositions comprising the same and to the use of these hexafluoroisopropanol derivatives in the treatment of atherosclerosis.

Hexafluoroisopropanol derivatives

The present invention relates to N-benzyl,N'-arylcarbonylpiperazine derivatives having the general formula I to pharmaceutical compositions comprising the same, and to the use of a these N-benzyl,N&#x2032;-arylcarbonylpiperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.

N-benzyl,N'-arylcarbonylpiperazine derivatives

The invention relates to the compound N-(2-oxo-2-propoxyethyl)-&#x3b2;-phenyl-D-phenyl-alanyl-N-[(1-amino-6-iso-quinolinyl)methyl]-L-prolinamide or a pharmaceutically acceptable salt thereof, to a pharmaceutical composition comprising said compound, as well as to the use of the compound for the manufacture of a medicament for treating or for preventing thrombin mediated diseases.

Aminoisoquinoline thrombin inhibitor with improved bioavailability

The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.

6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives

The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I wherein each of the substituents is given the definition as set forth in the specification and claims, pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S and/or cathepsin K related diseases such as osteoporosis, atherosclerosis, inflammation and immune disorders, such as rheumatoid arthritis, and chronic pain, such as neuropathic pain.

The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I  The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these alanine 2,6-dialkoxyphenyl ester derivatives as hypnotics for the induction and maintenance of general anaesthesia.

Alanine 2,6-dialkoxyphenyl ester derivatives as hypnotics

Disclosed is a 6-mercapto-cyclodextrin derivative having a general formula (I, ) wherein m is 0-7 and n is 1-8 and m+n=7 or 8; R is (C) alkylene, optionally substituted 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

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Newhouse, United Kingdom

David Jonathan Bennett