Timothy A. Blizzard - Middletown NJ Kevin D. Dykstra - West Milford NJ Ronald W. Ratcliffe - Matawan NJ
Assignee:
Merck Co., Inc. - Rahway NJ
International Classification:
C07D47714
US Classification:
51421009, 540302
Abstract:
Compounds of formula I: as well as pharmaceutically acceptable salts thereof useful as carbapenem antibacterial agents are disclosed wherein X is CH or C O.
Soumya P. Sahoo - Old Bridge NJ, US Meng-Hsin Chen - Westfield NJ, US Kevin D. Dykstra - West Milford NJ, US Hiroo Koyama - Hoboken NJ, US Peter T. Meinke - Scotch Plains NJ, US Stephen J. O'Keefe - Mountainside NJ, US Ginger Xu-qiang Yang - Jersey City NJ, US
Frank Dininno - Barnegat NJ, US Milton L. Hammond - Somerville NJ, US Kevin Dykstra - West Milford NJ, US Seongkon Kim - Holmdel NJ, US Qiang Tan - Westfield NJ, US Katherine Young - Metuchen NJ, US Jeffrey Donald Hermes - Warren NJ, US Helen Chen - Marlboro NJ, US Stephane Raeppel - St. Lazare, CA Michael Mannion - Montreal, CA Frederic Gaudette - Laval, CA Arkadii Vaisburg - Kirkland, CA Jubrail Rahil - Dollard des Ormeaux, CA Nafsika Georgopapadakou - Vaudreuil, CA Nancy Z. Zhou - Kirkland, CA
Assignee:
MethylGene Inc. - Montreal
International Classification:
A61K 31/675 A61K 31/67 A61K 31/665
US Classification:
514 80, 514 89, 514 92, 514 96, 514100
Abstract:
This invention provides novel β-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of β-lactamases and synergize the antibacterial effects of β-lactam antibiotics (e. g. , imipenem and ceftazimdime) against those micro-organisms normally resistant to the β-lactam antibiotics as a result of the presence of the β-lactamases.
Novel Sulfonamidomethylphosphonate Inhibitors Of Beta-Lactamase
Frank Dininno - Barnegat NJ, US Milton L. Hammond - Somerville NJ, US Kevin Dykstra - West Milford NJ, US Seongkon Kim - Holmdel NJ, US Qiang Tan - Westfield NJ, US Katherine Young - Metuchen NJ, US Jeffrey Donald Hermes - Warren NJ, US Stephane Raeppel - St. Lazare, CA Michael Mannion - Montreal, CA Nancy Z. Zhou - Kirkland, CA Frederic Gaudette - Verdun, CA Arkadii Vaisburg - Kirkland, CA Jubrail Rahil - Dollard Des Ormeaux, CA Nafsika Georgopapadakou - Kirkland, CA
This invention provides novel β-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class. The compounds inhibit three classes of β-lactamases and synergize the antibacterial effects of β-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the β-lactam antibiotics as a result of the presence of the β-lactamases.
Pyrrolo [2,3-C] Pyridine Derivatives As P38 Kinease Inhibiting Agents
Soumya P. Sahoo - Old Bridge NJ, US Meng-Hsin Chen - Westfield NJ, US Kevin D. Dykstra - West Milford NJ, US Hiroo Koyama - Hoboken NJ, US Peter T. Meinke - Scotch Plains NJ, US Stephen J. O'keefe - Mountainside NJ, US Ginger Xu-Qiang Yang - Jersey City NJ, US
Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: (A) are inhibitors N of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.
Osamu Okamoto - Ibaraki, JP Yasuhiro Sasaki - Okinawa, JP Hitomi Watanabe - Ibaraki, JP Hideki Jona - Ibaraki, JP Kevin D. Dykstra - West Milford NJ, US
International Classification:
A61K 38/12 C07K 5/00 A61P 3/10
US Classification:
514 69, 530317
Abstract:
The present invention relates to a compound represented by formula (I): wherein Rrepresents a hydrogen atom or the like; Rand Rrepresent a hydrogen atom or the like; Ris a group represented by (II) Rrepresents a phenyl group which may be substituted with a halogen or the like; m is an integer of from 1 to 3; and p is an integer of from 0 to 4; or a pharmaceutically acceptable salt thereof.
Carbapenem Antibacterial Compounds, Compositions Containing Such Compounds And Methods Of Treatment
Frank P. Dininno - Old Bridge NJ Milton L. Hammond - Somerville NJ Kevin D. Dykstra - West Milford NJ
Assignee:
Merck & Co., Inc. - Rahway NJ
International Classification:
C07D47714 C07D51906 A61K 31428 A61P 3104 C07F 718
US Classification:
51421009
Abstract:
The present invention relates to tricyclic carbapenem antibacterial agents in which the carbapenem nucleus is fused to a 6 membered carbocyclic ring. The compound is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula I: ##STR1## Pharmaceutical compositions and methods of use are also included.
Carbapenem Antibacterial Compounds, Compositions Containing Such Compounds And Methods Of Treatment
The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with an iodo-substituted phenyl linked through a CH. sub. 2 --O-- group. The compounds of the invention are represented by formula I: ##STR1## wherein A represent O, S or --CH. sub. 2 -- attached at position 3, 4 or 6; Q is selected from the group consisting of: ##STR2##. alpha. represents O, S or NR. sup. s ;. beta. ,. delta. ,. gamma. ,. mu. and. sigma. represent CR. sup. t, N or N+R. sup. s, provided that no more than one of. beta. ,. delta. ,. gamma. ,. mu. and. sigma. is N+R. sup. s, balanced by L. sup. - or a carboxylate anion. Salts and hydrates thereof are included. The iodo-substituted phenyl ring is further substituted with various substituent groups including at least one cationic group. Pharmaceutical compositions and methods of treatment are also included.
Kevin Dykstra 1995 graduate of Lake Stevens High School in Lake stevens, WA is on Memory Lane. Get caught up with Kevin and other high school alumni from