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Biotech / Medical : Neurogen (NRGN) -- Ignore unavailable to you. Want to Upgrade?

To: Jim Oravetz who wrote (318)	10/18/2001 12:56:40 PM
From: Jim Oravetz	Read Replies (1) \| Respond to of 523

This is old news by posted for the record. NEUROGEN neuroinvestment.com From January 2001 overview Perhaps the third time will be the charm for Neurogen and anxiety. Pfizer has taken the third selective GABA-A antagonist developed by Neurogen into Phase II. This will be a 280pt study, and its timeframe for completion will be considerably longer than we had previously estimated. With enrollment likely to take 15 months, and a six week dosing schedule, we doubt that data will come out until quite late in 2002. That data will compare two dose levels of NGD-95-3 to placebo and Xanax in the treatment of Generalized Anxiety Disorder. If successful, a Phase III would then follow. It thus remains two to three years behind Interneuron's pagoclone in the race for a new anxiolytic. The next most advanced program is NGD-97-1, which seeks to upregulate cognition in dementing disorders by serving as an inverse agonist for those GABA-A subtypes whose activation diminishes cognitive clarity and memory functions, as is seen with benzodiazepines. Phase I was successful, Phase II should begin during 1H:01. The insomnia program continues to be at an impasse, with the lead molecule (NGD-96-1) not suitable pharmacokinetically for commercialization. They continue to use it to explore potential adverse effect issues preclinically, but are still looking for a backup molecule with the kind of rapid onset and short half-life which is now de rigeur in insomnia treatment. The most advanced preclinical program is in CRF antagonism, the same area being pursued by Neurocrine Biosciences and others. Neurogen believes that the chemical structure of their compounds differs from that of the group that proved toxic for Neurocrine and Janssen, though we do not know how similar or dissimilar it is to the new NBIX CRF antagonist group. Neurogen is still conducting preclinical toxicology studies while assessing their compound in animal models of depression. Their complement (C5A antagonist) program is also in animal studies. Whereas Alexion's C5A drug is a peptide, Neurogen's is a small molecule, which would give it some manufacturing and delivery advantages. Pfizer ended the collaboration studying neuropeptide Y modulation for obesity, Pfizer choosing to take some compounds in-house for further work. The future of that particular approach seems quite murky at present. Neurogen is continuing early-stage research on their melanin concentrating hormone program for obesity, and the VR-1 antagonist for pain. When CEO Harry Penner announced he would be stepping down, it triggered quite a rally in Neurogen's stock price. Under his stewardship, Neurogen had maintained its reputation for strong science, a close but perhaps overly dependent alliance with Pfizer, and a solid balance sheet, but none of its compounds ever made it past Phase II. It will be interesting to see if the next CEO takes a more independent stance with the programs that remain inhouse.

To: Jim Oravetz who wrote (318)	5/30/2002 12:05:39 PM
From: Jim Oravetz	Read Replies (1) \| Respond to of 523

United States Patent 6,384,224 Greenlee , et al. May 7, 2002 Certain 1-(2-naphthyl) and 1-(2-azanaphthyl)-4-(1-phenylmethyl) piperazines; dopamine receptor subtype specific ligands Abstract Disclosed are compounds of the formula: ##STR1## or pharmaceutically acceptable addition salts thereof, wherein: X, Y and Z are the same or different and represent optionally substituted carbon or nitrogen; R.sub.1 and R.sub.2 independently represent organic or inorganic substituents; R.sub.3 and R.sub.4 are variables independently representing inorganic or organic substituents; A represents C.sub.1 -C.sub.4 alkylene; and R.sub.5, R.sub.6, and R.sub.7 independently represent hydrogen or C.sub.1 -C.sub.6 alkyl, which compounds bind selectively with high affinity to the dopamine D.sub.4 receptor subtype and are therefore of use in treatment of various neuropsychological disorders. Inventors: Greenlee; William (Teaneck, NJ); Gangly; Ashit (U. Montclair, NJ); Wasley; Jan W. F. (Guilford, CT) Assignee: Neurogen Corporation (Branford, CT) Appl. No.: 897352 Filed: July 2, 2001 Current U.S. Class: 544/356; 514/249 Intern'l Class: C07D 403/04 Field of Search: 544/356 ++++++++++++++++++++++++++++++++++++++ United States Patent 6,380,210 DeSimone , et al. April 30, 2002 Heteroaryl fused aminoalkyl-imidazole derivatives: selective modulators of GABAa receptors Abstract Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6, are variables defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness. Inventors: DeSimone; Robert W. (Durham, CT); Hutchison; Alan (Madison, CT); Shaw; Kenneth (Weston, CT); Rosewater; Daniel L. (Golden, CO) Assignee: Neurogen Corporation (Branford, CT) Appl. No.: 540454 Filed: March 31, 2000 +++++++++++++++++++++++++++++++++++++ United States Patent 6,380,209 Cai , et al. April 30, 2002 4-(4-piperidylmethylamino) substituted heteroaryl fused pyridines: GABA brain receptor ligands Abstract Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: R is hydrogen, alkyl, or(un)substituted alkoxy or amino; and W is (un)substituted alkyl, aryl, or heteroaryl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. The compounds of the invention are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness. Inventors: Cai; Guolin (Guilford, CT); Liu; Gang (Agoura, CA) Assignee: Neurogen Corporation (Branford, CT) Appl. No.: 583147 Filed: May 30, 2000