Merck Sharp + Dohme Corp.

The Scripps Research Institute

Other

Adrian Leonard Smith

Janusz Jozef Kulagowski

Raymond Baker

Paul D Leeson

Kyriacos Costa Nicolaou

Neil Roy Curtis

Mark Peter Ridgill

Peter Emmanuel Maligres

Wilhelm Stahl

Chan-Kou Hwang

Erwin Paul Schreiner

Wei-Min Dai

Toshio Suzuki

Sebastian V Wendeborn

Sebastian V Wenderborn

Colin John Kellett

Coaxial cable transition arrangement

The present invention relates to a traceless solid phase process for the preparation of an indole derivative, which comprises the following steps: (1) reaction of an optionally substituted 2-iodoaniline derivative via the nitrogen atom of the NH.sub.2 moiety thereof with a dihydropyran-functionalized polymeric resin under conditions effective to form an aminal linkage; (2) reaction of the tetrahydropyran aminal derivative thereby obtained with an acetylene derivative in the presence of a transition metal catalyst under conditions effective to promote indole formation; (3) treatment of the product thereby obtained with acid, whereby the aminal linkage is cleaved and the desired indole derivative is liberated from the resin; and (4) isolation of the desired indole derivative thereby obtained.

Traceless solid phase synthesis of indole derivatives

The present invention relates to a method for the synthesis of 1,3-disubstituted quinazolinedione derivatives which comprises:

Chemical synthesis of 1,3-disubstituted quinazolinediones

Antipsychotic indazole derivatives

Pyrrolo-pyridine derivatives

Indazole derivatives

A class of pyrrolo[2,3-b]pyridine derivatives, substituted at the 3-position by a substituted piperazinylmethyl moiety, are antagonists of dopamine receptor subtypes within the brain, having a selective affinity for the dopamine D.sub.4 receptor subtype over other dopamine receptor subtypes, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders such as schizophrenia whilst manifesting fewer side-effects than those associated with classical neuroleptic drugs.

A fused ring system compound is disclosed that contains an epoxide group on one side of the fused rings and an enediyne macrocyclic ring on the other side of the fused rings. The compounds have DNA-cleaving, antimicrobial and tumor growth-inhibiting properties. Chimeric compounds having the fused ring system compound as an aglycone bonded to (i) a sugar moiety as the oligosaccharide portion or (ii) a monoclonal antibody or antibody combining site portion thereof that immunoreacts with target tumor cells are also disclosed. Compositions containing a compound or a chimer are disclosed, as are methods of preparing a compound.

Dynemicin analogs: syntheses, methods of preparation and use

Dynemicin analogs: synthesis, methods of preparation and use

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Bishops Stortford, United Kingdom

Adrian Leonard Smith