Zeneca Limited

Imperial Chemical Industries Limited

Robert T Jacobs

Ashokkumar Bhikkappa Shenvi

Cyrus J Ohnmacht

Scott Carson Miller

Diane A Trainor

Michael Thaddeus Klimas

Marc Ornal Terpko

Andrew G Brewster

Chris Allan Veale

George Joseph Sependa

Stephen A Brook

Gerard F Costello

Peter J Harrison

Substituted heterocycles

Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4 and Q.sup.5 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists NKA, useful for the treatment of asthma etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4 and Q.sup.5 have any of the meanings given in the specification, their N-oxides, and their pharmacuetically acceptable salts are nonpeptide antagonists NKA, useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Compounds of formula I, and pharmaceutically acceptable salts thereof, useful in the treatment of neuropsychiatric disorders such as psychoses; pharmaceutical compositions comprising a compound of formula I and a pharmaceutically acceptable diluent or carrier; and methods of treating neuropsychiatric disorders comprising administering to a mammal (including man) in need of such treatment an effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof.

Therapeutic agents

Compounds of formula I or I', ##STR1## wherein X and Y are independently selected from hydrogen, halo, and (1-6C)alkoxy;

Tricyclic antipsychotic compounds

The present invention concerns the novel use of aryl substituted heterocycles of formula I, set out below, which antagonize the pharmacological actions of one of ent endogenous neuropeptide tachykinins an the neurokinin 2 (NK2) receptor making them useful whenever such antagonism is desired, such as in the treatment of asthma and related conditions. The invention also provides pharmaceutical compositions containing the aryl substituted heterocycles for use in such treatment. Certain novel aryl substituted heterocycles of formula I and novel intermediates for their manufacture are also provided. ##STR1##

Aryl substituted heterocycles

Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Piperidine derivatives useful as neurokinin antagonists

Compounds of formula I ##STR1## wherein X and Y are H or halo; R.sup.2 is: [structures Ia, Ib or Ic;] ##STR2## R.sup.3 is selected from unsubstituted or substituted alkyl, aryl or heteroaryl groups;

Methanoanthrancenyl piperidyl antipsychotics

Methanoanthraceneyl methyl piperidinyl compounds

The present invention concerns novel carbamoyl derivatives of formula I, set out herein, which antagonize the pharmacological actions of one or more of the arachidonic acid metabolites known as leukotrienes, making them useful whenever such antagonism is desired, such as in the treatment of those diseases in which leukotrienes are implicated, for example, in the treatment of allergic or inflammatory diseases, or of endotoxic or traumatic shock conditions. The invention also provides pharmaceutical compositions containing the novel derivatives for use in such treatments, methods for their use and processes and intermediates for the manufacture of the novel derivatives.

Carbamoyl derivatives

A process for the preparation of a 3-alkylated indole, which comprises:

Chemical process for the preparation of 3-alkylated indole

A process for the preparation of (2R)-methyl-4,4,4-trifluorobutylamine, or an acid addition salt thereof which comprises

Growing community of inventors

Wilmington, DE, United States of America

Robert T Jacobs