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The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Patent No.:

US 8354536 B1

PDFFull Text
Expired
Date of Patent:
Jan. 15, 2013

Filed:

Jun. 21, 2012

Diazonium-free method to make an indazole intermediate in the synthesis of bicyclic 5-(trifluormethoxy)-1h-3-indazolecarboxylic acid amides

Applicants:

Thomas Cleary, Florence, SC (US);

Yaohui Ji, Shanghai, CN;

Thimma Rawalpally, Florence, SC (US);

Inventors:

Thomas Cleary, Florence, SC (US);

Yaohui Ji, Shanghai, CN;

Thimma Rawalpally, Florence, SC (US);

Assignee:

Hoffman-La Roche Inc., Nutley, NJ (US);

Attorneys:

George W. Johnston

Patricia S. Rocha-Tramaloni

Kimberly J. Prior

Primary Examiner:

Charanjit Aulakh

Int. Cl.
CPC ...
C07D 453/02 (2006.01); C07D 241/38 (2006.01);
U.S. Cl.
CPC ...
Abstract

The present invention provides novel methods for preparing 5-(trifluoromethoxy)-1H-3-indazolecarboxylic acid (3), which is a useful precursor for the preparation of bicyclic-5-trifluoromethoxy-1H-indazole-3-carboxylic acid amides of Formula (1). Compounds of Formula (1) are active as agonists and partial agonists of the nicotinic α-7 receptor and are being studied for their use in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing compound (3) on scale up levels.

Find Patent Forward Citations

Cleary, Thomas. (2013). Diazonium-free method to make an indazole intermediate in the synthesis of bicyclic 5-(trifluormethoxy)-1h-3-indazolecarboxylic acid amides (U.S. Patent No. 8354536). U.S. Patent and Trademark Office. https://idiyas.com/patent/badge/8354536

Data source: USPTO (United States Patent and Trademark Office) public patent records. Weekly synchronization. How IDiyas builds this profile

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