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Nektar Therapeutics : Patent Issued for N-Optionally Substituted Aryl-2-Oligomer-3-Alkoxypropionamides (USPTO 9616136)

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04/20/2017 | 08:17pm CEST

By a News Reporter-Staff News Editor at Pharma Business Week -- From Alexandria, Virginia, NewsRx journalists report that a patent by the inventors Riggs-Sauthier, Jennifer (San Francisco, CA); Zhang, Wen (San Ramon, CA), filed on November 24, 2015, was published online on April 11, 2017 (see also Biotechnology Companies).

The patent's assignee for patent number 9616136 is Nektar Therapeutics (San Francisco, CA).

News editors obtained the following quote from the background information supplied by the inventors: "Epilepsy is a common chronic neurological disorder characterized by recurrent unprovoked seizures. These seizures are transient signs and/or symptoms of abnormal, excessive or synchronous neuronal activity in the brain. About 50 million people worldwide have epilepsy, with almost 90% of these people residing in developing countries. Epilepsy is more likely to occur in young children or people over the age of 65 years; however, it can occur at any age. Epilepsy is usually controlled, but not cured, with pharmacotherapy, although surgery may be indicated in exceptional cases. Despite the reliance on pharmacotherapy as the primary approach in controlling the disease, over 30% of people with epilepsy do not have seizure control even with the best available medications. Not all epilepsy syndromes are life-long; some forms are confined to particular stages of childhood. Epilepsy should not be understood as a single disorder, but rather as a group of syndromes with vastly divergent symptoms, but all involving episodic abnormal electrical activity in the brain.

"Seizure types are organized firstly according to whether the source of the seizure within the brain is localized (partial or focal onset seizures) or distributed (generalized seizures). Partial seizures are further divided on the extent to which consciousness is affected. If it is unaffected, then it is a simple partial seizure; otherwise it is a complex partial (psychomotor) seizure. A partial seizure may spread within the brain--a process known as secondary generalization. Generalized seizures are divided according to the effect on the body, but all involve loss of consciousness. These include absence (petit mal), myoclonic, clonic, tonic, tonic-clonic (grand mal) and atonic seizures.

"There are over 40 different types of epileptic conditions, including: absence seizures, atonic seizures, benign Rolandic epilepsy, childhood absence, clonic seizures, complex partial seizures, frontal lobe epilepsy, febrile seizures, infantile spasms, juvenile myoclonic epilepsy, juvenile absence epilepsy, Lennox-Gastaut syndrome, Landau-Klefier syndrome, myoclonic seizures, mitochondrial disorders, progressive myoclonic epilepsies, psychogenic seizures, reflex epilepsy, Rasmussen's syndrome, simple partial seizures, secondarily generalized seizures, temporal lobe epilepsy, toni-clonic seizures, tonic seizures, psychomotor seizures, limbic epilepsy, partial-onset seizures, generalized-onset seizures, status epilepticus, abdominal epilepsy, akinetic seizures, auto-nomic seizures, massive bilateral myoclonus, catamenial epilepsy, drop seizures, emotional seizures, focal seizures, gelastic seizures, Jacksonian march, Lafora disease, motor seizures, multifocal seizures, neonatal seizures, nocturnal seizures, photosensitive seizure, pseudo seizures, sensory seizures, subtle seizures, Sylvan seizures, withdrawal seizures, and visual reflex seizures, among others.

"Anticonvulsants are generally prescribed for the treatment of individuals suffering from or prone to epilepsy. The 3-alkoxypropionamides represent one such class of compounds. The 3-alkoxypropionamides are also used in the treatment of individuals suffering from or prone to neuropathic pain. Treatment of individuals with these compounds, however, is associated with many side effects, including: vertigo; diplopia; blurred vision; nausea; vomiting; dizziness; ataxia; and tremor.

"Therefore, pharmacotherapy with such therapeutic 3-alkoxypropionamides would be improved if these and/or other adverse or side effects associated with their use could be decreased or if their pharmacology could otherwise be improved for this and/or for other indications. Thus, there is a large unmet need for developing novel 3-alkoxypropionamides.

"The present invention seeks to address these and other needs in the art."

As a supplement to the background information on this patent, NewsRx correspondents also obtained the inventors' summary information for this patent: "In one or more embodiments of the invention, N-optionally substituted aryl-2-oligomer-3-alkoxypropionamides are provided.

"In one or more embodiments of the invention a compound is provided, the compound comprising a 3-alkoxypropionamide residue covalently attached via a stable or degradable linkage to a water-soluble, non-peptidic oligomer.

"The '3-alkoxypropionamide residue' is a compound having a structure of a therapeutically active 3-alkoxypropionamide that is altered by the presence of one or more bonds, which bonds serve to attach (either directly or indirectly) one or more water-soluble, non-peptidic oligomers.

"Exemplary compounds of the invention include those having the following structure:

"##STR00001## wherein:

"Ar is aryl, optionally substituted (e.g., optionally substituted with halo);

"R.sup.1 is lower alkyl;

"the dotted line ('---') represents a covalent bond, optionally oriented to provide the R enantiomer,

"X.sup.1 is a spacer moiety;

"POLY.sup.1 is a water-soluble, non-peptidic oligomer.

"In this regard, any 3-alkoxypropionamide having anti-epileptic and/or analgesic activity can be used as the 3-alkoxypropionamide from which the 3-alkoxypropionamide residue is obtained. Exemplary 3-alkoxypropionamides have a structure encompassed by Formula I:

"##STR00002## wherein:

"Ar is aryl, optionally substituted with halo; and

"R.sup.1 is lower alkyl.

"An exemplary 3-alkoxypropionamide for use in the current invention is lacosamide.

"In one or more embodiments of the invention, N-optionally substituted aryl-2-oligomer-3-alkoxypropionamides are provided.

"In one or more embodiments of the invention, a composition is provided, the composition comprising an N-optionally substituted aryl-2-oligomer-3-alkoxypropionamide, and optionally, a pharmaceutically acceptable excipient.

"In one or more embodiments of the invention, a compound is provided, the compound comprising a 3-alkoxypropionamide residue covalently attached via a stable or degradable linkage to a water-soluble, non-peptidic oligomer.

"In one or more embodiments of the invention, a composition is provided, the composition comprising a compound comprising a 3-alkoxypropionamide residue covalently attached via a stable or degradable linkage to a water-soluble, non-peptidic oligomer, and optionally, a pharmaceutically acceptable excipient.

"In one or more embodiments of the invention, a dosage form is provided, the dosage form comprising a compound as described herein, wherein the compound is present in a dosage form.

"In one or more embodiments of the invention, a method is provided, the method comprising covalently attaching a water-soluble, non-peptidic oligomer to a 3-alkoxypropionamide.

"In one or more embodiments of the invention, a method is provided, the method comprising administering a compound as described herein to a mammal in need thereof.

"Additional embodiments of the present conjugates, compositions, methods, and the like will be apparent from the following description, examples, and claims. As can be appreciated from the foregoing and following description, each and every feature described herein, and each and every combination of two or more of such features, is included within the scope of the present disclosure provided that the features included in such a combination are not mutually inconsistent. In addition, any feature or combination of features may be specifically excluded from any embodiment of the present invention. Additional aspects and advantages of the present invention are set forth in the following description and claims."

For additional information on this patent, see: Riggs-Sauthier, Jennifer; Zhang, Wen. N-Optionally Substituted Aryl-2-Oligomer-3-Alkoxypropionamides. U.S. Patent Number 9616136, filed November 24, 2015, and published online on April 11, 2017. Patent URL: http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&r=1&f=G&l=50&s1=9616136.PN.&OS=PN/9616136RS=PN/9616136

Keywords for this news article include: Pharmaceutical Companies, Epilepsy, Seizures, Pediatrics, Dosage Forms, Pharmacotherapy, Nektar Therapeutics, Biotechnology Companies, Neurologic Manifestations, Brain Diseases and Conditions, Central Nervous System Diseases and Conditions.

Our reports deliver fact-based news of research and discoveries from around the world. Copyright 2017, NewsRx LLC

(c) 2017 NewsRx LLC, source Health Newsletters

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