Sulfamate derivative compounds, processes for preparing them and their uses
Inventors
Assignees
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Publication Number
US-10351519-B2
Publication Date
2019-07-16
Expiration Date
Abstract
The present invention relates to a pharmaceutical composition for treating or preventing CNS disorders containing a sulfamate derivative compound and/or pharmaceutically acceptable salt thereof as an active ingredient. Furthermore, the present invention relates to a method for treatment or prevention CNS disorders comprising administering a sulfamate derivative compound in a pharmaceutically effective amount to a subject in need of treatment or prevention of CNS disorders.
Core Innovation
The invention relates to compounds having formula 1 or formula I and pharmaceutically acceptable salts thereof. The compounds are defined by a multi-parameter substituent scaffold in which Z and X are selected from specified groups, and indices n, m, p, and q define ranges of substitution patterns. The scaffold further includes R1, A, and B substituents, where at least one of A and B satisfies an additional structural condition, and R2 and R3 are each selected from defined groups.
The disclosure includes stereochemically defined sulfamate derivatives, carbamate and protected alcohol intermediates, and substituted aromatic or heteroaromatic moieties. Reported examples include 2-chloro-, 2-iodo-, and 2,6-dichloro-phenyl groups, pyridinyl and thiazolyl motifs, thiophene and vinyl-thiazole analogs, and stereochemical forms such as (1S,2S), (1R,2R), (1S,2R), and (1R,2S). The examples also include methoxymethoxy (MOM) and tert-butyldimethylsilyl (TBDMS) protected intermediates, with 1H NMR characterization data reported.
The compounds are provided for preventing or treating pain and/or treating CNS disorders. The disclosed pain indications include nociceptive, psychogenic, inflammatory, pathological, neuropathic, cancer, postoperative, trigeminal neuralgia, idiopathic, diabetic neuropathic, and migraine pain, and the CNS disorders include epilepsy, memory-loss-related disease, neurodegenerative disease, and Autism spectrum disease.
Claims Coverage
The claim coverage centers on the broad formula 1 or formula I compound scaffold and pharmaceutically acceptable salts, defined by variable substituents Z, X, R1, A, B, R2, and R3 together with integer indices n, m, p, and q. The coverage also includes pharmaceutical composition and method claims for pain and selected CNS disorders, giving three inventive feature groupings overall.
Formula 1 compound scaffold with variable substituents
A compound having formula 1 or formula I, or a pharmaceutically acceptable salt thereof, defined by selections for Z, X, R1, A, B, R2, and R3 and by integer ranges n, m, p, and q, with at least one of A and B meeting the stated structural requirement.
Pharmaceutical composition for pain and CNS disorders
A pharmaceutical composition for preventing or treating pain and/or treating a selected CNS disorder, where the CNS disorder is epilepsy, a memory-loss-related disease, a neurodegenerative disease, or Autism spectrum disease.
Method of preventing or treating pain and/or CNS disorder by administering formula 1 compound
A method for preventing or treating pain and/or for treating a CNS disorder by administering a therapeutically effective amount of a formula 1 compound or a pharmaceutically acceptable salt to a subject in need, with pain types and CNS disorders as stated in the claims.
Overall, the claim coverage focuses on the broad formula 1 or formula I scaffold defined by multi-variable substituent selection rules, together with independent coverage for pharmaceutical compositions and administration-based methods directed to pain and selected CNS disorders.
Stated Advantages
Provides compounds for preventing or treating pain and/or treating a CNS disorder.
Provides pharmaceutical compositions for preventing or treating pain and/or treating a CNS disorder.
Reports analgesic, antiallodynic, and anti-epilepsy activity in preclinical models.
Documented Applications
Pharmaceutical composition for preventing or treating pain and/or treating a selected CNS disorder, where the CNS disorder is epilepsy, a memory-loss-related disease, a neurodegenerative disease, or Autism spectrum disease.
Method of preventing or treating pain and/or treating a CNS disorder by administering a therapeutically effective amount of a formula 1 compound or a pharmaceutically acceptable salt to a subject in need.
Analgesic and antiallodynic evaluation in preclinical neuropathic pain and related models, including writhing test results and effectiveness metrics for neuropathic pain and inflammatory pain models.
Anti-epilepsy evaluation in preclinical seizure models, including MES, scPTZ, lithium-pilocarpine, PIC picrotoxin, strychnine, BIC, and infantile spasms models.
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