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57 results about "N-type calcium channel" patented technology

N-type calcium channels are voltage gated calcium channels that are distributed throughout the entire body. These channels are high voltage activated channels composed of alpha-1B subunits. The alpha subunit forms the pore through which the calcium enters and helps to determine most of the channel's properties. The alpha subunit is also known as the calcium channel/voltage dependent/N type, alpha 1 subunit (CACNA1B), or calcium voltage-gated channel subunit alpha1 B. The subunit is essential to modulate neurotransmitter release. They also contain associated subunits such as β1, β3, β4, α2δ, and possibly γ. These channels are known for their importance in the nervous system. They play a small role in the migration of immature neurons before the establishment of their mature synapses, and they are critically involved in the release of neurotransmitters, which is also similar to another type of calcium channels, known as P-type calcium channels. N-type calcium channels are targets for the development of drugs to relieve chronic and neuropathic pain. They are also used for the treatment of hypertension, Autism Spectrum Disorder, Osteoarthritis, and other medical diagnoses. Additionally, N-type calcium channels have known functions in the kidney, and heart. There are many known N-type calcium channel blockers that function to inhibit channel activity, although the most notable blockers are ω-Conotoxins. Blockers, like ω-Conotoxins, can interfere with many different biological and therapeutic processes.

Combination Therapy for Relief of Pain

The present invention relates to analgesic compositions comprising a non-peptidyl N-type calcium channel blocker, and at least one other analgesic compound, and to methods of using N-type calcium channel blockers in combination with at least one other pain-relieving compound that alleviates pain through a mechanism other than N-type calcium channel blockage, or with a non-pharmacological therapeutic protocol.
Owner:ZALICUS PHARMA LTD (CA)

Amino acid derivatives

A compound of the formula (I): [wherein R1 is (substituted) alkyl, alkoxy, phenyl, hetero ring etc.; A is bond, CO, SO2; R2 is H, (substituted) alkyl etc.; D is alkylene etc.; E is COO, OCO, O, S, SO, SO2 etc.; R3 is (substituted) alkyl, carbocyclic ring, hetero ring; J is O, NR16 (R16 is H, substituted alkyl); R4 is (substituted) alkyl, carbocyclic ring, hetero ring.] or non-toxic salt thereof, and an N-type calcium channel blocker comprising it as an active ingredient.The compounds of the formula (I) possess an inhibitory action on N-type calcium channel, so they are useful as agent for the prevention and / or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis or epilepsy etc. or agent for the treatment of pain.
Owner:ONO PHARMA CO LTD

Treating stroke and other diseases without inhibiting N-type calcium channels

The invention provides methods for treating stroke and compositions for use in the same. The methods employ a chimeric peptide of an active peptide and an internalization peptide. The internalization peptide is a tat variant that promotes uptake of itself and a linked active peptide into a cell without substantial binding to N-type calcium channels. Use of the tat variant allows treating of stroke free of certain side effects associated with binding to N-type calcium channels. Tat variant peptides can also be linked to other active agent for use in treating other diseases.
Owner:NONO INC

Pharmaceutical composition containing gabapentin or pregabalin and N-type calcium channel antagonist

The present invention relates to a pharmaceutical composition useful for preventing / treating pain, which comprises combination of gabapentin or pregabalin, or pharmaceutically acceptable salts thereof and N-type calcium channel antagonists or pharmaceutically acceptable salts thereof such as a compound having the following structure.
Owner:AJINOMOTO CO INC

N-type calcium channel blockers

InactiveUS20050165065A1BiocideNervous disorderCalcium channel activityIon channel
The invention relates to novel 3-amino pyrrolidine derivatives, as well as methods for modulating calcium channel activity and for treating conditions associated with calcium channel function. In particular, the compounds generally contain at least one benzhydril moiety, and are useful in treating conditions which benefit from blocking calcium ion channels.
Owner:ZALICUS PHARMA LTD (CA)

Dihydropyrimidine compounds and compositions containing the same

Dihydropyrimidine derivatives of the following formula or analogs thereof have selective N-type calcium channel antagonistic activity, and they are used as therapeutic agents for various diseases participating in the N-type calcium channels.
Owner:AJINOMOTO CO INC

Amorphous Composition

To provide an amorphous composition for nasal administration or for administration by adhering to oral mucosa in which absorption property and chemical and physical stabilities of (2R)—N-(1-benzylpiperidin-4-yl)-3-cyclohexylmethylthio-2-[(4R)-3-tert-butoxycarbonylthiazolidin-4-ylcarbonylamino]propanamide which is useful as an N type calcium channel inhibitor are improved. A preparation comprising the amorphous composition of the present invention has been found to be excellent in physical stability and chemical stability and to be useful as a nasal preparation or a preparation for adhering to the oral mucosa. As a result, the resulting preparation has a high BA value and is useful for prevention and / or the treatment of a disease mediated by the N type calcium channel including pain (such as neuropathic pain, cancerous pain, intractable pain, postoperative pain, acute pain, chronic pain, neuralgia and infectious pain).
Owner:ONO PHARMA CO LTD

Cyclopropyl-piperazine compounds as calcium channel blockers

InactiveUS20100105682A1Extended half-lifeAltered pharmacokineticsOrganic active ingredientsNervous disorderCalcium channel activityCalcium channel blocker
Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type calcium channel activity are disclosed. Specifically, a series of compounds containing both a piperazine ring and a cyclopropyl ring are disclosed of the general formula (I) where X1 and X2 are linkers.
Owner:ZALICUS PHARMA LTD (CA)

Method of modulating activity of calcium channels in cardiac cells and reagents therefor

The present invention relates generally to novel peptides that are capable of modulating the activity of calcium channels in cardiac cells. More specifically, the present invention provides a method of modulating the activity of a cardiac calcium channel comprising contacting a cardiac ryanodine receptor (RyR2) with an amount of a fragment of a dihydropyridine receptor (DHPR) polypeptide sufficient to modulate the activity of said RyR2, and determining the activity of said calcium channel. The inventive method is useful for the treatment of a range of disorders and diseases associated with cardiac dysfunction, particularly those diseases and disorders involving reduced cardiac output and / or aberrant excitation-contraction coupling, calcium overload, or calcium leakage, in cardiac cells.
Owner:AUSTRALIEN NAT UNIV

Diaryl piperidine compounds as calcium channel blockers

InactiveUS20100168103A1Enhance calcium channel blocking activityExtended half-lifeBiocideNervous disorderCalcium channel activityCalcium channel blocker
Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type calcium channel activity are disclosed. Specifically, a series of diaryl piperidine compounds are disclosed of the general formula (I) where X is a linker and Y may be C, O, S or N.
Owner:ZALICUS PHARMA LTD (CA)

Heterocyclic compounds as calcium channel blockers

Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type calcium channel activity are disclosed. Specifically, a series of heterocyclic compounds are disclosed of the general formula (1) where X1 and X2 are linkers and W is an optionally substituted imidazolyl, oxazolyl, thiazolyl, benzimidazolyl, benzoxazolyl, or benzothiazolyl.
Owner:ZALICUS PHARMA LTD (CA)

Ion Channel Inhibitory Compounds, Pharmaceutical Formulations, and Uses

The present invention is directed towards new chemical entities which primarily inhibit the human T-type calcium channels and differentially modulate other key ion channels to control cell excitability, and abnormal neuronal activity particularly involved in the development and maintenance of persistent or chronic pain, and / or neurological disorders. These novel compounds are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which these ion channels are involved. The invention is also directed towards pharmaceutical formulations comprising these compounds and the uses of these compounds.
Owner:AFASCI

Omega Conotoxins

The present invention relates to a method for increasing the binding reversibility of a ω-conotoxin to a N-type calcium channel, which comprises preparing a ω-conotoxin having a Ile and / or Ala residue at a position of amino acid (11 and / or 12), respectively in the second loop between cysteine residues (2 and 3) of the ω-conotoxin represented by the formula I, such that the prepared ω-conotoxin has the increased binding reversibility to N-type calcium channel. In addition, the present invention relates to a novel ω-conotoxin and a pharmaceutical composition having plausible properties in view of blocking activity to and specificity to N-type calcium channel, and dramatically improved binding reversibility to N-type calcium channel.
Owner:ANYGEN

Pyrimidine compounds useful as N-type calcium channel antagonists

Achiral pyrimidine derivatives and pyridine derivatives of the following formulae or analogs thereof have selective N-type calcium channel antagonistic activity and showed analgesic action when they were taken orally. They are useful as therapeutic agents for pains and various diseases associated with the N-type calcium channels
Owner:AJINOMOTO CO INC

Application of valeriana jatamansi Jones part in preparation of N-type calcium channel inhibitor

The invention discloses an application of a valeriana jatamansi Jones part in preparation of an N-type calcium channel inhibitor and belongs to the field of medicine. The effect of the valeriana jatamansi Jones part in the N-type calcium channel inhibition is provided and two iridoid components of the valeriana jatamansi Jones part for playing a role in the N-type calcium channel inhibition are verified. The inhibition effect of the acidic hydrolysis product of the iridoid in the N-type calcium channel is firstly found. The valeriana jatamansi Jones part provided by the invention taken as a novel N-type calcium channel inhibitor has a wide application prospect and can be applied to the healthcare and treatment of the related diseases such as pain.
Owner:KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +1

Reduced dipeptide analogues as calcium channel antagonists

The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma. The novel compounds provided by this invention have Formula (1), wherein R1 is H or methyl; R2 is H, azepanylcarbonyl, C1-C7 alkyl, -(CH2)n-phenyl, wherein the phenyl is unsubstituted or substituted with C1-C4 alkyl, C1-C4 alkoxy, or halo; R3 is C1-C5 alkyl; X is -NR4R5 or -OR7; R4 and R5 are independently H, C1-C5 alkyl; or R4 and R5 together with the nitrogen to which they are both bound form formulae (a); (b); (c); (d) or (e); R6 is -(CH2)n-phenyl, wherein the phenyl is unsubstituted or substituted with C1-C4 alkyl, C1-C4 alkoxy, or halo; A and B are independently -CO- or -CH2-, provided that A and B are not both -CO-; R7 is C1-C5 alkyl; Z is -CH2-, -O-, -S-, or -N(R8)-; R8 is H or C1-C6 alkyl; and n is 1 or 2.
Owner:WARNER-LAMBERT CO

Dihydropyridine derivative

Dihydropyridine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an activity of selectively inhibiting the action of N-type calcium channel. They are used as remedies for various diseases relating to the N-type calcium channel such as encephalopathies caused by the ischemia in the acute phase after the onset of cerebral infarction, cerebral hemorrhage or the like, Alzheimer's disease, etc.
Owner:AJINOMOTO CO INC

Dihydropyridine derivatives

Compounds having a selective N-type calcium channel antagonistic activity are provided. Dihydropyridine derivatives represented by the following formula:analogs thereof and pharmaceutically acceptable salts thereof have an activity of selectively inhibiting the action of N-type calcium channel, and they are used as therapeutic agents for various diseases relating to N-type calcium channel.
Owner:AJINOMOTO CO INC
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