37 results about "Calcium Channel Inhibition" patented technology

The present invention is directed to drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, wherein each substituent is defined in the specification.The present invention also relates to a pharmaceutical composition containing an effective amount of the compound of formula (I) and a pharmaceutically effective carrier.The present invention further relates to methods of treatment of diseases associated with calcium release-activated calcium channels, diseases associated with IL-2 production, and methods of treatment of allergic, inflammatory or auto-immune diseases.

The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification).The compounds of the formula (I) possess inhibitory activity of N-type calcium channel, so they are useful as drug for prevention and / or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis, epilepsy, asthma and pollakiuria etc. or agent for the treatment of pain.

The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

The present application relates to calcium channel inhibitors containing compounds of formula (I)wherein Ar1, n, R1, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

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).

The present application relates to calcium channel inhibitors containing compounds of formula (I)wherein L1, L2, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

This invention is about a functional after-operation isolation membrane and method for making same. The functional after-operation isolation membrane is composed of the drugs taken by biodegradable isolation membrane host material, and the drugs contain antiphlogiston drugs, fibrin inhibitor drugs, calcium channel inhibitor drugs, anticoagulant drugs and antibiotics drugs or one or several kinds of Chinese patent drugs; while the isolation membrane host material is made of one or several kinds degradation rate differed materials, whose half-decay times are 1 week to 6 months. Alerting membrane materials kinds and charging amount, drugs kinds and charging amount and isolation membrane layers can make multifunctional, degradation rate different and drug-release characteristic different functional after-operation isolation membrane products, so as to adapt to different using demands. Experiments prove that this functional after-operation isolation membrane can effectively accelerate tissue healing after operation, diminish infection and prevent after-operation adhesions.

The present application relates to calcium channel inhibitors containing compounds of formula (I)wherein Ar1, Ar2, L1, L2, n, R1, R4, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

A regime or regimen for loosening / slackening and / or relaxing cutaneous and / or subcutaneous human skin tissue, advantageously for cosmetically / therapeutically treating skin wrinkles and fine lines, comprises administering to a candidate subject in need of such treatment, a thus-effective amount of at least one inhibitor of at least one calcium channel.

The present application relates to calcium channel inhibitors containing compounds of formula (I)wherein Ar1, Ar2, L1, L2, n, R1, R4, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

The invention discloses a biodegradable shape-memory polymer based composite material used for loading drugs, which comprises 100 portions of biodegradable polymer material and 0.01 to 25 portions of drugs, wherein, the drugs refer to one of or a mixture from more than one of antibiotics, hormone, a fibrous protein inhibitor, an anticoagulant, a calcium channel blocker, an antiphlogistic drug or a Chinese patent drug. The material not only has good properties of biodegradable shape-memory polymer material, but also is loaded with effective drug ingredients, thereby being capable of providing the function with controllable time of long-term and effective treatment for patients, quickening the physical rehabilitation of patients, reducing the drug dosage of the patients with oral administration or injection and alleviating pains and inconvenience of the patients.

The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

The present invention relates to a calcium channel inhibitor comprising a compound of formula (I), wherein L1, L2, R1, R2 and R3 are as defined in the specification. The invention also relates to compositions comprising such compounds and methods of using such compounds and compositions to treat diseases and conditions. (I)

The invention discloses a therapeutically active compositions of matter and member species thereof which comprise indazole-containing compounds, said compounds and their therapeutic activity resulting directly from an indazole-for-catechol bioisostere replacement of a catechol-containing compound having the same therapeutic activity, where non-catechol substituents are the same or homologous before and after said replacement, and wherein said compositions of matter comprise a compound of Formula (I<1>) or (I<2>), or a pharmaceutically acceptable salt thereof, wherein in a preferred embodiment R is hydrogen; R is cyclohexyl; and R is ethyl. Ra and Rb are each individually and independently hydrogen or non-catechol substituents of said compounds resulting directly from an indazole-for-catechol bioisotere replacement of said catechol-containing compound having said therapeutic activity, where said non-catechol substituents are the same or homologous before and after said replacement, provided that both of Ra and Rb cannot be hydrogen at the same time. The therapeutic activity involved may comprise cholinesterase inhibitory activity, adrenergic alpha 1-antagonist and beta 1-agonist activity, calcium channel inhibitory activity, antineoplastic activity, and phosphodiesterase type IV inhibitor activity.

The present application relates to: (a) compounds of Formula (I):and salts thereof, wherein Z1, Z2, Z3, Z4, R1, R2, and R3 are as defined in the specification; (b) compositions comprising such compounds and salts; and (c) methods of use of such compounds, salts, and compositions, particularly use as calcium channel inhibitors.

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.

The invention provides a manidipine hydrochloride compound. Manidipine hydrochloride is a lipophilic third generation dihydropyridine calcium channel blocker, and is mainly used for inhibiting calcium influx by inhibiting L type calcium channels on vascular smooth muscle, so as to realize relaxation of vascular smooth muscle and reduce blood pressure.

The invention discloses a hexahydrobenzonaphthyridine-type optically active compound and a pharmaceutical use thereof. The compound is L-(S)-5-amino-4-(2-chlorophenyl)-2,7,7-trimethyl-1,4,6,7,8,9-hexahydrobenzo[b][1,8]naphthyridine-3-ethyl carboxylate with a T1 structure, or a pharmaceutically acceptable salt thereof. The invention also discloses a composition of the optical isomer, and an application thereof. Compared with the dextroisomer compound T2 and the racemic compound T of the compound T1 provided by the invention, the compound T1 shows higher inhibitory activity on acetylcholinesterase and calcium channels, better drug absorption and metabolism properties, and comprehensively high in-vivo efficacy results.

A new analgesic has been developed for T-type calcium channels as therapeutic targets.The present invention provides a T-type calcium channel inhibitor which is a compound represented by formula (1):whereineach of R1 and R2 independently represents —H or —OH;R3 represents —OH;R4 represents —OH or —H;R5 represents a straight or branched alkyl or cycloalkyl-alkyl group having one to ten carbon atoms or a straight or branched alkenyl or cycloalkyl-alkenyl group having two to ten carbon atoms,or a pharmaceutically acceptable salt or solvate thereof.The present invention also provides this T-type calcium channel inhibitor, a medicament containing the T-type calcium channel inhibitor, and a therapeutic or prophylactic agent for a disease having an effective T-type calcium channel inhibitory action.

The present invention provides novel T type calcium channel inhibitors of formula (I), the use thereof in the treatment of a disease or condition in a mammal associated with influx of extracellular calcium via T type calcium channels,whereinR1 is C1-C4 alkyl, hydroxy, or C1-C4 alkoxy;Z is NH, NCH3, O, S, or CH2;Y is NH, O, or CH2 with the proviso that Y and Z are not the same;R2 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy;m and n are independently selected from integers ranging from 1-5 with the proviso that m+n=an integer ranging from 2-9; andR3 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy.

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.

The present application relates to calcium channel inhibitors containing compounds of formula (I)wherein α, R1, R2, R3, and R4 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

Presented herein are compounds that inhibit T-type Ca2+ channel activity in a cell when the cell membrane potential is about -90 mV. Preferred compounds inhibit T-type Ca2+ channel activity with an IC50 of 10 [mu]M or less at a membrane potential of about -90 mV. Preferred compounds show selectivity for inhibiting T-type Ca2+ channel activity at about -90 mV, relative to inhibition of T-type Ca2+ channel activity at about -30 mV to -60 mV, of 10: 1 or less. Also provided are methods for identifying compounds that inhibit T-type Ca2+ channel activity in a cell when the cell membrane potential is about -90 mV, and compounds identified by such methods.