92 results about "Sigma receptor" patented technology

Novel compounds represented by the following formula (I) that act as a ligand to sigma receptor/binding cite and a medicament comprising the same as an active ingredient:

wherein X represents an alkyl group, an aryl group, a heterocyclic group or the like; Q represents a group represented by —CH₂—, —CO—, —O—, —CH(OR₇)— or the like wherein R₇ represents a hydrogen atom, an alkyl group or the like; n represents an integer of from 0 to 5; R₁ and R₂ each represent a hydrogen atom, an alkyl group or the like; B represents either of the following groups:

wherein R₃, R₄, R₅, and R₆ each represent a hydrogen atom, a halogen atom, an alkoxyl group or the like; m represents 1 or 2; and the ring of:

represents an aromatic heterocyclic ring.

The present invention refers to the use of compounds active on the sigma receptor for the production of a medicament for the treatment of diabetes-associated pain.

The present invention provides an indanone derivative and an excellent sigma receptor binding agent comprising an indanone derivative. More specifically, it provides a sigma receptor binding agent comprising an indanone derivative represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate of them.

In the formula (I), R¹, R², R³ and R⁴ are the same as or different from each other and each represents hydrogen atom, a halogen atom, hydroxyl group, nitrile group, a C_1-6 alkyl group which may be substituted, a cycloalkyl group having three to eight carbon atoms which may be substituted, a C_1-6 alkoxy group which may be substituted, a cycloalkoxy group having three to eight carbon atoms which may be substituted, an acyl group having one to six carbon atoms which may be substituted, a C_1-6 alkoxycarbonyl group which may be substituted, a C_1-6 alkylaminocarbonyloxy group which may be substituted, a di(C_1-6 alkyl)aminocarbonyloxy group which may be substituted, nitro group, an amino group which may be substituted, an amido group which may be substituted, mercapto group or a thio-C_1-6 alkoxy group which may be substituted, and further R¹ with R², R² with R³, or R³ with R⁴ may together form an aliphatic ring, an aromatic ring, a heterocyclic ring or an alkylenedioxy ring; the partial structure:

represents a group represented by >CH—CH₂—, >C═CH— or >C(—R⁷)—CH₂—; m represents an integer of 0 or 1 to 5; and R⁵ represents hydrogen atom, a C_1-6 alkyl group which may be substituted, a C_2-6 alkenyl group which may be substituted, a C_2-6 alkynyl group which may be substituted, a cycloalkyl group having three to eight carbon atoms which may be substituted, a 2,2-(alkylenedioxy)ethyl group or a group represented by the formula:

(wherein the ring C represents benzene ring, an aliphatic ring or a heterocyclic ring; R⁶s are the same as or different from each other and each represents hydrogen atom, a halogen atom, hydroxyl group, nitrile group, a C_1-6 alkyl group which may be substituted, a C_2-6 alkenyl group which may be substituted, a C_2-6 alkynyl group which may be substituted, a cycloalkyl group having three to eight carbon atoms which may be substituted, a C_1-6 alkoxy group which may be substituted, a C_1-6 alkoxyalkoxy group which may be substituted, an aryloxy group which may be substituted or an aralkyloxy group which may be substituted, and further two of R⁶s may together form an aliphatic ring, an aromatic ring, a heterocyclic ring or an alkylenedioxy ring; R⁷ represents a halogen atom, hydroxyl group, a C_1-6 alkyl group which may be substituted, a C_1-6 alkoxy group, nitrile group, a halogeno-C_1-6 alkyl group, a hydroxyl-C_1-6 alkyl group, a cyano-C_1-6 alkyl group, an amino-C_1-6 alkyl group, nitro group, azide group, an amino group which may be substituted, a carbamoyl group which may be substituted, a carboxyl group which may be substituted, mercapto group or a thio-C_1-6 alkoxy group; and n represents an integer of 1 to 5), provided that 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine, a pharmacologically acceptable salt thereof or a hydrate of them are excluded.

The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.

The present invention refers to the use of compounds binding to the sigma receptor for the treatment of metabolic syndrome.

The present invention provides an excellent sigma receptor binding agent and/or acetylcholinesterase inhibitor containing an (1-indanone)-(1,2,3,6-tetrahydropyridine) compound. More specifically, it provides an (1-indanone)-(1,2,3,6-tetrahydropyridine) compound represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate thereof:

In the formula (I), R¹, R², R³ and R⁴ are the same as or different from each other.

The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.

The present invention refers to the use of compounds binding to the sigma receptor for the treatment or prevention of neuropathic pain resulting from chemotherapy.

A method of post-stroke treatment at delayed timepoints with sigma receptor agonists. Sigma receptors are promising targets for neuroprotection following ischemia. One of the key components in the demise of neurons following ischemic injury is the disruption of intracellular calcium homeostasis. The sigma receptor agonist, DTG, was shown to depress [Ca²⁺]_i elevations observed in response to ischemia induced by sodium azide and glucose deprivation. Two sigma receptor antagonists, metaphit and BD-1047, were shown to blunt the ability of DTG to inhibit ischemia-evoked increases in [Ca²⁺]_i. DTG inhibition of ischemia-induced increases in [Ca²⁺]_i was mimicked by the sigma-1 receptor-selective agonists, carbetapentane, (+)-pentazocine and PRE-084, but not by the sigma-2 selective agonist, ibogaine, showing that activation of sigma-1 receptors is responsible for the effects. Activation of sigma receptors can ameliorate [Ca²⁺]_i dysregulation associated with ischemia in cortical neurons, providing neuroprotective properties. The effects of 1,3-di-o-tolyguanidine (DTG), a high affinity sigma receptor agonist, as a potential treatment for decreasing infarct area at delayed time points was further examined in rats. DTG treatment significantly reduced infarct area in both cortical/striatal and cortical/hippocampal regions by >80%, relative to control rats. These findings were confirmed by immunohistochemical experiments using the neuronal marker, mouse anti-neuronal nuclei monoclonal antibody (NeuN), which showed that application of DTG significantly increased the number of viable neurons in these regions. Furthermore, DTG blocked the inflammatory response evoked by MCAO, as indicated by decreases in the number of reactive astrocytes and activated microglia/macrophages detected by immunostaining for glial fibrillary acidic protein (GFAP) and binding of isolectin IB4, respectively. Thus, the sigma receptor-selective agonist, DTG, can enhance neuronal survival when administered 24 hr after an ischemic stroke. In addition, the efficacy of sigma receptors for stroke treatment at delayed time points is likely the result of combined neuroprotective and anti-inflammatory properties of these receptors.

The genome of the non-human mutant mammal, deficient in an endogenous Sigma receptor, contains a mutation that comprises a disruption in an endogenous Sigma rteceptor gene, wherein said gene disruption gives rise to a mutant lacking detectable levels of endogenous Sigma receptor. The mutant may be used as a control animal for in vivo tests, as well as a source of cells that can be used in in vitro tests, Mutants deficient in the Sigma-1 receptor can be used as models for in vivo study of disorders of the central nervous system, memory alterations, stress conditions and drug addictions, analgesia processes and neuroprotection. Mutants deficient in the Sigma-2 receptor can be used to study diagnostic or therapeutic tools to fight cance and/or degenerative processes and/or to design compounds capable of preventing, reducing or alleviating the secondary pathology associated with administration of neuroleptic agents.

The present invention relates to a pharmaceutical composition that comprises a compound of formula (I) as active pharmaceutical ingredient:

The invention relates to compounds of formula I

The present invention refers to the use of compounds active on the sigma receptor for the treatment of allodynia.

A method for localizing and quantifying S1R role in nociceptive processing; for providing a guide to providing an analgesic therapy; of using an S1R selective ligand as a biomarker for pathphysiological study of memory deficits and cognitive disorders; or of detecting increased S1R density at the site of nerve injury arising from neuropathic pain comprising using as a probe at least one SR1 selective compound or radioligand of the general formula III′, or IV′:

The invention relates to compounds of formula (I) or formula (II)

having pharmacological activity towards the sigma receptor, for use in the treatment or prevention of osteoarthritis and pain due to osteoarthritis.