69 results about "Dopamine receptor" patented technology

The present invention relates to a new use for compounds that inhibit phosphodiesterase 1 (PDE1), e.g., that inhibit PDE1-mediated suppression of the dopamine D1 receptor and / or progesterone signaling pathways, including, e.g., methods of treatment or prophylaxis for conditions which may be ameliorated by enhancing the progesterone signaling response, particularly female sexual dysfunction.

Opioid receptors form functional heterodimers with each other and with other G-protein coupled receptors, such as dopamine receptors, adrenergic receptors, or chemokine receptors. These receptors can be exploited for high throughput screening of compounds to identify heterodimer opioid receptor modulators (agonists and antagonists). The invention also relates to identification of novel heterodimer receptor ligands and synergistic compositions, which can provide strategies for analgesia, narcotic addiction, hypertension, HIV infection, and immune system function.

The invention provides a selective Sigma 1 or Dopamine D3 receptor agonist or a 5HT2c receptor ligand for use in the treatment of symptoms of anxiety and / or depression associated with an affective disorder and / or symptoms associated with cognitive impairment disorder. Particularly useful are diphenhydramine derivatives of Formula (I) and particularly (2-[(4-butylsulfanylphenyl)-phenyl-methyl]sulfanyl-N,N-dimethyl-ethanamin) (Captodiamine).

The present invention provides tetrahydro protoberberine compounds as shown and their pharmaceutically acceptable inorganic or organic salts, crystallized hydrates, solvates and medicinal compositions. The present invention also provides their preparation process and application in preparing medicine for treating neurological diseases, especially dopamine acceptor related neurological diseases.

The present invention relates to a novel class of substituted phenylpiperazinyl derivatives having the formula (I) wherein X, Z, Y, U,V, Alk, W, R<1> , R<2>, R<3>, R<11>, R<12>, R<13> n, m and the dotted line are as defined in the description. The compounds of the invention are dopamine D4 receptor ligands and are therefore useful for the treatment of certain psychiatric and neurologic disorders, including psychosis.

The invention relates to triazole compounds of the general formula I whereinR1 is hydrogen or methyl, andR2 is C3-C4 alkyl or C1-C2 fluoroalkyl,as well as the physiologically tolerated acid addition salts of these compounds.The invention also relates to a pharmaceutical composition that comprises at least one triazole compound of the formula I and / or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one triazole compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.

The invention discloses a phenyl piperazidine heterocyclic medicinal compound. The compound has high affinity to a dopamine D3 receptor, so that the compound can be used for treating addiction to and dependence on medicines such as cocaine, and a central nervous system disorder relevant to the addiction and the dependence. The compound is a 4-[4-(substituted phenyl) piperazine piperazinyl-1]-butylcarbamic acid substituted aromatic ester derivative with a structural formula as Formula (1) as shown in the specification. A synthetic method of the derivate comprises the steps that substituted aniline and 2-(beta-chloroethyl) amine hydrochloride reacts in a solvent by taking inorganic base as an acid-binding agent to form corresponding substituted phenyl piperazidine hydrochloride 1; substituted phenyl piperazidine hydrochloride 1 and N-(delta-bromobutyl) phthalimide react in acetonitrile by taking K2CO3 as an acid-binding agent and under catalysis of KI to form a reaction intermediate 2; the intermediate 2 is subjected to hydrazinolysis to form an intermediate 3; and the intermediate 3 and an intermediate 5 are condensed by taking triethylamine as an acid-binding agent and a catalyst to form a target product I. The intermediate 5 is obtained in a manner that triphosgene and substituted aromatic phenol conduct partial condensation reaction in methylene chloride.

The present invention relates to novel functionally selective ligands of dopamine D2 receptors, FIG. 1 including agonists, antagonists, and inverse agonists. The invention further relates to the use of these compounds for treating central nervous system disorders related to D2 receptors.

The invention belongs to the field of biological pharmacy, relates to a medicinal use of 4-(4-phenylpiperazino)quinazoline derivatives and especially relates to a use of the 4-(4-phenylpiperazino)quinazoline derivatives in preparation of drugs for treating nervous system diseases and especially in preparation of dopamine D3 receptor inhibitors. A result of a biological activity test shows that the 4-(4-phenylpiperazino)quinazoline derivatives have good effects of inhibiting D3 receptors. The 4-(4-phenylpiperazino)quinazoline derivatives can be used as drug lead compounds, be synthesized into dopamine D3 receptor inhibitors, and be further used for preparation of drugs for treating schizophrenia and Parkinsonism caused by dopamine system dysfunction.

The present invention belongs to the technical field of medicine, and provides a pramipexole oral liquid and a preparation method thereof. Pramipexole is a dopamine D2 receptor agonist for treatment of Parkinson's disease; early symptoms of the Parkinson's disease comprise static tremor, myotonia, bradykinesia, and abnormal posture and gait; and moderate and advanced symptoms of the Parkinson's disease patients often comprise difficult chewing and swallowing. With the pramipexole oral liquid of the present invention, medication compliance of patients is easily improved, and a therapeutic effect is improved.

The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopammode inergic activity. The present invention relates to novel compounds that modulate dopamine D2 receptors. In particular, compounds of the present invention show functional selectivity at the dopamine D2 receptors and exhibit selectivity downstream of the D2 receptors, on the 0-arrestin pathway and / or on the cAMP pathway.

The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson's disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction.

The invention relates to compounds of the formula I:whereinn is 1 or 2,Ar is a C-bound 1,2,4-triazol radical which carries a radical R1 on the remaining carbon atom and a radical R1a on one of the nitrogen atoms;R1 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C4 alkoxymethyl, fluorinated C1-C6 alkyl, fluorinated C3-C6 cycloalkyl, fluorinated C1-C4 alkoxymethyl, or optionally substituted phenyl or 5- or 6-membered heteroaryl;R1a is hydrogen or C1-C4 alkyl; andR2 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C6 alkyl or fluorinated C3-C6 cycloalkyl;and to the physiologically tolerated acid addition salts of these compounds.The invention also relates to a pharmaceutical composition that comprises at least one triazole compound of the formula I and / or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one triazole compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.

The present invention relates to compounds of formula (I)wherein R1 and A are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use as medicaments. Compounds of general formula (I) have high affinity for the dopamine D3 and serotonin (5-Hydroxytryptamine; 5-HT) 5-HT2A receptors and are effective in the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.

[Problem] A compound which is useful as a dopamine D1 receptor positive allosteric modulator (D1 PAM) is provided. [Means for Solution] The present inventors have studied a compound which has a dopamine D1 receptor positive allosteric modulating activity and is useful as an active ingredient of a pharmaceutical composition for preventing and / or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like, and they have thus found that a heterocyclic acetamide compound has a dopamine D1 receptor positive allosteric modulating activity, thereby completing the present invention. The heterocyclic acetamide compound of the present invention has a dopamine D1 receptor positive allosteric modulating activity and can be used as an agent for preventing and / or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like.

Mono-ester and asymmetrically substituted diesters of dihydrexidine, dinapsoline and A-86929 and substituted derivatives thereof are described. The novel ester / diester derivatives exhibit improved pharmacokinetic characteristics relative to their unesterified parent compounds and can be formulated into pharmaceutical compositions useful for the treatment of a wide variety of dopamine related disorders.

The invention relates to compounds of the formula (I) wherein n is 0, 1 or 2; G is CH2 or CHR3; R1 is H, C1-C6-alkyl, C1-C6-alkyl substituted by C3-C6-cycloalkyl, C1-C6-hydroxyalkyl, fluorinated C1-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6-alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; R2, R3 and R4 are, independently of each other, H, methyl, fluoromethyl, difluoromethyl, or trifluoromethyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one or more substituents selected from halogen, methyl, methoxy and CF3; E is NR5 or CH2, wherein R5 is H or C1-C3-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, O and S and / or 1, 2 or 3 heteroatom-containing groups each independently selected from NR8, where R8 is H, C1-C4-alkyl, fluorinated C1-C4-alkyl, C1-C4-alkylcarbonyl or fluorinated C1-C4-alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents Ra, wherein the variable Ra has the meanings given in the claims and in the description; and physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

The invention relates to the pharmaceutical synthesis field and discloses N-(naphthoxyalkyl)heteroarylpiperidine compounds and a preparation method and applications thereof. The compounds disclosed by the invention are the compound shown in the formula I and pharmaceutically acceptable acid addition salts thereof, wherein n is 0, 1, 2 or 3; R is acetamino, acetoxy, acethythio, oximido, amino, aminocarbonyl, dimethylamino, diethylamino, hydroxyl, trifluoromethyl, trifluoroacetyl, cyano, phenyl, aldehyde group, benzoyl, fluorine, chlorine, bromine or iodine. The preparation method is as follows: 7-methoxynaphthalene compound used as raw material and 6-fluoro-3-(4-piperidyl)-1,2-benzoisoxazole are used to perform N-alkylation reaction. The N-(naphthoxyalkyl)heteroarylpiperidine compounds can act on 5-HT2A receptor, dopamine D2 receptor and melatonin receptor, are the compounds with the multi-target function and have the antipsychotic function.

The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula IwhereinAr is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered C-bound heteroaromatic radical comprising as ring member 1, 2 or 3 heteroatoms which are, independently of each other, selected from O, S and N, and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, 0 and S and / or 1, 2 or 3 heteroatom-containing groups each independently selected from NR8, where R8 is H, C1-C4-alkyl, fluorinated C1-C4-alkyl, C1-C4-alkylcarbonyl or fluorinated C1-C4-alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents Ra, wherein the variable Ra has the meanings given in the claims and in the description;X is a covalent bond or N—R2, CHR2, CHR2CH2, N or C—R2;Y is N—R2a, CHR2a, CHR2aCH2 or CHR2aCH2CH2; is a single bond or a double bond;E is CH2 or NR3;R1 is H, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl;R1a is H, C1C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-alkenyl,R2 and R2a each independently are H, CH3, CH2F, CHF2 or CF3 or R1a and R2 or R1a and R2a together are (CH2)n with n being 1, 2 or 3;R3 is H or C1C4-alkyl;R4 and R5 independently of each other are H, C1-C4-alkyl, fluorinated C1-C4-alkyl or C1-C4-alkoxy or may form, together with N, a 4-, 5- or 6-membered saturated or unsaturated ring;R6 and R7 independently of each other are H or halogen;and the physiologically tolerated acid addition salts thereof.

The present invention relates to aromatic compounds of the formula I wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, or R1a and R2 together are (CH2)n with n being 2, 3 or 4, or R1a and R2a together are (CH2)n with n being 2, 3 or 4; R2 and R2a are are independently of each other H, C1-C4-alkyl or fluorinated C1-C4-alkyl or R2a and R2 together are (CH2)m with m being 1, 2, 3, 4 or 5; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, fluorine, C1-C4-alkyl and fluorinated C1-C4-alkyl or together form a moiety (CH2)p with p being 2, 3, 4 or 5; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

The invention discloses an indoline-2-ketone D3 receptor ligand, which is a compound as shown in the formula I or pharmaceutical salt thereof, wherein n=2 or 3; R represents H, 4-CH3, 2,3-diCH3, 2-CH3, 4-OCF3, 3-OCH3, 3,4-diCH3 or 4-Cl. In comparison with the prior art, the compound has a strong activity to a dopamine D3 receptor, is used in treating or preventing central nervous and metal diseases such as schizophrenia, Parkinson's disease, drug dependence and relapse, etc., can be used in neuroprotection, and is used as a tool drug for researching D3 receptor structure, function and diseases related to D3 receptor dysfunction.

The invention provides 2,3,4,5-tetrahydro-1H-3-benzazepines of general formula (I) wherein: R<1> is hydrogen, halogen, C1-C4 alkyl, or CF3; R<2> is hydrogen, methyl, or lower alkenyl of 3-5 carbon atoms; R<3> and R<4> together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane or cyclohexane ring and R<5> is hydrogen or R<4> and R<5> together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane or cyclohexane ring and R<3> is hydrogen; R<6> is hydrogen, halogen, CF3, CN, NO2 or NH2; R<7> is hydrogen, halogen, CF3, CN, NO2 or NH2. The specific combination of substituents: R1 = H, R2 = H and R4 and R5 together forming a cyclohexane ring is excluded, namely 1-(5,6,7,8-tetrahydronaphthalen-2-yl)-2,3,4,5-tetrahydro-1H-benzol[d]azepine-7,8-diol. The compounds of the invention provide therapeutic agents that selectively interact positively with postsynaptic dopamine D1 receptors in the striatum, directly or in-directly (termed dopamine D1 agonists) and are particularly valuable as anti-Parkinsonian agents.

The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.

The invention provides an application of a partial agonist of a dopamine (DA) D2 receptor to preparation of drugs for inhibiting myopia and a using method of the partial agonist. The application and the using method have the beneficial effects that the functions of the DA D2 receptor in myopia are stabilized by applying the partial agonist aripiprazole of the DA D2 R; aripiprazole has the effect of inhibiting lengthening of vitreous cavities and oculi axes in the form deprivation myopia process, thus inhibiting formation of experimental myopia of animals.