52 results about "Arylpiperazine derivatives" patented technology

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

The present invention related to a novel urea derivative for formula (I):which is useful as an anti-cancer agent, its pharmaceutically acceptable acid addition salt or stereoisomer, and to a process for preparing the urea derivative and an anti-cancer composition comprising the same as an active ingredient.

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression.

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

The present invention provides arylpiperazine derivatives having Formula I which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression.

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Processes for preparing N-aryl-piperazine derivatives of formula I particularly (R)-4-cyano-N-[2-[4-(2,3-dihydro-1,4-benzodioxan-5-yl)-1-piperazinyl-propyl]-N-(2-pyridinyl)-benzamide, are disclosed. Compositions comprising N-aryl-piperazine derivatives and low levels of common impurities are also disclosed. In addition, products produced by the process are disclosed.

The present invention relates to novel quinoxaline-piperazine compounds, 1-[(6,7-substituted alkoxyquinoxalinyl)aminocarbonyl]-4-(hetero)arylpiperazine derivatives and their pharmaceutically acceptable salts, a process for their preparation thereof, and compositions containing such compounds. Therapeutic methods for the treatment of hyperproliferative disorders, including cancers, by administering quinoxalin-piperazine compounds are also included.

The invention relates to ten amide arylpiperazine derivatives, their preparation method, and their use in the preparation of benign prostatic hyperplasia treatment medicines. The preparation method of the amide arylpiperazine derivatives comprises the following steps: reacting free alkali of 3-bromopropylamine hydrobromide with di-tert-butyl dicarbonate to obtain a colorless oily liquid, reacting the colorless oily liquid with o-methoxyphenylpiperazine to obtain a light yellow oily material, reacting the light yellow oily material with trifluoroacetic acid to obtain a product, and reacting the product with N,N-diisopropylethylaine, 2-(7-azobenzotriazol)-N,N,N',N'-tetramethylformamidinium hexafluorophosphate, and 5-indoleacetic acid or 3-indoleacetic acid or 3-indolepropionic acid or 3-indolebutyric acid or 5-hydroxy-2-indoleacetic acid or 5-methoxy-2-indoleacetic acid or 1-methyl-3-indoleacetic acid or 6-bromo-2-indoleacetic acid or 5-chloro-2-indoleacetic acid or 7-nitro-2-indoleacetic acid to obtain final products. Experiments prove that the benign prostatic hyperplasia resistance activities of eight compounds in the amide arylpiperazine derivatives are stronger than a contrast drug prazosin.

The invention discloses a benzo-aza-alkyl aryl piperazine derivative and applications in preparation of drugs. The derivative shows the effect on central nervous systems, especially on the double highaffinity activity of a 5-HT<1A> acceptor and a Sigma-1 acceptor. Various physiological and pharmacological effects are brought into play in the body; and the compound can be used as a pharmaceuticalactive substance, especially used for anti-depression, anti-anxiety, anti-bipolar affective disorder and anti-neuropathic pain, and can also be used as an intermediate to prepare other pharmaceuticalactive compounds. The compound is fast in effect and small in toxic and side effect, and can meet demands of clinical applications; and the compound is a compound or a free base or salt thereof havingthe following structural formula (IV). The structure of the compound or the free base or salt thereof is shown as the structural formula (IV).

The invention discloses a 3-cyanoaniline alkyl aryl piperazine derivative and application thereof in preparing medicaments. The 3-cyanoaniline alkyl aryl piperazine derivative disclosed by the invention has very useful pharmaceutical properties and excellent tolerance, and especially can be used as a novel analgesia, a novel antidepressant medicament, and a novel analgesic and antidepressant medicament. The compounds are 5-hydroxytryptamine regulated central analgesias, and also are 5-hydroxytryptamine regulated novel antidepressant medicaments. The compounds also are low in toxic and side effects and large in safety range. The 3-cyanoaniline alkyl aryl piperazine derivatives are compounds as shown in a formula (III), or free bases or salts thereof.

The present invention relates to certain biarylz and arylheteroaryl piperazine derivatives of Formula (Ia) that are modulators of the 5HT2c receptor. Accordingly, compounds of the present invention are useful for the treatment of 5HT2c receptor associated diseases or disorders, such as, obesity, Alzheimer Disease, erectile dysfunction and related disorders.

The invention relates to a novel N-aryl piperazine compound having double activity of dopamine D2 and 5-HT2a, a preparation method, a medicine combination containing the compound and an application thereof on treating mental diseases.

The invention discloses application of an aryl piperazine compound shown in a formula (I) in preparing medicines for treating acute pain, nerve pain and nociceptive pain of mammals including human beings. The medicines are particularly suitable for treating complex pain caused by various reasons.

The invention relates to the fields of pharmaceutical chemistry and pharmaceutical lead compound research, and specifically relates to aryl piperazine derivatives (I); wherein the definitions of R1 to R5 are defined in the description. The invention also discloses a preparation method of the aryl piperazine derivatives and an antitumor application of the novel derivatives. The compounds have been subjected to primary pharmacodynamics research and in-vitro antitumor experiments, and the results show that some compounds have good antitumor activity and can be used to develop novel antitumor drugs.

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

The invention provides an N-aryl piperazine derivative, i.e. a compound shown in formula (I) or pharmaceutically acceptable salt, wherein n is 1-6. The invention provides the compound shown in formula (I) and a drug composition thereof which have excellent effect in treating nervous and mental diseases caused by central nervous system dopamine and serotonin transmittance disorder.

Compounds of the formula I:are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive-compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

Heteroarylpiperidine and -piperazine derivatives of the formula (I)in which the symbols A, X, Y, L1, L2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).

An anti-depression 4-[2-(arylthio) benzyl]-1-arylpiperazine derivative used to prepare the medicine for treating depression is prepared through Ullmann reaction between p-methoxy benzeneethiol and p-chlorobenzoic acid to generate thioether, reducing, chlorinating and N-alkylation.

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

This invention provides novel aryl piperazine derivatives represented by Formula (I) having medical utility, in particular as modulators of dopamine and serotonin receptors, preferably the D3, 5HT1A and 5-HT2A receptor subtypes, and in particular useful for the treatment of neuropsychiatric disorders, incl. schizophrenia.

The invention relates to the fields of pharmaceutical chemistry and medicament lead compound discovery, and concretely relates to arylpiperazine derivatives (1) and (2). The invention also discloses a preparation method for the novel arylpiperazine derivatives and application of the arylpiperazine derivatives to resist tumors. The compounds are subjected to preliminary pharmacodynamics research and in-vitro antineoplastic experiment, results show that the compounds show relatively good antineoplastic activity and can be used to develop and exploit novel antitumor drugs.

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.