- ANTI-PULMONARY TUBERCULOSIS NITROIMIDAZOLE DERIVATIVE
-
Disclosed is a substituted nitroimidazole derivative, which is mainly used for treating related diseases caused by mycobacterial infections, such as Mycobacterium tuberculosis, especially being suitable for diseases caused by resistant Mycobacterium tuberculosis.
- -
-
Paragraph 0530-0532
(2017/12/31)
-
- 5- or 6-substituted benzofuran-2-carboxamide compounds and methods for using them
-
The disclosure relates particularly to certain carboxamide, sulfonamide and amine compounds and pharmaceutical compositions thereof, and to methods of treating and ameliorating disorders and conditions related to the adiponectin pathway, sphingolipid metabolism, oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. In certain embodiments, the compounds have the structures (I-1), (2-I) and (3-I) in which the variables are as described herein.
- -
-
-
- CHEMOKINE RECEPTOR ANTAGONISTS AND METHODS OF USE THEREOF
-
Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.
- -
-
Paragraph 1193; 1194
(2016/02/21)
-
- BENZAMIDE DERIVATIVE USEFUL AS FASN INHIBITORS FOR THE TREATMENT OF CANCER
-
The present invention is directed to benzamide derivatives, pharmaceutical compositions containing them, and their use as FASN inhibitors, in for example, the treatment of cancer, obesity related disorders, liver related disorders and viral infections. Such compounds are represented by formula (I) as follows: wherein R1, R2, R3, R4, R5, m, n, (II) and (III) are defined herein.
- -
-
Page/Page column 111
(2015/06/18)
-
- A novel and concise synthetic access to chiral 2-substituted-4-piperidone
-
A novel and concise synthetic access to enantiopure chiral 2-aryl/alkyl substituted 4-piperidone has been demonstrated. This new route features two key steps: the highly diastereoselective conjugate addition of homochiral lithium amides to trans-β-substituted-α,β-unsaturated methyl esters guaranteed the enantiopurity at 2 position (de >19:1) and the intramolecular attacking of carbanions to methyl esters led to the formation of the piperidone ring. A wide range of substrates, including chiral 2-aryl and 2-alkyl-4-piperidones, were successfully synthesized with modest to high yield. Moreover, some non-chiral 3-substituted-4-piperidones were also synthesized with enhanced ring-formation yield, implicating the versatility of this method in construction of various piperidine rings.
- Chen, Bai-Ling,Wang, Bing,Lin, Guo-Qiang
-
p. 945 - 953
(2014/07/21)
-
- CONDENSED PYRIDINE DERIVATIVE AND USE THEREOF
-
Provided are a condensed pyridine derivative having a serotonin 5-HT2C receptor activation action, a prophylactic or therapeutic agent for a lower urinary tract symptom, obesity and/or organ prolapse and the like containing the condensed pyridine derivative, a screening method for a substance that increases leak point pressure upon a rise in the intravesical pressure or a prophylactic or therapeutic drug for stress urinary incontinence, a prophylactic or therapeutic drug for cystoceles or enteroceles, containing a substance that activates serotonin 5-HT2C receptor, and a method of screening for a therapeutic drug for cystoceles or enteroceles, including increasing an intravesical pressure after bilateral transection of the hypogastric nerve and pudendal nerve of an animal, and measuring a closure response in the urethra, the rectum or the vagina observed at that time. A serotonin 5-HT2C receptor activator containing a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof.
- -
-
Page/Page column 115-116
(2010/08/18)
-
- NOVEL SUBSTITUTED PIPERIDONES AS HSP INDUCERS
-
The present invention relates to novel compounds of formula (I) or (II), their pharmaceutically acceptable salts and their hydrates, solvates, stereoisomers, conformers, tautomers, polymorphs and prodrugs and also pharmaceutically acceptable compositions containing them Wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification. The compounds of the present invention are HSP inducers and by virtue of this effect, useful for the treatment of various diseases accompanying pathological stress. The present invention also relates to a process for the preparation of the said novel compounds. The invention also relates to the use of the above-mentioned compounds for the preparation of medicament for use as pharmaceuticals.
- -
-
Page/Page column 68-69
(2009/03/07)
-
- PYRIMIDINONE DERIVATIVES AND METHODS OF USE THEREOF
-
The present invention relates to Pyrimidinone Derivatives, compositions comprising a Pyrimidinone Derivative, and methods of using the Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disease, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
- -
-
Page/Page column 161
(2008/12/08)
-
- PIPERIDINOYL-PYRROLIDINE AND PIPERIDINOYL-PIPERIDINE COMPOUNDS
-
The present invention relates to a class of compounds of general formula (I) and the salts, hydrates, solvates, polymorphs and prodrugs wherein n, R6, R7 and R10 are as defined herein and especially to MCR4 agonist compounds of formula (I), to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.
- -
-
Page/Page column 83-84
(2010/11/25)
-
- QUINOLONE ANTIBACTERIAL AGENTS
-
Compounds of formula (I, II, III, IV, V, and VI) and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula (I) as well as pharmaceutically acceptable compositions comprising compounds of formula (I). Compounds of formula (I) as disclosed herein can be used in a variety of applications including use as antibacterial agents.
- -
-
Page/Page column 102; 103
(2010/02/11)
-
- Chemokine receptor antagonists and methods of use thereof
-
Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: formula (1) or physiologically acceptable salt thereof.
- -
-
-
- Generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, their preparation, compositions and use as medicaments
-
This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.
- -
-
-
- CCR8 INHIBITORS
-
Disclosed is an inhibitor of CCR8 that is represented by Structural Formula (I). Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier or diluent and a CCR8 inhibitor represented by Structural Formula (I). Also disclosed is a method of treating inflammatory disorders in a subject by administering a CCR8 inhibitor to the subject.
- -
-
-
- CCR8 INHIBITORS
-
Disclosed are CCR8 inhibitors represented by Structural Formulas (I). The variables in Structural Formula (I) are described herein. Also disclosed are methods of treating a subject with a CCR8 mediated condition, especially asthma, by administering one of the disclosed CCR8 inhibitors to the subject.
- -
-
-
- SEROTONERGIC BENZOTHIOPHENES
-
The present invention provides serotonergic benzothiophenes of Formula (I), where A, R, R, R, R, and R are as described in the specification.
- -
-
-
- Indole derivatives for the treatment of depression and anxiety
-
The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.
- -
-
Page/Page column 17
(2010/02/05)
-
- Piperidine derivatives as reuptake inhibitors
-
The present invention provides compounds of formula (I) and a method of inhibiting the reuptake of serotonin and antagonizing the serotonin receptor which comprises administering to a subject in need of such treatment an effective amount of a compound of formula (I).
- -
-
Page column 29-30
(2010/02/09)
-
- Benzofuran derivatives
-
The present invention provides compounds of formula (I) which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.
- -
-
-
- SEROTONERGIC BENZOFURANS
-
The present invention provides serotonergic benzofurans of Formula (I): where A, R, R, R, R, and R are as described in the specification.
- -
-
-
- Piperidines derivatives and their use as serotonin receptor antagonists
-
The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.
- -
-
-
- Preparation of substituted piperidin-4-ones
-
The present invention provides a novel process for the preparation of substituted piperidine-4-ones useful as intermediates in the preparation of pharmaceuticals.
- -
-
-
- Piperidine derivatives as serotonine reuptake inhibitors
-
The present invention provides compounds of formula I and a method of inhibiting the reuptake of serotonin, antagonizing the 5-HT1Areceptor and antagonizing the 5-HT2Areceptor which comprises administering to a subject in need of such treatment an effective amount of a compound of formula I.
- -
-
Page column 21; 22
(2010/02/05)
-
- The design of 8,8-dimethyl[1,6]naphthyridines as potential anticonvulsant agents
-
Starting from a series of 7-linked tetrahydroisoquinoline derivatives, as exemplified by SB-270664, a new series of 8,8-dimethylnaphthyridine compounds has been identified. SAR studies around these attractive leads have provided compounds such as 12 which display excellent anticonvulsant activity and an encouraging pharmacokinetic profile in vivo.
- Austin, Nigel E.,Hadley, Michael S.,Harling, John D.,Harrington, Frank P.,Macdonald, Gregor J.,Mitchell, Darren J.,Riley, Graham J.,Stean, Tania O.,Stemp, Geoffrey,Stratton, Sharon C.,Thompson, Mervyn,Upton, Neil
-
p. 1627 - 1629
(2007/10/03)
-
- Chemokine receptor anagonists and methods of use therefor
-
Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.
- -
-
-
- Piperidine derivatives having effects on serotonin related systems
-
The present invention provides the compounds of the following formula: Wherein the variables are as defined in the specification and a method for inhibiting the reuptake of seretonin, antagonizing the 5-HT1Areceptor and antagonizing the 5-HT2Areceptor which comprises administering to a subject in need of such treatment an effective amount of the compound of above formula.
- -
-
-