- ANTI-BACTERIAL HETEROCYCLIC COMPOUNDS AND THEIR SYNTHESIS
-
The compounds of Formula I and Formula (B) are described herein along with their stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms, and pharmaceutically active
- -
-
Paragraph 000170; 000177
(2019/06/17)
-
- Design, synthesis and biological evaluation of 1,4-Diazobicylco[3.2.2]nonane derivatives as α7-Nicotinic acetylcholine receptor PET/CT imaging agents and agonists for Alzheimer's disease
-
α7-Nicotinic acetylcholine receptor (α7-nAChR) agonists are promising therapeutic drug candidates for treating the cognitive impairment associated with Alzheimer's disease (AD). Thus, a novel class of derivatives of 1,4-diazobicylco[3.2.2]nonane has been synthesized and evaluated as α7-nAChR ligands. Five of them displayed high binding affinity (Ki = 0.001–25 nM). In particular, the Ki of 14 was 0.0069 nM, which is superior to that of the most potent ligand that was previously reported by an order of magnitude. Four of them had high selectivity for α7-nAChRs over α4β2-nAChRs and no significant hERG (human ether-a-go-go-related gene) inhibition. Their agonist activity was also discussed preliminarily. One of the compounds, 15 (Ki = 2.98 ± 1.41 nM), was further radiolabeled with 18F to afford [18F]15 for PET imaging, which exhibited high initial brain uptake (11.60 ± 0.14%ID/g at 15 min post injection), brain/blood value (9.57 at 30 min post injection), specific labeling of α7-nAChRs and fast clearance from the brain. Blocking studies demonstrated that [18F]15 was α7-nAChR selective. In addition, micro-PET/CT imaging in normal rats further indicated that [18F]15 had obvious accumulation in the brain. Therefore, [18F]15 was proved to be a potential PET radiotracer for α7-nAChR imaging.
- Wang, Shuxia,Fang, Yu,Wang, Huan,Gao, Hang,Jiang, Guohua,Liu, Jianping,Xue, Qianqian,Qi, Yueheng,Cao, Mengying,Qiang, Bingchao,Zhang, Huabei
-
p. 255 - 266
(2018/10/17)
-
- COMPOUNDS AND THEIR METHODS OF USE
-
The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.
- -
-
Page/Page column 104
(2018/09/08)
-
- ORGANIC COMPOUND FOR OPTOELECTRONIC DEVICE AND ORGANIC OPTOELECTRONIC DEVICE AND DISPLAY DEVICE
-
The present invention relates to a compound for an organic optoelectronic device represented by chemical formula 1, an organic optoelectronic device applying the same and a display device including the organic optoelectronic device. The detailed content with respect to the chemical formula 1 are the same as defined in the specification. The compound can provide an organic optoelectronic device having high efficiency, long lifespan, etc.COPYRIGHT KIPO 2017
- -
-
Paragraph 0142-0146
(2017/08/03)
-
- FORMULATIONS FOR 2-HETEROARYL SUBSTITUTED BENZOFURANS
-
Processes and compositions for 2-heteroaryl substituted benzofuran derivatives are described. The 2-heteroaryl substituted benzofuran derivatives may be suitable for preparing radiolabeled 2-heteroaryl substituted benzofuran derivatives for imaging amyloid deposits in living patients.
- -
-
Page/Page column 24
(2017/06/12)
-
- BRIDGED PIPERIDINE DERIVATIVES
-
The present invention relates to a compound of formula (I), wherein Het Ar is a five or six membered hetaryl group, containing one, two or three heteroatoms, selected from N, O or S; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, or lower alkoxy; R2 is lower alkyl substituted by halogen, -CH2-C3-6-cycloalkyl, substituted by one or two substituents, selected from lower alkyl substituted by halogen or halogen, or is lower alkenyl substituted by halogen; R3 is hydrogen, lower alkyl substituted by halogen, lower alkyl, halogen, C3-6-cycloalkyl or lower alkyl substituted by hydroxy; n is 1 or 2; for n = 2, R1 can be independent to each other; Y is CH or N; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
- -
-
Page/Page column 151
(2017/07/06)
-
- Ligand compound of alpha7 nicotinic acetylcholine receptor and application of ligand compound
-
The embodiment of the invention provides a ligand compound of an alpha7 nicotinic acetylcholine receptor, the ligand compound has one of the following general formulas: wherein (1) X and R1 are shown in the description, and R7 is halogen; (2) R2 is hydrogen, and R3 is halogen or amino; or R3 is hydrogen, and R2 is halogen or amino; (3) R6 is hydrogen, and R4 and R5 are synthesized into a compound shown in the description; or R4 is hydrogen, and R5 and R6 are synthesized into a compound shown in the description; R8 is halogen; and (4) Y is nitrogen or carbon, Z is shown in the description, and R9 and R10 are respectively halogens. The provided ligand compound is an excellent ligand compound of the alpha7 nicotinic acetylcholine receptor. After being chemically marked radioactively, the provided ligand compound of the alpha7 nicotinic acetylcholine receptor can serve as a PET photographic developer.
- -
-
Page/Page column 0039; 0040; 0041
(2017/10/09)
-
- HETEROCYCLIC COMPOUNDS USEFUL AS ANTI-BACTERIAL AGENTS AND METHOD FOR PRODUCTION
-
The present disclosure relates to compounds of Formula I, its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms thereof and pharmaceutical compositions containing them as the active ingredient which can be used as medicaments. The aforementioned substances can also be used in the manufacture of medicaments for treatment, prevention or suppression of diseases, and conditions mediated by microbes. The present disclosure also relates to the synthesis.and characterization of aforementioned substances.
- -
-
Paragraph 000132
(2017/12/15)
-
- MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
-
The present invention features a compound of formula I: or a pharmaceutically acceptable salt thereof, where R1, R2, R3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.
- -
-
Page/Page column 1106-1107
(2021/02/10)
-
- Modulators of Cystic Fibrosis Transmembrane Conductance Regulator
-
The present invention features a compound of formula I: or a pharmaceutically acceptable salt thereof, where R1, R2, R3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.
- -
-
Paragraph 5359; 5360
(2016/05/02)
-
- BRIDGED COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
-
Novel bridged compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.
- -
-
Paragraph 0075-0076
(2016/08/23)
-
- OREXIN RECEPTOR ANTAGONISTS
-
The disclosures herein relate to novel compounds of formula wherein W, X and Y1, Y2, Y3 and Y4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.
- -
-
Page/Page column 85
(2014/01/18)
-
- Oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad spectrum antibacterial agents
-
Bacterial resistance is eroding the clinical utility of existing antibiotics necessitating the discovery of new agents. Bacterial type II topoisomerase is a clinically validated, highly effective, and proven drug target. This target is amenable to inhibit
- Singh, Sheo B.,Kaelin, David E.,Wu, Jin,Miesel, Lynn,Tan, Christopher M.,Meinke, Peter T.,Olsen, David,Lagrutta, Armando,Bradley, Prudence,Lu, Jun,Patel, Sangita,Rickert, Keith W.,Smith, Robert F.,Soisson, Stephen,Wei, Changqing,Fukuda, Hideyuki,Kishii, Ryuta,Takei, Masaya,Fukuda, Yasumichi
-
supporting information
p. 609 - 614
(2014/06/09)
-
- TRIAZOLONE COMPOUNDS AND USES THEREOF
-
The invention disclosed herein is directed to compounds of Formula (I) and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula (I), or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention disclosed herein is further directed to methods of treating prostate, breast, colon, pancreatic, chronic lymphocytic leukemia, melanoma and other cancers comprising administration of a of a therapeutically effective amount of a selective PPARα antagonist. The compounds and pharmaceutical compositions of the invention are also useful in the treatment of viral infections, such as HCV infections and HIV infections. The invention disclosed herein is also directed to a methods of preventing the onset of and/or recurrence of acute and chronic myeloid leukemia, as well as other cancers, comprising administration of a of a therapeutically effective amount of a selective PPARα antagonist.
- -
-
Paragraph 00218
(2013/09/26)
-
- BRIDGED BICYCLIC COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
-
Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.
- -
-
Page/Page column 78-79
(2013/03/26)
-
- RING-FUSED MORPHOLINE DERIVATIVE HAVING PI3K-INHIBITING ACTIVITY
-
The present invention provides compounds or a pharmaceutically acceptable salt thereof which inhibit the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and are therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a ring-fused morpholine compound shown in the present specification, or a pharmaceutically acceptable salt thereof.
- -
-
Page/Page column 35
(2011/07/30)
-
- BICYCLIC PYRIDINES AND ANALOGS AS SIRTUIN MODULATORS
-
Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
- -
-
Page/Page column 64
(2011/06/16)
-
- The design of efficient and selective routes to pyridyl analogues of 3-oxo-3,4-dihydro-2H-1,4-(benzothiazine or benzoxazine)-6-carbaldehydes
-
This Letter describes the synthesis of challenging pyridyl analogues of 3-oxo-3,4-dihydro-2H-1,4-(benzothiazine or benzoxazine)-6-carbaldehydes. The six different routes described are high yielding, contain no major purification issues and have been used to give gram quantities of each aldehyde.
- Brooks, Gerald,Dabbs, Steven,Davies, David T.,Hennessy, Alan J.,Jones, Graham E.,Markwell, Roger E.,Miles, Timothy J.,Owston, Nathan A.,Pearson, Neil D.,Peng, Tony W.
-
scheme or table
p. 5035 - 5037
(2011/01/04)
-
- Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2] nonane (CP-810,123), a novel α7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: Synthesis, SAR development, and in vivo efficacy in cognition models
-
A novel α7 nAChR agonist, 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4- diazabicyclo[3.2.2]nonane (24, CP-810,123), has been identified as a potential treatment for cognitive deficits associated with psychiatric or neurological conditions including schizophrenia and Alzheimer's disease. Compound 24 is a potent and selective compound with excellent pharmaceutical properties. In rodent, the compound displays high oral bioavailability and excellent brain penetration affording high levels of receptor occupancy and in vivo efficacy in auditory sensory gating and novel object recognition. The structural diversity of this compound and its preclinical in vitro and in vivo package support the hypothesis that α7 nAChR agonists may have potential as a pharmacotherapy for the treatment of cognitive deficits in schizophrenia. 2009 American Chemical Society.
- O'Donnell, Christopher J.,Rogers, Bruce N.,Bronk, Brian S.,Bryce, Dianne K.,Coe, Jotham W.,Cook, Karen K.,Duplantier, Allen J.,Evrard, Edelweiss,Hajós, Mihaly,Hoffmann, William E.,Hurst, Raymond S.,Maklad, Noha,Mather, Robert J.,McLean, Stafford,Nedza, Frank M.,O'Neill, Brian T.,Peng, Langu,Qian, Weimin,Rottas, Melinda M.,Sands, Steven B.,Schmidt, Anne W.,Shrikhande, Alka V.,Spracklin, Douglas K.,Wong, Diane F.,Zhang, Andy,Zhang, Lei
-
experimental part
p. 1222 - 1237
(2010/08/05)
-
- Antibacterial Agents
-
Naphthalene, quinoline, quinoaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
- -
-
Page/Page column 10; 12
(2008/12/07)
-
- ANTIBACTERIAL AGENTS
-
Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
- -
-
Page/Page column 35
(2010/11/25)
-
- ANTIBACTERIAL AGENTS
-
2H-chromen-2-one derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
- -
-
Page/Page column 30
(2008/06/13)
-
- ANTIBACTERIAL AGENTS
-
Naphthyridine and related derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
- -
-
Page/Page column 22
(2008/06/13)
-
- ANTIBACTERIAL AGENTS
-
Naphthyridine and related derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
- -
-
Page/Page column 23
(2008/06/13)
-
- ANTIBACTERIAL AGENTS
-
Naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
- -
-
Page/Page column 24-25
(2008/06/13)
-
- ANTIBACTERIAL AGENTS
-
Naphthyridine and quinoline derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
- -
-
Page/Page column 22
(2008/06/13)
-
- ANTIBACTERIAL AGENTS
-
Naphthyridine and related derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
- -
-
Page/Page column 22-23
(2008/06/13)
-
- ANTIBACTERIAL AGENTS
-
Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
- -
-
Page/Page column 92-93; 96-97; 100
(2010/02/15)
-
- ANTIBACTERIAL AGENTS
-
Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
- -
-
Page/Page column 43-45
(2010/10/19)
-
- ANTIBACTERIAL AGENTS
-
Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
- -
-
Page/Page column 24
(2010/10/20)
-
- ANTIBACTERIAL AGENTS
-
Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
- -
-
Page/Page column 23
(2010/10/20)
-
- ANTIBACTERIAL AGENTS
-
Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
- -
-
Page/Page column 34; 37
(2010/10/20)
-
- Bicyclic pyrazole compounds as antibacterial agents
-
Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection.
- -
-
Page/Page column 24-25
(2010/11/24)
-
- COMPOUNDS
-
Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
- -
-
Page/Page column 40
(2008/06/13)
-
- ANTIBACTERIAL COMPOUNDS
-
Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man
- -
-
-
- AMINOCYCLOHEXENE QUINOLINES AND THEIR AZAISOSTERIC ANALOGUES WITH ANTIBACTERIAL ACTIVITY
-
Cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
- -
-
Page/Page column 32-33
(2010/02/06)
-
- NITROGEN-CONTAINING BICYCLIC HETEROCYCLES FOR USE AS ANTIBACTERIALS
-
Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives hereof useful in methods of treatment of bacterial infections in mammals, particularly man.
- -
-
Page/Page column 99-100
(2010/02/07)
-
