- FUSED BICYCLIC RAF INHIBITORS AND METHODS FOR USE THEREOF
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The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method o
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Paragraph 0586-0588
(2022/02/09)
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- PROCESSES FOR PREPARING AN S1P-RECEPTOR MODULATOR
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This application relates to processes for preparing an S1P-receptor modulator "Compound 1", which is useful in the treatment of diseases or disorders associated with activity of S1P, including CNS disorders. The process comprises reacting "compound 2" with "compound 3" in the presence of a reducing agent.
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Page/Page column 32
(2021/05/07)
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- sEH Inhibitor or pharmaceutically acceptable composition thereof as well as preparation method and application thereof
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The invention provides sEH inhibitor or a pharmaceutically acceptable composition and a preparation method and application thereof, and belongs to the technical field of medicines. sEH Inhibitor or a pharmaceutically acceptable composition thereof according to the present invention is provided, and the sEH inhibitor has the structure shown I. sEH Inhibitor provided by the invention can stabilize an endogenous substance epoxy fatty acid with wide physiological activity, has a strong inhibition effect on human recombinant sEH, and can be used for regulating the generation of a plurality of pro-inflammatory cytokines. The invention relieves the stress of endoplasmic reticulum, prevents or reverses the dysfunction of endothelial dysfunction, stabilizes mitochondria function multiple action mechanisms to obviously relieve neuropathic pain, and can effectively avoid adverse reactions related to the target spot. Furthermore, the sEH inhibitor structure provided by the invention does not contain free carboxyl groups, can avoid adverse reactions such as gastrointestinal irritation caused by oral administration, and is small in adverse reaction, high in bioavailability, excellent in analgesic effect and small in administration amount.
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Paragraph 0117-0118
(2021/09/21)
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- NOVEL INDOLE-2-CARBOXAMIDES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
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Page/Page column 178-179
(2020/11/13)
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- NOVEL PHENYL AND PYRIDYL UREAS ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
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Page/Page column 161
(2020/11/13)
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- 1, 3, 4, 5-TETRAHYDRO-2H-PYRIDO[4,3-B]INDOLE DERIVATIVES FOR THE TREATMENT, ALLEVIATION OR PREVENTION OF DISORDERS ASSOCIATED WITH TAU AGGREGATES LIKE ALZHEIMER'S DISEASE
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The present invention relates to novel compounds that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neurofibrillary Tangles (NFTs), such as Alzheimer's disease (AD).
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Page/Page column 124
(2019/07/20)
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- 3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 00318
(2017/09/27)
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- An efficient catalytic method for the Beckmann rearrangement of ketoximes to amides and aldoximes to nitriles mediated by propylphosphonic anhydride (T3P)
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An efficient method for the Beckmann rearrangement of ketoximes to amides mediated by a catalytic amount (15 mol %) of propylphosphonic anhydride (T3P) is described. Aldoximes underwent second order Beckmann rearrangement to provide the corresponding nitriles in excellent yields on reacting with T3P (15 mol %) at room temperature. The main advantages of this environmentally friendly protocol include procedural simplicity, and particularly ease of isolation of the products.
- Augustine, John Kallikat,Kumar, Rajesha,Bombrun, Agnes,Mandal, Ashis Baran
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experimental part
p. 1074 - 1077
(2011/03/22)
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- 1-(1-Acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea (AR9281) as a potent, selective, and orally available soluble epoxide hydrolase inhibitor with efficacy in rodent models of hypertension and dysglycemia
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1-(1-Acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea 14a (AR9281), a potent and selective soluble epoxide hydrolase inhibitor, was recently tested in a phase 2a clinical setting for its effectiveness in reducing blood pressure and improving insulin resistance in pre-diabetic patients. In a mouse model of diet induced obesity, AR9281 attenuated the enhanced glucose excursion following an intraperitoneal glucose tolerance test. AR9281 also attenuated the increase in blood pressure in angiotensin-II-induced hypertension in rats. These effects were dose-dependent and well correlated with inhibition of the sEH activity in whole blood, consistent with a role of sEH in the observed pharmacology in rodents.
- Anandan, Sampath-Kumar,Webb, Heather Kay,Chen, Dawn,Wang, Yi-Xin,Aavula, Basker R.,Cases, Sylvaine,Cheng, Ying,Do, Zung N.,Mehra, Upasana,Tran, Vinh,Vincelette, Jon,Waszczuk, Joanna,White, Kathy,Wong, Kenneth R.,Zhang, Le-Ning,Jones, Paul D.,Hammock, Bruce D.,Patel, Dinesh V.,Whitcomb, Randall,MacIntyre, D. Euan,Sabry, James,Gless, Richard
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scheme or table
p. 983 - 988
(2011/03/20)
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- Structure-based rational design, synthesis and antifungal activity of oxime-containing azole derivatives
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In an attempt to find novel azole antifungal agents with improved activity and broader spectrum, computer modeling was used to design a series of new azoles with piperidin-4-one O-substituted oxime side chains. Molecular docking studies revealed that they formed hydrophobic and hydrogen-bonding interactions with lanosterol 14α-demethylase of Candida albicans (CACYP51). In vitro antifungal assay indicates that most of the synthesized compounds showed good activity against tested fungal pathogens. In comparison with fluconazole, itraconazole and voriconazole, several compounds (such as 10c, 10e, and 10i) show more potent antifungal activity and broader spectrum, suggesting that they are promising leads for the development of novel antifungal agents.
- Xu, Yulan,Sheng, Chunquan,Wang, Wenya,Che, Xiaoying,Cao, Yongbing,Dong, Guoqiang,Wang, Shengzheng,Ji, Haitao,Miao, Zhenyuan,Yao, Jianzhong,Zhang, Wannian
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supporting information; experimental part
p. 2942 - 2945
(2010/08/19)
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- N-Boc 4-nitropiperidine: preparation and conversion into a spiropiperidine analogue of the eastern part of maraviroc
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Previously unreported N-Boc 4-nitropiperidine was prepared in two steps from N-Boc-piperidone. The synthetic utility of this new intermediate was demonstrated by the development of a new and simple route to spirolactam piperidines. Further synthetic work involving a challenging triazole cyclisation allowed the preparation of a spiropiperidine analogue of the eastern part of maraviroc.
- Mullen, Philip,Miel, Hugues,Anthony McKervey
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scheme or table
p. 3216 - 3217
(2010/08/19)
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- HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF
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Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
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Page/Page column 108
(2010/08/18)
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- Routes to HIV-integrase inhibitors: efficient synthesis of bicyclic pyrimidones by ring expansion or amination at a benzylic position
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Ring expansion of [6,6] bicyclic pyrimidones led, through an aziridinium intermediate, to potent HIV-integrase inhibitors with a [7,6] core. A more flexible and diversity-oriented synthesis of functionalized pyrimidohexahydrodiazepines was then developed;
- Ferreira, Maria del Rosario Rico,Cecere, Giuseppe,Pace, Paola,Summa, Vincenzo
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scheme or table
p. 148 - 151
(2009/04/14)
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- AMIDE COMPOUNDS AND THE USE THEREOF
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The invention relates to amide compounds of Formula I: (I) and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SOm; Z is each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl, etc.; R
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Page/Page column 206
(2009/01/24)
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- PIPERAZINO DERIVATIVES AS NEUROKININ ANTAGONISTS
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The invention relates to compounds of formula (I) wherein Z, Rc, y, m, u, Ar2, n, X, Rc', l and Ar2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
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Page/Page column 46-47
(2010/11/08)
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- DIAZEPINE OXAZOLIDINONES AS ANTIBACTERIAL AGENTS
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The present invention relates to a new class of oxazolidinone derivatives, to their use as antibacterial agents, to pharmaceutical compositions containing these compounds and to methods for their preparation.
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Page/Page column 23-24
(2008/06/13)
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- INSECTICIDAL 2,4-DIAMINOQUINAZOLINES AND RELATED DERIVATIVES
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Certain novel 2,4-diaminoquinazolines, related derivatives and agriculturally acceptable salts thereof have provided unexpected pesticidal activity. These compounds are represented by formula (I): wherein R, R2, R4, R5 and A are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of a second compound are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
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Page/Page column 16-17
(2008/06/13)
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- PYRROLOPYRIMIDINE DERIVATIVE
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A pyrrolo[3,2-d]pyrimidine derivative represented by the formula (I) or a pharamaceutically acceptable salt of the derivative. The derivative or salt is useful as a GSK-3 inhibitor.
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- Hemoregulatory compounds
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The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.
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- Oxime derivatives
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An oxime derivative of the formula: STR1 wherein R is a hydrogen atom or a C1-5 alkyl group, R1 is a hydrogen atom, a C1-5 alkyl group or a carboxyl-protecting group, R2 is a hydrogen atom, a halogen atom, a hydroxyl group or an amino group, R3 is a C3-7 cycloalkyl group, R4 is a hydrogen atom, a halogen atom or a C1-4 alkoxy group, each of R5 and R6 which may be the same or different, is a hydrogen atom or a C1-5 alkyl group, or R5 and R6 together represent a C2-4 alkylene group which forms together with the adjacent carbon atom a C3-5 ring, provided that when R2 is a hydrogen atom, R4 is a C1-4 alkoxy group, m is an integer of 0 or 1, and n is an integer of from 1 to 3; or its pharmaceutically acceptable salt.
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