- Regioselective Radical Arene Amination for the Concise Synthesis ofortho-Phenylenediamines
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The formation of arene C-N bonds directly from C-H bonds is of great importance and there has been rapid recent development of methods for achieving this through radical mechanisms, often involving reactiveN-centered radicals. A major challenge associated with these advances is that of regiocontrol, with mixtures of regioisomeric products obtained in most protocols, limiting broader utility. We have designed a system that utilizes attractive noncovalent interactions between an anionic substrate and an incoming radical cation in order to guide the latter to the areneorthoposition. The anionic substrate takes the form of a sulfamate-protected aniline and telescoped cleavage of the sulfamate group after amination leads directly toortho-phenylenediamines, key building blocks for a range of medicinally relevant diazoles. Our method can deliver both free amines and monoalkyl amines allowing access to unsymmetrical, selectively monoalkylated benzimidazoles and benzotriazoles. As well as providing concise access to valuableortho-phenylenediamines, this work demonstrates the potential for utilizing noncovalent interactions to control positional selectivity in radical reactions.
- Gillespie, James E.,Morrill, Charlotte,Phipps, Robert J.
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p. 9355 - 9360
(2021/07/19)
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- N-SUBSTITUTED-3-TRICYCLYL PIPERIDINE DERIVATIVES AS ANTICANCER AND NEUROPROTECTIVE AGENTS
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A genus of N-substituted-3-tricyclyl piperidine derivatives is disclosed. The compounds are of the following genus: The compounds induce FOXO1 transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.
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Paragraph 00116-00117
(2021/07/31)
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- 3-DIARYLMETHYLENES AND USES THEREOF
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3-Diarylmethylenes are disclosed. The compounds activate PP2A, suppress oncogenic kinase signaling, and negatively regulate MYC and MYCN in cancer. The compounds also induce FOXO transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.
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Paragraph 0001
(2021/09/26)
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- COMPOUNDS
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A compound of formula (I), or a pharmaceutically acceptable salt thereof.
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Page/Page column 76
(2020/01/24)
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- PROTEIN KINASE MKK4 INHIBITORS FOR PROMOTING LIVER REGENERATION OR REDUCING OR PREVENTING HEPATOCYTE DEATH
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The invention relates to pyrazolo-pyridine compounds which inhibit mitogen-activated protein kinase kinase 4 (MKK4) and in particular, selectively inhibit MKK4 over protein kinases JNK1 and MKK7. The compounds are useful for promoting liver regeneration or reducing or preventing hepatocyte death. They are further useful for treating osteoarthritis or rheumatoid arthritis, or CNS-related diseases.
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- MORPHINAN DERIVATIVE AND MEDICAL USAGE THEREOF
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The purpose of the present invention is to provide a compound useful as a prophylactic or therapeutic agent for various diseases and symptoms related to orexin receptors, and a medical usage of the same. The present invention provides a morphinan derivati
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Paragraph 0101
(2018/09/20)
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- HETEROCYCLIC INHIBITORS OF THE SODIUM CHANNEL
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The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (l)-(ll l) or Compounds (1 )-(65) of Table 1 ) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotropic lateral sclerosis, glaucoma, ischaemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.
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Page/Page column 133
(2015/09/28)
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- ANTIBACTERIAL THIAZOLECARBOXYLIC ACIDS
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Compounds of general formula (I), wherein R1, R11, Y, R2, n and A are as defined herein are useful as inhibitors or metallo-β-lactamase (MBL) enzymes and can be used for reducing or removing antibiotic resistance in bacteria.
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- Directed heterodimerization: Stereocontrolled assembly via solvent-caged unsymmetrical diazene fragmentation
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A general strategy for the directed and stereocontrolled assembly of carbon-carbon linked heterodimeric hexahydropyrroloindoles is described. The stepwise union of complex amines in the form of mixed diazenes followed by photoexpulsion of dinitrogen in a
- Movassaghi, Mohammad,Ahmad, Omar K.,Lathrop, Stephen P.
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supporting information; experimental part
p. 13002 - 13005
(2011/10/12)
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- AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS
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The present invention provides a novel class of azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
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Page/Page column 68
(2010/02/13)
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- Indole, azaindole and related heterocyclic sulfonylureido piperazine derivatives
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This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with sulfonylureido piperazine derivatives of Formula I. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. 1wherein: Z is 2Q is selected from the group consisting of: 3—W— is 4—represents a carbon-carbon bond or does not exist; and A is NR13R14.
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Page/Page column 33-34
(2010/02/05)
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- Potent and selective, sulfamide-based human β3-adrenergic receptor agonists
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A series of sulfamide-based analogs related to L-796568 were prepared and evaluated for their biological activity at the human β3- adrenergic receptor (AR). This modification allows for a significant reduction in molecular weight, while maintai
- Dow, Robert L.,Paight, Ernest S.,Schneider, Steven R.,Hadcock, John R.,Hargrove, Diane M.,Martin, Kelly A.,Maurer, Tristan S.,Nardone, Nancy A.,Tess, David A.,DaSilva-Jardine, Paul
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p. 3235 - 3240
(2007/10/03)
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- 2,3-oxidosqualene-lanosterol cyclase inhibitors
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The present invention relates to aminocyclohexanol derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
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- Chemical and Biological Reactivity of Sulfamidopenicillins
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A number of semisynthetic penicillins bearing a sulfamido side chain at the 6-position have been prepared and their chemical and biological reactivity examined.The compounds do not show antibiotic activity against Escherichia coli but do show activity aga
- Davern, Peter,Sheehy, James,Smyth, Timothy
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p. 381 - 388
(2007/10/02)
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- Anticonvulsant O-Alkyl Sulfamates. 2,3:4,5-Bis-O-(1-methylethylidene)-β-D-fructopyranose Sulfamate and Related Compounds.
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Novel sugar sulfamate 1 (McN-4853, topiramate) has been found to exhibit potent anticonvulsant activity analogous to that of phenytoin.In the maximal electroshock seizure test, orally at 2 h in mice, 1 had an ED50 of 39 mg/kg.Orally, 1 had a duration of action in excess of 8 h.Other aspects of the pharmacology of 1, as well as neurochemistry and carbonic anhydrase inhibition, are discussed.The conformational behavior of 1 in solution and in the solid state are discussed.A series of analogues of 1 were synthesized and examined for anticonvulsant properties.
- Maryanoff, Bruce E.,Nortey, Samuel O.,Gardocki, Joseph F.,Shank, Richard P.,Dodgson, Susanna P.
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p. 880 - 887
(2007/10/02)
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