- FUNCTIONALIZED LONG-CHAIN HYDROCARBON MONO- AND DI-CARBOXYLIC ACIDS AND THEIR USE FOR THE PREVENTION OR TREATMENT OF DISEASE
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This invention provides compounds of Formulae (IA), (IB), (IC), (ID), (IE), (IF), (IG), (IH), (IJ), (IK), (IL), (II), (III), (IIIA), and (IIIB); pharmaceutically acceptable salts and solvates thereof; and compositions thereof. This invention further provides methods for treating a disease, including but not limited to, liver disease or an abnormal liver condition; cancer (such as hepatocellular carcinoma or cholangiocarcinoma); a malignant or benign tumor of the lung, liver, gall bladder, bile duct or digestive tract; an intra- or extra-hepatic bile duct disease; a disorder of lipoprotein; a lipid-and-metabolic disorder; cirrhosis; fibrosis; a disorder of glucose metabolism; a cardiovascular or related vascular disorder; a disease resulting from steatosis, fibrosis, or cirrhosis; a disease associated with increased inflammation (such as hepatic inflammation or pulmonary inflammation); hepatocyte ballooning; a peroxisome proliferator activated receptor-associated disorder; an ATP citrate lyase disorder; an acetyl-coenzyme A carboxylase disorder; obesity; pancreatitis; or renal disease.
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Paragraph 0544; 0546
(2021/01/29)
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- SULFONIMIDAMIDE COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
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In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: (Formula AA) or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.
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Page/Page column 496
(2020/08/13)
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- SULFONAMIDE DERIVATIVES AND USES THEREOF
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The present disclosure relates to compounds of Formula (I) or (II): and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.
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Paragraph 0915
(2020/12/30)
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- COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
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In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured.The variables shown in Formula AA are as defined in the claims. The compounds of formula AA are NLRP3 activity modulators and, as such, can be used in the treatment of metabolic disorders (e.g. Type 2 diabetes, atherosclerosis, obesity or gout), a disease of the central nervous system (e.g. Alzheimer's disease, multiple sclerosis, Amyotrophic Lateral Sclerosis or Parkinson's disease), lung disease (e.g. asthma, COPD or pulmonary idiopathic fibrosis), liver disease (e.g. NASH syndrome, viral hepatitis or cirrhosis), pancreatic disease (e.g. acute pancreatitis or chronic pancreatitis), kidney disease (e.g. acute kidney injury or chronic kidney injury), intestinal disease (e.g. Crohn's disease or Ulcerative Colitis), skin disease (e.g. psoriasis), musculoskeletal disease (e.g. scleroderma), a vessel disorder (e.g. giant cell arteritis), a disorder of the bones (e.g. osteoarthritis, osteoporosis or osteopetrosis disorders), eye disease (e.g. glaucoma or macular degeneration), a disease caused by viral infection (e.g. HIV or AIDS), an autoimmune disease (e.g. Rheumatoid Arthritis, Systemic Lupus Erythematosus or Autoimmune Thyroiditis), cancer or aging.
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Page/Page column 518
(2019/02/13)
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- Iron-Catalyzed β-Alkylation of Alcohols
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β-Branched alkylated alcohols have been prepared in good yields using a double-hydrogen autotransfer strategy in the presence of our diaminocyclopentadienone iron tricarbonyl complex Fe1. The alkylation of some 2-arylethanol derivatives was successfully addressed with benzylic alcohols and methanol as alkylating reagents under mild conditions. Deuterium labeling experiments suggested that both alcohols (2-arylethanol and either methanol or benzyl alcohol) served as hydrogen donors in this cascade process.
- Bettoni, Leó,Gaillard, Sylvain,Renaud, Jean-Luc
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supporting information
p. 8404 - 8408
(2019/10/16)
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- Occupying a flat subpocket in a tRNA-modifying enzyme with ordered or disordered side chains: Favorable or unfavorable for binding?
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Small-molecule ligands binding with partial disorder or enhanced residual mobility are usually assumed as unfavorable with respect to their binding properties. Considering thermodynamics, disorder or residual mobility is entropically favorable and contrib
- Neeb, Manuel,Hohn, Christoph,Ehrmann, Frederik Rainer,H?rtsch, Adrian,Heine, Andreas,Diederich, Fran?ois,Klebe, Gerhard
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supporting information
p. 4900 - 4910
(2016/10/04)
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- Anti-cancer compositions and methods
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Anti-cancer compositions and methods are described including one or more compounds having the structural formula I: where R is phenyl, where R1 is (CH2)n—Se—C(═NH)—NH2, where R2 is (CH2)n—Se—C(═NH)—NH
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Page/Page column 19
(2011/09/15)
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- Synthesis and characterization of a novel iNOS/Akt inhibitor Se,Se′-1,4-phenylenebis(1,2-ethanediyl)bisisoselenourea (PBISe)-against colon cancer
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Our studies demonstrate that substitution of sulfur with selenium in known iNOS inhibitor increases the compound's potency by several folds in variety of different cancers cell lines tested. Hence, this approach may be used as a strategy to increase the e
- Desai, Dhimant,Madhunapantula, SubbaRao V.,Gowdahalli, Krishnegowda,Sharma, Arati,Chandagaludoreswamy, Raghavendragowda,El-Bayoumy, Karam,Robertson, Gavin P.,Amin, Shantu
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scheme or table
p. 2038 - 2043
(2010/09/18)
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- Synthesis of new cores and their use in the preparation of polyester dendrimers
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Six dendrimer and dendron cores terminated by hydroxyl groups that are neither phenolic nor cleavable by hydrogenolysis have been prepared in a consistent one-pot manner from terminal allyl groups by reduction of the product of reductive ozonolysis. Some of the terminal allyl derivatives are new and others have been prepared by new methods. The well-known O-benzylidene derivative of 2,2′-bis(hydroxymethyl)propanoic acid was shown to be the cis-stereoisomer. A new AB3-type anhydride, tris(benzyloxymethyl) acetic anhydride has been prepared. It was demonstrated that these cores and dendrons could be assembled into first and second generation homo- and mixed polyester dendrimers.
- Twibanire, Jean-D'Amour K.,Al-Mughaid, Hussein,Grindley, T. Bruce
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experimental part
p. 9602 - 9609
(2011/01/03)
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- Synthesis of naphthalenes and 2-naphthols by the electrophilic cyclization of alkynes
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A wide variety of substituted naphthalenes are readily prepared regioselectively under mild reaction conditions by the 6-endo-dig electrophilic cyclization of appropriate arene-containing propargylic alcohols by IC1, I 2, Br2, NBS, and PhSeBr. 3-Iodo-2-naphthols have also been prepared in excellent yields by the cyclization of analogous 1-aryl-3-alkyn-2-ones. This methodology readily accommodates various functional groups and has been successfully extended to the synthesis of substituted carbazoles and dibenzothiophenes.
- Zhang, Xiaoxia,Sarkar, Sampa,Larock, Richard C.
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p. 236 - 243
(2007/10/03)
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- Diphenylmethyl compounds useful as muscarinic receptor antagonists
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This invention provides compounds of formula I: wherein a, b, c, e, m, n, Ar1, R1, R2, R3, R4a, R4b, R5 and R6 are as defined in the specification. The compounds of fo
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Page/Page column 21
(2008/06/13)
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- Indoles
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A 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: wherein A, B, C, D, T, Y, and Z each represent a methine or a nitrogen linkage; R1, R2, R3, R4, and R5 each represent a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3. The compounds have serotonin antagonism. They are therefore clinically useful as medicaments, in particular, for treating, ameliorating, and preventing spastic paralysis. They are also useful as central muscle relaxants for ameliorating myotonia.
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- A New General Synthesis of Polycyclic Aromatic Compounds Based on Enamine Chemistry
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Alkylation of enamines and enamine salts by benzylic and (β-haloethyl)aryl halides, respectively, followed by acidic cyclodehydration and dehydrogenation provides an efficient synthetic approach to a wide range of polycyclic aromatic compounds of diverse structural types.Specific polycyclic hydrocarbons synthesized by this route include benzo- and benzofluorene, 7H-dibenzo-, 13H-dibenzo-, and 13H-dibenzofluorene, 15H-tribenzofluorene, dibenzochrysene, benzopentaphene, indenofluorene, fluorenofluorene, octahydrodibenzanthracene, dibenzanthracene, octahydrodibenzanthracene, dibenzanthracene, picene, benzopicene, 1H-benzaceanthrylene, and 4H-cyclopentachrysene.This method with appropriate modifications appears to be potentially broader in scope than established traditional methods of polycyclic hydrocarbon synthesis.
- Harvey, Ronald G.,Pataki, John,Cortez, Cecilia,Raddo, Pasquale Di,Yang, ChengXi
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p. 1210 - 1217
(2007/10/02)
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- Side chain hydroxylation of aromatic compounds by fungi. 1. Products and stereochemistry
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The fungus Mortierella isabellina can convert ethylbenzene and a number of para-substituted derivatives to the corresponding optically active 1-phenylethanols with enantiomeric excess between 5 and 40percent and chemical yields up to 45percent. 2-Ethylnaphthalene, 2-ethylthiophene, and n-propylbenzene were similarly converted, as were the bicyclic compounds indane and tetraline.In most cases, the R absolute configuration of product predominated.The fungi Cunninghamella echinulata var. elegans and Helminthosporium species are also capable of performing some of these transformations.M. isabellina and C. elegans also produce 2-phenylethanols as products in some cases.The highest enantiomeric excesses during benzylic hydroxylation were obtained with Helminthosporium and are attributable, at least in part, to further stereoselective oxidation of the alcohol.Cross induction experiments with M. isabellina indicate that the same enzyme may be responsible for the benzylic hydroxylation of ethylbenzene, 2-ethylthiophene, and 2-ethylnaphthalene.
- Holland, Herbert L.,Bergen, Eleanor J.,Chenchaiah, P. Chinna,Khan, Shaheer H.,Munoz, Benito,et al.
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p. 502 - 507
(2007/10/02)
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- Ethylenic silicon compounds and thermoplastic elastomers obtained therefrom
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The invention provides organosilicon compounds of the formula: STR1 in which: N IS 1, 2 OR 3; Each R, which may be identical or different, is a monovalent organic group which contains a carbon-carbon double bond and from 2 to 10 carbon atoms; Each R1, which may be identical or different, is a straight or branched alkyl radical optionally substituted by one or more halogen atoms or cyano groups; an aryl radical or an alkylaryl radical optionally substituted by one or more halogen atoms; R2 is a straight or branched divalent alkylene or alkylidene radical possessing up to 4 carbon atoms; X is a divalent radical consisting of, or containing, at least one hetero-atom selected from oxygen, sulphur and nitrogen atoms, the radical being attached to the radical R2 via a said hetero-atom; G is an organic radical of valency (m+ l) possess from 1 to 30 carbon atoms; m is 1, 2 or 3; And each Y, which may be identical or different, is a functional group selected from: --NO2, STR2 --COOM (where M represents a sodium, potassium or lithium atom); --COOR4 ; STR3 --COCl; --OH; --OR4 ; STR4 --SH; --SR4 ; STR5 --CONH2 ; --CSNH2 ; --CN; --CH2 --NH2 ; --CHO; STR6 --NCO; STR7 wherein R3 represents a hydrogen atom or a straight or branched alkyl radical possessing up to 6 carbon atoms and R4 represents an alkyl radical possessing up to 4 carbon atoms, with the proviso that two Y groups can together constitute an imide group STR8 wherein R5 represents a hydrogen atom or a straight or branched alkyl radical possessing up to 4 carbon atoms. These are useful intermediates in the preparation of disilanes and silicon polymers, in particular of polyethylenic silicon compounds which can be polymerized with an α, ω-dihydrogenopolysiloxane to give thermoplastic elastomers.
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