- DERIVATIVES OF PIPERLONGUMINE AND USES THEREOF
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The present invention relates to a group of 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3-dihydropyridin-6-one (piperlongumine) derivatives, analogs and pharmaceutically acceptable salts thereof. The present invention also relates to a pharmaceutical composition and formulation containing a derivative of piperlongumine; and use of the derivatives and analogs for treating cancer, reducing inflammation and/or treating an autoimmune or inflammatory disease.
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- DERIVATIVES OF PIPERLONGUMINE AND USES THEREOF
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The present invention relates to a group of 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3- dihydropyridin-6-one (piperlongumine) derivatives, analogs and pharmaceutically acceptable salts thereof. The present invention also relates to processes for preparing the same; a pharmaceutical composition and formulation containing a derivative of piperlogumine; and use of the derivatives and analogs for treating cancer.
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- MODULATORS OF SESTRIN-GATOR2 INTERACTION 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 00532; 00536; 00537
(2018/11/22)
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- MODULATORS OF SESTRIN-GATOR2 INTERACTION 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 0615
(2017/05/15)
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- SUBSTITUTED PYRAZOLE AND TRIAZOLE COMPOUNDS AS KSP INHIBITORS
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Disclosed are new substituted pyrazole and triazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof
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Page/Page column 72-73
(2008/12/05)
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- Substituted imidazole compounds as KSP inhibitors
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The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses of the compounds. The compounds of the invention have the following general formula:
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Page/Page column 34
(2008/06/13)
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- Beta-agonists, methods for the preparation thereof and their use as pharmaceutical compositions
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The present invention relates to new beta-agonists of general formula (I) wherein the groups R1 to R4 have the meanings given in ths claims and specification, the tautomers, racemates, enantiomers, diastereomers, solvates, hydrates,
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Page/Page column 22-23
(2010/11/27)
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- Compounds with growth hormone releasing properties
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Disclosed are compounds of formula I formula I wherein R1, R2, R5, R6, R7, R8, G, J, L, M, a, b, c, d, e, and f are as defined in the specification, and compositions containing them. These
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- COMPOUNDS WITH GROWTH HORMONE RELEASING PROPERTIES
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This invention relates to novel compounds, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.
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- Method for preparing a compound with growth hormone releasing properties
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A method for preparing a compound of formula I or a salt thereof is disclosed.
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- Bicyclicpyrimidones and their use to treat diseases
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The present invention is directed to dihydropyrimidones having formula I or II and methods of using them to induce mitotic arrest, thereby making them useful as anti-cancer agents and other diseases that can be treated by inducing mitotic arrest.
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- Pyrrolotriazinone compounds and their use to teat diseases
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The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof useful for inducing mitotic arrest thereby making them useful as anti-cancer agents and other diseases which can be treated by inducing mitotic arrest.
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- Compounds with growth hormone releasing properties
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This invention relates to novel compounds, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.
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- Benzoamide piperidine containing compounds and related compounds
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The present invention relates to certain benzoamide piperidine containing compounds and related compounds that exhibit activity as NK-1 receptor antagonists, (e.g., substance P receptor antagonists), to pharmaceutical compositions containing them, and to their use in the treatment and prevention of central nervous system disorders, inflammatory disorders, cardiovascular disorders, ophthalmic disorders, gastrointestinal disorders, disorders caused by helicobacter pylori, disorders of the immune system, urinary incontinence, pain, migraine, emesis, angiogenesis and other disorders.
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- PYRROLOTRIAZINONE COMPOUNDS AND THEIR USE TO TREAT DISEASES
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The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts thereof useful for inducing mitotic arrest thereby making them useful as anti-cancer agents and other diseases which can be treated by inducing mitotic arrest.
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- Use of growth hormone or a growth hormone secretagogue for promoting bone formation
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The invention provides a method of enhancing the healing of bone fractures in an animal subjected to distraction osteogenesis, the method comprising administering, to the animal in need thereof, a growth hormone or a growth hormone secretagogue in an amou
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- Compounds with growth hormone releasing properties
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There are disclosed novel synthetic peptides of the general formula (I) Compounds of formula (I) stimulate the release of growth hormone from the pituitary in humans and animals. A method for increasing the rate and extent of growth of animals to increase their milk and wool production or for the treatment of ailments, and the use of the compounds of formula (I) for the preparation of medicaments, are also disclosed.
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- Compounds with growth hormone releasing properties
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The present invention relates to compounds, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.
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Page column 59
(2010/02/06)
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- Synthesis of N-protected 14C-labelled (2E)-5-amino-5-methylhex-2-enoic acid analogues
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A novel method of preparing N-protected (2E)-5-amino-5-methylhex-2-enoic acids has been developed based on the synthesis of 3-methyl-3-amino-butanol. The method was used to synthesise 14C-labelled compounds of (1) via synthesis of triethylphosphono[1-14C]acetate.
- Jessen, Claus U.,Selvig, Helle,Valsborg, Jacob S.
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p. 265 - 275
(2007/10/03)
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- Compounds with growth hormone releasing properties
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Compounds of the general formula I STR1 compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are described.
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- Compounds with growth hormone releasing properties
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There are disclosed novel synthetic peptides of formula (I) where A, B, D, E, F, G, J, m, n, and p are defined in the specification. Compounds of formula (I) promote the release of growth hormone in humans and animals. Growth promoting compositions containing such compounds of formula (I) as the active ingredient, methods of stimulating the release of growth hormone, and the use of such compounds of formula (I) are also disclosed.
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- Compounds with growth hormone releasing properties
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Compounds of peptide mimetic nature having the general formula I STR1 wherein a and b are independently 1 or 2, R1 and R2 are independently H or C1-6 alkyl, G and J are independently, inter alia, aromats, and D and E are independently several different groups are growth hormone secretagogous with improved bioavailability.
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- Compounds with growth hormone releasing properties
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Novel peptide derivatives, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are disclosed. The peptides have the formula (I): STR1 wherein a, b, A, R1, L1, D, R3, R4, R2, L2, E and G are as defined in the specification. These peptides exhibit improved resistance to proteolytic degradation, and hence, improved bioavailability.
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- Novel orally active growth hormone secretagogues
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A novel class of growth hormone-releasing compounds with a molecular weight in the range from 500 to 650 has been discovered. The aim of this study was to obtain growth hormone secretagogues with oral bioavailability. By a rational approach we were able t
- Hansen, Thomas K.,Ankersen, Michael,Hansen, Birgit S.,Raun, Kirsten,Nielsen, Karin K.,Lau, Jesper,Peschke, Bernd,Lundt, Behrend F.,Th?gersen, Henning,Johansen, Nils L.,Madsen, Kjeld,Andersen, Peter H.
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p. 3705 - 3714
(2007/10/03)
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- Benzolactam growth hormone secretagogues: Replacement of the C-3 amide bond in L-692,429
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The synthesis and structure-activity relationships of various C-3 amide bond modifications in the novel nonpeptidyl growth hormone secretagogue L-692,429 are described. Several C-3 amide surrogates were prepared and the urea moiety was found to exhibit growth hormone releasing activity similar to that observed with L-692,429.
- Ok, Hyun O.,Szumiloski, John L.,Doldouras, George A.,Schoen, William R.,Cheng, Kang,Chan, Wanda W.-S.,Butler, Bridget S.,Smith, Roy G.,Fisher, Michael H.,Wyvratt, Matthew J.
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p. 3051 - 3056
(2007/10/03)
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