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Ophthalmic formulation of polyoxyl lipid or polyoxyl fatty acid and treatment of ocular conditions (Fri, 13 Mar 2015)
Provided herein include formulations for topical administration, such as ophthalmic formulations, and methods of using such formulations. In some aspects and embodiments the formulations may include a polyoxyl lipid or fatty acid, and or a polyalkoxylated alcohol and may include nanomicelles. Also include methods of treating or preventing diseases or conditions, such as ocular diseases or conditions.
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Novel 11 Beta-hydroxyandrosta-4-ene-3-ones (Fri, 01 Jul 2011)
Patent 569867 Disclosed is an 11-beta-hydroxyandrosta-4-ene-3-one, or a physiologically acceptable salt thereof wherein Z represents O or S; R1 represents hydrogen or methyl; R2 and R3 are the same or different and each independently represents hydrogen or halogen; R5 represents a group selected from alkyl, cycloalkyl, -O-alkyl, aryl or heterocyclic ring and R4 and R6 are defined in the specification.
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Novel 11 beta - hydroxyandrosta-4-ene-3-ones (Fri, 22 Aug 2008)
11 β-hydroxyandrosta-4-ene-3-one, compound of formula (I), and physiologically acceptable salt thereof; wherein R4 represents moiety selected from a group consisting of (A), (B) and (C), with a proviso that when R4 represents moiety (C), Z is S.
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Diarylacetylene hydrazide containing tyrosine kinase inhibitors (Fri, 23 Aug 2013)
The present invention relates to novel diarylacetylene hydrazide compounds of formula (I) or pharmaceutically acceptable salt thereof, as tyrosine kinase inhibitors, the process for their preparation, and to the use of the compounds of formula (I) in the preparation of pharmaceutical compositions for the therapeutic treatment of disorders related to tyrosine kinases, in warm-blooded animals
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NOVEL AMINOOLIGOSACCHARIDE DERIVATIVE AND PROCESS FOR PREPARING THE SAME (Fri, 12 Jul 1996)
The present invention relates to novel aminooligosaccharide derivative and pharmaceutically acceptable non-toxic salts thereof, which possess potent saccharide hydrolase inhibition and antibacterial activities. The invention also relates to a process for preparing the same and to pharmaceutical compositions containing the same as active ingredients. In accordance with the present invention, the inventors isolated novel aminooligosaccharide derivative from a soil microorganism categorized as Streptomyces sp., and discovered that it can be applied as potent inhibitors for saccharide hydrolases and antibacterial agents as well.
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DIARYLACETYLENE HYDRAZIDE CONTAINING TYROSINE KINASE INHIBITORS (Thu, 28 Nov 2013)
The present invention relates to novel diarylacetylene hydrazide compounds of formula (I) or pharmaceutically acceptable salt thereof, as tyrosine kinase inhibitors, the process for their preparation, and to the use of the compounds of formula (I) in the preparation of pharmaceutical compositions for the therapeutic treatment of disorders related to tyrosine kinases, in warm-blooded animals
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4-(DIARYLMETHYL)-1-PIPERAZINYL DERIVATIVES (Thu, 23 Dec 2004)
A compound of formula (I) wherein X, Y, X' & Y' are selected from hydrogen, halogen, substituted or unsubstituted alkyl (linear, branched or cyclo), aryl, alkyloxy and haloalkyl group; R1, R2, R3 & R4 are selected from hydrogen, substituted or unsubstituted alkyl groups (linear, branched or cyclo), aryl, heteroaryl groups or aralkyl groups, heterocycles containing one or more of hetero atoms (viz., N, S, O), substituted or unsubstituted alkenyl or alkynyl groups of carbon 2 to 6, wherein the substituents R1 & R2 on the piperazinyl moiety are either syn or anti to each other and optionally R3 and R4 together with the carbons to which they are attached form a monocyclic saturated or aryl or substituted aryl or heteroaryl or substituted heteroaryl ring containing one or more hetero atoms selected from N, S and O with a ring size ranging from 3 to 6; with a proviso that when R3 & R4 together do not form part of a ring they may exist in either E or Z configuration;R5 is (CH2)n-O-CH2-CO-Z wherein n is 1 to 6; Z is selected from OH, OR, NRR', N(OR)R', N(R)-N(R)R' and wherein R & R' are selected from hydrogen, substituted or unsubstituted alkyl groups (linear, branched or cyclo), aryl, heteroaryl groups or aralkyl groups, heterocycles containing one or more of hetero atoms (viz., N, S, O), substituted or unsubstituted alkenyl or alkynyl groups of carbon 2 to 6; and B is selected from -(CH2)n- (n is 1 to 6) and -(CH2)x-D-(CH2)y where D is O, NR, S or SO2, x and y are independently 1 to 6; and m is selected from 1 to 6; and pharmaceutically acceptable salts thereof.
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4-(diarylmethyl)-1-piperazinyl derivatives (Fri, 29 Aug 2003)
A compound of formula (I) wherein X, Y, X' & Y' are selected from hydrogen, halogen, substituted or unsubstituted alkyl (linear, branched or cyclo), aryl, alkyloxy and haloalkyl group; R1, R2, R3 & R4 are selected from hydrogen, substituted or unsubstituted alkyl groups (linear, branched or cyclo), aryl, heteroaryl groups or aralkyl groups, heterocycles containing one or more of hetero atoms (viz., N, S, O), substituted or unsubstituted alkenyl or alkynyl groups of carbon 2 to 6, wherein the substituents R1 & R2 on the piperazinyl moiety are either syn or anti to each other and optionally R3 and R4 together with the carbons to which they are attached form a monocyclic saturated or aryl or substituted aryl or heteroaryl or substituted heteroaryl ring containing one or more hetero atoms selected from N, S and O with a ring size ranging from 3 to 6; with a proviso that when R3 & R4 together do not form part of a ring they may exist in either E or Z configuration;R5 is (CH2)n-O-CH2-CO-Z wherein n is 1 to 6; Z is selected from OH, OR, NRR', N(OR)R', N(R)-N(R)R' and wherein R & R' are selected from hydrogen, substituted or unsubstituted alkyl groups (linear, branched or cyclo), aryl, heteroaryl groups or aralkyl groups, heterocycles containing one or more of hetero atoms (viz., N, S, O), substituted or unsubstituted alkenyl or alkynyl groups of carbon 2 to 6; and B is selected from -(CH2)n- (n is 1 to 6) and -(CH2)x-D-(CH2)y where D is O, NR, S or SO2, x and y are independently 1 to 6; and m is selected from 1 to 6; and pharmaceutically acceptable salts thereof.
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Compounds and compositions as hedgehog pathway modulators (Fri, 14 Nov 2008)
The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-furiction or GIi gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.
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DERIVATIVES OF 17α-ACYLOXY,11β-HYDROXYANDROST-4-ENE-3-ONE 17β-ESTERS (Thu, 12 Feb 2009)

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TOPICAL FORMULATIONS AND USES THEREOF (Fri, 23 Nov 2018)
Provided herein include formulations of defined active agents for topical administration, such as ophthalmic formulations, and methods of using such formulations. In some aspects and embodiments the formulations may include a polyoxyl lipid or fatty acid, and or a polyalkoxylated alcohol and may include nanomicelles. Also included are methods of treating or preventing diseases or conditions, such as ocular diseases or conditions.
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IMIDAZOLE DERIVATIVES AS ALDOSTERONE SYNTHASE INHIBITORS (Sat, 04 Jun 2011)
The present invention provides a compound of formula (I) or pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, R5, R7 and p are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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Topical formulations and uses thereof (Fri, 19 May 2017)
Provided herein include formulations for topical administration, such as ophthalmic formulations, and methods of using such formulations. In some aspects and embodiments the formulations may include a polyoxyl lipid or fatty acid, and/or a polyalkoxylated alcohol and may include nanomicelles. Also include methods of treating or preventing diseases or conditions, such as ocular diseases or conditions.
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NOVEL DICARBOXYLIC ACID DERIVATIVES AS S1P1 RECEPTOR AGONISTS (Sat, 28 Jan 2012)
Patent 581933 Disclosed are dicarboxylic acid derivatives of general formula (I), wherein 1,2,4-oxadiazole group, or enantiomers, diastereomers, hydrates, solvates and pharmaceutically acceptable salts thereof. Such compounds of formula (I) include 1-{4-[5-(4-isobutylphenyl)-1,2,4-oxadiazol-3-yl]benzyl}piperidine-4,4-dicarboxylic acid. Processes for preparing the compounds of formula (I) are also disclosed as well as their use for treating transplant rejection, tissue graft rejection, immune disorders, autoimmune disorders, inflammatory and chronic inflammatory conditions, asthma, pollinosis, psoriasis, myocarditis, atopic dermatitis, lymphocytic leukemias, lymphomas, multiple sclerosis, lupus erythematosus, inflammatory bowel diseases, diabetes mellitus, glomerulo-nephritis, atherosclerosis, multi-organ failure, sepsis, pneumonia, optic neuritis, polymyalgia rheumatica, uveitis, vasculitis, osteoarthritis, respiratory distress syndrome, ischemia reperfusion injury, chronic obstructive pulmonary disease, infection associated with inflammation, viral inflammation, influenza, hepatitis, Guillian-Barre syndrome, chronic bronchitis, restenosis, granulomatous disease, sarcoidosis, leprosy, scleroderma, Alzheimer's disease as well as disorders related to impaired vascular integrity, cancers, disregulated angiogenesis or excessive neoangiogenesis...
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NOVEL DICARBOXYLIC ACID DERIVATIVES AS S1P1 RECEPTOR AGONISTS (Fri, 19 Dec 2008)
The present invention relates to new compounds of formula (I) possessing agonistic activity at sphingosine-1 -phosphate (S1 P) receptors, their process of preparation and their use as immunosuppressive agents. The invention is also directed to pharmaceutical compositions containing these compounds and use of these compounds for treatment/prevention of immune medi-ated diseases and conditions or inflammatory diseases and conditions.
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Novel dicarboxylic acid derivatives as S1P1 receptor agonists (Fri, 26 Feb 2010)
The present invention relates to new compounds of formula (I) possessing agonistic activity at sphingosine-1 -phosphate (S1 P) receptors, their process of preparation and their use as immunosuppressive agents. The invention is also directed to pharmaceutical compositions containing these compounds and use of these compounds for treatment/prevention of immune mediated diseases and conditions or inflammatory diseases and conditions.
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Biphenylcarboxamide derivatives as hedgehog pathway modulators (Fri, 23 Jan 2015)
The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula 1.
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NOVEL HYDRAZIDE CONTAINING TYROSINE KINASE INHIBITORS (Sat, 12 Sep 2009)
The present invention relates to compounds of formula (I), and salts thereof, wherein P represents a 5 or 6-membered heteroaryl ring; R1 is aryl or unsaturated heterocyclyl radical optionally substituted by one or more identical or different radicals R5.
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METHODS FOR TREATMENT OF INFLAMMATORY CONDITIONS USING S-[4-(3-FLUORO-3-METHYLBUTYRYLOXY) BUT-2-YNYL]6ALPHA, 9ALPHA-DIFLUORO-17ALPHA-(FURAN-2-YL) CARBONYLOXY-11BETA -HYDROXY-16ALPHA-METHYL-3-OXOANDROSTA-1,4-DIENE-17BETA -CARBOTHIOATE. (Thu, 14 Apr 2016)
The present invention relates to methods of treatment of inflammatory conditions using S -[4-(3-fluoro-3-methylbutyryloxy)-but-2-ynyl]6α,9α-difluoro-17α-(furan-2-yl)carbonyloxy-11β-hydroxy-16α-methyl-3-oxoandrosta-1,4-diene-17β-carbothioate (compound of formula I), a novel anti-inflammatory compound of the androstane series and its processes of preparation.
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Methods for treatment of inflammatory conditions using S-[4-(3-fluoro-3-methylbutyryloxy) but-2-ynyl] 6alpha, 9alpha-difluoro-17alpha-(furan-2-yl) carbonyloxy-11beta -hydroxy-16alpha-methyl-3-oxoandrosta-1,4-diene-17beta -carbothioate. (Fri, 27 Nov 2015)
The present invention relates to methods of treatment of inflammatory conditions using S -[4-(3-fluoro-3-methylbutyryloxy)-but-2-ynyl]6α,9α-difluoro-17α-(furan-2-yl)carbonyloxy-11β-hydroxy-16α-methyl-3-oxoandrosta-1,4-diene-17β-carbothioate (compound of formula I), a novel anti-inflammatory compound of the androstane series and its processes of preparation.
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