PATENTSCOPE: EN_ALL:nmr AND PA:sun pharma

NOVEL ANTIESTROGENIC HETEROCYCLIC COMPOUNDS (Fri, 03 Aug 2018)
The present invention provides novel heterocyclic compounds of Formula I wherein A, B, E, ring Z, Y, L, ring X, D, m, n, R7 and R8 are as defined in the specification as estrogen receptor antagonists/degraders. The compound of Formula I can be used for the treatment of cancers mediated by estrogen receptors. (Formula I ).
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NOVEL HYDRAZIDE CONTAINING COMPOUNDS AS BTK INHIBITORS (Fri, 05 Jan 2018)
The present invention relates to novel hydrazide containing compounds as Bruton tyrosine kinase inhibitors, process of preparation thereof, and to the use of the compounds in the preparation of pharmaceutical compositions for the therapeutic treatment of disorders involving mediation of Bruton tyrosine kinase in humans.
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NOVEL COMPOUNDS AS BTK INHIBITORS (Fri, 06 Oct 2017)
The present invention relates to novel compounds of Formula I as Bruton tyrosine kinase inhibitors, process of preparation thereof, and to the use of the compounds in the preparation of pharmaceutical compositions for the therapeutic treatment of disorders involving mediation of Bruton tyrosine kinase in humans.
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PHOSPHONATE-DRUG CONJUGATES (Fri, 04 Aug 2017)
This invention relates to drug conjugates useful for localized treatment of diseases or disorders of the middle ear and/or inner ear. Methods of treating diseases or disorders of the middle ear and/or inner ear, pharmaceutical compositions comprising the conjugates, and methods of inhibiting a Tropomyosin receptor kinase are also provided.
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TOPICAL FORMULATIONS AND USES THEREOF (Fri, 19 May 2017)
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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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 N-ARYL CONTAINING FUSED HETEROCYCLIC COMPOUNDS (Fri, 07 Apr 2017)
The present invention provides novel N-aryl containing fused heterocyclic compounds as anticancer agents, especially as estrogen receptor (ER) antagonists/ degraders and process for their preparation.
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2-PYRAZINE CARBOXAMIDES AS SPLEEN TYROSINE KINASE INHIBITORS (Fri, 18 Sep 2015)
The invention provides certain pyrazine-2-carboxamide compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A, B, and X are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
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NOVEL INTERMEDIATE OF TAPENTADOL (Fri, 29 May 2015)
The present invention relates to novel carbamate intermediate of formula (II), process for its preparation and process for its conversion into 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol, tapentadol and its pharmaceutically acceptable salts.
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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, 05 Dec 2014)
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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PYRAZOLYL DERIVATIVES AS SYK INHIBITORS (Sat, 28 Dec 2013)
The present invention provides novel pyrazole derivatives of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
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COMPOSITION FOR PROMOTING STEM CELL PROLIFERATION COMPRISING PHLORIDZIN ISOLATED FROM ACANTHOPANAX SENTICOSUS HARMS (ARALIACEAE) EXTRACT (Fri, 29 Nov 2013)
The present invention relates to a composition containing phloridzin as a novel bioactive substance, which composition is applicable to a cell culture composition for promoting cell proliferation and providing a substitute for an animal serum, and a composition for improving skin conditions, such as for alleviating inflammatory skin diseases, improving skin wrinkles, suppressing skin aging, improving skin elasticity, and helping regeneration of wounds or skin.
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NANOPARTICLES COATED WITH AMPHIPHILIC BLOCK COPOLYMERS (Fri, 13 Sep 2013)
Amphiphilic block copolymer coated surfaces and methods of preparing such surfaces. Amphiphilic block copolymer coated single dispersed nanoparticles, which are stable in buffer and have neutral but functionable surfaces, and methods of preparing the same. Methods of producing stable amphiphilic block copolymer coated gold nanoparticles comprising: a) preparing a stable colloidal suspension of gold nanoparticles in an organic solvent by a top-down nanofabrication method using bulk gold as a source material and preparing a solution of amphiphilic block copolymers in the organic solvent; b) mixing the solution of amphiphilic block copolymer with the colloidal suspension of gold nanoparticles, then treating the mixture at elevated temperature, and then cooling the resultant mixture.
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NOVEL PRODRUGS OF PHENOLIC DRUGS (Fri, 28 Jun 2013)
The present invention relates to novel hydrazide group containing carbamate prodrugs of phenolic drugs of formula (I) or pharmaceutically acceptable salt thereof, and process for the preparation thereof.
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QUINOLINE-, QUINOXALINE OR BENZOTHIAZOLE BASED CYSTEINYL LEUKOTRIENE ANTAGONISTS (LTC4) (Fri, 12 Apr 2013)
The present invention relates to novel cysteinyl leukotriene (specifically LTD4) antagonists, mainly to quinolin, quinoxaline or benz[c]thiazole derivatives represented by the general formula (I), or the pharmaceutically acceptable salt thereof, process of preparation thereof, and to the use of the compounds in the preparation of pharmaceutical compositions for the therapeutic treatment of disorders related to cysteinyl leukotriene, in mammals, more specially in humans.
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NANOPARTICLES FOR DELIVERY OF BIOACTIVE AGENTS (Fri, 21 Dec 2012)
Biocompatible polymeric nanoparticles for delivery of bioactive agents, and methods for preparing the particles, are described. Polyoxalate nanoparticles of the subject technology show desired particle sizes suitable for use in drug delivery and a substantially uniform or narrow particle size distribution. The polyoxalate nanoparticles can contain water-soluble, poorly water-soluble, or water-insoluble drugs. The nanoparticles are nontoxic and are generally safe for use in humans. After being administered into the body, the nanoparticles with a high content of a bioactive agent entrapped therein can safely deliver the agent to target sites and stably release the drug at a controlled rate.
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PIPERAZINE DERIVATIVES, COMPOSITIONS, AND USES RELATED THERETO (Fri, 21 Dec 2012)
The disclosure relates to piperazine derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidase.
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TRIPEPTIDES INCORPORATING DEUTERIUM AS INHIBITORS OF HEPATITIS C VIRUS (Fri, 07 Dec 2012)
Hepatitis C virus inhibitors having the general formula (I) [INSERT CHEMICAL STRUCTURE HERE] are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
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SPATIAL SEQUESTRATION OF DYNAMIC NUCLEIC ACID CIRCUITS (Fri, 09 Nov 2012)
The invention provides systems and methods for spatial sequestration of elements in nucleic acid circuits.
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HEPATITIS C VIRUS INHIBITORS (Fri, 09 Nov 2012)
Hepatitis C virus inhibitors having the following general formula (I); are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
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