- TOPICAL FORMULATIONS
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Provided herein are gelled topical formulations for the treatment of skin diseases comprising: a) a MEK inhibitor; b) one or more organic solvents in an amount of about 70% to about 99% by weight; and c) a gelling agent; wherein the one or more organic solvents are selected from the group consisting of C2-6 alcohol, a C2-6 alkylene glycol, a di-(C2-6 alkylene) glycol, a polyethylene glycol, C1-3 alkyl-(OCH2CH2)1-5-OH, DMSO, ethyl acetate, acetone, N-methyl pyrrolidone, benzyl alcohol, glycerin, and an oil; the gelling agent is hydroxypropyl cellulose having a molecular weight ranging from about 40,000 Dato about 2,500,000 Da; and wherein the gelled topical formulation has a viscosity of from 1 to 25,000 cps; and DMSO, when present, is combined with at least one other of said organic solvents such that DMSO is present in an amount of less than 50% by weight.
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Paragraph 0726-0727; 0737; 0740
(2020/06/10)
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- ARYL-ANILINE AND HETEROARYL-ANILINE COMPOUNDS FOR TREATMENT OF BIRTHMARKS
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Provided herein are compounds and pharmaceutical compositions thereof for treating a birthmark in a subject in need thereof, wherein the compound is according to any one of formula (1), (II), (III), (IV), and (V). wherein X1, X2, X3, R1, R2, R2a, R13, R13a, R23, R23a, R23b, R33, R33a, R33b, R43, R43a, R51, R53, R53a, R53b, bond "a", and subscript n are described herein.
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Paragraph 0523
(2020/06/10)
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- ARYL-ANILINE AND HETEROARYL-ANILINE COMPOUNDS FOR TREATMENT OF SKIN CANCERS
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Provided herein are compounds and pharmaceutical compositions thereof for treating a skin cancer in a subject in need thereof, wherein the compound is according to any one of formula (I), (II), (III), (IV), and (V): wherein X1, X2, X3, R1, R2, R2a, R13, Rl3a, R23, R23a, R23b, R33, R33a, R33b, R43, R43a, R51, R53, R53a, R53b, bond "a", and subscript n are described herein.
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Paragraph 0538; 0539; 0552
(2020/06/10)
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- SUBSTITUTED BENZOFURAN, BENZOPYRROLE, BENZOTHIOPHENE, AND STRUCTURALLY RELATED COMPLEMENT INHIBITORS
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Disclosed are compounds of formulae I and II, and pharmaceutically acceptable salts and prodrugs thereof, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such a compound, and methods of using the compounds and compositions in the treatment or prevention of a disease or condition characterized by aberrant complement system activity.
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Page/Page column 532
(2019/10/29)
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- Preparation method of 3-pyridylacetic acid hydrochloride
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The invention discloses a preparation method of 3-pyridylacetic acid hydrochloride and belongs to the field of chemistry. A 3-pyridylacetic acid hydrochloride product is prepared from 3-methylpyridine chlorination side product 2-chloro-3-methylpyridine as a raw material through cyanidation, alkaline hydrolysis, hydrogenation reduction and salification. The 3-pyridylacetic acid hydrochloride product has purity of 98.5% or more.
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Paragraph 0021; 0022; 0026; 0027
(2017/02/28)
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- FAK AND FLT3 INHIBITORS
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The use of a compound of the formula (I): (Formula (I)) in the preparation of a medicament for treating Acute Myeloid Leukemia or a disease ameliorated by the inhibition of Flt3, or Flt3 and FAK.
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Page/Page column 141
(2014/03/22)
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- FAK INHIBITORS
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A compound of the formula (I): where R1 or R2 is a cycle amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.
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Page/Page column 138; 139
(2012/09/10)
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- THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS
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A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2- position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment, of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.
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Page/Page column 26
(2009/03/07)
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- THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS
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The invention provides a series of thieno[2,3-b]pyridine derivatives wherein Y represents a linkage of formula C(O) or S(O)2; R1 represents hydrogen, halogen, cyano, nitro, C|-6 alkyl, trifluoromethyl, Ci.6 alkoxy, trifluoromethoxy,
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Page/Page column 25-26
(2009/09/05)
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- THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS
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A series of thieno[2,3-6]pyridine derivatives, attached at the 2-position to a substituted anilino moiety, which are substituted in the 3-position by a carbonyl group linked to a pyrrolidin-1-yl ring which in turn forms part of a heteroatom-containing fus
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Page/Page column 36
(2010/01/12)
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- FUSED HETEROCYCLIC COMPOUND AND USE THEREOF
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The present invention relates to a serotonin 5-HT2C receptor activator containing a compound represented by the formula wherein ring A is a 5- or 6-membered aromatic heterocycle optionally having substituent(s), and ring B is a 7- to 9-membered
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Page/Page column 74
(2009/02/10)
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- Substituted indoles as inhibitors of poly (ADP-ribose) polymerase (PARP)
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The present invention relates to a series of substituted indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5′-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.
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Page/Page column 24
(2010/02/11)
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- Substituted 1,3-Dihydro-2H-pyrrolopyridin-2-ones as Potential Antiinflammatory Agents
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A series of analogues based on the 1,3-dihydro-2H-pyrrolopyridin-2-one ring system have been synthesized and shown to possess oral antiinflammatory activity in both the reverse passive Arthus reaction (RPAR) pleural cavity assay in rats and in the adjuvant-induced arthritic rat model (AAR).Several members of this series additionally exhibit an inhibitory effect on the in vivo production of prostaglandin- and leukotriene-derived products or arachidonic acid metabolism although these compounds exhibit no significant inhibitory activity against the cyclooxygenase and 5-lipoxygenase enzymes in vitro.Structure-activity relationships in this series are discussed.
- Ting, Pauline C.,Kaminski, James J.,Sherlock, Margaret H.,Tom, Wing C.,Lee, Joe F.,et al.
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p. 2697 - 2706
(2007/10/02)
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