Abstract: Provided herein are inhibitors of protein arginine deiminases (PADs), pharmaceutical compositions comprising said the compounds, and methods for using the compounds for the treatment of diseases.

Abstract: The present invention relates to processes and intermediates useful for the manufacture of spiroindolone compounds such as (1?R,3?S)-5,7?-dichloro-6?-fluoro-3?-methyl-2?,3?,4?,9?-tetrahydrospiro[indoline-3,1?-pyrido[3,4-b]indol]-2-one and salts and hydrates and solvates thereof.

Abstract: Process for the preparation of sunitinib malate form I via sunitinib acetate and polymorphs of said intermediate.

Abstract: The present invention relates to pure crystalline Form II of an L-malic acid salt of sunitinib and a process for its preparation. The invention further provides crystalline Form II of an L-malic acid salt of sunitinib having a purity of at least 97.0%. The invention also provides crystalline Form II of an L-malic acid salt of sunitinib substantially free of an anti-oxidant. The invention also provides crystalline Form II of L-malic acid salt of sunitinib which remains chemically pure on storage at 25° C.±2° C. and 40° C.±2° C. at a relative humidity of 60%±5% and 75%±5%, respectively, for at least 1 month.

Abstract: The present invention relates to an ascorbic acid salt of sunitinib and a process for its preparation. The present invention further provides a crystalline Form I of an L-ascorbic acid salt of sunitinib.

Abstract: The invention provides compositions and methods for wound healing and scar reduction. The compositions and methods of the invention include at least one EP4 agonist set forth herein. Wounds and or scars that can be treated by the compositions and methods of the invention can arise from events such as surgery, trauma, disease, mechanical injury, burn, radiation, poisoning, and the like.

Abstract: The present invention relates to solid salt forms of the 3-pyrrole substituted 2-indolinone compound 5-[5-fluoro-2-oxo-1, 2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pirrolidin-1-yl-ethyl)-amide. It also relates to polymorphs of the phosphate salt of the amide. The invention further relates to the use of the salts and polymorphs in the treatment of protein kinase related disorders.

Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3) using compounds of formula (I), wherein the substituents are as defined herein.

Abstract: The present invention relates to processes and intermediates useful for the manufacture of spiroindolone compounds such as (1?R,3?S)-5,7?-dichloro-6?-fluoro-3?-methyl-2?,3?,4?,9?-tetrahydrospiro[indoline-3,1?-pyrido[3,4-b]indol]-2-one and salts and hydrates and solvates thereof.

Abstract: The present application relates to new binder-drug conjugates (ADCs) of N,N-dialkylauristatins that are directed against the target C4.4a, to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for treating and/or preventing illnesses, and also to the use of these ADCs for producing medicaments for treating and/or preventing illnesses, more particularly hyperproliferative and/or angiogenic diseases such as, for example, cancer diseases. Such treatments may be practised as a monotherapy or else in combination with other medicaments or further therapeutic measures.

Abstract: The present invention relates to an improved process for the preparation of Sunitinb. The process involves the activation of 5-((Z)-(5-fluoro-2-oxoindolin-3-ylidene) methyl)-2,4-dimethyl-1H-pyrrole-3carboxylic acid to corresponding suitable carboxylic acid activating group. The present invention also relates to novel acid addition salts of Sunitinb and preparation thereof.

Abstract: The present invention provides methods for obtaining specific and non-toxic inhibitors of AID nuclear import. The methods comprise a primary screen and a counter screen to identify a pool of AID specific nuclear import inhibitors that do not have off-target of toxic effects. AID specific nuclear import inhibitors identified by the screens of the invention prevent nuclear entry, limit the access of AID to genomic DNA, and inhibit AID mutagenic activity. Preparations, including pharmaceutical preparations, comprising specific nuclear import inhibitors, used for example, to inhibit cancer progression, are also encompassed in the invention.

Abstract: The present invention provides a succinimide compound represented by the following formula (1-1) or (1-2), and a lubricating oil additive and a lubricating oil composition which contain the succinimide compound. wherein R represents an alkyl group or an alkenyl group having a number-average molecular weight of 500 or greater and less than 5000. wherein R represents an alkyl group or an alkenyl group having a number-average molecular weight of 500 or greater and less than 5000.

Abstract: The present invention relates to stable crystalline Form II of L-malic acid salt of sunitinib and its preparation.

Abstract: Compounds are disclosed that have a formula represented by the following: These compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example inflammatory conditions, infectious diseases, autoimmune diseases, diseases involving impairment of immune cell functions, cardiometabolic diseases, and/or proliferative diseases.

Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

Abstract: Some embodiments include compositions and methods of using or identifying compounds that modulate the activity of the granulocyte colony-stimulating factor receptor (GCFR). Some embodiments include use of compounds to treat certain disorders, such as hematopoietic or neurological disorders.

Abstract: The present invention provides for synthetic processes for the making of substituted 3-((pyrrol-2-yl)methylene)-2-pyrrolones, including sunitinib. The present invention also provides for a process of crystallizing substantially pure sunitinib L-malate.

Abstract: Novel 3,6-disubstituted pyrans, optionally with a further substituent at the 4-position, are monoamine reuptake inhibitors with activity profiles of anti-depressants.

Abstract: The invention provides novel inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, and methods of making such compounds and compositions.

Abstract: Disclosed are dihydroindolone compounds which can modulate the activity of protein tyrosine kinases, a method for preparing the same, and pharmaceutical compositions comprising the same. Also disclosed are use of such compounds and pharmaceutical compositions thereof in the treatment and/or prophylaxis of protein tyrosine kinase associated diseases in an organism, particularly in the treatment and/or prophylaxis of tumors and fibroblast proliferation associated diseases.

Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a benzene ring, a pyridine ring, or the like; Y1 represents a C1-6 alkylene group or the like; Y2 represents a single bond or the like; Z represents —C(?O)—NHSO2R6, an acidic 5-membered hetero ring group, or the like; R1 represents a hydrogen atom or the like; R2 represents a phenyl group, a 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.

Abstract: Provided is a medicinal agent for medical applications, which can act on the function of a target cell specifically. The medicinal agent for medical applications comprises: a cell-incorporated substance that can be incorporated into a target cell specifically; and an acting substance that can act on the function of the target cell and is bound to the cell-incorporated substance.

Abstract: There is provided an actinic ray-sensitive or radiation-sensitive resin composition containing (A) a compound represented by the following formula (1-1); an actinic ray-sensitive or radiation-sensitive film using the composition; and a pattern forming method: in the formula, R1, R2, R3, R4 and Y? are the same as those in formula (1-1) set forth in the description.

Abstract: A process for preparation of eletriptan hydrobromide having ?-form of formula (I) is described that includes reducing 3-((R)-1-methylpyrrolidin-2-yl)methyl)-5-((E)-2-(phenylsulfonyl)vinyl)-1H-indole of formula (II) in presence of a metal catalyst to the product of formula (III) and then converting to hydrobromide salt having ?-form of formula (I).

Abstract: Inhibition of protein kinases having one or more cysteine residues within the ATP binding site is effected by contacting the kinase, per se or in a cell or subject, with an inhibitory-effective amount of a compound having a heterocyclic core structure comprised of two or more fused rings containing at least one nitrogen ring atom, and an electrophilic substituent that is capable of reacting with a cysteine residue within the ATP binding site of a kinase. Preferred compounds include certain pyrrolopyrimidines and oxindoles having such an electrophilic substituent and optionally an aromatic or heteroaromatic substituent that is capable of interacting with a threonine or smaller residue located in the gatekeeper position of the kinase. Kinases lacking such cysteine residues may be engineered or modified so that they are capable of being inhibited by such compounds by replacing a valine or other amino acid residue within the ATP binding site by a cysteine residue.

Abstract: Receptor type oligothiopene compounds, methods of preparing the compounds, and use of the compounds in photoelectric materials.

Abstract: A process for the preparation of a new crystal form of sunitinib malate, along with pharmaceuticals comprising the same are described.

Abstract: Catalysts and methods for the carbonylation of epoxides to substituted 3-hydroxy-?-lactones and ?-lactones are disclosed.

Abstract: The present invention provides a novel indoline derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or a salt thereof represented by the following formula (1) that has an excellent butyrylcholinesterase inhibitory activity. In the formula, R1 represents an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a heteroaryl group, an arylalkyl group, a heteroarylalkyl group, a cycloalkylalkyl group, a heterocycloalkylalkyl group, a dihydrofurylalkyl group, an alkenyl group, a tetrahydronaphthyl group, or an indanyl group; R2 represents a hydrogen atom, an alkyl group, an arylalkyl group, a cycloalkylalkyl group, a heteroarylalkyl group, a heterocycloalkylalkyl group, an aryl group, or an acyl group; R3 each independently represents a hydrogen atom, an alkyl group, or a dialkylaminocarbonyl group; R4 each independently represents a hydrogen atom or an alkyl group; and R5 represents a hydrogen atom or an alkyl group.

Abstract: The present invention provides compounds according to general formula (I) which are proposed for the treatment of respiratory complaints, particularly asthma and COPD.

Abstract: Pharmaceutically acceptable salts of sunitinib, processes of making sunitinib salts, as well as related pharmaceuticals and methods of treating are described.

Abstract: This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).

Abstract: The invention relates to (among other things) polymer-des-ethyl sunitinib conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over des-ethyl sunitinib in unconjugated form.

Abstract: The present invention provides an indole derivative having a melanin-concentrating hormone receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

Abstract: The invention provides fluorescent schweinfurthin analogs of formula (I) which are useful as probes and for the treatment of cancer and other diseases.

Abstract: Provided are pyrrolyl substituted dihydroindol-2-one derivatives represented by formula (I), pharmaceutically acceptable salts or solvates of said derivatives, or solvates of said salts, which are effective tyrosine kinase inhibitors. Also provided are the preparation methods of the above compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in manufacturing drugs useful for the treatment or adjunctive treatment of tumors medicated by tyrosine kinases or proliferation or migration of tumor cells driven by tyrosine kinases in mammals (including human).

Abstract: The present invention relates to a novel process for the preparation of (R)-3-((1-methylpyrrolidin-2-yl)methyl)-5-(2-(phenylsulfonyl)ethyl)-1H-indole and its intermediates thereof.

Abstract: The invention relates to (among other things) polymer-semaxanib moiety conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over the semaxanib moiety in unconjugated form.

Abstract: Disclosed are CCR2 antagonists of Formula (I) or pharmaceutically acceptable thereof, wherein R1, L1 and A are defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compounds, and compositions to treat diseases or disorders associated with CCR2 activity.

Abstract: Process for the preparation of sunitinib malate form I via sunitinib acetate and polymorphs of said intermediate.

Abstract: The invention relates to (among other things) polymer-sunitinib conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over sunitinib in unconjugated form.

Abstract: Disclosed are compositions and methods for treating and/or preventing infections in mammals, by administering to a mammal a therapeutically effective amount of at least one defensin-like molecule, e.g., in a composition that includes such molecule. Also disclosed are kits that include such molecules, or compositions that include such molecules, as well as instructions for using such molecules to treat a mammal.

Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3).

Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a benzene ring, a pyridine ring, or the like; Y1 represents a C1-6 alkylene group or the like; Y2 represents a single bond or the like; Z represents —C(?O)—NHSO2R6, an acidic 5-membered hetero ring group, or the like; R1 represents a hydrogen atom or the like; R2 represents a phenyl group, a 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.

Abstract: Process for the preparation of sunitinib malate form I via sunitinib acetate and polymorphs of said intermediate.

Abstract: The present invention relates to a process for the preparation of statins by means of a Julia-Kocienski reaction between an aldehyde and a sulfone derivative in the presence of an alkaline metal alkoxy base. The resulting derivatives are suitable as building blocks for statin type compounds such as cerivastatin, fluvastatin, pitavastatin and rosuvastatin.

Abstract: Substituted indole derivatives of formula (I) wherein the radicals have e.g. the following meaning: R1 is hydrogen, C1-6-alkyl, R2 is hydrogen, —C1-6-alkyl or cycloC3-12-alkyl; R3 is OR R4 is hydrogen or halogen, R5 is hydrogen, —C1-6-alkyl R6 is hydrogen, —C1-6-alkyl R is hydrogen or —C1-6-alkyl; X is a group —C(O)CH2— or —CH?CH—; R7 is hydrogen are potent inhibitors of Abeta peptide polymerization and can be used for the treatment of e.g. Alzheimers disease or ocular disorders.

Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPB (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less than 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposed are also disclosed.

Abstract: A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer.