566 results about "Indoline" patented technology

The present invention provides compounds of Formula (I):or a stereoisomer or pharmaceutically acceptable salt or hydrate form thereof, wherein the variables A, B, L1, L2, X1, X2, X3, X4 and W are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and / or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and / or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and / or inflammatory disorders using the same.

The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI)wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

In its many embodiments, the present invention provides a novel class of indolines as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.

The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds of the invention. The invention also relates to methods of modulating the function of protein kinases using indolinone compounds of the invention and methods of treating diseases by modulating the function of protein kinases and related signal transduction pathways.

The present invention discloses a novel process and novel intermediates for the Preparation of 4-[2-(di-n-propyl amino) ethyl]-1,3-dihydro-2H-indol-2-one, commonly known as Ropinirole (I) and pharmaceutical composition comprising the same. Further the present invention also discloses a method of treatment for cardiovascular disorders and Parkinson's disease.

Novel isoindoline compounds are disclosed. Methods of treating, preventing and / or managing cancer, diseases and disorders associated with, or characterized by, undesired angiogenesis, and diseases and disorders mediated by PDE 4, using the compounds are also disclosed.

The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI)wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

A crystal for oral solid medicament comprised of indoline compound (KMD-3213) which exerts α1-adrenaline receptor blocking effect, is useful as a therapeutic agent for dysuria and is represented by the formula: (I) wherein in the powder X-ray diffraction pattern, the compound is characterized by main peaks of 5.5°±0.2°, 6.1°±0.2°, 9.8°±0.2°, 11.1°±0.2°, 12.2°±0.2°, 16.4°±0.2°, 19.7°±0.2° and 20.0°±0.2° as 2θ. There is further provided an oral solid medicament for dysuria treatment containing the crystal as an active ingredient.

The invention relates to a method of maleate formation of a silodosin intermediate indoline compound 1 - (3 - (4 - fluoro benzoyl) hydroxypropyl) -5 - ((2R) -2 - (2 - (2 - (2,2,2 - trifluoroethoxyl) phenoxy) ethylamine) propyl) indoline -7 - cyano (compound (1)), i.e., a crude product of the compound (1) forms a salt with maleic acid in a mixed solvent of a good solvent and a poor solvent. The maleate of the compound can be stably obtained by the method, and the method has the advantages of good impurity removal effect, stable process, high yield, simpleness in operation and the like.

The invention provides derivatives of 5-arylsulfonyl indole and 5-arylsulfonyl indoline compounds which may be in the form of pharmaceutical acceptable salts or compositions that are useful in treating central nervous system diseases such as anxiety and depression. The invention also includes intermediates and processes to make the compounds, isotopically-labeled forms of the compounds and the use of the isotopically labeled forms of the compounds to perform nuclear magnetic resonance imaging and positron emission tomography.

The invention relates to a heptamethine cyanine active fluorescent probe and a preparation method and application thereof. The structural formula of the heptamethine cyanine active fluorescent probe is as shown in the specification, wherein X=II-IX; each of R1 and R2 is (CH2)mCH3, (CH2)nOH, (CH2CH2O)pCH3 and CH2C6H5; each of R3 and R4 is H, SO3H, SO3Na and SO3K; each of a, b, c, d, e, f and g is 2-8; each of n, m and p is 1-10. The heptamethine cyanine active fluorescent probe has the advantages that the heptamethine cyanine active fluorescent probe is based on near-infrared long-wave heptamethine cyanine dye, indoline is selected as the aroma parent nucleus to increase fluorescence intensity, and methenyl chain intermediate cyclohexene rigid bridging enhances stability; nitrogen derivatives with chemical reactivity sites are used to perform nucleophilic substitution on the meso-position of the heptamethine cyanine parent dye, and accordingly Stokes shift and active chemical groups areincreased greatly to facilitate the fluorescent labeling of various substances; the fluorescent probe is of a symmetrical structure, preparation and purification processes are simplified, and cost islowered favorably; the probe can be used as the fluorescent labeling probe of biological molecules such as high-sensitivity protein, sugar and DNA and nano carriers to perform cell or living-body horizontal fluorescence imaging, and the like.

The invention discloses a preparation method of a silodosin intermediate, wherein the structure of the silodosin intermediate is represented as the formula A. The preparation method, wherein indoline is employed as a start raw material, includes the reactions of Friedel-Crafts acylation, carbonyl reduction, Gabriel reaction and chiral resolution and the like. The preparation method is simple in operation, is low in cost, is high in yield, allows the product to purify easily and is stable in processes, and is suitable for industrial production. The invention also discloses a new intermediate compound which is related in the method.

3-pyrrolo[b]cyclohexylene-2-dihydro-indolinone derivatives of formula (I) or their pharmaceutically acceptable salts and uses thereof. The intermediates of formula (II) for preparing the above compounds. The bioassay shows that the above compounds and their pharmaceutically acceptable salts can modulate the activity of protein kinases (PKs), inhibit the activity of tyrosine kinases (PTKs) and inhibit many kinds of tumor cells as well as.

The invention provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates and stereoisomers thereof, wherein A, B, E, G, W, X, Y, Z, o, and R1 are as disclosed herein (“Compound(s) of the Invention”), which are useful as cardio-protective and / or neuro-protective agents. The invention also provides pharmaceutical compositions comprising a Compound of the Invention and methods for treating, preventing and / or managing a vascular, cardiovascular or neurological disease or disorder, comprising administering to a patient in need thereof a Compound of the Invention.

The invention relates to compounds of the formula I wherein the variables are as defined in the claims. The compounds are useful in the treatment of a disease where a D4 receptor and / or a 5-HT2A receptor is implicated.

The invention discloses a Fe<3+> molecular fluorescence sensor based on Rhodamine B and a preparation method and application of the Fe<3+> molecular fluorescence sensor. Rhodamine B is taken as a precursor, and a target product N1-(benzene[d] thiazole-2-yl)-N4-(2-(3',6'-bi(diethylin)-3-carbonyl screw[iso-indoline-1,9'-xanthene]-2-yl)ethyl) maleimide is synthesized at two steps. Detection on Fe<3+> by using the target product shows that the target product has a very good detection effect on Fe<3+>; and meanwhile the raw materials of the Fe<3+> molecular fluorescence sensor are easy to obtain, synthesis steps are simple, after-treatment is convenient to implement, and large-scale production can be relatively easily achieved.

In its many embodiments, the present invention provides a novel class of indolines as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.

The invention provides a novel optical active compound 5-[(2R)-2-(benzyl amino) propyl]-1-[3-( benzoyloxy) propyl]-7-cyanogroup indoline and a preparation method of the novel optical active compound. The compound can be used as an intermediate for synthesizing silodosin.

Disclosed are substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compounds, pharmaceutical compositions comprising at least one such 4 substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compound processes for the preparation thereof, and the use thereof for inhibiting BET family of bromodomains and for treating disorders mediated thereby, such as certain cancers.

The invention relates to novel compounds of formula I which are inhibitors of deubiquitylating enzymes (DUBs) and / or desumoylating enzymes. In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 7 or ubiquitin specific peptidase 7 (USP7). The invention further relates to methods for the preparation of these compounds and to their use in the treatment of cancer.

The invention discloses a preparation method and application of a near infrared GSH (glutathione) fluorescent probe. The structural formula of the fluorescent probe is shown as the accompanying drawing. On one hand, the Rhodamine wavelength is increased by 1,3,3-Trimethyl-2-(formylmethylene)indoline, so that the wavelength is prolonged to be 750nm; on the other hand, SH of an analyte and an aldehyde group of the probe take an addition-hydrolysis reaction for realizing GSH, Cys (cysteine) and Hcy(homocysteine) distinguishing. The near infrared GSH fluorescent probe is the first near infrared fluorescent probe which is based on rhodamine derivatives and can efficiently distinguish the GSH, the Cys and the Hcy; the probe shows high sensitivity on the GSH. When the pH value is 6.0 to 8.0, the determination on the GSH by the fluorescent probe is not influenced; the fluorescent probe and the GSH response is fast; the probe cannot be interfered by other biological mercaptan (Cys and Hcy) and other 19 kinds of amino acids; good selectivity is shown. More importantly, the near infrared GSH fluorescent probe can be applied to optical imaging and detection of GSH in cells and tissues.

The invention provides a preparation method of 1-(3-protecting propyl)-5-((2R)-2-(2-(2-(2,2,2-trifluoroethyoxyl)phenoxy)ethylamine)propyl)indoline-7-cyan and 1-(3-(4-flurobenzoyl)hydroxyl propyl)-5-((2R)-2-(2-(2-(2,2,2-trifluoroethyoxyl)phenoxy)ethylamine)propyl)indoline-7-cyan shown as in a specific compound structure (Ia) in the specification. The method is characterized in that water is used as a solvent and the yield is high. The 1-(3-(4-flurobenzoyl)hydroxyl propyl)-5-((2R)-2-(2-(2-(2,2,2-trifluoroethyoxyl)phenoxy)ethylamine)propyl)indoline-7-cyan shown as in the specific compound structure (Ia) can be used as an intermediate to be applied to the preparation of an indoline derivative. The method of the invention is simple in operation and high in yield.

The invention provides an optical active compound of 1-(3-benzoyloxy-propyl)-5-(2-(1-phenyl ethyl amine) propyl-7-cyano indoline as well as a preparation method and the application thereof. The optical active compound is shown in a formula (1), comprises a (R,R) configuration and a (S,S) configuration and can be used as an intermediate for synthetizing silodosin. The optical active compound of the single formula (1) can be used for preparing an optical high-purity product and has good yield on the premise of ensuring good optical purity. The preparation method of the optical active compound uses low-cost chiral assistant agent of alpha-phenethylamine and derivatives thereof, has mild reaction conditions, low cost and controllable optical purity and is easy for industrialized production.

The invention is directed to indole and indoline cyclopropyl amide derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.

This invention relates to 5-substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.