Diuretics

A compound having the structure (I) wherein R is selected from the group consisting of 1) and 2), or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.

Treatment of cancers having k-ras mutations

The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.

Harmful organism control agent

The present invention provides a composition for use as a harmful organism control agent comprising as an active ingredient one or more of compounds represented by formula (I) or salts thereof and an agriculturally or zootechnically acceptable carrier. wherein Het represents pyridyl; X represents an oxygen atom; R 1 , R 2 , R 3 , R 7 , R 10a , R 10b , R 11 , and R 12 represent a hydrogen atom; R 4 , R 5 , and R 6 represent a hydrogen atom, hydroxyl, optionally substituted C 1-18 alkylcarbonyloxy, optionally substituted C 1-18 alkylsulfonyloxy, optionally substituted arylcarbonyloxy, C 1-6 alkyloxy-C 1-6 alkyloxy, C 1-6 alkyloxy-C 1-6 alkyloxy-C 1-6 alkyloxy; R 8 represents a hydrogen atom; and R 13a , R 13b , and R 13c represent methyl.

ASENAPINE MALEATE

Aspects of the present application relate to a microcrystalline monoclinic form of asenapine maleate represented by structural Formula (I); processes for its preparation; and pharmaceutically acceptable dosage forms thereof. 112-. (canceled)13. A microcrystalline monoclinic form of asenapine maleate.14. The microcrystalline monoclinic form of asenapine maleate of with a powder X-ray diffraction (PXRD) pattern with peaks located substantially as illustrated by .15. A process for the preparation of the microcrystalline monoclinic form of asenapine maleate of claim 13 , comprising:(a) providing a solution of asenapine maleate in a solvent;(b) optionally, seeding the solution prepared in step (a) with crystals of the monoclinic form; and(c) isolating the monoclinic form of asenapine maleate.16. A process for the preparation of the microcrystalline monoclinic form of asenapine maleate of claim 14 , comprising:(a) providing a solution of asenapine maleate in a solvent;(b) optionally, seeding the solution prepared in step (a) with crystals of the monoclinic form; and(c) isolating the monoclinic form of asenapine maleate.17. A process for the preparation of the microcrystalline monoclinic form of asenapine maleate of claim 13 , comprising:(a) providing a solution of asenapine in a solvent;(b) combining the solution of asenapine obtained in step (a) with a solution of maleic acid in a solvent; and(c) isolating the microcrystalline monoclinic form of asenapine maleate.18. A process for the preparation of the microcrystalline monoclinic form of asenapine maleate of claim 14 , comprising:(a) providing a solution of asenapine in a solvent;(b) combining the solution of asenapine obtained in step (a) with a solution of maleic acid in a solvent; and(c) isolating the microcrystalline monoclinic form of asenapine maleate.19. A process for the preparation of the microcrystalline monoclinic form of asenapine maleate of claim 13 , comprising micronizing a monoclinic form of asenapine ...

NOVEL PROCESS FOR THE PREPARATION OF ASENAPINE

The present invention is directed to novel compounds of formula (I) as well as to the process for their preparation. Novel compounds of formula (I) can be converted into asenapine through an efficient process. The invention also relates to novel intermediates used in this process and their use in the preparation of compounds of formula (I). 2. A compound according to selected from the group consisting of trans-N-(8-Chloro-11-hydroxymethyl-10 claim 1 ,11-dihydro-dibenzo[b claim 1 ,f]oxepin-10-ylmethyl)-formamide claim 1 , trans-N-(2-Chloro-11 -hydroxymethyl-10 claim 1 ,11-dihydro-dibenzo[b claim 1 ,f]oxepin-10-ylmethyl)-formamide claim 1 , trans-(8-Chloro-11-hydroxymethyl-10 claim 1 ,11-dihydro-dibenzo[b claim 1 ,f]oxepin-10-ylmethyl)-carbamic acid benzyl ester claim 1 , trans-(2-Chloro-11-hydroxymethyl-10 claim 1 ,11-dihydro-dibenzo[b claim 1 ,f]oxepin-10-ylmethyl)-carbamic acid benzyl ester claim 1 , trans-(8-Chloro-11-hydroxymethyl-10 claim 1 ,11-dihydro-dibenzo[b claim 1 ,f]oxepin-10-ylmethyl)-carbamic acid ethyl ester claim 1 , trans-(2-Chloro-11-hydroxymethyl-10 claim 1 ,11-dihydro-dibenzo[b claim 1 ,f]oxepin-10-ylmethyl)-carbamic acid ethyl ester claim 1 , or a salt thereof.4. A process according to wherein the formic acid anhydride of formula III is selected from the group consisting of formic acetic anhydride claim 3 , formic propionic anhydride or formic isobutyric anhydride.6. A process according to wherein the reducing agent of step (a) or step (b-i) is a boron hydride or an aluminum hydride.7. A process according to wherein the leaving group is a halogen.8. A process according to wherein steps (b) and (c) are performed in one-pot manner without isolating intermediate compound of formula VI.9. A process for preparing asenapine or a salt of asenapine comprising treating compound of formula I according to with a reducing agent.15. Use of one or more compounds of for the preparation of asenapine or salts thereof.16. Use of compound of formula II prepared ...

PROCESS FOR THE PREPARATION OF OLOPATADINE

A process for the preparation of olopatadine hydrochloride starting from an advanced intermediate. 2. The process of wherein R is n-butyl.3. The process of claim 1 , wherein the obtained olopatadine hydrochloride has an HPLC purity equal or higher than about 99.90% (Area %) and each single impurity lower than about 0.05% (HPLC Area %).4. The process of claim 1 , containing less than about 30 ppm of bromide ion.5. Olopatadine hydrochloride containing less than 300 ppm of bromide ion.6. The olopatadine hydrochloride of claim 5 , containing less than 30 ppm of bromide ion.7. Oloptadine hydrochloride having an HPLC purity equal or higher than about 99.90% (Area %) and each single impurity lower than about 0.05% (HPLC Area %).8. A pharmaceutical composition comprising the olopatadine hydrochloride of .9. A pharmaceutical composition comprising the olopatadine hydrochloride of .10. A method for the treatment of pathologies comprising allergic rhinitis claim 8 , urticaria claim 8 , dermatitis claim 8 , asthma claim 8 , conjunctivitis and/or of their symptoms claim 8 , comprising administering the pharmaceutical composition of .11. A method for the treatment of pathologies comprising allergic rhinitis claim 9 , urticaria claim 9 , dermatitis claim 9 , asthma claim 9 , conjunctivitis and/or of their symptoms claim 9 , comprising administering the pharmaceutical composition of . This is a divisional of application Ser. No. 12/990,442, filed Nov. 18, 2010, which is a 371 of International Application No. PCT/EP2010/053783, filed Mar. 23, 2010, which claims priority to Italian Application No. MI2009A000659, filed Apr. 21, 2009, the disclosures of which are incorporated by reference in their entireties.The present invention relates to a novel process for the preparation of olopatadine hydrochloride.Olopatadine hydrochloride, chemical name dibenz[b,e]oxepin-2-acetic acid, 11-[3-(dimethylamino)propylidene]-6,11-dihydro hydrochloride, (11Z), of formula (I)is a novel antihistamine ...

Crystalline salts of asenapine

Disclosed is asenapine phosphate of formula (I) and its enantiomer (I) which can be used to prepare asenapine maleate. Further disclosed is a monoclinic crystalline form of asenapine maleate.

CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): 130-. (canceled)321. The composition of claim , wherein the additional therapeutic agent is an acetylcholinesterase inhibitor.331. The composition of claim , wherein the acetylcholinesterase inhibitor is donepezil.35. The composition of claim 34 , wherein the additional therapeutic agent is an acetylcholinesterase inhibitor.365. The composition of claim claim 34 , wherein the acetylcholinesterase inhibitor is donepezil.38. The method of claim 37 , wherein the treating is for Alzheimer's Disease.39. The method of claim 38 , wherein the treating is for mood disorder.40. The method of claim 39 , wherein the mood disorder is depression.41. The method of claim 38 , further comprising administration of an acetylcholinesterase inhibitor.42. The method of claim 41 , wherein the acetylcholinesterase inhibitor is donepezil.44. The method of claim 43 , wherein the treating is for Alzheimer's Disease.45. The method of claim 43 , wherein the treating is for mood disorder.46. The method of claim 45 , wherein the mood disorder is depression.47. The method of claim 44 , further comprising administration of an acetylcholinesterase inhibitor.48. The method of claim 47 , wherein the acetylcholinesterase inhibitor is donepezil. The invention is directed to certain chromane, isochromane, and dihydroisobenzofuran derivatives, their salts, pharmaceutical compositions comprising them and their use in therapy of the human body. The compounds of the invention have been found to modulate the metabotropic glutamate receptor 2 (mGluR2), and hence are expected to be useful in the treatment of Alzheimer's Disease and other diseases mediated by the mGuR2 receptor.The metabotropic glutamate receptors are known to contain one or more allosteric sites, which may alter the affinity with which glutamate and other metabotropic glutamate (mGuR) ligands bind to the primary binding ...

PROCESS FOR PRODUCING HERBICIDAL PYRIDAZINONE COMPOUNDS

The present invention provides, inter alia, a process for producing a compound of Formula (I): wherein A, R, R, R, R, Rand Rare as defined herein. The present invention further provides intermediate compounds utilised in said process, and methods for producing said intermediate compounds. 2. A process according to claim 1 , wherein Ris an optionally substituted heteroaryl.3. A process according to claim 1 , wherein Ris an optionally substituted phenyl.4. A process according to claim 1 , wherein Ris phenyl optionally substituted by one or two substituents independently selected from the group consisting of halo claim 1 , C-Calkyl claim 1 , C-Chaloalkyl claim 1 , C-Calkoxy claim 1 , cyano and nitro.5. A process according to claim 1 , wherein Ais CRRand R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare hydrogen.6. A process according to claim 1 , wherein steps (i) claim 1 , (ii) and (iii) are performed in a single operation.9. A process according to claim 1 , wherein Ris 3 claim 1 ,4-dimethoxyphenyl.10. A process according to claim 1 , wherein Ris methyl. The present invention relates to a process for producing herbicidal pyridazinone compounds. Such compounds are known, for example, from WO 2012/136703 and WO2017/178582. As explained therein, such compounds are typically prepared by reacting an acid chloride of the corresponding pyridazinone with cyclohexanedione in the presence of a base to first make an enol ester which is then rearranged to the pyridazinone triketone using a catalytic amount of cyanide source, typically acetone cyanohydrin. This reaction is understood to proceed via an intermediate acyl cyanide as described in, for example, Montes, I. F.; Burger, U. Tetr. Lett. 1996, 37, 1007. However the yields achieved using such a cyanide rearrangement procedure are not ideal for a large scale production and the use of toxic cyanides in commercial manufacturing remains undesirable. Therefore a new, more efficient synthesis method not involving the use of ...

Bicyclic and Tricyclic Pyrimidine Tyrosine Kinase Inhibitors with Antitubulin Activity and Methods of Treating A Patient

Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed. 3. A pharmaceutical composition according to comprising at least one pharmaceutically acceptable carrier.6. A pharmaceutical composition according to comprising at least one pharmaceutically acceptable carrier.9. A pharmaceutical composition according to comprising at least one pharmaceutically acceptable carrier. This divisional utility patent application claims the benefit of co-pending U.S. patent application Ser. No. 16/460,631, filed Jul. 2, 2019, which is a divisional application and claims the benefit of U.S. patent application Ser. No. 15/659,155, filed Jul. 25, 2017, now U.S. Pat. No. 10,385,064, granted Aug. 20, 2019, which is a divisional application and claims the benefit of U.S. patent application Ser. No. 14/859,854, filed Sep. 21, 2015, now U.S. Pat. No. 9,732,090, granted Aug. 15, 2017, which is a divisional patent application and claims the benefit of U.S. patent application Ser. No. 13/364,930, filed on Feb. 2, 2012, now U.S. Pat. No. 9,139,590, granted Sep. 22, 2015, which claims the benefit of U.S. Provisional Patent Application Ser. No. 61/439,470, filed Feb. 4, 2011 (expired). The entire contents of U.S. patent application Ser. Nos. 16/460,631, 15/659,155, 14/859,854, and 13/364,930, and U.S. Provisional Patent Application Ser. No. 61/439,470 are incorporated by reference into this divisional utility patent application.The present invention relates to bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with ...

COMPOUND FOR ORGANIC ELECTRONIC ELEMENT, ORGANIC ELECTRONIC ELEMENT USING SAME, AND ELECTRONIC DEVICE THEREFOR

The present disclosure provides: a compound capable of providing high light-emitting efficiency, low driving voltage, and improved lifetime of a device; an organic electronic element using the same; and an electronic device therefor. 4. An organic electric element comprising:a first electrode;a second electrode; andan organic material layer positioned between the first electrode and the second electrode,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein the organic material layer contains the compound of .'}5. The organic electric element of claim 4 , wherein the compound is contained in at least one layer of a hole injection layer claim 4 , a hole transport layer claim 4 , a light emitting auxiliary layer claim 4 , a light emitting layer claim 4 , an electron auxiliary layer claim 4 , an electron transport layer claim 4 , and an electron injection layer of the organic material layer claim 4 , and the compound is contained as a single kind of compound alone or a mixture of two or more kinds of compounds.6. The organic electric element of claim 4 , wherein the compound is used for a hole injection layer or a light emitting auxiliary layer.7. The organic electric element of claim 4 , further comprising a light efficiency improving layer formed on one surface of at least one of the first and second electrodes claim 4 , the surface being the opposite side to the organic material layer.8. The organic electric element of claim 5 , wherein the organic material layer is formed by a spin coating process claim 5 , a nozzle printing process claim 5 , an inkjet printing process claim 5 , a slot coating process claim 5 , a dip coating process claim 5 , or a roll-to-roll process.9. An electronic device comprising:{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'a display device comprising the organic electric element of ; and'}a controller for driving the display device.10. The electronic device of claim 9 , wherein the organic electric element is one of an organic ...

Aromatic heterocyclic compound, manufacturing method thereof, organic semiconductor material, and organic semiconductor device

Provided are an organic semiconductor material having a high charge mobility, oxidation stability, and solvent solubility, an organic semiconductor device using the same, and a novel aromatic heterocyclic compound to be used for the same and a production method therefor. The aromatic heterocyclic compound is represented by the following general formula (1), has two heteroatoms, and has a structure in which six rings are fused. In the formula, X represents an oxygen atom or N—R, and R represents hydrogen or a monovalent substituent. The organic semiconductor material contains the aromatic heterocyclic compound, and is used for an organic semiconductor film or an organic device, such as an organic thin-film transistor or an organic photovoltaic device.

BENZIMIDAZOLE DERIVATIVES AS ERBB TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CANCER

Provided herein are benzimidazole derivatives, for example, of Formula (I), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease. 232-. (canceled)33. The compound of claim 1 , wherein Ris —C(O)CH═CHCR claim 1 , wherein Ris hydrogen claim 1 , demethylaminomethyl claim 1 , pyrrolidin-1-ylmethyl claim 1 , or piperidin-1-ylmethyl.3536-. (canceled)37. The compound of claim 1 , wherein Ris Caryl claim 1 , heteroaryl claim 1 , or heterocyclyl claim 1 , each of which is optionally substituted with one or more substituents Q.38. The compound of claim 37 , wherein Ris 6- to 10-membered monocyclic or bicyclic aryl claim 37 , optionally substituted with one or more substituents Q.39. The compound of claim 37 , wherein Ris 5- to 10-membered monocyclic or bicyclic heteroaryl comprising 1 to 4 heteroatoms selected from N claim 37 , O claim 37 , and S claim 37 , optionally substituted with one or more substituents Q.40. (canceled)41. The compound of claim 37 , wherein Ris phenyl claim 37 , pyridinyl claim 37 , pyridazinyl claim 37 , benzo[c][1 claim 37 ,2 claim 37 ,5]oxodiazolyl claim 37 , or benzo[c][1 claim 37 ,2 claim 37 ,5]thiodiazolyl claim 37 , each of which is optionally substituted with one or more substituents Q.42. The compound of claim 1 , wherein Ris hydrogen.43. The compound of claim 1 , wherein Rand Rare linked together to form heterocyclyl claim 1 , optionally substituted with one or more substituents Q.45. The compound of claim 1 , wherein Ris hydrogen.46. The compound of claim 1 , wherein Ris chloro claim 1 , methyl claim 1 , or methoxy.47. The compound of claim 1 , wherein Rand Rare linked together to form heterocyclyl claim 1 , optionally substituted with one or more substituents Q.49. The compound of claim 1 , wherein Ris hydrogen.5051-. (canceled)5355-. (canceled)57. A pharmaceutical composition comprising the compound of claim 1 , and a ...

Composition for organic optoelectronic device, organic optoelectronic device and display device

A composition for an organic optoelectronic device, an organic optoelectronic device including the same, and a display device, the composition including a first compound represented by a combination of Chemical Formula 1 and Chemical Formula 2, and a second compound represented by a combination of Chemical Formula 3 and Chemical Formula 4:

COMPOUND OF EOC315 MOD.I CRYSTAL FORM AND PREPARATION METHOD THEREOF

The present application relates to a crystalline form of 4-(4-chloroanilino)-7-(2-methylaminocarbonyl-4-oxymethyl)pyridylfuro[2,3-d]pyridazine mesylate (EOC315) that contains crystalline form Mod. I. The present application also relates to a process for the preparation of the crystalline form and the pharmaceutical use of the crystalline form. 2. The crystalline form of claim 1 , wherein said crystalline form Mod. I has an X-ray powder diffraction diagram substantially the same as the X-ray powder diffraction diagram shown in when analyzed with the X-ray powder diffraction using CuKα radiation.3. The crystalline form of claim 1 , wherein said crystalline form Mod. I has absorption peaks at 3415 cm±2 cm claim 1 , 3058 cm±2 cm claim 1 , 2805 cm±2 cm claim 1 , 1668 cm±2 cm claim 1 , 1652 cm±2 cm claim 1 , and 1227 cm ±2 cm claim 1 , when analyzed with an infrared spectroscopy using KBr pellet.4. The crystalline form of claim 1 , wherein said crystalline form Mod. I has an infrared spectrum substantially the same as the infrared spectrum shown in .5. The crystalline form of claim 1 , wherein said crystalline form Mod. I has a melting point of about 200.6° C.6. The crystalline form of claim 1 , wherein said crystalline form Mod. I has a differential scanning calorimetry thermogram that is substantially the same as that shown in .7. A process for preparing the crystalline form of claim 1 , the process comprising:crystallizing a compound of Formula I from a solvent selected from the group consisting of methanol, ethanol, isopropanol, butanol, hexane, heptane, acetone, ethyl propyl ether, tetrahydrofuran, toluene, ethyl acetate, acetonitrile, and a mixture thereof.8. The process of claim 7 , wherein said solvent is selected from the group consisting of methanol claim 7 , ethanol claim 7 , isopropanol claim 7 , butanol claim 7 , and a mixture thereof.9. The process of claim 7 , comprising:a) dissolving the compound of Formula I in said solvent to obtain a solution of the ...

2-(aryl- or heteroaryl-)phenyl (aza)benzofuran compounds for the treatment of hepatitis c

Compounds of Formula I, including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV: formula (I).

BICYCLIC AND TRICYCLIC PYRIMIDINE TYROSINE KINASE INHIBITORS WITH ANTITUBULIN ACTIVITY AND METHODS OF TREATING A PATIENT

Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed. 17-. (canceled)10. The pharmaceutical composition according to comprising at least one pharmaceutically acceptable carrier.12. The method of wherein said disease is at least one selected from the group consisting of cancer claim 11 , macular degeneration claim 11 , and arthritis.13127-. (canceled)130. The pharmaceutical composition according to comprising at least one pharmaceutically acceptable carrier.132. The method of wherein said disease is at least one selected from the group consisting of cancer claim 131 , macular degeneration claim 131 , and arthritis.133145-. (canceled) This divisional utility patent application claims the benefit of co-pending U.S. patent application Ser. No. 14/859,854, filed on Sep. 21, 2015, which claims the benefit of U.S. patent application Ser. No. 13/364,930, filed on Feb. 2, 2012 (now U.S. Pat. No. 9,139,590), which claims the benefit of U.S. Provisional Patent Application Ser. No. 61/439,470, filed Feb. 4, 2011. The entire contents of U.S. patent application Ser. No. 14/859,854, U.S. patent application Ser. No. 13/364,930 and U.S. Provisional Patent Application Ser. No. 61/439,470 are incorporated by reference into this divisional utility patent application.The present invention relates to bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity. The compositions of this invention have dual activity of potent vascular endothelial growth factor receptor inhibitory activity ...

CRYSTAL FORM OF ACID ADDITION SALT OF FUROPYRIMIDINE COMPOUND

Provided are crystalline forms of acid addition salts of N-(3-(2-(4-(4-methylpiperazin-1-yl)phenylamino)furo[3,2-d]pyrimidin-4-yloxy)phenyl)acrylamide, and a pharmaceutical composition including the same. The crystalline forms may be easily used in preparing the pharmaceutical composition including the same as an active ingredient. 2. The crystalline form of claim 1 , wherein the acid addition salt is a hydrochloride.3. The crystalline form of claim 2 , wherein the crystalline form is a crystalline form of dihydrochloride trihydrate (2HCl.3HO) of the compound of Formula 1 and has an X-ray powder diffraction (XRPD) spectrum comprising peaks at diffraction angles (2θ±0.2°) of 6.4° claim 2 , 7.1° claim 2 , 11.1° claim 2 , 12.8° claim 2 , and 21.2° claim 2 , when irradiated with a Cu-Kα light source.4. The crystalline form of claim 2 , wherein the crystalline form is a crystalline form of monohydrochloride dihydrate (1HCl.2HO) of the compound of Formula 1 and has an X-ray powder diffraction (XRPD) spectrum comprising peaks at diffraction angles (2θ±0.2°) of 7.0° claim 2 , 7.9° claim 2 , 15.8° claim 2 , 17.2° claim 2 , 18.6° claim 2 , 20.6° claim 2 , 21.3° claim 2 , and 23.2° claim 2 , when irradiated with a Cu-Kα light source.5. The crystalline form of claim 2 , wherein the crystalline form is a crystalline form of monohydrochloride anhydrous (1HCl) of the compound of Formula 1 and has an X-ray powder diffraction (XRPD) spectrum comprising peaks at diffraction angles (2θ±0.2°) of 4.9° claim 2 , 14.8° claim 2 , and 21.2° claim 2 , when irradiated with a Cu-Kα light source.6. The crystalline form of claim 1 , wherein the acid addition salt is a sulfonate.7. The crystalline form of claim 6 , wherein the sulfonate is methanesulfonate.8. The crystalline form of claim 7 , wherein the crystalline form is a crystalline form of methanesulfonic anhydride (1MsOH) of the compound of Formula 1 and has an X-ray powder diffraction (XRPD) spectrum comprising peaks at diffraction angles ...

Compound of eoc315 mod.i crystal form and preparation method thereof

The present application relates to a crystalline form of 4-(4-chloroanilino)-7-(2-methylaminocarbonyl-4-oxymethyl)pyridylfuro[2,3-d]pyridazine mesylate (EOC315) that contains crystalline form Mod. I. The present application also relates to a process for the preparation of the crystalline form and the pharmaceutical use of the crystalline form.

BENZIMIDAZOLE DERIVATIVES AS ERBB TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CANCER

Provided herein are benzimidazole derivatives, for example, or Formula (I), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease. 131-. (canceled)3335.-. (canceled)3732. The compound of , wherein Ris Caryl , heteroaryl , or heterocyclyl , each of which is optionally substituted with one or more substituents Q.38. The compound of claim 37 , wherein Ris 6- to 10-membered monocyclic or bicyclic aryl claim 37 , optionally substituted with one or more substituents Q.39. The compound of claim 37 , wherein Ris 5- to 10-membered monocyclic or bicyclic heteroaryl comprising 1 to 4 heteroatoms selected from N claim 37 , O claim 37 , and S claim 37 , optionally substituted with one or more substituents Q.40. The compound of claim 37 , wherein Ris 5- to 10-membered monocyclic or bicyclic heterocyclic comprising 1 to 4 heteroatoms selected from N claim 37 , O claim 37 , and S claim 37 , optionally substituted with one or more substituents Q.41. The compound of claim 37 , wherein Ris phenyl claim 37 , pyridinyl claim 37 , pyridazinyl claim 37 , benzo[c][1 claim 37 ,2 claim 37 ,5]oxodiazolyl claim 37 , or benzo[c][1 claim 37 ,2 claim 37 ,5]thiodiazolyl claim 37 , each of which is optionally substituted with one or more substituents Q.42. The compound of claim 41 , wherein Ris hydrogen.43. The compound of claim 42 , wherein Rand Rare linked together to form heterocyclyl claim 42 , optionally substituted with one or more substituents Q.45. The compound of claim 44 , wherein Ris hydrogen.46. The compound of claim 44 , wherein Ris chloro claim 44 , methyl claim 44 , or methoxy.47. The compound of claim 42 , wherein Rand Rare linked together to form heterocyclyl claim 42 , optionally substituted with one or more substituents Q.49. The compound of claim 48 , wherein Ris hydrogen.5051-. (canceled)5355.-. (canceled)57. A pharmaceutical composition comprising the ...

AZIRIDINE SPINOSYN DERIVATIVES AND METHODS OF MAKING

Compositions including derivatives of spinosyns and methods for the production of derivatives of spinosyns are provided. The spinosyn derivatives described herein include those functionalized on the C-5,6 double bond to provide an aziridine ring system. The method produces spinosyn derivatives that exhibit activity towards insects, arachnids, and nematodes and are useful in the agricultural and animal health markets. 2. The spinosyn compound of claim 1 , wherein when Xand Xare selected from NR claim 1 , CR claim 1 , and CR claim 1 , the R groups of Xand Xcombine to form a substituted or unsubstituted cycloalkyl claim 1 , substituted or unsubstituted cycloalkenyl claim 1 , substituted or unsubstituted heterocycloalkyl claim 1 , substituted or unsubstituted heterocycloalkenyl claim 1 , substituted or unsubstituted aryl claim 1 , and substituted or unsubstituted heteroaryl.3. The spinosyn compound of claim 1 , wherein when Xand Xare selected from NR claim 1 , CR claim 1 , and CR claim 1 , the R groups of Xand Xcombine to form a substituted or unsubstituted cycloalkyl claim 1 , substituted or unsubstituted cycloalkenyl claim 1 , substituted or unsubstituted heterocycloalkyl claim 1 , substituted or unsubstituted heterocycloalkenyl claim 1 , substituted or unsubstituted aryl claim 1 , and substituted or unsubstituted heteroaryl.4. The spinosyn compound of claim 1 , wherein A comprises forosamine.5. The spinosyn compound of claim 1 , wherein B comprises rhamnose or a (2R claim 1 ,5S)-5-ethoxy-3 claim 1 ,4-dimethoxy-6-methyloxy group.6. The spinosyn compound of claim 1 , wherein A is forosamine claim 1 , B is rhamnose claim 1 , C is O claim 1 , Xis N claim 1 , Xis C(CH) claim 1 , and Xis S.7. The spinosyn compound of claim 1 , wherein the spinosyn compound is (1S claim 1 ,2R claim 1 ,8R claim 1 ,10S claim 1 ,12S claim 1 ,13R claim 1 ,17R claim 1 ,18S claim 1 ,22S)-18-{[(2R claim 1 ,5S claim 1 ,6R)-5-(dimethylamino)-6-methyloxan-2-yl]oxy}-22-ethyl-5 claim 1 ,17-dimethyl-10 ...

BENZIMIDAZOLE DERIVATIVES AS ERBB TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CANCER

Provided herein are benzimidazole derivatives, for example, of Formula (I), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease. 2. The compound of claim 1 , wherein T is —N═.3. The compound of claim 1 , wherein T is —C(R)═.4. The compound of any one of to claim 1 , wherein U is —N═.5. The compound of any one of to claim 1 , wherein U is —C(R)═.6. The compound of any one of to claim 1 , wherein V is —N═.7. The compound of any one of to claim 1 , wherein V is —C(R)═.8. The compound of any one of to claim 1 , wherein W is —N═.9. The compound of any one of to claim 1 , wherein W is —C(R)═.10. The compound of any one of to claim 1 , wherein X is N.11. The compound of any one of to claim 1 , wherein X is C.12. The compound of any one of to claim 1 , wherein Y is N.13. The compound of any one of to claim 1 , wherein Y is C.16. The compound of any one of to claim 1 , wherein Lis a bond claim 1 , —O— claim 1 , —N(R)— claim 1 , or —C(RR)—.17. The compound of claim 16 , wherein Lis a bond.18. The compound of claim 16 , wherein Lis —O—.19. The compound of claim 16 , wherein Lis NH or CH.20. The compound of any one of to claim 16 , wherein Lis Ccycloalkylene claim 16 , heteroarylene claim 16 , or heterocyclylene claim 16 , each of which is optionally substituted with one or more substituents Q.21. The compound of claim 20 , wherein Lis heteroarylene or heterocyclylene claim 20 , each of which is optionally substituted with one or more substituents Q.26. The compound of any one of to claim 20 , wherein r is 0.37. The compound of any one of to claim 20 , wherein Ris Caryl claim 20 , heteroaryl claim 20 , or heterocyclyl claim 20 , each of which is optionally substituted with one or more substituents Q.38. The compound of claim 37 , wherein Ris 6- to 10-membered monocyclic or bicyclic aryl claim 37 , optionally substituted with one or more substituents Q.39. ...

Method for preparing intermediate of 6-arylaminopyridonecarboxamide compound as mek inhibitor

Provided is a method for preparing an intermediate of 6-arylaminopyridonecarboxamide compound as an MEK inhibitor, comprising preparing a compound of formula (III) as an intermediate of 6-arylaminopyridonecarboxamide compound using a compound of formula V as a raw material.

Heterocyclic compounds as anti-viral agents

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:which inhibit Respiratory Syncytial Virus (RSV) or HMPV. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV or HMPV infection. The invention also relates to methods of treating an RSV or HMPV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

PROCESS FOR THE PREPARATION OF PHARMACEUTICAL INTERMEDIATES

Process for the preparation of intermediates that are useful in the synthesis of active pharmaceutical ingredients (API), in particular active in the central nervous system. 2. (canceled)3. The process according to wherein the catalytic amount of FeClis between about 2% and 8% molar.4. The process according to claim 1 , wherein the reaction is carried out in a solvent in an amount of two or three mL of solvent per g of compound.5. The process according to claim 4 , wherein the solvent is an apolar aprotic organic solvent having a boiling point between about 50° C. and about 150° C.6. The process according to claim 4 , wherein the solvent is selected from the group consisting of a straight or branched C-Calkane claim 4 , a cyclic C-Chydrocarbon claim 4 , an aromatic hydrocarbon and a mixture of two or more of them.7. The process according to claim 1 , wherein the reaction is carried out without the use of any solvent.8. The process according to wherein the reaction is carried out in a range of temperature between about 0° C. and the reflux temperature of the reaction mixture.9. The process according to claim 8 , wherein claim 8 , when in the compound of formula (II) X is O claim 8 , the reaction is carried out at a temperature between about 0° C. and 40° C.; and claim 8 , when in the compound of formula (II) X is S claim 8 , the reaction is carried out at a temperature between about 60° C. and the reflux temperature of the reaction mixture.12. The process of wherein the conversion of the compound of formula (I) into Doxepin or Dothiepin claim 11 , wherein X is O or S respectively claim 11 , further comprises treating the compound of formula (I) with 3-dimethylaminopropyl magnesium chloride and subsequent treatment with an acid.13. The process according to claim 6 , wherein the solvent is selected from the group consisting of heptane claim 6 , cyclohexane claim 6 , toluene and mixtures thereof.14. The process according to claim 7 , wherein the reaction is carried out ...

A PROCESS FOR THE PREPARATION OF OLOPATADINE AND SYLIL INTERMEDIATES THEREOF

The present invention refers to a new “one-pot” process for the preparation of olopatadine via intermediates of formula (III). 2. The process according to claim 1 , wherein the Wittig reaction is carried out using 3-dimethylaminopropyltriphenylphosphonium bromide hydrobromide and a strong base.5. The process according to claim 1 , wherein said aprotic solvent is an ether.6. The process according to claim 5 , wherein said ether is selected from tetrahydrofuran (THF) claim 5 , dioxane claim 5 , dimethoxyethane and mixtures thereof.7. The process according to claim 1 , wherein said strong base is sodium hydride.8. The process according to claim 11 , wherein in phase (i) hydrochloric acid is added and olopatadine hydrochloride is isolated.9. The process according to claim 2 , wherein R is a hydrogen atom and said silylating agent is N claim 2 ,O-bis(trimethyl-silyl)acetamide.10. The process according to wherein said solvent of step (i) is 2-methyl-THF and 2-propanol.11. The process according to claim 2 , wherein the ratio between compound (II) or (II′)/3-dimethylaminopropyltriphenylphosphonium bromide hydrobromide/strong base is about 1/2.5/8.12. The process according to claim 2 , wherein claim 2 , after the protecting group cleaving steps (c) and (h) claim 2 , an extraction with organic solvents is performed claim 2 , and then acid is added to remove the possible impurities and reaction byproducts. The present invention refers to a new “one-pot” process for the preparation of olopatadine and salts thereof, and a reaction intermediate.Olopatadine is the international non-proprietary name of {(11Z)-11-[3-(dimethylamino)propylidene]-6,11-dihydrodibenzo[b,e]oxepin-2-yl}acetic acid, having the following formula (I)and is usually employed as an antihistaminic and is, at present, commercialized to treat eye disorders associated with allergies and allergic conjunctivitis or to treat hives and dermatitis as well.Several syntheses of olopatadine are known. Such syntheses often ...

CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): 3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein{'sup': '2', 'sub': 3', '3', '2', '2', '2', '3', '3', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '3', '2', '2', '2', '3', '2', '3', '2', '3, 'Ris selected from H, cyclopropyl, —CH, —CH(CH), —CH—OH, —CH—OCH, —CF, —CHCHF, —CHCHF, —CHCF, —CH—O—CHF, —CH—O—CHF, —CH(CH)—O—CHF, —CH(CH)—O—CHF, —CH—NH—CHCF, and —CH—N(CH)—CHCF;'}{'sup': '2A', 'Ris selected from H and methyl;'}{'sup': '3', 'Ris selected from H and methyl; and'}{'sup': '3A', 'Ris selected from H and methyl.'}4. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein{'sup': 2', '2A, 'Rand Rare both methyl; and'}{'sup': 3', '3A, 'Rand Rare both H.'}8. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein:ring B is a moiety selected from the group consisting of phenyl, cyclopentyl, cyclohexyl, pyridinyl, pyrimidinyl, pyrazolyl, thienyl, thiazolyl, thiadiazolyl, isoxazolyl, oxadiazolyl and oxazolyl;n is 0, 1, 2, or 3, provided that the value of n does not exceed the maximum number of substitutable hydrogen atoms on ring B; and{'sup': '1', 'sub': 1', '6', '1', '6', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6, 'each R(when present) is independently selected from the group consisting of halogen, —CN, —OH, —(C-C) alkyl, —O—(C-C) alkyl, —(C-C) haloalkyl, —O—(C-C) haloalkyl, cyclopropyl, cyclobutyl, —NH, —NH(C-C)alkyl, —N(C-Calkyl), —C(O)O(C-C) alkyl, and phenyl.'}9. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein:ring B is a moiety selected from the group consisting of: phenyl, pyrazolyl, pyridinyl, thienyl, isoxazolyl, oxadiazolyl and oxazolyl;n is 0, 1, or 2; and{'sup': '1', 'sub': 3', '2, 'each R(when present) is independently selected from the group consisting of ...

A PROCESS FOR THE SYNTHESIS OF OLOPATADINE

The present invention provides a process for the synthesis of olopatadine. Further, the invention discloses a process that results in improved yield of the desired Z isomer. 2. The process according to claim 1 , wherein alcohol used in step (a) is methanol.3. The process according to claim 1 , wherein solvent used in step (b) is dimethyl formamide (DMF). This invention relates to a process for the synthesis of olopatadine. Particularly the invention relates to a process that results in improved yield of the desired Z isomer.Olopatadine is an antihistaminic drug, used for the treatment of ocular symptoms of seasonal allergic conjunctivitis. Olopatadine was developed by Kyowa Hakko Kirin Co. Ltd. and produced commercially by the synthetic route using Wittig reaction as key step. Although both olopatadine Z and E isomers show similar HR affinities, only the Z isomer is the marketed drug. Because of antiallergic activity many chemists are involved developing a better process for Z-isomer of olopatadine ().Several literature reports are available for process of synthesis of olopatadine. In most of the processes, the side chains was introduced by ‘Grignard reaction’ or by ‘Wittig reaction’, refer WO 2011/033532, US 2007/105234 and WO 2010/0121877, US 20120016138 respectively. In previous approaches the main drawback was the Z/E stereoselectivity. These references describe the usage of Grignard and/or Wittig reactions which necessitates the usage of dry solvents and the reactions to be performed at low temperatures and make use of hazardous reagents like n-butyl lithium, hexyl lithium, sodium hydride etc. and Grignard reagents which are difficult to perform on an industrial scale with lot of risk elements incorporated in them and hence are not desirous. In addition excess of reagents are required and the process is very long making it expensive.References may be made to journal entitled “A New Efficient Synthetic Route for the Synthesis of the Antiallergic Drug, ...

Inhibitors of hif prolyl hydroxylase

The present invention concerns compounds of formula I or a pharmaceutically acceptable salt thereof which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.

OPIOID RECEPTOR ANTAGONIST PRODRUGS

Provided herein are prodrugs of opioid receptor antagonists such as nalmefene and naltrexone, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of behavioral disorders. 2. A compound , or pharmaceutically acceptable salt thereof , wherein the compound is (((4aS ,7aS ,12bS)-3-(cyclopropylmethyl)-4a-hydroxy-7-methylene-2 ,3 ,4 ,4a ,5 ,6 ,7 ,7a-octahydro-1H-4 ,12-methanobenzofuro[3 ,2-e]isoquinolin-9-yl)oxy)methyl ((E)-octadec-9-en-1-yl) carbonate.3. A compound , or pharmaceutically acceptable salt thereof , wherein the compound is (((4aS ,7aR ,12bS)-3-(cyclopropylmethyl)-4a-hydroxy-7-oxo-2 ,3 ,4 ,4a ,5 ,6 ,7 ,7a-octahydro-1H-4 ,12-methanobenzofuro[3 ,2-e]isoquinolin-9-yl)oxy)methyl ((E)-octadec-9-en-1-yl) carbonate.4. A pharmaceutical composition comprising a compound of claim 1 , or pharmaceutically acceptable salt thereof claim 1 , and at least one pharmaceutically acceptable excipient.5. The pharmaceutical composition of claim 4 , wherein the pharmaceutically acceptable excipient is cottonseed oil.6. The pharmaceutical composition of claim 4 , wherein the pharmaceutically acceptable excipient is sesame oil.7. A pharmaceutical composition comprising a compound of claim 2 , or pharmaceutically acceptable salt thereof claim 2 , and at least one pharmaceutically acceptable excipient.8. The pharmaceutical composition of claim 7 , wherein the pharmaceutically acceptable excipient is cottonseed oil.9. The pharmaceutical composition of claim 7 , wherein the pharmaceutically acceptable excipient is sesame oil.10. A pharmaceutical composition comprising a compound of claim 3 , or pharmaceutically acceptable salt thereof claim 3 , and at least one pharmaceutically acceptable excipient.11. The pharmaceutical composition of claim 10 , wherein the pharmaceutically acceptable excipient is cottonseed oil.12. The pharmaceutical composition of claim 10 , wherein the pharmaceutically acceptable excipient is sesame oil. This ...

Monoclinic crystalline form of asenapine maleate with a specific particle size distribution

A monoclinic crystalline form of asenapine maleate is described, which is characterized in that it is not micronised and has a particle size distribution characterized by a d90 of 40 μm or less. A process for the preparation of a monoclinic crystalline form of asenapine maleate is also described, the process comprising the following steps: a) providing a mixture of monoclinic asenapine maleate and an organic solvent which, under the conditions of the process, acts as an antisolvent; b) stirring the mixture at a temperature between 15 and 60° C.; and c) collecting the crystals, wherein the organic solvent is selected from alcohols, ketones, ethers, esters, hydrocarbons or mixtures thereof.

COMPOSITIONS AND METHODS FOR THE TREATMENT OF MUCOSITIS

The invention relates to the compounds of formula I, formula II, formula III, formula IV, formula V, formula VI, formula VII and formula VIII, or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV, formula V, formula VI, formula VII and formula VIII, and methods for the treatment of mucositis may be formulated for oral, mouth wash, buccal, rectal, topical, transdermal, transmucosal, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of oral and gastrointestinal mucositis, mucosal inflammatory and oral infectious diseases.

Compounds Useful in HIV Therapy

The invention relates to compounds of Formula (I), (II) or (III), salts thereof, pharmaceutical compositions thereof, as well as therapeutic methods of treatment and prevention.

METHYLENEDIOXYBENZO PHENANTHRIDINE DERIVATIVES USED TO TREAT CANCER

The invention provides compounds of formula I: 2. The compound of wherein A is —C(O)NH(CRR)CRRNRRand B is H.3. The compound of wherein B is —C(O)NH(CRR)CRRNRRand A is H.4. The compound of wherein n is 1.5. The compound of wherein each CRRis CH.6. The compound of wherein X is —OCHand Y is —OR.7. The compound of wherein Y is —OCHand X is —OR.8. The compound of wherein Ris —C(O)R claim 6 , —C(O)ORor —C(O)NRR.9. The compound of wherein Rand Rare (C-C)alkyl.10. The compound of wherein Rand Rare each independently H or (C-C)alkyl.11. The compound of wherein Ris CH.12. A composition comprising a compound as described in or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable excipient claim 1 , diluent or carrier.13. A method for modulating topoisomerase activity in a mammal in need of such treatment comprising administering to the mammal claim 1 , an amount of a compound as described in or a pharmaceutically acceptable salt thereof claim 1 , effective to provide a topoisomerase modulating effect.14. A method comprising inhibiting cancer cell growth by contacting the cancer cell in vitro or in vivo with an amount of a compound as described in or a salt thereof claim 1 , effective to inhibit the growth of said cancer cell.15. A therapeutic method for treating cancer in a mammal comprising claim 1 , administering to the mammal an effective amount of a compound as described in or a pharmaceutically acceptable salt thereof. This application is a Continuation of U.S. application Ser. No. 13/255,081, filed Sep. 6, 2011, which is a 35 U.S.C. 371 application of International Application No. PCT/US2010/026381, filed Mar. 5, 2010, which claims the benefit of priority to U.S. Provisional Application No. 61/158,156, filed on Mar. 6, 2009, the contents of each of which are incorporated herein by reference in their entirety.This invention was made with government support under CA098127, CA39662, and CA077433 awarded by the National Cancer Institute. The ...

Bicyclic and Tricyclic Pyrimidine Tyrosine Kinase Inhibitors with Antitubulin Activity and Methods of Treating A Patient

Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed. 2. The compound of wherein Rand Rare each CH.4. The pharmaceutical composition according to comprising at least one pharmaceutically acceptable carrier.7. A pharmaceutical composition according to comprising at least one pharmaceutically acceptable carrier.10. A pharmaceutical composition according to comprising at least one pharmaceutically acceptable carrier.13. A pharmaceutical composition according to comprising at least one pharmaceutically acceptable carrier. This divisional utility patent application claims the benefit of co-pending U.S. patent application Ser. No. 15/659,155, filed Jul. 25, 2017, which is a divisional application and claims the benefit of U.S. patent application Ser. No. 14/859,854, filed Sep. 21, 2015, now U.S. Pat. No. 9,732,090, granted Aug. 15, 2017, which is a divisional patent application and claims the benefit of U.S. patent application Ser. No. 13/364,930, filed on Feb. 2, 2012, now U.S. Pat. No. 9,139,590, granted Sep. 22, 2015, which claims the benefit of U.S. Provisional Patent Application Ser. No. 61/439,470, filed Feb. 4, 2011 (expired). The entire contents of U.S. patent application Ser. Nos. 15/659,155, 14/859,854, and 13/364,930, and U.S. Provisional Patent Application Ser. No. 61/439,470 are incorporated by reference into this divisional utility patent application.The present invention relates to bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity. The ...

Substituted heterobicyclic alkyl amines and their use as squalene oxide cyclase inhibitors

This invention provides new condensed furan compounds of formula (I) which exhibit excellent 2,3-oxidosqualene cyclase inhibition and high-density lipoprotein-cholesterol elevating activities. This invention also provides a therapeutic and prophylactic agent of formula (I') for hyperlipidemia, hypercholesterolemia and atherosclerosis.

Production of dibenzothiepinpropionamide derivative

Method for preparing bis (4- (1-quinazolinyl-4) -piperidyl) -alkanes derivatives

PYRIDO-FELLED 4-OXO-4H-BENZOPYRANES, METHOD FOR THEIR PRODUCTION AND THEIR USE AS ANTIDOTS.

Производные 4-хиномиодигидропиридина, смесь их изомеров или отдельные изомеры и их соли

Объектом изобретения являются производные 4-хинолилдигидропиридина общей формулы I, приведенной в описании. смесь их изомеров или отдельные изомеры и их соли.

Anisole derivatives

Anisole derivs. of formula (I), useful as an intermediate for sythesizing a cotarnine, are prepd. In (I), when A, B and C are hydrogen respectively, D is -OH, halogen, -CO2R1[R1 = lower alkyl or -SO2R2[R2 = lower alkyl ; when A and C are hydrogen, and B is -OH, D is -CO2R3[R3 =lower alkyl ; when A is hydrogen, and B and C form oxo group(=0), D is -CO2R4[R4 =lower alky ; when B and C are hydrogen respectively, and D is halogen, A is -CHO. The cotarnine is used as a starting material for antiallergic tritoqualine.

Method of producing dihydrochloride of 2-oxymethyl-3-oxy-6-(1-oxy-2-tret, butylaminoethyl)pyridine

一种制备阿塞那平去甲基杂质的新方法

<b>本发明涉及一种制备阿塞那平去甲基杂质的新方法。该方法以马来酸阿塞那平为原料，解盐得到游离碱和氯甲酸乙酯在甲苯中回流，所得产物再与氢溴酸回流反应，可以得到阿塞那平的去甲基杂质。本发明方法收率高，操作简便。</b>

Compounds

Protease inhibitor and preparing method and use thereof

本发明公开了一种蛋白酶抑制剂的制备及用途，这种蛋白酶抑制剂是一类化合物，本发明公开了此类化合物及其药物组合物的制备方法和用途，本发明涉及一种降低或抑制细胞或受试者的双亮氨酸拉链激酶活性的化合物，使用本发明的化合物或其溶剂化物、水合物或可药用盐在预防或治疗病患因双亮氨酸拉链激酶异常而引起的病症或相关病症的用途。

Bicyclic enamino(thio)carbonyl compounds

Noxious organism control agent

A composition which comprises at least one compound represented by formula (I) or at least one salt thereof as an active ingredient and an agriculturally or zootechnically acceptable carrier, and which can be used as a noxious organism control agent. [In the formula, Het represents a pyridyl group; X represents an oxygen atom; R 1 , R 2 , R 3 , R 7 , R 10a , R 10b , R 11 and R 12 independently represent a hydrogen atom; R 4 , R 5 and R 6 independently represent a hydrogen atom, a hydroxy group, an optionally substituted C 1-18 alkylcarbonyloxy group, an optionally substituted C 1-18 alkylsulfonyloxy group, an optionally substituted arylcarbonyloxy group, a (C 1-6 alkyloxy)-(C 1-6 alkyloxy) group, or a (C 1-6 alkyloxy)-(C 1-6 alkyloxy)-(C 1-6 alkyloxy) group; R 8 represents a hydrogen atom; and R 13a , R 13b and R 13c independently represent a methyl group.]

INTERMEDIATE COMPOUNDS FOR SYNTHESIS OF TRANS-5-CHLORO-2-METHYL-2,3,3a,12b-TETRAHYDRO-1H-DIBENZ[2,3:6,7]-OXEPINO[4,5-c]PYRROLE

FIELD: chemistry. ^ SUBSTANCE: invention relates to novel amino acid derivatives of formula or formula , their synthesis methods and their use as intermediate products during synthesis of trans-5-chloro-2-methyl-2,3,3a, 12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole (asenapine), which have central nervous system depressant effect, as well as antihistamine and antiserotonin effect. ^ EFFECT: use of intermediate compounds I and II considerably increases output of asenapine. ^ 12 cl, 9 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 397 164 (13) C2 (51) МПК C07D 313/14 (2006.01) C07D 491/044 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (72) Автор(ы): КЕМПЕРМАН Герардус Йоханнес (NL), ВАН ДЕР ЛИНДЕН Якобус Йоханнес Мария (NL), РИДЕР Майкл Р. (US) (21), (22) Заявка: 2007141161/04, 06.04.2006 (24) Дата начала отсчета срока действия патента: 06.04.2006 (73) Патентообладатель(и): Н.В. ОРГАНОН (NL) (43) Дата публикации заявки: 20.05.2009 2 3 9 7 1 6 4 R U (85) Дата перевода заявки PCT на национальную фазу: 07.11.2007 C 2 C 2 (56) Список документов, цитированных в отчете о поиске: Vader J. et al, J. of Labelled Compounds and Radiopharmaceuticals, v.34, no.9, p.845-869. US 4145434 A, 20.03.1979. US 6002632 A, 11.01.1977. RU 2211837 C2, 10.09.2000. RU 96102419 A, 20.05.1998. RU 93050126 A, 20.06.1996. (86) Заявка PCT: EP 2006/061409 (06.04.2006) (87) Публикация PCT: WO 2006/106136 (12.10.2006) Адрес для переписки: 129090, Москва, ул.Б.Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры", пат.пов. Е.Е.Назиной (54) ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ ДЛЯ ПОЛУЧЕНИЯ ТРАНС-5-ХЛОР-2МЕТИЛ-2,3,3f,12b-ТЕТРАГИДРО-1Н-ДИБЕНЗ[2,3:6,7]-ОКСЕПИНО[4,5-c]ПИРРОЛА (57) Реферат: Изобретение относится к новым аминокислотным производным формулы I или формулы II: Ñòð.: 1 ru 2 3 9 7 1 6 4 (45) Опубликовано: 20.08.2010 Бюл. № 23 R U (30) Конвенционный приоритет: 07.04.2005 EP 05102742.3 способам их получения и их ...

Heterocyclic compound and organic light emitting device comprising same

본 명세서는 화학식 1로 표시되는 헤테로고리 화합물 및 이를 포함하는 유기 발광 소자에 관한 것이다.

Quinoline alkaloid compound with antibacterial activity in cigar rhizome and preparation method and application thereof

本发明公开了一种喹啉生物碱化合物(Ⅰ)及其制备方法和应用。以雪茄烟根茎为原料，以高浓度甲醇、高浓度丙酮/水或高浓度乙醇/水提取，提取液合并，过滤，减压浓缩成浸膏；浸膏用硅胶干法装柱进行硅胶柱层析；以氯仿‑丙酮溶液进行梯度洗脱；洗脱液的8:2部分进一步用高压液相色谱分离纯化即得所需的喹啉生物碱化合物。本发明还公开了上述化合物的用途，经活性测试表明，其具有较好的抑菌作用。本发明化合物结构新颖，且具有较好的抗菌活性。将该化合物用于卷烟接装纸，能够消除或降低卷烟接装纸中细菌滋生和繁殖的可能性。

Process for the preparation of aziridinyl epothilones from oxiranyl epothilones

The present invention relates to a stereospecific process to produce aziridinyl epothilones from oxiranyl epothilones and the intermediates derived therein.

Process for preparing cotarnine

내용 없음. No content.

Patent JPS603387B2

Pyrrolopyrimidinyalglutaminate derivatives and their use

A condensed pyrimidine derivative of the formula (I): ##STR1## wherein the ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent 5- or 6-membered homo- or hetero-cyclic group; X stands for, among others, amino group; Y stands for, among others, hydrogen atom, halogen atom or amino group; Z stands for a divalent aliphatic group having five or less atoms forming straight chain, optionally having nitrogen, whose chain portion may optionally have a hetero-atom; W stands for, among others, --NH--CO-- or --CO--NH--; R 1 stands for an optionally substituted cyclic or chain-like group; COOR 2 stands for an optionally esterified carboxyl group; and p denotes an integer of 1 to 4, provided that when --W--R 1 denotes a moiety represented by the formula: ##STR2## wherein COOR 16 and COOR 17 are, independently, an optionally esterified carboxyl group and n denotes an integer of 1 to 5, p denotes 1, 3 or 4, or a salt thereof, exhibiting highly specific toxicities to various tumor cells and excellent therapeutic effects on methotrexate-resistant tumor cells as well.

Synthetic route for preparation of 3-amino-piperidine compounds

本发明一般涉及有机化学领域，特别涉及3‑氨基‑哌啶化合物的制备。这些化合物可用作合成药学活性剂如优选托法替尼或其衍生物或包含3‑氨基哌啶部分结构的其它药学活性剂中的中间体。

Direct racemization of indole derivatives

The present invention discloses processes for the racemization of enantiomers of etodolac and other tetra-hydropyrano indole derivatives.

Process for the synthesis of n9-(3,5-dichloro-4-pyridyl)-6- difluoromethoxybenzo(4,5)furo(3,2-c)pyridine-9-carboxamide and salts thereof

The present invention relates to a process for the synthesis of N9-(3,5- dichloro-4-pyridyl)-6-difluoromethoxybenzo[4,5]furo[3,2-c]pyridine-9-carboxamide and salts thereof which are useful as a PDE4 inhibitor. The invention also relates to a process for the synthesis of methyl-2-formyl-7-cyclopentyloxybenzo[b]furan-4-carboxylate and salts thereof, which are useful as intermediates in preparing compounds with PDE4 inhibitory activity.

Certain substituted benzofuro-and benzothienoquinolines for use in organic light emitting diodes

特定取代的苯并呋喃并‑和苯并噻吩并喹啉类以及它们在电子器件，尤其是电致发光器件中的用途。当用作电致发光器件中的电荷传输材料、电荷阻挡材料和/或主体材料时，特定取代的苯并呋喃并‑和苯并噻吩并喹啉类可以提供电致发光器件的改进的效率、稳定性、可制造性或光谱特性以及降低的电致发光器件的驱动电压。

Electron transporting compounds

Compounds comprising an aza-dibenzo moiety and a condensed aromatic moiety having at least three benzene rings are provided. In particular, the compounds may comprise an azadibenzofuran, azadibenzothiophene, or azadibenzoselenophene joined directly or indirectly to an anthracene. The compounds may be used in the electron transport layer of organic light emitting devices to provide devices with improved properties.

Compounds with diazadibenzofurane or diazadibenzothiophene structures

The present invention relates to diazadibenzofurane or diazadibenzothiophene derivatives which are substituted with carbazole, fluorene, phenanthrene, benzofuran and/or benzothiophene groups, in particular for use in electronic devices. The invention further relates to a method for producing the compounds according to the invention, and to electronic devices comprising the same.

Materials for organic electroluminescent devices

The invention relates to compounds which are suitable for use in electronic devices, and to electronic devices, in particular organic electroluminescent devices, containing said compounds.

METHOD FOR PREPARATION OF Pyridoxine or its acid-additive salts

Twisted polymers, uses thereof and processes for the preparation of statistical copolymers

The invention relates to optical devices comprising a substrate and at least one semiconductive polymer supported by said substrate, wherein said semiconductive polymer is a copolymer in which one of the repeat units is a group of formula (I) or a homopolymer in which the repeat unit is a group of formula (I): wherein: A and B are the same or different and each comprises wholly or partially an aryl moiety or a heteroaryl moiety, said moiety in A being fused to the bond a-b and said moiety in B being fused to the bond c-d, and X is a linking unit, X being such that there is a torsion angle of at least 5° between the bond a-b and the bond c-d about the bond b-d. The invention also relates to semiconductive polymers, monomers for preparing same, and methods for preparing random statistical conjugated polymers.

Twisted polymers, their use and methods of making random copopymeres

The method of obtaining pyridine derivatives or their salts

The method of obtaining derivatives of 6,7 methylenedioxy-2 (1H) -quinazolinone

Water-soluble rhodamine dye peptide conjugates

The present invention provides novel, water-soluble, red-emitting fluorescent rhodamine dyes and red-emitting fluorescent energy-transfer dye pairs, as well as labeled conjugates comprising the same and methods for their use. The dyes, energy-transfer dye pairs and labeled conjugates are useful in a variety of aqueous-based applications, particularly in assays involving staining of cells, protein binding, and/or analysis of nucleic acids, such as hybridization assays and nucleic acid sequencing.

Preparation method of high-purity asenapine maleate

本发明公开了高纯度马来酸阿塞那平的制备方法，以阿塞那平游离碱粗品和马来酸阿塞那平粗品作为起始原料，将阿塞那平游离碱粗品与有机酸反应成盐，或马来酸阿塞那平粗品经加碱解离成为阿塞那平游离碱后与有机酸反应成盐，得阿塞那平对苯甲磺酸盐，结晶、过滤，加碱解离成为阿塞那平游离碱，再与马来酸反应得到马来酸阿塞那平，结晶、过滤。本发明高纯度马来酸阿塞那平的制备方法，工艺路线新颖、工艺条件温和、操作简单，无需多次重结晶操作，只需一次即能得到纯度≥99%的合格产品；同时，本发明制备方法还提高了反应收率，降低了生产成本，适合在工业生产中大规模应用，具有较好的实用价值和社会经济效益。

Quinoxaline-di-N-oxide-lactones

Optically active dihydropyridine lactones, process for their preparation, and their use

The invention relates to novel optically active dihydropyridine lactones of the general formula I <IMAGE> in which R - stands for hydrogen or - for straight-chain or branched alkyl having up to 4 carbon atoms, a process for their preparation, and their use as intermediates for the production of optically active pharmaceutical active compounds.

Compound for organic electronic element, organic electronic element using the same, and a electronic device thereof

본 발명은 소자의 발광효율, 안정성 및 수명을 향상시킬 수 있는 신규 화합물 및 이를 이용한 유기전기소자, 그 전자 장치를 제공한다.

Novel compound, polymerizable composition, color filter and production method thereof, solid-state imaging device, and planographic printing plate precursor

(Problem) It is providing the photopolymerizable composition which can form the cured film which is high in the sensitivity with respect to the light source of wavelength 365nm vicinity, is excellent in storage stability, and can suppress film | membrane physical property fall with time of heating. (Measures) (A) The oxime polymerization initiator whose molar extinction coefficient in (lambda) max in wavelength 300nm or more and less than 400nm in ethyl acetate is 20000 or more, and the molar extinction coefficient in ((lambda) max + 20nm) is 400 or less, (B) Polymerizable composition containing a polymeric compound. Polymerizable composition, color filter, solid state image pickup device, flat plate printing plate

New method for preparing dibenzothiepin derivatives

본 발명은 디벤조티에핀 유도체의 신규 제조방법에 관한 것으로, 보다 상세하게는 간단하고 새로운 방법으로 제조된 중간체 화합물인 5-(1-카르복시에틸)-2-페닐티오페닐-아세트산을 산촉매하에서 고리화 반응시키는 하기 화학식 1의 2-(10,11-디하이드로-10-옥소벤조[b,f]티에핀-2-일)프로피온산의 제조방법에 관한 것이다. The present invention relates to a novel process for the preparation of dibenzothiepine derivatives, and more particularly, to a 5- (1-carboxyethyl) -2-phenylthiophenyl-acetic acid, an intermediate compound prepared by a simple and novel method, under an acid catalyst. The present invention relates to a method for preparing 2- (10,11-dihydro-10-oxobenzo [b, f] thiinpin-2-yl) propionic acid of Chemical Formula 1, wherein the reaction is carried out. [화학식 1] [Formula 1] 본 발명의 제조방법에 따르면 종래 방법에 비해 간단한 방법으로 공업적으로 적용이 용이하며 약학적 활성을 가지는 프로피온산계 소염진통제인 2-(10,11-디하이드로-10-옥소벤조[b,f]티에핀-2-일)프로피온산을 고순도 및 고수율로 제공할 수 있다. According to the preparation method of the present invention, 2- (10,11-dihydro-10-oxobenzo [b, f], a propionic acid-based anti-inflammatory analgesic agent, which is easily applied industrially and has pharmaceutical activity, is simpler than the conventional method. Thiefin-2-yl) propionic acid can be provided in high purity and high yield. 2-(10,11-디하이드로-10-옥소벤조[b,f]티에핀-2-일)프로피온산, 5-(1-카르복시에틸)-2-페닐티오페닐-아세트산, 산, 고리화반응, 약학적 활성 2- (10,11-dihydro-10-oxobenzo [b, f] thiin-2-yl) propionic acid, 5- (1-carboxyethyl) -2-phenylthiophenyl-acetic acid, acid, cyclization , Pharmaceutical activity

The method of obtaining 4-phenyl- or 4 (2-thienyl) -6,7-methylenedioxy-2 (in) quinazolinones or -2 (in) quinazolinethions

One prepares the method for 4-amino-3-(4-amino-benzene) furo [2,3-d] pyrimidine

一种制备4-氨基-3-(4-氨基苯)呋喃并[2,3-d]嘧啶的方法，以硝基苯乙酮为原料，和N-溴代丁二酰亚胺反应，对甲苯磺酸作为催化剂生成2-溴-1-(4-硝基苯基)-乙酮，再和醋酸钠及四丁基溴化铵反应生成2-乙酰氧基-1-(4-硝基苯基)-乙酮，2-乙酰氧基-1-(4-硝基苯基)-乙酮通过把硝基还原为氨基，再和盐酸反应，把乙酰氧基还原为羟基得到1-(4-氨基苯基)-2-羟基-乙酮，然后1-(4-氨基苯基)-2-羟基-乙酮和丙二腈及二乙胺反应得到2-氨基-4-(4-氨基苯基)-3-呋喃腈，最后和醋酸甲脒反应得到4-氨基-3-(4-氨基苯)呋喃并[2,3-d]嘧啶。本方法操作简单，总收率高。

Flavoring with an oxocyclic pyrimidine

WHEREIN R1 is alkyl, halogen or hydrogen and R2, R3, R4, R5 and R6 are the same or different and are hydrogen or alkyl; flavoring and flavor-enhancing compositions containing such oxocyclic pyrimidines; and novel oxocyclic pryimidines and processes for the preparation of such oxocyclic pyrimidines. Processes for altering the flavors of consumable products, including foodstuffs and tobaccos, which comprise adding thereto a small but effective amount of at least one oxocyclic pyrimidine having the formula

Intermediate Compounds for the Preparation of Glycogen Phosphorylase Inhibitors

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (51) ÌÏÊ 7 (11) 2004 121 986 (13) A C 07 D 403/12, 491/04 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2004121986/04, 06.01.2003 (71) Çà âèòåëü(è): ÏÔÀÉÇÅÐ ÏÐÎÄÀÊÒÑ ÈÍÊ. (US) (30) Ïðèîðèòåò: 18.01.2002 US 60/349,647 (43) Äàòà ïóáëèêàöèè çà âêè: 20.11.2005 Áþë. ¹ 32 (86) Çà âêà PCT: IB 03/00034 (06.01.2003) Àäðåñ äë ïåðåïèñêè: 129010, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. À.Â. Ìèö (74) Ïàòåíòíûé ïîâåðåííûé: Ìèö Àëåêñàíäð Âëàäèìèðîâè÷ Ôîðìóëà èçîáðåòåíè 1. Ñîåäèíåíèå ñòðóêòóðíîé ôîðìóëû A 2. Ñîåäèíåíèå ñòðóêòóðíîé ôîðìóëû R U 2 0 0 4 1 2 1 9 8 6 A (54) ÏÐÎÌÅÆÓÒÎ×ÍÛÅ ÑÎÅÄÈÍÅÍÈß ÄËß ÏÎËÓ×ÅÍÈß ÈÍÃÈÁÈÒÎÐΠÃËÈÊÎÃÅÍÔÎÑÔÎÐÈËÀÇÛ Ñòðàíèöà: 1 RU 2 0 0 4 1 2 1 9 8 6 (87) Ïóáëèêàöè PCT: WO 03/059910 (24.07.2003) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 16.07.2004 (72) Àâòîð(û): ÁÀÐÐÈËÀ Ìàðê Òîìàñ (US), ÁÓØ Ôðýíê Ðîáåðò (US), ÊÓÒÞÐÜÅ Ìèøåëü Àíäðå (US), ÎÐÐÈËË Ñüþçàí Ëè (US), ÐÎÓÇ Ïèòåð Ðîáåðò (US), ÒÈÊÍÅÐ Äåðåê Ëîóðåíñ (US), ÒÎÁÈÀÑÑÅÍ Ãàððè Îää (US), ÓÈÒÁÐÎ Ãðåãîðè Äæîí (US) A 2 0 0 4 1 2 1 9 8 6 A 2 0 0 4 1 2 1 9 8 6 R U R U Ñòðàíèöà: 2

Tertiary alkyl ester of oxodibenzoxepin acetic acid

本发明提供式(2)所示的叔烷基酯及其制法。 (式中，R 1 、R 2 各自独立地表示碳原子数为1～4的烷基。)

Method of preparing 3-quinolinecarboxylic acid derivatives or their salts

A compound having a diazadibenzofuran or diazadibenzothiophene structure

본 발명은 특히 전자 소자에서의 사용을 위한 카르바졸, 플루오렌, 페난트렌, 벤조푸란 및/또는 벤조티오펜 기로 치환된 디아자디벤조푸란 또는 디아자디벤조티오펜 유도체에 관한 것이다. 본 발명은 또한 본 발명에 따른 화합물의 제조 방법, 및 본 발명에 따른 화합물을 포함하는 전자 소자에 관한 것이다. The present invention relates to diazadibenzofuran or diazadibenzothiophene derivatives substituted with carbazole, fluorene, phenanthrene, benzofuran and/or benzothiophene groups, particularly for use in electronic devices. The invention also relates to a process for preparing the compound according to the invention and an electronic device comprising the compound according to the invention.

Synthetic method of natural product 6-HHC

本发明公开了一种化合物6‑hydroxyethyldihydrochelerythrine的合成方法，包括如下步骤：S1：将式1化合物在室温下溶于 N,N ‑二甲基甲酰胺溶剂中，在室温下依次加入无水磷酸氢二钠、溴乙酸乙酯、Ir(ppy) 2 (dtbbpy)PF 6 ，在氮气的保护下，搅拌10分钟混匀，用灯照射，室温搅拌24 h，得到式2化合物；S2：将式2化合物溶于四氢呋喃溶剂中，0℃加入氢化铝锂，0℃条件下搅拌6h，得到标的物。本发明为天然产物6‑hydroxyethyldihydrochelerythrine（6‑HHC）的首次合成报道，路线设计独特新颖，反应条件温和，催化效率高，路线短，副反应少，操作简便。

Pyranoindoles for treating glaucoma

Substituted pyranoindoles useful for lowering and controlling IOP and glaucoma are disclosed.

Substituted furo[2,3-g]indazoles for the treatment of glaucoma

Substituted furo[2,3-g]indazoles for lowering intraocular pressure and treating glaucoma are disclosed.

Pyrazolo[3,4- e]benzoxazoles for the treatment of glaucoma

Pyrazolo[3,4-e]benzoxazoles and analogues thereof for lowering intraocular pressure and treating glaucoma are disclosed.

Use of dioxindoindazoles and dioxoloindazoles for treating glaucoma

Novel dioxinoindazole compounds and dioxoloindazole compounds are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions of one or more of the compounds of the present invention.

[Indole] naphthopyrans, prepn., compositions and (co) polymer matrics contg. them, synthesis intermediates

本发明的对象是新颖[吲哚]萘并吡喃化合物和含有此类化合物的组合物和(共)聚合物基体。所述化合物具有引入注意的光致变色性能。本发明的另一个对象是制备所述新颖化合物的方法以及用于所述制备的中间体。

Novel compound and organic light emitting device comprising the same

본 발명은 신규한 화합물 및 이를 이용한 유기 발광 소자를 제공한다.

COMPOUND HAVING ACRYDAN RING STRUCTURE AND ORGANIC ELECTROLUMINESCENT DEVICE

本発明によれば、一般式（１）で表されるアクリダン環構造を有する化合物、及び、一対の電極とその間に挟まれた少なくとも一層の有機層を有する有機エレクトロルミネッセンス素子において、該化合物が、該有機層の構成材料として用いられている有機エレクトロルミネッセンス素子が提供される。本発明の化合物は、高効率、高耐久性の有機エレクトロルミネッセンス素子用の材料として、正孔の注入・輸送性能に優れ、電子阻止能力を有し、薄膜状態での安定性が高く、耐熱性に優れた特性を有する。 【化１】

Process for the preparation of halo acetal compound

내용 없음. No content.

Pyrido-fused 4-oxo-4H-benzopyrans, methods for their preparation and their use as antidote

본 발명은 하기 일반식(Ⅰ)의 피리도 융합된 4-옥소-4H-벤조피란 및 그의 염, 그리고 제초 활성 성분으로서 2-(4-헤타릴옥시)-및 2-(4-아릴옥시)-페녹시아세트산 유도체 또는 시클로헥세논 유도체와 해독제로서 일반식(Ⅰ`)의 피리도 융합된 4-옥소-4H-벤조피란을 함유하는 제초제에 관한 것이다. (Ⅰ) 상기 식에서, m 은 0,1 또는 2이고, R 1 , R 6 및 R 7 은 본 명세서에 정의한 바와 같다.

2 3 4 9 - tetrahydro - 9 -phenyl-oxazirino-(2 3-d)(1 4)benzodiazepines and preparation thereof

NOVEL 2,3,4,9-TETRAHYDRO - 9 - PHENYL-OXAZIRINO(2,3-D)(1,4)BENZODIAZEPINES AND PREPARATION THEREOF PREPARED VIA OXIDATION OF 2,3-DIHYDRO-5-PHENYL-1H-1,4-BENZODIAZEPINES, ARE DESCRIBED. THESE NOVEL PRODUCTS ARE USEFUL AS INTERMEDIATES IN THE PREPARATION OF 2,3-DIHYDRO-5-PHENYL1H-1,4-BENZODIAZEPINE 4-OXIDES, USEFUL AS ANTI-CONVULSANT AGENTS.

Blood lipid metabolism improver

Method of producing furo[3,2-c]isoquinoline-5(4h)-one derivatives

FIELD: chemistry. SUBSTANCE: invention relates to organic chemistry, and more specifically to a method of producing heterocyclic compounds of the isoquinolinone series, which can be of interest as biologically active substances or semi-products for synthesis thereof. Method of producing furo[3,2-c]isoquinoline-5(4H)-one derivatives of general formula I, where R=tert-butyl, 1-adamantyl; R'=phenyl, substituted phenyl, involves reaction at room temperature of 2-imino-1H-indene-1,3(2H)-diones with 1-alkynes in a medium of chlorinated solvents in presence of 100–300 mol% trifluoroacetic acid for 1–3 hours. EFFECT: efficient method of producing furo[3,2-c]isoquinoline-5(4H)-one derivatives using commercially available compounds which enable to vary the substituent in position 2 of the furan ring. 5 cl, 1 tbl, 8 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 713 199 C1 (51) МПК C07D 491/048 (2006.01) C07D 471/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07D 491/04 (2019.08); C07D 471/04 (2019.08) (21)(22) Заявка: 2019134581, 28.10.2019 (24) Дата начала отсчета срока действия патента: Дата регистрации: 04.02.2020 (45) Опубликовано: 04.02.2020 Бюл. № 4 2 7 1 3 1 9 9 R U (56) Список документов, цитированных в отчете о поиске: DAQIAN ZHU et al.: "Heterocyclic Iodoniums for the Assembly of Oxygen-Bridged Polycyclic Heteroarenes with Waters as the Oxygen Source", ORGANIC LETTERS, 2018, vol.20, p.4815-4818. HARI PRASAD KOKATLA et al.: "Exquisite Selectivity for Human Toll-Like Receptor 8 in Substituted Furo[2,3-c]quinolines", JOURNAL OF MEDICINAL CHEMISTRY, 2013, (см. прод.) (54) Способ получения производных фуро[3,2-c]изохинолин-5(4Н)-она (57) Реферат: Изобретение относится к органической химии, Технический результат – эффективный способ а точнее к способу получения гетероциклических получения производных фуро[3,2-с]изохинолинсоединений ряда изохинолинона, которые могут 5(4Н)-она с использованием коммерчески ...

[Indole] naphthopyrans, their preparation, compositions and (co) polymer matrices containing them, synthetic intermediates

(57)【要約】 本発明の目的は、新規な［インドール］ナフトピラン化合物並びにそれらを含有する組成物および（コ）ポリマーマトリクスにある。本発明の別の目的は、その新規な化合物を調製する方法、並びにその調製に有用な中間体にある。

Inhibitors of checkpoint kinases (Wee1 and Chk1)

This invention relates to pyrrolocarbazole derivatives according formula I wherein R 1 , R 2 , R 7 , R 8 , R 9 , X and Y are as defined in the specification wherein said derivatives specifically inhibit one or both of the checkpoint kinases Wee1 and Chk1

Novel compound and organic light emitting device comprising the same

본 발명은 신규한 화합물 및 이를 이용한 유기 발광 소자를 제공한다. The present invention provides a novel compound and an organic light emitting device using the same.

Adenosine incorporation inhibitor.

An adenosine incorporation inhibitor and a drug for protecting cardiac muscles or preventing or treating inflammatory edema, each containing as the active ingredient a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, wherein R1 represents hydrogen, (un)substituted lower alkyl, alkenyl or (un)substituted aralkyl; R?2, R3, R4 and R5¿ represent each independently hydrogen, halogen, amino, mono- or di(lower alkyl) amino, lower alkanoyl amino, nitro, cyano, (un)substituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy or lower alkanoyloxy; R?6, R7, R8 and R9¿ represent each independently hydrogen, hydroxy, (un)substituted lower alkoxy or aralkyloxy, or alternatively the two adjacent groups among them may be combined together to represent methylenedioxy; R10 represents hydrogen or lower alkyl; and Y and Z represent each independently N or C-R'', wherein R'' represents hydrogen, (un)substituted lower alkyl or halogen.

BASIC SUBSTITUTED PYRIMIDONE (4) DERIVATIVES, THE PROCESS FOR THEIR PRODUCTION AND THE MEDICINAL PRODUCTS CONTAINING THEM

Method of the preparation of 2-oxymethyl-3-oxy-6-(1-oxy-2-tertbutylaminoethyl)-pyridine or its salts

Drug used in cardiac failure

FIELD: medicine, pharmacy. SUBSTANCE: invention proposes drugs used in medicine for treatment of patients with cardiac failure which have as an active components at least one of compounds of the formula (I) or their pharmacologically acceptable salts where n = 0 or 1; A means hydroxyl-group or hydrogen atom; B means hydrogen atom; X means oxygen atom, nitrogen atom; R 1 and R 2 mean hydrogen atom, C 1 -C 4 -alkyl; R 3 and R 4 mean hydrogen atom, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, or C(=Y)Z-R 6 where Z is NH; Y is O, S, ≡ or they form together 1,4-butylene or 1,5-pentylene. These compounds show the enhanced activity with respect to cardiac muscle contractions and strong activity with respect to cardiac contraction rate decrease. EFFECT: enhanced effectiveness of compounds proposed. 5 cl, 6 tbl, 71 ex СУОЗСТсС ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) (51) МПК ВИ” 21428 043 ' 13) Сл А 61 К 31/41 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 95119384/14, 01.04.1994 (30) Приоритет: 02.04.1993 УР 5-76,860 08.03.1994 УР 6-37,303 (46) Дата публикации: 27.03.1999 (56) Ссылки: ЦЗ 5164509 А, 17.11.92. 4$ 5026712 А, 25.06.91. 4$ 4900752 А, 13.02.90. ЕР 0488107 А, 03.06.92. (86) Заявка РСТ: УР 9400544 (01.04.94) (98) Адрес для переписки: 103735, Москва, ул.Ильинка, 5/2, Союзпатент (71) Заявитель: Ниссан Кемикал Индастриз, Лтд. (Р) (72) Изобретатель: Киетомо Сето (4Р), Хироо Матсумото (.Р), Есимаса Камикавадзи (/Р), Казухико Охраи (.Р), Тору Ямасита (УР), Юкинори Масуда (/Р) (73) Патентообладатель: Ниссан Кемикал Индастриз, Лтд. (Р) (54) ЛЕКАРСТВЕННЫЕ СРЕДСТВА ДЛЯ СЕРДЕЧНОЙ НЕДОСТАТОЧНОСТИ (57) Реферат: Кардиотонические лекарственные средства, используемые в медицине для лечения сердечной недостаточности, содержат в качестве активного компонента по меньшей мере одно из соединений формулы | или их фармакологически приемлемых солей. где п =0 или 1; А представляет собой ОН или Н;: В представляет собой атом водорода; Х представляет ...