41 results about "Ciclopentolato" patented technology

This invention relates to a 1,3,4-thiadiazole peptide deformylase inhibitor and its preparation and application. The structural formula is shown in formula (1): wherein, R 1 It is n-butyl or cyclopentylmethyl; R 2 The compounds are hydrogen-containing, straight-chain alkanes, cyclic alkanes, aromatic rings, substituted biphenyls, or heterocyclic rings. The 1,3,4-thiadiazole peptide deformylase inhibitors provided by this invention can effectively inhibit bacterial protein synthesis, thereby achieving sterilization. These compounds exhibit excellent inhibitory activity against Gram-positive drug-resistant bacteria, especially the clinically challenging methicillin-resistant Staphylococcus aureus (MRSA). In particular, some preferred compounds show inhibitory activity 4-8 times that of the control standards vancomycin and linezolid. The 1,3,4-thiadiazole peptide deformylase inhibitors provided by this invention also exhibit inhibitory activity against Gram-negative drug-resistant bacteria, especially against drug-resistant Acinetobacter baumannii, known as "superbugs," with an inhibitory activity reaching 0.5 μg / mL, far superior to vancomycin and linezolid.

Methods of treating tinnitus, acute sensorineural hearing loss, Meniere's disease, Tourette's syndrome, ADHD or addiction with (1S,3S)-3-amino-4-(difluoromethylidene) cyclopentane-1-carboxylic acid or a pharmaceutically acceptable salt thereof are provided. Methods of treating tinnitus, acute sensorineural hearing loss, Meniere's disease, Tourette's syndrome, ADHD or addiction with (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid are provided. Also provided are therapeutic compositions that may be used to improve one or more symptoms of tinnitus, acute sensorineural hearing loss, Meniere's disease, Tourette's syndrome, ADHD or addiction.

A drug is provided, which contains, as an active ingredient, a compound having ABHD6 inhibitory activity in prevention and / or treatment of a disease associated with ABHD6. A compound of formula (I-A) or a pharmaceutically acceptable salt thereof has ABHD6 inhibitory activity and therefore is useful as a pharmaceutical ingredient having potent ABHD6 inhibitory activity in the prevention and / or treatment of a disease associated with ABHD6:in which all symbols represent the same meaning as the symbols described in the specification.

The present application relates to a process for synthesizing (S)-3-amino-4-(difluoromethylene)cyclopent-1-ene-1-carboxylic acid. Provided herein are processes, compounds, and compositions for preparing (S)-3-amino-4-(difluoromethylene)cyclopent-1-ene-1-carboxylic acid. Also provided herein are pharmaceutical compositions containing (S)-3-amino-4-(difluoromethylene)cyclopent-1-ene-1-carboxylic acid.

The invention provides a polymer based on 2, 6-dibromo-4H-cyclopenta [1, 2-B: 5, 4-B] dithiophene-4-ketone as well as a preparation method and application of the polymer, and belongs to the technical field of organic photoelectric materials. The polymer based on the 2, 6-dibromo-4H-cyclopenta [1, 2-B: 5, 4-B] dithiophene-4-ketone provided by the invention is a polymer P-ODDTO-BT, a polymer P-ODDTO-TT and a polymer P-ODDTO-T with structures shown in a formula I, a formula II and a formula III respectively. The polymer provided by the invention has high carrier mobility on the basis of good thermal stability and photochemical stability, and is beneficial to application in the field of organic semiconductor materials.

The invention provides a preparation method of tetrahydrocyclopropane [3, 4] cyclopenta [1, 2-c] quinoline-(5H)-ketone, and belongs to the technical field of heterocyclic compounds. The preparation method comprises the following steps: adding a palladium catalyst, a ligand, alkali and bicyclo [1.1. 0] butyramide into an organic solvent, reacting at 50-70 DEG C for 10-14 hours, and performing post-treatment to obtain tetrahydrocyclopropane [3, 4] cyclopenta [1, 2-c] quinoline-(5H)-ketone. The preparation method has the advantages of simple operation, cheap and easily available initial raw materials, high reaction efficiency and good substrate compatibility, and can realize one-step efficient and rapid synthesis of tetrahydrocyclopropane [3, 4] cyclopenta [1, 2-c] quinoline-(5H)-ketone.

Methods and compositions for treating rheumatoid arthritis are provided which include administering an effective amount of (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid or a pharmaceutically acceptable salt thereof to a subject in need thereof. In embodiments, compositions for treating rheumatoid arthritis that include (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid or a pharmaceutically acceptable salt thereof are administered to a subject in need thereof.

The present disclosure relates to choline salts, and crystalline forms thereof, of a compound which is N—((S)-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-((3bS,4aR)-5,5-difluoro-3- (trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide, which is useful in the treatment and prevention of a Retroviridae viral infection including an infection caused by the HIV virus.

The present disclosure provides for a compound according to formula (I)or a pharmaceutically acceptable salt thereof as CaV1.22 activators for the treatment of schizophrenia, bipolar disorder, major depressive disorder, substance use disorder, ADHD, Phelan-McDermid Syndrome, autism spectrum disorder, multiple sclerosis, frontotemporal dementia, Alzheimer's disease, Brugada Syndrome, Short QT syndrome, or early repolarization syndrome.

The invention relates to the technical field of material synthesis, and discloses a synthesis process of a medical intermediate ((2S)-4-(cyclopentylamino)-3-hydroxy-4-oxo-1-((S)-2-oxo-pyrrolidone-3-yl) butyl-2-yl) tert-butyl carbamate, which comprises the following steps: by taking N-benzyl-3-hydroxypiperidine as a raw material, reacting at the temperature of 60-80 DEG C for 2-4 hours; the preparation method comprises the following steps: carrying out resolution, alkali dissociation, palladium-carbon hydrogenation debenzylation / tert-butyloxycarboryl protection, sulfonyl chloride acylation, hydrolysis, salification purification and crystal form optimization to obtain the high-purity (more than or equal to 95%) and high-optical-purity target product through multi-step fine reaction and subsequent salification purification and crystal form optimization steps. According to the present invention, the strict requirements on the compound quality in the fields of medicine, material science and the like are met, the reliable material basis is provided for the related applications, and compared with the traditional synthesis method, the reaction steps and conditions are optimized to a certain extent, the reaction efficiency is improved, the production time is shortened from about 10 days to about 7 days, and the production cost is reduced; and the market competitiveness of the product is enhanced.

Provided herein are processes, compounds and compositions for making (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid. Also provided herein a pharmaceutical compositions containing (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid.

Methods and compositions for treating multiple sclerosis are provided which include administering an effective amount of (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid or a pharmaceutically acceptable salt thereof to a subject in need thereof. In embodiments, compositions for treating multiple sclerosis that include (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid or a pharmaceutically acceptable salt thereof are administered to a subject in need thereof.

Methods and compositions including (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid or a pharmaceutically acceptable salt thereof are provided for use in treating cancer and inhibiting cancer proliferation and metastasis.

The application belongs to the technical field of pharmaceutical chemistry, and particularly relates to application of 1-pentyl-tetradecahydro-1H-cyclopenta[1,2-a]phenanthrene in treatment of acute myeloid leukemia. The application provides 1-pentyl-tetradecahydro-1H-cyclopenta[1,2-a]phenanthrene compounds with a novel skeleton. Experimental verification shows that the compounds have excellent inhibitory activity on AML cancer cells, and the mechanism is clear: the compounds can directly inhibit the activity of AML cancer cells, inhibit the proliferation of cancer cells by blocking the cell cycle process, and can specifically induce AML cancer cell apoptosis, thereby realizing the AML treatment effect. The application provides a new active compound candidate for the targeted treatment of acute myeloid leukemia, and lays an important foundation for the research and development of related drugs.

The invention provides a synthesis method and application of a treprostinil chiral intermediate and a synthesis method of treprostinil, and relates to the technical field of pharmaceutical chemical synthesis. According to the synthesis method of the treprostinil chiral intermediate, provided by the invention, efficient synthesis of a key intermediate is realized by chemical synthesis methods of constructing a cyclopentanaphthalene skeleton through a Dieckmann reaction catalyzed by LiHMDS and the like in combination with a chiral alcohol preparation technology through asymmetric reduction of carbonyl reductase. The method is efficient, low in cost and environmentally friendly, the total yield is larger than or equal to 75%, the chiral purity ee is larger than or equal to 99%, the method is suitable for large-scale production, and core technical support is provided for large-scale patent medicine of treprostinil.

The present application relates to compounds of formula (I) as defined herein and pharmaceutically acceptable salts thereof. Also described are pharmaceutical compositions comprising the compounds of Formula (I) and pharmaceutically acceptable salts thereof, as well as methods of using the compounds and compositions for the treatment of diseases such as cancer, autoimmune disorders, and inflammatory disorders.

The invention relates to a plant DHODH inhibitor as well as a preparation method and application thereof. The DHODH inhibitor is a compound as shown in a formula I or an isomer, a salt or a solvate or a crystal form thereof: # imgabs 0 #, wherein R1 is selected from substituted tetrahydronaphthyl, C3-C8 cycloalkyl, phenyl, biphenyl, tetrahydronaphthyl, benzocycloheptyl, benzocyclopentyl, substituted C3-C8 cycloalkyl and # imgabs 1 # cyclohexylpyridyl; r2 is selected from C1-C8 straight-chain and branched-chain alkylene or isomers thereof, and C3-C8 cycloalkyl; and R3 is selected from a substituted phenyl group, a biphenyl group, a benzocyclohexyl group, a tetrahydronaphthyl group, a benzocyclopentyl group and a benzopiperidyl group. The compound provided by the invention is novel in structure, has better DHODH inhibition activity than most of known structures in the market, and is expected to be used as a novel weed control drug to be applied to rice planting.

The invention provides a preparation method of 4-chloro-6, 7-dihydro-5H-cyclopenta [B] pyridine-7-alcohol, and relates to the technical field of organic synthesis. A compound 1 and first m-chloroperoxybenzoic acid are subjected to a first oxidation reaction to obtain a compound 2 crude product, the compound 2 crude product and acid anhydride are directly subjected to a Boekelhede reaction to obtain a compound 3, the water solubility of the compound 3 is poor, the compound 3 is easily separated from a water-soluble byproduct m-chlorobenzoic acid, and a large amount of loss of the compound 3 in the subsequent separation process cannot be caused; the yield of the compound 3 is improved; and carrying out a second oxidation reaction on the compound 3 and second m-chloroperoxybenzoic acid, carrying out a chlorination reaction on the obtained compound 4 and phosphorus oxychloride, and carrying out a hydrolysis reaction on the obtained compound 5 to obtain the 4-chloro-6, 7-dihydro-5H-cyclopenta [B] pyridine-7-ol. According to the preparation method provided by the invention, the total yield of the 4-chloro-6, 7-dihydro-5H-cyclopenta [B] pyridine-7-alcohol is high.

Provided are methods and compositions for treating multiple sclerosis, comprising administering to a subject in need thereof an effective amount of (S)-3-amino-4-(difluoromethylene) cyclopent-1-en-1-carboxylic acid, or a pharmaceutically acceptable salt thereof. In an embodiment, a composition for the treatment of multiple sclerosis, comprising (S)-3-amino-4-(difluoromethylene) cyclopent-1-en-1-carboxylic acid, or a pharmaceutically acceptable salt thereof, is administered to a subject in need thereof.

Methods and compositions for treating pain are provided which include administering an effective amount of (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid, or a pharmaceutically acceptable salt thereof, to a subject in need thereof. In embodiments, compositions for treating pain which include (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid, or a pharmaceutically acceptable salt thereof, are administered to a subject in need thereof.

Disclosed are amino, halo-substituted cyclopentene, cyclopentane, or 4- methylenecyclopent- l-ene carboxylic acid compounds. The disclosed compounds and compositions thereof may be utilized in methods for modulating human ornithine δ- aminotransferase (hOAT) activity, including methods for treating diseases or disorders associated with hOAT activity or expression such as cell proliferative diseases and disorders.

The present application relates to processes for the synthesis of (S)-3-amino-4- (difluoromethylidene)cyclopent-1-en-1-carboxylic acid. Provided herein are processes, compounds, and compositions for the preparation of (S)-3-amino-4- (difluoromethylidene)cyclopent-1-en-1-carboxylic acid. Also provided herein are pharmaceutical compositions containing (S)-3-amino-4- (difluoromethylidene)cyclopent-1-en-1-carboxylic acid.

Methods and compositions are provided for use in treating cancer and inhibiting the growth and metastasis of cancer, which comprise (S)-3-amino-4-(difluoromethylene)cyclopent-1-ene-1-carboxylic acid or a pharmaceutically acceptable salt thereof.

The invention belongs to the technical field of high-molecular compounds, and particularly relates to an electrochromic polymer, a film, a preparation method and application. The preparation method comprises the following steps: carrying out structural modification on diketopyrrolopyrrole, firstly, carrying out normal-temperature Boc protection reaction to prepare a diketopyrrolopyrrole derivative containing a t-Boc solubilizing group, then, carrying out Stille coupling polymerization on the diketopyrrolopyrrole derivative, a cyclopentadithiophene tin reagent and dibromofluorene to obtain a soluble polymer, subsequently, dissolving the polymer in trichloromethane, and spraying to form a film. And removing t-Boc groups by combining photo-acid spraying and short-time ultraviolet radiation, and inducing to form a hydrogen bond cross-linked network, thereby finally obtaining the yellow-green insoluble high-performance electrochromic polymer film and the patterned device. According to the electrochromic polymer film, t-Boc group removal and hydrogen bond crosslinking are realized in a mild manner of photo-acid-ultraviolet radiation, and the problems that a traditional thermal annealing treatment process is complex in preparation process and low in reaction controllability are thoroughly solved.

Provided are methods for effecting immune modulation and treating gastrointestinal disorders, comprising administering to a subject in need thereof an effective amount of (S)-3-amino-4-(difluoromethylene) cyclopent-1-en-1-carboxylic acid, or a pharmaceutically acceptable salt thereof. In an embodiment, a composition comprising (S)-3-amino-4-(difluoromethylene) cyclopent-1-en-1-carboxylic acid, or a pharmaceutically acceptable salt thereof, for effecting immune modulation and treating gastrointestinal disorders is administered to a subject in need thereof.

The present invention is related to a novel compound of formula (I) wherein A represents –C≡C– or the bond represents a single bond or a double bond, Z1 represents CH or N; X represents carbon or nitrogen, and when X represents nitrogen then the bond represents a single bond; R 1 is hydrogen, C1-4a1ky1 or halo; R 2 is hydrogen, C1-4a1ky1 or halo; R 3 is hydrogen, C1-6a1ky1, hydroxy or halo; R 4 is hydrogen; halo; C1-6a1ky1; C2-6alkenyl; C26alkynyl; C1-6alkyloxy; C1-4alkyloxycarbonyl; aminocarbonyl; mono- or di(C1-4alkyl)-aminocarbonyl; aryl; aryloxy; arylcarbonyl; arylsulfonyl; heteroaryl; C1-6alkyl substituted with cyano; C1-6a1ky1 substituted with aryl or aryloxy; or C1-6alkyl substituted with heteroaryl; aryl is phenyl; phenyl substituted with one, two or three substituents each individually selected from halo, hydroxy,C1-4 alkyl, C1-4alkyloxy, polyhaloC1-4alkyl, polyhaloC1-4alkyloxy, cyano, nitro, and amino; heteroaryl is furanyl, thiophenyl, pyrrolyl, pyrazolyl, imidazolyl, isoxazolyl, thiazolyl, triazolyl, tetrazolyl, isothiazolyl, thiadiazolyl, oxadiazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, benzo[l ,3]dioxolyl, benzofuranyl, benzothiazolyl, indolyl, 2,3 -dihydro- 1 H-indolyl, tetrahydrothiophenyl, or quinolinyl, wherein each heteroaryl may be substituted with one or two substituents each independently selected from halo, cyano, C1-4alkyl, C14alkyloxy, C1-4alkylcarbonyl, or phenyl; that inhibits the activity of the fatty acid biosynthesis enzyme (FabI enzyme) which is therefore useful in the treatment of bacterial infections. It further relates to a pharmaceutical composition comprising the compound, and a chemical process for preparing the compound.

This invention belongs to the field of novel excipients and dosage forms for pharmaceutical preparations, and relates to the construction of four cabazitaxel prodrugs and their self-assembled nanoparticles. Specifically, it involves the synthesis of four different cabazitaxel prodrugs using three different disulfide bonds as connecting bonds and 9-fluorenylmethanol or cyclopentylmethanol as side chains, further preparing self-assembled nanoparticles, and exploring their application in drug delivery systems. The prodrugs are prepared by forming anhydrides from dithiodiacetic acid, 3,3'-dithiodipropionic acid, or 4,4'-dithiodibutyric acid, followed by esterification with 9-fluorenylmethanol or cyclopentylmethanol to obtain intermediate products. These intermediate products then undergo esterification with cabazitaxel to obtain the cabazitaxel prodrugs. Self-assembled nanoparticles of the cabazitaxel prodrugs are obtained through a one-step nanoprecipitation method. The prepared prodrug self-assembled nanoparticles can rapidly release the parent drug at the tumor site, exerting their tumor-killing effect and demonstrating excellent anti-tumor efficacy.

The present invention relates to a process for the preparation of a compound of formula (I) based on optical resolution of an enantiomer mixture of 1, 4-dichloro-5-(methyl-d3)-6, 7-dihydro-5H-cyclopenta [d] pyridazine; the method comprises the following steps: reacting the enantiomer mixture with an optically active compound to form a compound of isomers, and separating the obtained compound through crystallization to obtain the compound shown in the formula (I), the method has the advantages of low price of the reaction initiator, simple post-treatment operation, high yield, high chemical and chiral purity of the product, and suitableness for large-scale industrial production. The compounds of formula (I) are useful for the preparation of a thyroxine [beta] receptor agonist (R)-2-(3, 5-dichloro-4-((7-(methyl-d3)-1-oxo-2, 5, 6, 7-tetrahydro-1H-cyclopenta [d] pyridazine-4-yl) oxy) phenyl)-3, 5-dioxo-2, 3, 4, 5 + tetrahydro-1, 2, 4-triazine-6-formonitrile, which agonist is useful for the treatment of primary hypercholesteremia in adults.

The present invention relates to a Derivative Compound of Bixanthene and Bi(cyclopenta[b]chromene) of formula I. More particularly, the present invention relates to a process for preparation of a Derivative Compound of Bixanthene and Bi(cyclopenta[b]chromene) of formula I. Further, the present invention relates to Derivative Compound of Bixanthene and Bi(cyclopenta[b]chromene) with potent anti-cancer activity as pharmaceutical agents and their pharmaceutically acceptable salts and their pharmaceutically acceptable solvents or mixture thereof.a derivative of compound bixanthene and bi(cyclopenta[ b]chromene)