- GPR52 MODULATOR COMPOUNDS
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The disclosures herein relate to novel compounds of Formula (1): (1) and salts thereof, wherein R1, Q, X, Y and Z are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with GPR52 receptors.
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Page/Page column 80
(2021/05/15)
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- Preparation method of pyraclostrobin intermediate
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The invention discloses a preparation method of pyraclostrobin intermediate 3 - hydroxyl - 1H - pyrazole and 1 - (4 - chlorophenyl) -3 - pyrazol, which comprises: synthesizing 3 - hydroxyl - 1H - pyrazole -4 - carboxylic acid ethyl ester by cyclization re
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Paragraph 0021; 0046-0049
(2021/09/15)
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- PROCESS OF MAKING CFTR MODULATORS
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The disclosure provides processes for synthesizing Compound I, and pharmaceutically acceptable salts thereof.
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Paragraph 0460; 0462
(2021/02/19)
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- PROCESSES FOR MAKING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
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The disclosure provides processes for preparing a compound of Formula (I).
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Paragraph 0590-0592
(2021/08/13)
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- SOLID FORMS OF MODULATORS OF CFTR
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Crystalline and amorphous forms of a potassium salt of Compound (I): are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.
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Paragraph 00242; 00247; 00256
(2020/10/27)
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- USE OF MORPHINAN DERIVATIVES FOR TREATMENT OF OPIOID RECEPTOR AGONIST-RELATED DISEASES
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The present invention relates to a pharmaceutical composition comprising a morphinan derivative that exhibits an opioid δ receptor agonist activity. By administering the pharmaceutical composition provided by the present invention, opioid δ receptor-related diseases (for example, headache) can be treated or prevented.
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Paragraph 0202; 0203; 0204
(2019/08/01)
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- CRYSTALLINE FORMS AND COMPOSITIONS OF CFTR MODULATORS
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Crystalline Forms of Compound I: and pharmaceutically acceptable salts thereofare disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.
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Paragraph 0489; 0490
(2019/05/07)
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- MORPHINAN DERIVATIVE
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A morphinan derivative represented by the following general formula (I): (wherein R1 represents hydrogen, C1-10 alkyl, cycloalkylalkyl where the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms, etc., R2 represents heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S and at least one carbon atom as ring-constituting atoms, containing at least one set of adjacent ring-constituting atoms bound by a double bond, and further substituted with at least one oxo group, Y binds to a carbon atom as a ring-constituting atom of R2, R3, R4, and R5 represent hydrogen; hydroxy, etc., R6a and R6b represent hydrogen, etc., R7 and R8 represent hydrogen, etc., R9 and R10, which are the same or different, represent hydrogen, etc., X represents O or CH2, and Y represents C(=O)), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof is used as an anxiolytic drug, antidepressant, etc.
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Paragraph 0219; 0220
(2018/03/02)
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- MODULATOR OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR, PHARMACEUTICAL COMPOSITIONS, METHODS OF TREATMENT, AND PROCESS FOR MAKING THE MODULATOR
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Compounds of Formula (I), pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.
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Paragraph 00263; 00264
(2018/04/17)
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- Preparation method of topramezone
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The invention discloses a preparation method of topramezone. The particularly comprises the steps of carrying out cyclization, methylation, hydrolysis, amidation, Grignard reaction, oxidation and demethylation on 2-(alkoxymethylene)malonate as a raw material, so as to obtain a target product, wherein the yield of the target product reaches 61.8%-63.2%. According to the preparation method, the raw materials such as a palladium/platinum catalyst which is high in cost and difficult to recycle, a virulent rearrangement catalyst and high-cost methylhydrazine are not adopted, and the preparation method which is low in cost, easy in operation, low in pollution and accordant with large-scale industrial production requirements is provided.
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Paragraph 0040; 0042; 0043; 0057; 0071
(2017/11/29)
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- N-((HETEROARYLMETHYL)-HETEROARYL-CARBOXAMIDE DERIVATIVES AS PLASMA KALLIKREIN INHIBITORS
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The present invention provides a selection of compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds.
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Page/Page column 48
(2016/06/14)
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- 1-(HET)ARYLSULFONYL-(PYRROLIDINE OR PIPERIDINE)-2-CARBOXAMIDE DERIVATIVES AND THEIR USE AS TRPA1 ANTAGONISTS
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The invention is concerned with the compounds of formula I and salts thereof and other compounds of formulas II-IX as disclosed herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formulas I-IX as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain or asthma.
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Paragraph 0755; 0756; 0757
(2016/09/22)
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- Use of activated enol ethers in the synthesis of pyrazoles: Reactions with hydrazine and a study of pyrazole tautomerism
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Activated enol ethers derived from esters or the dinitrile of malonic acid, or from pentane-2,4-dione were treated with hydrazine hydrate. The structures of the obtained products - pyrazoles 5 - were studied with a focus on tautomerism and supramolecular structure. A reverse addition of the reagents led to the isolation of two novel products, namely bis-enehydrazines 6 with an unsymmetrical arrangement of the formally equivalent subunits.
- Tarabova, Denisa,Soralova, Stanislava,Breza, Martin,Fronc, Marek,Holzer, Wolfgang,Milata, Viktor
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supporting information
p. 752 - 760
(2014/05/06)
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- Alkoxypyrazoles and the process for their preparation
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The present invention relates to a process for the preparation of alkoxypyrazoles and new alkoxypyrazole compounds.
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Page/Page column 7; 12
(2010/03/02)
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- 5-Iodo-3-ethoxypyrazoles: An entry point to new chemical entities
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Our program, which has focused on the preparation of new pyrazole derivatives, has led us to report here an original and simplified preparation of ethyl 3-ethoxy-lW-pyrazole-4-carboxylate. This is based on the reaction of hydrazine monohydrochloride and diethyl 2-(ethoxymethylene)malonate. Further transformations of this key compound allowed the preparation of the two possible iodinated isomers, namely, 3-ethoxy-4-iodo- and 3-ethoxy-5-iodo-1H-pyrazole. These compounds have opened the way to a quick access to many original pyrazole series. As an illustration, we report here on the selectivity of N-arylation, by using the Lam and Cham method, the C4- and C5-arylation of some of these 3-ethoxy-pyrazole derivatives by using the Suzuki-Miyaura reaction, and C5-benzylation reactions by means of the Negishi reaction. This was followed by hydrolysis of the ethoxy group, which led to the corresponding pyrazol-3-one derivatives. As a conclusion of this work, we conducted an investigation into the regiochemistry of the condensation between diethyl 2-(ethoxymethylene) malonate and the hydrochloride salts of methyl, benzyl, or phenyl hydrazine.
- Guillou, Sandrine,Janin, Yves L.
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experimental part
p. 4669 - 4677
(2010/08/06)
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- AMIDE DERIVATIVES AS ION-CHANNEL LIGANDS AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME
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Compounds are disclosed that have a formula represented by the following: (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including
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Page/Page column 56
(2009/09/04)
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- 5-MEMBERED HETEROCYCLIC AMIDES AND RELATED COMPOUNDS
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5-Membered heterocyclic amides and related compounds are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly usef
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Page/Page column 82
(2009/03/07)
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- Vitamin D derivatives with cyclic substructures in the side chains, process and intermediate products for their production, and the use for the production of pharmaceutical agents
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The invention relates to vitamin D derivatives of general formula I, process for their production, intermediate products of the process as well as the use for the production of pharmaceutical agents.
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- Bone targeted drugs 2. Synthesis of estrogens with hydroxyapatite affinity
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The utility of the bone targeting 4-carboxy-3-hydroxy-1,2-pyrazole heterocycle was tested by the synthesis of hybrids with the non-steroidal estrogen hexestrol. Compounds 1 and 2 demonstrated significant hydroxyapatite affinity, while maintaining weak estrogenic activity in whole cell assays. Copyright
- Willson, Timothy M.,Henke, Brad R.,Momtahen, Tanya M.,Garrison, Deanna T.,Moore, Linda B.,Geddie, Nora G.,Baer, Philip G.
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p. 1047 - 1050
(2007/10/03)
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- Diversity of Intramolecular Rearrangements of Uracil Derivatives to Pyrazolones and Hydantoins Governed by a Prominent 5-Substituent Effect
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Reaction of 1,3-dimethyluracil-5-carbohydrazides (4) with sodium ethoxide gave 4-ethoxycarbonyl-1,2-dihydro-3-pyrazolones (5) via a conventional intramolecular nucleophilic attack at the 6-position.In contrast, 1,3-disubstituted 5-(3-methylureido)uracil derivatives (6) were converted into the corresponding 3-methyl-5-ureidomethylenehydantoins (7) under analogous conditions.The latter rearrangement is unprecedented on account of the involvement of an initial nucleophilic attack at the 4-carbonyl carbon.The diversity of the intramolecular rearrangements of the uracil ring can be explained in terms of electronic nature of the substituent a t the 5-position.
- Kitade, Yukio,Hirota, Kosaku,Maki, Yoshifumi
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p. 101 - 112
(2007/10/02)
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- PHOTOCHEMICAL SYNTHESIS OF 4-ETHOXYCARBONYL-5-HYDROXYPYRAZOLES
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The photochemical decomposition of 4-ethoxycarbonyl-5-diazopyrazoles in tetrafluoroboric acid results in corresponding 4-ethoxycarbonyl-5-hydroxypyrazoles (V-VII).The irradiation of the diazocompound in dioxane, toluene or tetrahydrofurane proceeds with a reductive decomposition producing corresponding 4-ethoxycarbonylpyrazole (VIII) as the main photoproduct.
- Spassova, Maria K.,Zakharieva, Rossitza D.
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p. 196 - 199
(2007/10/02)
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