- CYCLOALKYLIDENE CARBOXYLIC ACIDS AND DERIVATIVES AS BTK INHIBITORS
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The present invention relates to novel cycloalkylidene carboxylic acids and derivatives thereof useful as Bruton tyrosine kinase (BTK) inhibitors. The present disclosure also relates to processes for their preparation, pharmaceutical compositions containing one or more such compounds, and to the use of such compounds and pharmaceutical compositions for the treatment of disorders involving mediation of BTK in humans (Formula I).
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Page/Page column 138-139
(2021/03/05)
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- COMPOUNDS THAT INHIBIT MCL-1 PROTEIN
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Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
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Page/Page column 337; 338
(2017/09/15)
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- Containing cyclobutane substituent of pyrazines, its composition and use thereof
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The invention relates to a cyclobutane substituent group-containing pyrazine compound and application thereof as a drug, and particularly relates to application of the cyclobutane substituent group-containing pyrazine compound in preparing the drug for preventing and treating various influenza viruses. Especially, the invention relates to a compound as shown in a general formula (I) or a stereomer, a geometrical isomer, a tautomer, a nitrogen oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and various variables are defined in the specification. The invention also relates to application of the compound as shown in the general formula (I) or the stereomer, geometrical isomer, tautomer, nitrogen oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug thereof as the drug, and particularly relates to application of the compound as shown in the general formula (I) or the stereomer, geometrical isomer, tautomer, nitrogen oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug thereof as the drug for preventing and treating the influenza viruses.
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- Containing cyclobutane substituent of pyrazines, its composition and use thereof
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The invention relates to a pyrazine compound containing a diethylene substituent and application thereof as a medicine, particularly application thereof to preparation of medicines for preventing and treating various influenza viruses. Particularly, the invention relates a compound of which the general formula I is shown in the specification, or a stereoisomer, a geometrical isomer, a tautomer, a nitrogen oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and all variables are defined in the specification. The invention also relates to application of the compound of which the general formula I is shown in the specification, or the stereoisomer, the geometrical isomer, the tautomer, the nitrogen oxide, the hydrate, the solvate, the metabolite, the pharmaceutically acceptable salt or the prodrug thereof as medicines, particularly application of the compound as a medicine for preventing and treating influenza viruses.
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- Substituted purine neuraminidase inhibitor and method of use thereof, and use thereof
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The invention provides novel substituted purine compounds or stereoisomers, tautomers, nitric oxides, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof. The substituted purine compounds are used for inhibiting neuraminidase. The invention also provides a drug composition comprising the compounds, and a method for preventing or treating virus infectious diseases by using the compounds or the drug composition.
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- CYCLOBUTANE CONTAINING CARBOXYLIC ACID GPR120 MODULATORS
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The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.
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Paragraph 00223
(2016/06/01)
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- OXAZOLIDINONES AS MODULATORS OF MGLUR5
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The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.
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- The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: A novel potent antibacterial analog derived from hygromycin A
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SAR studies and optimization of various modified Hygromycin A fluoroalkyl ethers, which led to the discovery of the highly potent 4′-(2-cyclopropyl- 2-fluoroethyl ether) antibacterial CE-156811 (1) derived from truncation of the ribose ring and difluorination of the phenyl found in Hygromycin A, are discussed.
- Le, Phuong T.,Brickner, Steven J.,Wade, Sarah K.,Brighty, Katherine,Monahan, Rhonda,Stone, Gregory G.,Girard, Dennis,Finegan, Steve,Duignan, Joan,Schafer, John,Maloney, Meghan,Zaniewski, Richard P.,Connolly, Ann G.,Liras, Jennifer,Bordner, Jon,Samardjiev, Ivan
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scheme or table
p. 276 - 279
(2011/02/27)
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- Pyrazole glucokinase activators
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Disclosed herein are pyrazole glucokinase activators of the formula (I) useful for the treatment of metabolic diseases and disorders, preferably diabetes mellitus.
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- 1-(1-CYCLOBUTYL-4-PIPERIDINYL)-1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES WHICH HAVE ACTIVITY ON THE ML RECEPTOR AND THEIR USE IN MEDICINE
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Compounds of formula I or a salt thereof are provided wherein R4, R5, R6, Q, L and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders and cognitive impairments are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
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- HETEROARYL AMIDES AS TYPE I GLYCINE TRANSPORT INHIBITORS
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The present invention relates to a series of substituted heteroaryl amides of the Formula I, wherein HET, A, X1 -X4, and R1-R12 groups are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.
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Page/Page column 32; 33-34
(2008/12/06)
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- OXINDOLE DERIVATIVE AS FEEDING CONTROL AGENT
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Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.)
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Page/Page column 22
(2008/12/06)
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- Histamine-3 receptor modulators
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This invention is directed to a compound of the formula I as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by modulating histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-intestinal tract, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above.
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Page/Page column 18
(2010/02/13)
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- An efficient route to 3-substituted cyclobutanone derivatives
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An efficient route to 3-(hydroxymethyl)cyclobutanone acetals via a [2+2] cycloaddition reaction is reported. The dramatic effect of different diol acetals on benzyl deprotection is discussed. Efficient synthesis of two synthetically useful intermediates, 3-methylenecyclobutanone acetal and 3-(bromomethyl)cyclobutanone, are provided.
- Kabalka, George W.,Yao, Min-Liang
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p. 1879 - 1881
(2007/10/03)
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- A new entry into 2-azabicyclo[2.1.1]hexanes via 3-(chloromethyl)cyclobutanone
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2-Azabicyclo[2.1.1]hexanes, which possess the skeleton of 2,4-methanoproline (a naturally occurring insect antifeedant), were synthesized by imination of the previously unknown 3-(chloromethyl)cyclobutanone and subsequent reductive cyclization. The precursor of the latter, 3-oxocyclobutane carboxylic acid, was prepared by two pathways in multigram quantities.
- Stevens,De Kimpe
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p. 2174 - 2178
(2007/10/03)
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