27067-03-4Relevant academic research and scientific papers
PEPTIDOMIMETIC N5-METHYL-N2-(NONANOYL-L-LEUCYL)-L-GLUTAMINATE DERIVATIVES, TRIAZASPIRO[4.14]NONADECANE DERIVATIVES AND SIMILAR COMPOUNDS AS INHIBITORS OF NOROVIRUS AND CORONAVIRUS REPLICATION
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Paragraph 00455; 00634-00635, (2021/09/26)
Peptidomimetic N5-methyl-N2-(nonanoyl-L-leucyl)-L-glutaminate derivatives, triazaspiro[4.14]nonadecane derivatives and similar compounds for use in methods of inhibiting the replication of noroviruses and coronaviruses in a biological sample or patient, for use in reducing the amount of noroviruses or coronaviruses in a biological sample or patient, and for use in treating norovirus and coronavirus in a patient, comprising administering to said biological sample or patient a safe and effective amount of a compound represented by formulae I or II, or a pharmaceutically acceptable salt thereof. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. page 99 to page 271; examples 1 to 3; compounds A1 to A104 and Bl to B66; tables A to E).
INHIBITORS OF NOROVIRUS AND CORONAVIRUS REPLICATION
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Paragraph 00269-00271; 00385-00387; 00671-00673, (2021/10/15)
Compounds of Formula (I) and methods of inhibiting the replication of viruses in a biological sample or patient, of reducing the amount of viruses in a biological sample or patient, and of treating a virus infection in a patient, comprising administering to said biological sample or patient an effective amount of a compound represented by Formula (I), a compound of Table A or B or a pharmaceutically acceptable salt thereof.
Method for producing hematopoietic stem cells using pyrazole compounds
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Page/Page column 183, (2016/01/10)
An expanding agent for hematopoietic stem cells and/or hematopoietic progenitor cells useful as a therapy for various hematopoietic diseases and useful for improvement in the efficiency of gene transfer into hematopoietic stem cells for gene therapy is provided. A method of producing hematopoietic stem cells and/or hematopoietic progenitor cells, which comprises expanding hematopoietic stem cells by culturing hematopoietic stem cells ex vivo in the presence of a compound represented by the formula following (I), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof (wherein R1 to R8 are as defined in the description).
PYRAZOLE COMPOUNDS HAVING THERAPEUTIC EFFECT ON MULTIPLE MYELOMA
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Paragraph 0262; 0263, (2013/10/07)
Novel therapeutic agents for myeloma are provided. A therapeutic agent for multiple myeloma containing a pyrazole compound represented by the formula (1): wherein R1 is C1-C6 alkyl, C1-C6 alkyl substituted with R17, C1-C6 haloalkyl, phenyl, phenyl substituted with a R11's or the like, R2 is a hydrogen atom, C1-C6 alkyl, phenyl or phenyl optionally substituted with e R21's or the like, R3 is a hydrogen atom or the like, X is a single bond or —(CR6, R7)n—, each of R4 and R5 is independently C1-C6 alkyl or the like, R6 and R7 are hydrogen atoms or C1-C6 alkyl, R8 is phenyl, phenyl optionally substituted with k R81's or the like, a tautomer of the compound or a pharmaceutically acceptable salt or solvate thereof, as an active ingredient.
AMINOETHYLAROMATIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
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Page/Page column 97, (2010/11/08)
The present invention relates to aromatic compounds of the formula (I) wherein Ar is phenyl or an aromatic 5-or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; E is CR6R7 or NR3;R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated Cl-C4--alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C 4-cycloalkylmethyl, fluorinated C3-C4--alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1--C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C 3-C4-cycloalkylmethyl, fluorinated C3--C 4-alkenyl, or R1a and R2 together are (CH 2)n with n being 2, 3 or 4, or R1a and R 2a together are (CH2)n with n being 2, 3 or 4; R2 and R2a are independently of each other H, C1-C4-alkyl or fluorinated C1-C 4-alkyl or R2a and R2 together are (CH 2)m with m being 1, 2, 3, 4 or 5; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, fluorine, C1-C4-alkyl and fluorinated C1-C4-alkyl or together form a moiety (CH2)p with p being 2, 3, 4 or 5; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.
PHTHALAMIDE DERIVATIVES FOR USE AS INSECTICIDES
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Page/Page column 70, (2010/10/20)
Compounds of formula (I), wherein the substituents are as defined in claim (1), and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula (I) can be used as agrochemical active ingredients and can be pr
Substituted cycloalkyl derivatives for the treatment of respiratory diseases
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Page/Page column 19, (2008/06/13)
N-(Phenyl-substituted cycloalkyl or cycloalkylmethyl)-phenylethanolamine derivatives (I) (including benzo-heterocyclic analogs) are new. Also new are cyclopropylamine or cyclopropylmethylamine derivative intermediates (II). Phenylethanolamine derivatives of formula (I) (including optical isomers, enantiomer mixtures and racemates) and their salts, solvates and hydrates are new. n : 0 or 1; m : 1-4; X : direct bond, 2-6C alkenylene, -O-Q-, -NH-Q-, -S-Q- or -Q-; Q : 1-6C alkylene; R 1>H; and R 3>hydroxyalkyl or halo; or R 1> + R 2>OCH 2CONH, CH 2CH 2CONH, CH=CHCONH, NHCH 2CONH, SCH 2CONH, OCONH, SCONH, NHCONH or OCH 2SO 2NH (all optionally substituted (os) by 1 or 2 of alkyl, OH or halo); R 3>, R 4>H, OH, halo, 1-6C alkyl, 1-6C haloalkyl, 1-6C hydroxyalkyl, NH 2 or mono- or dialkylamino; R 5> - R 8>H, OR 9>, halo, 1-6C alkyl, 1-6C haloalkyl, 1-6C hydroxyalkyl, 3-6C cycloalkyl, 3-6C hydroxycycloalkyl, CN, NO 2, COR 9>, COOR 9>, CONR 10>R 11>, NR 10>R 11>, NR 10>COR 9>, NR 10>SO 2R 12>, SR 12>, SOR 12>, SO 2R 12>, SO 2NR 10>R 11> or halo; or two vicinal groups R 6> - R 8> together= 2-6C alkylene, 2-6C alkenylene or O-Q-O (all os by 1 or 2 of alkyl, alkoxy, OH or halo); R 9> - R 11>H, alkyl, aryl or arylalkyl; R 12>alkyl, aryl or arylalkyl; unless specified otherwise alkyl moieties have 1-4C and aryl moieties 6-10C. An independent claim is included for cycloalkylamine or cycloalkylalkylamine derivative intermediates of formula (II) as new compounds, provided that m= 1. [Image] [Image] ACTIVITY : Antiinflammatory; antiasthmatic; antiallergic; virucide; antibacterial; fungicide; protozoacide; anthelmintic; cardiant; dermatological; immunosuppressive; tocolytic; antiarrhythmic; vasotropic; antipruritic. MECHANISM OF ACTION : beta -Mimetic.
New and easy route to primary cyclopropylamines from nitriles
Bertus,Szymoniak
, p. 1792 - 1793 (2007/10/03)
Starting from readily available substrates, we have developed a new synthesis of primary cyclopropylamines. The reaction involves a cooperative Ti(II)- and Lewis acid-mediated coupling of alkanenitriles with Grignard reagents.
