- CYCLOALKANE-1,3-DIAMINE DERIVATIVE
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The present invention provides a compound or a pharmaceutically acceptable salt thereof having an inhibitory action on the interaction between menin and an MLL protein. The compound represented by the formula (1) or a pharmaceutically acceptable salt thereof. wherein, in the formula (1), the dotted circle, R1, R2, R3, R4, R5, R6, R7, R8, Ring Q1, W, m and n are each as defined in the description.
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- Optical pure amino alcohol hydrochloride preparation method
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The invention relates to a preparation method for optically pure aminoalcohol hydrochloride. The optically pure aminoalcohol hydrochloride is any one selected from optically pure aminoalcohol hydrochloride 1 and optically pure aminoalcohol hydrochloride 2 and is prepared by subjecting a compound 4 to an esterification ring-opening reaction, an amino protection reaction, an ester reduction reaction and a deprotection salt forming reaction. The optically pure aminoalcohol hydrochloride 1 or optically pure aminoalcohol hydrochloride 2 prepared in the invention can be directly used for synthesis of abacavir and carbovir. The preparation method provided by the invention has the advantages of high product optical purity, stable product quality, high product yield, a small amount of environmental pollution, low production cost, easy industrialization, etc.
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- PYRIMIDINE AND PYRIDINE DERIVATIVES AND USE IN TREATMENT, AMELIORATION OR PREVENTION OF INFLUENZA THEREOF
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Provided herein is a compound of formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, codrug, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameliorating or preventing influenza.
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Page/Page column 128
(2017/12/28)
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- OCTAHYDRO-CYCLOPENTAPYRROLYL ANTAGONISTS OF CCR2
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The present invention comprises compounds of Formula (I). Formula (I) wherein: R1, R2, R3, R4, R5, Z1 and Z2 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
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- Chiral aminocyclopentene-based cycloaddition strategies to bicyclic [3.3.0] rings
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Two cycloaddition methods were applied to chiral protected aminocyclopentenes 2 and 9 and provided novel bicyclic products 3 and 4 in good yields. The explanation for the observed stereochemistry was based on the sterically encumbered β-face forcing the c
- Cai, Chaozhong,Kang, Fu-An,Beauchamp, Derek A.,Sui, Zhihua,Russell, Ronald K.,Teleha, Christopher A.
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p. 651 - 656
(2013/07/05)
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- FUSED CYCLOPENTYL ANTAGONISTS OF CCR2
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The present invention comprises compounds of Formula (I). wherein: R0, R1, R2, R3, R4, R5, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I)
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Page/Page column 82-83
(2013/10/22)
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- Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist
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We report the discovery of a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist (3S,4S)-N-[(1R,3S)-3-isopropyl-3-({4-[4- (trifluoromethyl)pyridin-2-yl]piperazin-1-yl}carbonyl)cyclopentyl] -3-methoxytetrahydro-2H-pyran-4-amine (19). After evaluation in 28-day toxicology studies, compound 19 (INCB10820/PF-4178903) was selected as a clinical candidate.
- Zheng, Changsheng,Cao, Ganfeng,Xia, Michael,Feng, Hao,Glenn, Joseph,Anand, Rajan,Zhang, Ke,Huang, Taisheng,Wang, Anlai,Kong, Ling,Li, Mei,Galya, Laurine,Hughes, Robert O.,Devraj, Rajesh,Morton, Phillip A.,Rogier, D. Joseph,Covington, Maryanne,Baribaud, Fred,Shin, Niu,Scherle, Peggy,Diamond, Sharon,Yeleswaram, Swamy,Vaddi, Kris,Newton, Robert,Hollis, Greg,Friedman, Steven,Metcalf, Brian,Xue, Chu-Biao
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scheme or table
p. 1442 - 1446
(2011/04/22)
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- PRODUCTION OF TRANS-4-AMINOCYCLOPENT-2-ENE-1-CARBOXYLIC ACID DERIVATIVES
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Methods of producing compositions of trans-4-amino-2-cyclopentene-1-carboxylic acid derivatives are described. Also described is an amine salt of a compound having formula A, having components present in both cis and trans structures.
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Page/Page column 14-15
(2011/02/24)
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- Heterocyclic cyclopentyl tetrahydroisoquinoline and tetrahydropyridopyridine modulators of chemokine receptor activity
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The present invention is directed to compounds of the formula I: Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
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Page/Page column 37-38
(2008/06/13)
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- BENZOXAZINYL-AMIDOCYCLOPENTYL-HETEROCYCLIC MODULATORS OF CHEMOKINE RECEPTORS
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Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.
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Page/Page column 25
(2010/11/28)
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- 3-AMINOCYCLOPENTANECARBOXAMIDES AS MODULATORS OF CHEMOKINE RECEPTORS
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The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.
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Page/Page column 22-23
(2008/06/13)
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- 3-(4-Heteroarylcyclohexylamino)cyclopentanecarboxamides as modulators of chemokine receptors
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The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or act
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Page/Page column 8; 17-18
(2010/02/14)
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- TETRAHYDROPYRAN HETEROCYCLIC CYCLOPENTYL HETEROARYL MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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The present invention is further directed to compounds of the formulas: (I) (II) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24 and R25 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.
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- HETEROCYCLIC CYCLOPENTYL TETRAHYDROISOQUINOLINE AND TETRAHYDROPYRIDOPYRIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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The present invention is directed to compounds of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
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- BENZOXAZINYL-AMIDOCYCLOPENTYL-HETEROCYCLIC MODULATORS OF CHEMOKINE RECEPTORS
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Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula (I): which are used to modulate the CCR-
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- TETRAHYDROPYRANYL CYCLOPENTYL TETRAHYDROPYRIDOPYRIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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The present invention is directed to compounds of the formula (I): (wherein R3 et R8 are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
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Page/Page column 28
(2010/02/07)
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- An efficient route to all eight stereoisomers of a tri-functionalised cyclopentane scaffold for drug discovery
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A route to all eight stereoisomers of 3-(tert-butoxycarbonylamino)-4-hydroxycyclopentanecarboxylic acid methyl ester is presented; these products should prove to be valuable scaffolds in pharmaceutical discovery.
- Smith, Mark E.B.,Lloyd, Michael C.,Derrien, Nadine,Lloyd, Richard C.,Taylor, Stephen J.C.,Chaplin, David A.,Casy, Guy,McCague, Raymond
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p. 703 - 705
(2007/10/03)
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- Inhibition and substrate activity of conformationally rigid vigabatrin analogues with γ-aminobutyric acid aminotransferase
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Several cyclopentene GABA analogues were synthesized as conformationally rigid analogues of the epilepsy drug vigabatrin and tested as inhibitors and substrates of γ-aminobutyric acid aminotransferase (GABA-AT). None of these compounds produced time-dependent inhibition. (1R,4S)-(+)-4-Amino-2- cyclopentene-1-carboxylic acid ((+)-3), (4R)-(-)-4-amino-1-cyclopentene-1- carboxylic acid ((-)-4), and d,l-3-amino-1-cyclopentene-1-carboxylic acid (6) are good substrates. The K(m) and k(cat) values for the latter two compounds are very similar to those of GABA, suggesting that they bind in an orientation similar to that of GABA. The K(m) value for (+)-3 is 24 times lower than that for GABA, although its k(cat) value is only one-fourth that for GABA; nonetheless, it is a better substrate for GABA-AT than is GABA. All of these compounds, as well as the enantiomers of 3 and 4 and d,l-trans-4- amino-2-cyclopentene-1-carboxylic acid (5), are competitive inhibitors of GABA-AT. These results demonstrate the effects of the carboxylate group orientation and the stereochemistry of the amino and carboxylate groups on the substrate activity and inhibitor activity, and this should be important to the future design of inhibitors of GABA-AT.
- Qiu, Jian,Pingsterhaus, Joyce M.,Silverman, Richard B.
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p. 4725 - 4728
(2007/10/03)
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