862129-72-4Relevant academic research and scientific papers
PYRIDINYL PYRAZOLES AS MODULATORS OF RORyT
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Paragraph 0203, (2020/01/08)
The present invention comprises compounds of Formula I. wherein: R1, R3, R4, R5, R6, and Q are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-γ-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
PHENYL AND PYRIDINYL SUBSTITUTED IMIDAZOLES AS MODULATORS OF RORyT
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Paragraph 0266-0267, (2020/01/08)
The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, Ra, Rb, Q1, and Q2 are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-γ-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
6-AMINOPYRIDIN-3-YL PYRAZOLES AS MODULATORS OF RORgT
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Paragraph 0187-0188, (2020/01/08)
The present invention comprises compounds of Formula I. wherein: R1, Q, R3, R4, R5, R6, A1, and A2 are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-γ-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
PHENYL SUBSTITUTED PYRAZOLES AS MODULATORS OF RORgT
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Paragraph 0287-0288, (2020/01/09)
The present invention comprises compounds of Formula I. wherein: R1, R3, R4, R5, R6, R7, R8, and Q are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-γ-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
SUBSTITUTED 5-CYANOINDOLE COMPOUNDS AND USES THEREOF
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Paragraph 00300, (2019/01/10)
A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for the treatment of lysine (K)-specific demethylase 1A (LSD1) - mediated diseases or disorders, Formula (I), wherein R1, R2, R3, R4, and R5 are as defined herein.
C-3 AND C-17 MODIFIED TRITERPENOIDS AS HIV-1 INHIBITORS
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Page/Page column 209; 210, (2017/12/28)
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula (I). These compounds are useful for the treatment of HIV and AIDS.
TRITERPENOIDS WITH HIV MATURATION INHIBITORY ACTIVITY, SUBSTITUTED IN POSITION 3 BY A NON-AROMATIC RING CARRYING A HALOALKYL SUBSTITUENT
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, (2015/11/03)
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: with X selected from C4-8 cycloalkyl, C4-8 cycloalkenyl, C4-9 spirocycloalkyl, C4-9 spirocycloalkenyl, C4-8 oxacycloalkyl, C4-8 dioxacycloalkyl, C6-8 oxacycloalkenyl, C6-8 dioxacycloalkenyl, C6 cyclodialkenyl, C6 oxacyclodialkenyl, C6-9 oxaspirocycloalkyl and C6-9 oxaspirocycloalkenyl ring, such that X is substituted with A, wherein A is -C1-6 alkyl- halo. These compounds are useful for the treatment of HIV and AIDS.
STRAIGHTFORWARD ENTRY TO 7-AZABICYCLO[2.2.1]HEPTANE-1-CARBONITRILES AND SUBSEQUENT SYNTHESIS OF EPIBATIDINE ANALOGUES
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Page/Page column 7, (2009/12/02)
The present invention relates to a group of substituted-7-azabicyclo-[2.2.1]heptyl derivatives with biological activity. The present invention also relates to synthetic methods for producing said substituted-7-azabicyclo-[2.2.1]heptyl derivatives. The present invention also relates to certain intermediates for producing such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as a synthetic method for producing such intermediates. The present invention also relates to pharmaceutical compositions comprising such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as their use as medicaments for the treatment of diseases mediated by a Nicotinic Acetylcholine Receptor or a receptor being a member of the Neurotransmitter-gated Ion Channel Superfamily, such as pain, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy and nicotine addiction.
Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety
Richardson, Timothy I.,Frank, Scott A.,Wang, Minmin,Clarke, Christian A.,Jones, Scott A.,Ying, Bai-Ping,Kohlman, Dan T.,Wallace, Owen B.,Shepherd, Timothy A.,Dally, Robert D.,Palkowitz, Alan D.,Geiser, Andrew G.,Bryant, Henry U.,Henck, Judith W.,Cohen, Ilene R.,Rudmann, Daniel G.,McCann, Denis J.,Coutant, David E.,Oldham, Samuel W.,Hummel, Conrad W.,Fong, Kin C.,Hinklin, Ronald,Lewis, George,Tian, Hongqi,Dodge, Jeffrey A.
, p. 3544 - 3549 (2008/02/07)
Structure-activity relationship studies are described, which led to the discovery of novel selective estrogen receptor modulators (SERMs) for the potential treatment of uterine fibroids. The SAR studies focused on limiting brain exposure and were guided by computational properties. Compounds with limited impact on the HPO axis were selected using serum estrogen levels as a biomarker for ovarian stimulation.
SELECTIVE ESTROGEN RECEPTOR MODULATORS
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Page/Page column 10-11, (2008/06/13)
The present invention relates to a selective estrogen receptor modulator of formula I: or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and uterine leiomyoma.
