- 2-ALKOXY-6-[18F]FLUORONICOTINOYL SUBSTITUTED LYS-C(O)-GLU DERIVATIVES AS EFFICIENT PROBES FOR IMAGING OF PSMA EXPRESSING TISSUES
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6-[18HF]Fluoro-2-alkoxynicotinoyl substituted Lys-C(O)-Glu derivatives were identified as efficient imaging probes for PSMA expressing tissues in comparison to other known PSMA specific ligands like [18F]DCFPyL, [68Ga]HBED-CC-PSMA, [
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Page/Page column 11; 30
(2019/10/04)
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- HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Heterocyclic compounds as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
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Paragraph 0424-0426
(2019/04/25)
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- PYRIMIDINE TBK/IKKε INHIBITOR COMPOUNDS AND USES THEREOF
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The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKKε inhibitors.
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Paragraph 00248
(2019/05/10)
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- PYRIDINYL PYRAZOLES AS MODULATORS OF RORyT
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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.
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Paragraph 0461
(2020/01/08)
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- 6-AMINOPYRIDIN-3-YL PYRAZOLES AS MODULATORS OF RORgT
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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.
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Paragraph 0310-0311
(2020/01/08)
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- PYRIDINYL-SUBSTITUTED PYRAZOLYL CARBOXAMIDES
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The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to methods of using these compounds for the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.
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- Structure-based design of substituted piperidines as a new class of highly efficacious oral direct renin inhibitors
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A cis-configured 3,5-disubstituted piperidine direct renin inhibitor, (syn,rac)-1, was discovered as a high-throughput screening hit from a target-family tailored library. Optimization of both the prime and the nonprime site residues flanking the central piperidine transition-state surrogate resulted in analogues with improved potency and pharmacokinetic (PK) properties, culminating in the identification of the 4-hydroxy-3,5-substituted piperidine 31. This compound showed high in vitro potency toward human renin with excellent off-target selectivity, 60% oral bioavailability in rat, and dose-dependent blood pressure lowering effects in the double-transgenic rat model.
- Ehara, Takeru,Irie, Osamu,Kosaka, Takatoshi,Kanazawa, Takanori,Breitenstein, Werner,Grosche, Philipp,Ostermann, Nils,Suzuki, Masaki,Kawakami, Shimpei,Konishi, Kazuhide,Hitomi, Yuko,Toyao, Atsushi,Gunji, Hiroki,Cumin, Frederic,Schiering, Nikolaus,Wagner, Trixie,Rigel, Dean F.,Webb, Randy L.,Maibaum, Jurgen,Yokokawa, Fumiaki
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p. 787 - 792
(2014/08/05)
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- ALKYL-AMIDE-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFNα RESPONSES
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Compounds having the following formula (I): or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.
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Paragraph 00163
(2014/05/24)
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- TRICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
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The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthama, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases. (I)
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- ORGANIC COMPOUNDS
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The present invention relates to a compound of the formula I wherein R1, R2, R3, R4 and R5 are as defined in the specification, for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations a compound of that class; a method of treatment comprising administering a compound of that class and a method for its manufacture.
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Page/Page column 25
(2009/01/24)
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