- SOLID FORMS OF 3-(5-AMINO-2-METHYL-4-OXO-4H-QUINAZOLIN-3-YL)-PIPERIDINE-2,6-DIONE, AND THEIR PHARMACEUTICAL COMPOSITIONS AND USES
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Solid forms comprising 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)- piperidine-2,6-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their uses are disclosed.
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Paragraph 00426
(2018/09/28)
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- METHODS FOR TREATING CHRONIC LYMPHOCYTIC LEUKEMIA AND THE USE OF BIOMARKERS AS A PREDICTOR OF CLINICAL SENSITIVITY TO IMMUNOMODULATORY THERAPIES
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A method of identifying a subject having chronic lymphocytic leukemia (CLL) who is likely to be responsive to a treatment compound, comprising obtaining a first sample and a second sample from the subject having CLL; administering 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione (Compound A) to the first sample and administering lenalidomide to the second sample; determining the level of a biomarker in the first sample and determining the level of the biomarker in the second sample; and diagnosing the subject as being likely to be responsive to the treatment compound if the level of the biomarker in the first sample is different from the level of the biomarker in the second sample.
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Paragraph 00341
(2017/02/28)
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- METHODS FOR TREATING DIFFUSE LARGE B-CELL LYMPHOMA AND THE USE OF BIOMARKERS AS A PREDICTOR OF RESPONSIVENESS TO DRUGS
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In one aspect, provided herein are methods for predicting the responsiveness of DLBCL patients to treatment with lenolidomide or Compound A; or a stereoisomer thereof; or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate thereof; or a polymorph thereof utilizing biomarkers or classfiers that correlate with responsiveness to one of these drugs. In another aspect, provided herein are methods for treating a DLBCL patient determined to be responsive to treatment with lenolidomide or Compound A; or a stereoisomer thereof; or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate thereof; or a polymorph thereof utilizing biomarkers or classifiers (or output thereof) that correlate with responsiveness to one of these drugs.
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Paragraph 00170
(2017/04/11)
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- CYCLING THERAPY USING 3-(5-AMINO-2-METHYL-4-OXO-4H-QUINAZOLIN-3-YL)-PIPERIDINE-2,6-DIONE
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Provided herein are methods of treating, preventing and/or managing cancer, including lymphoma, which comprise administering to a patient 3-(5-amino-2-methyl-4- oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione, or an enantiomer or a mixture of enantiomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate, or polymorph thereof in a cyclic therapy regimen.
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Paragraph 00201; 00202
(2017/08/04)
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- COMPOSITIONS AND METHODS FOR INDUCING CONFORMATIONAL CHANGES IN CEREBLON AND OTHER E3 UBIQUITIN LIGASES
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Provided herein are compositions, therapeutic methods, screening methods, computational methods and biomarkers based upon the elucidation of the interaction among cereblon, its substrates and certain compounds or agents, including small molecules, peptides, and proteins.
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Paragraph 00457
(2017/07/14)
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- METHODS FOR TREATING SOLID TUMORS AND THE USE OF BIOMARKERS AS A PREDICTOR OF CLINICAL SENSITIVITY TO IMMUNOMODULATORY THERAPIES
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A method of identifying a subject having a solid tumor who is likely to be responsive to a treatment compound, comprising: administering the treatment compound to a subject having the solid tumor; obtaining a sample from the subject; determining the level of a biomarker in the sample from the subject, and diagnosing the subject as being likely to be responsive to the treatment compound if the level of the biomarker in the sample of the subject changes as compared to a reference level of the biomarker.
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Paragraph 00462
(2016/05/24)
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- Zn-Catalyzed Enantio- and Diastereoselective Formal [4 + 2] Cycloaddition Involving Two Electron-Deficient Partners: Asymmetric Synthesis of Piperidines from 1-Azadienes and Nitro-Alkenes
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We report a catalytic asymmetric synthesis of piperidines through [4 + 2] cycloaddition of 1-azadienes and nitro-alkenes. The reaction uses earth abundant Zn as catalyst and is highly diastereo- and regioselective. A novel BOPA ligand (F-BOPA) confers high reactivity and enantioselectivity in the process. The presence of ortho substitution on the arenes adjacent to the bis(oxazolines) was found to be particularly impactful, due to limiting the undesired coordination of 1-azadiene to the Lewis acid and thus allowing the reaction to be carried out at lower temperature. A series of secondary kinetic isotope effect studies using a range of ligands implicates a stepwise mechanism for the transformation, involving an initial Michael-type addition of the imine to the nitro-alkene followed by a cyclization event. The stepwise mechanism obviates the electronic requirement inherent to a concerted mechanism, explaining the successful cycloaddition between two electron-deficient partners. (Chemical Equation Presented).
- Chu, John C. K.,Dalton, Derek M.,Rovis, Tomislav
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supporting information
p. 4445 - 4452
(2015/04/14)
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- METHODS FOR THE TREATMENT OF LOCALLY ADVANCED BREAST CANCER
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Provided herein are methods of treating, preventing and/or managing locally advanced breast cancer, including inflammatory breast cancer, which comprise administering to a patient one or more immunomodulatory compounds or enantiomers or mixtures of enantiomers thereof, or pharmaceutically acceptable salts, solvates, hydrates, co-crystals, clathrates, or polymorphs thereof.
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Page/Page column 58; 59
(2014/03/26)
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- QUINAZOLINONE AND RELATED ANALOGS AS SIRTUIN MODULATORS
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Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
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Page/Page column 25
(2012/07/13)
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- PYRAZINYL CARBOXAMIDES AS FUNGICIDES
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This present disclosure is related to the field of pyrazine carboxamides and their derivatives and the use of these compounds as fungicides.
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Page/Page column 6-7
(2011/12/14)
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- Pyrrolidine(thi)ones Substituted by Heterocyclic Substituents in The 3-Position
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Pyrrolidine(thi)one compounds substituted by heterocyclic substituents in the 3-position, their preparation and use in pharmaceutical compositions, in particular as immunomodulators for treatment and/or inhibition of inflammatory and autoimmune diseases and haematological-oncological diseases.
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Page/Page column 18
(2009/01/20)
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- PROCESS FOR THE PRODUCTION OF AMIDES
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The present invention relates to a process for the preparation of compounds of formula (I) wherein R1 and R2 are each independently of the other hydrogen or C1-C5alkyl and R3 is CF3or CF2H, by a) reaction of a compound of formula (Il) wherein R1 and R2 are as defined for formula (I), with at least one reducing agent to form a compound of formula (III) wherein R1 and R2 are as defined for formula (I), and b) reaction of that compound with at least one reducing agent to form a compound of formula (IV) wherein R1 and R2 are as defined for formula (I), and (c) reaction of that compound with a compound of formula (V) wherein Q is chlorine, fluorine, bromine, iodine, hydroxy or C1-C6alkoxy and R3 is as defined for formula (I), to form the compound of formula (I); and to novel intermediates for use in that process.
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Page/Page column 38
(2008/06/13)
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- DESIGN OF ANTINEOPLASTIC AGENTS ON THE BASIS OF THE "2-PHENYLNAPHTHALENE-TYPE" STRUCTURAL PATTERN.I. SYHTHESIS OF SUBSTITUTED 3-PHENYLQUINAZOLONES, BENZOXAZOLOQUINAZOLONES AND BENZOTHIAZOLOQUINAZOLONES
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A number of substituted 3-phenylquinazolin-4-ones, 12H-benzoxazoloquinazolin-12-ones and 12H-benzothiazoloquinazolin-12-ones were designed and synthesized on the basis of a "2-phenylnaphthalene-type" structural pattern hypothesis.The posulated pattern, which was uncovered among a substantial number of compounds of both natural and synthetic origins, was noted to be associated with compounds possessing a variety of biological properties which include the antineoplastic activity.Several compounds designed for the present study were found to exhibit potentcytotoxicity against the growth of human promyelocytic leukemia (HL-60)cells.
- Cheng, Chia-Chung,Liu, Den-Fu,Chou, Ting-Chao
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p. 775 - 789
(2007/10/02)
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