- COMPOUNDS, COMPOSITIONALS, AND METHODS FOR TREATING T-CELL ACUTE LYMPHOBLASTIC LEUKEMIA
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In an aspect, the disclosure provides for compounds (II), compositions, and methods of administering the compounds and compositions to a patient in need thereof. In another aspect, the disclosure relates to compounds and compositions for treating cancer,
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Page/Page column 48
(2019/02/15)
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- HETEROARYL DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSTION FOR PREVENTING OR TREATING DISEASES ASSOCIATED WITH PI3 KINASES, CONTAINING SAME AS ACTIVE INGREDIENT
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The present invention relates to a heteroaryl derivative or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition for preventing or treating diseases associated with PI3 kinases, containing the same as an active ingredient. The heteroaryl derivative according to the present invention has an excellent effect of selectively inhibiting PI3 kinases, thereby being useful in preventing or treating PI3 kinase diseases such as: cancers, autoimmune diseases, and respiratory diseases.
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Paragraph 0506-0507
(2018/04/26)
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- Pyrimido oxazine derivatives or pharmaceutically acceptable salts thereof, preparation method thereof and pharmaceutical composition for use in preventing or treating PI3 kinase related diseases
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The present invention relates to pyrimido oxazine derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same as an effective component for preventing or treating PI3 kinase-related diseases. The pyrimido oxazine derivatives according to the present invention have excellent selective inhibitory effects on PI3 kinase, and thus may be beneficially used in preventing or treating PI3 kinase-related diseases such as the following: cancers including blood cancer, ovarian cancer, cervical cancer, breast cancer, large intestine cancer, liver cancer, stomach cancer, pancreatic cancer, colon cancer, periotoneal cancer, skin cancer, bladder cancer, prostate cancer, lung cancer, osteosarcoma, fibrous tumor, and brain tumor; autoimmune diseases including rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, type 1 diabetes, hyperthyroidism, myasthenia gravis, Crohnandprime;s disease, ankylosing spondylitis, psoriasis, pernicious anemia, and Sjogrenandprime;s syndrome; and respiratory diseases including chronic obstructive pulmonary disease (COPD), rhinitis, asthma, chronic bronchitis, chronic pulmonary inflammatory diseases, silicosis, pulmonary sarcoidosis, pleuritis, alveolitis, vasculitis, emphysema, pneumonia, and bronchiectasis.COPYRIGHT KIPO 2017
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Paragraph 0161-0164
(2017/08/02)
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- Dihydropteridin-one derivatives or pharmaceutically acceptable salts thereof, preparation method thereof and pharmaceutical composition for use in preventing or treating PI3 kinase related diseases
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The present invention relates to dihydropteridin-one derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same as an effective component for preventing or treating PI3 kinase-related diseases. According to the present invention, the dihydropteridin-one derivatives have excellent selective inhibitory effects on PI3 kinase, and thus may be beneficially used in preventing or treating PI3 kinase-related diseases such as the following: cancers including blood cancer, ovarian cancer, cervical cancer, breast cancer, large intestine cancer, liver cancer, stomach cancer, pancreatic cancer, colon cancer, periotoneal cancer, skin cancer, bladder cancer, prostate cancer, lung cancer, osteosarcoma, fibrous tumor, and brain tumor; autoimmune diseases including rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, type 1 diabetes, hyperthyroidism, myasthenia gravis, Crohnandprime;s disease, ankylosing spondylitis, psoriasis, pernicious anemia, and Sjogrenandprime;s syndrome; and respiratory diseases including chronic obstructive pulmonary disease (COPD), rhinitis, asthma, chronic bronchitis, chronic pulmonary inflammatory diseases, silicosis, pulmonary sarcoidosis, pleuritis, alveolitis, vasculitis, emphysema, pneumonia, and bronchiectasis.COPYRIGHT KIPO 2017
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Paragraph 0156-0159
(2017/09/12)
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- QUINAZOLINE DERIVATIVE OR ITS SALT AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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The present invention provides a quinazoline derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same and a use thereof. The quinazoline derivative or its pharmaceutically acceptable salt has a selective inhibitory activity against the phosphatidylinositol 3-kinase delta subunit, and therefore can be usefully applied for preventing or treating cancer, along with avoiding side effects such as lymphopenia-associated inflammatory responses.
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Paragraph 218
(2017/12/15)
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- SUBSTITUTED AMINOPYRIMIDINE COMPOUNDS AND METHODS OF USE
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The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not restricted to leukemias and solid tumors, in mammals, especially humans.
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Paragraph 0522
(2015/03/31)
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- HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Compounds and pharmaceutical compositions of formulae (I), (XI) and (XII) as PI3 kinase modulators and their use in the treatment of diseases such as cancer.
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Paragraph 00536; 00537
(2013/03/26)
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- HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.
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Paragraph 1094; 1095
(2013/03/26)
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- HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
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Paragraph 0760; 0810
(2013/10/22)
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- Nickel or phenanthroline mediated intramolecular arylation of sp 3 C-H bonds using aryl halides
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The development of the intramolecular arylation of sp3 C-H bonds adjacent to nitrogen using aryl halides is described. Arylation was accomplished using either Ni(COD)2 or 1,10-phenanthroline in substoichiometric amounts, and the reaction conditions were applied to a variety of electronically differentiated benzamide substrates. Preliminary studies suggest a mechanism involving aryl and alkyl radical intermediates.
- Wertjes, William C.,Wolfe, Lydia C.,Waller, Peter J.,Kalyani, Dipannita
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supporting information
p. 5986 - 5989
(2014/01/06)
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- PROCESSES FOR PREPARING ISOQUINOLINONES AND SOLID FORMS OF ISOQUINOLINONES
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Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.
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Page/Page column 78-79
(2012/07/28)
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- THERAPEUTIC OR PROPHYLACTIC AGENT FOR MULTIPLE SCLEROSIS
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A therapeutic or prophylactic agent for multiple sclerosis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for multiple sclerosis according to the present invention shows the excellent absorbability and in vivo stability when orally administered, and exhibits high therapeutic or prophylactic effects.
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Page/Page column 70-71
(2009/04/23)
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- SUBSTITUTED BENZOYLAMINO-INDAN-2-CARBOXYLIC ACIDS AND RELATED COMPOUNDS
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The present invention relates to A compound of the formula Ia wherein in any of its stereoisomers forms or a mixture of stereoisomeric forms in any ratio, or a physiologically acceptable salt thereof, wherein the substituents are as described herein. The inventive compounds have CXCR5 inhibitory activity are particularly useful in treating or preventing various inflammatory diseases, such as rheumatoid arthritis, multiple sclerosis, lupus, Crohn's Disease, associated with the modulation of the human CXCR5 receptor.
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Page/Page column 145
(2009/01/24)
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- PHARMACEUTICAL COMPOSITION AND PROCESS
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There is provided a formulation comprising N-(2-chloro-6-methylbenzoyl)-4- [(2,6-dichlorobenzoyl)amino]-L-phenylalanine-2(diethylamino)ethyl ester and poloxamer 188 which is manufactured by a hot melt process.
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Page/Page column 7
(2008/06/13)
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- Novel potent and efficacious nonpeptidic urotensin II receptor agonists
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Six different series of nonpeptidic urotensin II receptor agonists have been synthesized and evaluated for their agonistic activity in a cell-based assay (R-SAT). The compounds are ring-opened analogues of the isochromanone-based agonist AC-7954 with different functionalities constituting the linker between the two aromatic ring moieties. Several of the compounds are highly potent and efficacious, with N-[1-(4-chlorophenyl)-3-(dimethylamino)- propyl]-4-phenylbenzamide oxalate (5d) being the most potent. The pure enantiomers of 5d were obtained from the corresponding diastereomeric amides. It was shown by a combination of X-ray crystallography and chemical correlation that the activity resides in the S-enantiomer of 5d (pEC50 7.49).
- Lehmann, Fredrik,Pettersen, Anna,Currier, Erika A.,Sherbukhin, Vladimir,Olsson, Roger,Hacksell, Uli,Luthman, Kristina
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p. 2232 - 2240
(2007/10/03)
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- PYRAZOLE DERIVATIVES FOR THE INHIBITION OF CDK' S AND GSK' S
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The invention provides compounds of the formula (I), or salts, tautomers, N-oxides or solvates thereof wherein: R1 is selected from: (a) 2,6-dichlorophenyl; (b) 2,6-difluorophenyl; (c) a 2,3,6-trisubstituted phenyl group wherein the substituents for the phenyl group are selected from fluorine, chlorine, methyl and methoxy; (d) a group R0; (e) a group R a; (f) a group Rlb; (g) a group Rlc; (h) a group Rld; and 0) 2,6-difluorophenylamino ; wherein R )0υ, r R> llaa, T Rj I1bD, T R) I1cC, r R> Iidα, r R?2zaa, r R>22bD and RJ are as defined in the claims. The compounds have activity as inhibitors of cdk kinase (such as cdkl or cdk2) and glycogen synthase kinase-3 activity.
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Page/Page column 149-150
(2008/06/13)
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- ISOQUINOLINONE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS
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This invention is directed to isoquinolinone derivatives and their use in modulating the activity of orphan nuclear receptors, pharmaceutical compositions containing such derivatives, and methods of using such derivatives in treating disease-states associ
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- Two efficient methods for the preparation of 2-chloro-6-methylbenzoic acid
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Two efficient methods for the preparation of 2-chloro-6-methylbenzoic acid were developed: one based on nucleophilic aromatic substitution and the other based on carbonylation. In the first approach, 2-chloro-6-fluorobenzaldehyde was converted to its n-butylimine, then treated with 2 equiv of methylmagnesium chloride in THF to give, after hydrolysis, 2-chloro-6-methylbenzaldehyde. Subsequent oxidation of this compound gave the title compound in 85% overall yield. In the second approach, 3-chloro-2-iodotoluene was efficiently carbonylated in methanol to give methyl 2-chloro-6-methylbenzoate, which after hydrolysis afforded the title compound in 94% yield (84% yield after recrystallization). The carbomethoxylation proceeded smoothly even at a high substrate-to-Pd ratio of 10 000. Both methods do not require isolation of intermediates and are suitable for the preparation of kilogram quantities of 2-chloro-6-methylbenzoic acid.
- Daniewski, Andrzej R.,Liu, Wen,Puentener, Kurt,Scalone, Michelangelo
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p. 220 - 224
(2013/09/06)
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