- REGULATOR OF NITROGEN-CONTAINING HETEROAROMATIC DERIVATIVES, PREPARATION METHOD THEREFOR AND USE THEREOF
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The present invention relates to a regulator of nitrogen-containing heteroaromatic derivatives, a preparation method therefor and the use thereof. In particular, the present invention relates to a compound as shown in the general formula (I), a preparation method therefor and a pharmaceutical composition containing the compound, and the use thereof as a protein tyrosine phosphatase-2C (SHP2) inhibitor in the treatment of diseases or conditions such as leukemia, neuroblastoma, melanoma, breast cancer, lung cancer and colorectal cancer, wherein the definition of each substituent in the general formula (I) is the same as that in the description.
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Paragraph 0461; 0474-0476
(2021/08/27)
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- PYRIMIDINE AND FIVE-MEMBERED NITROGEN HETEROCYCLE DERIVATIVE, PREPARATION METHOD THEREFOR, AND MEDICAL USES THEREOF
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The present invention relates to a pyrimidine and a five-membered nitrogen heterocycle derivative, a preparation method therefor, and the medical uses thereof. Particularly, the present invention relates to a pyrimidine and a five-membered nitrogen hetero
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Paragraph 0117; 0118
(2021/10/07)
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- Compound serving as SHP2 inhibitor and application thereof
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The invention belongs to the field of medical chemistry, relates to a compound serving as an SHP2 inhibitor and an application of the compound, and particularly provides a compound shown in a formula (I) or an isomer, pharmaceutically acceptable salt, solvate, crystal or prodrug of the compound, processes for the preparation, pharmaceutical compositions containing these compounds and the use of these compounds or compositions for the treatment of SHP2 mediated diseases.
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Paragraph 0103; 0105-0107; 0340; 0342-0343
(2021/05/12)
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- Salt of nitrogen-containing heteroaromatic derivative and crystal form thereof
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The invention relates to a salt of a nitrogen-containing heteroaromatic derivative and a crystal form thereof. The invention specifically relates to a salt with a general formula (I) and a crystal form thereof. A preparation method and a pharmaceutical composition containing the salt of the derivative and a crystal form thereof, as a protein tyrosine phosphatase - 2C (SHP2) inhibitor, and application thereof to treatment of diseases or diseases such as leukemia, neuroblastoma, melanoma, breast cancer, lung cancer and colon cancer.
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Paragraph 0702; 0721-0724
(2021/10/13)
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- SHP2 INHIBITORS, COMPOSITIONS AND USES THEREOF
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Provided herein are compounds of Formula (I), methods of using the compounds as SHP2 inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating SHP2-mediated diseases.
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Page/Page column 45
(2021/11/06)
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- SHP2 INHIBITORS, COMPOSITIONS AND USES THEREOF
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Provided are compounds of Formula (I), methods of using the compounds as SHP2 inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating SHP2-mediated diseases.
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Page/Page column 68-69
(2021/12/30)
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- PROTEIN TYROSINE PHOSPHATASE INHIBITORS
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Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
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- NOVEL HETEROCYCLIC DERIVATIVES USEFUL AS SHP2 INHIBITORS
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Provided is a compound of formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, provided is a pharmaceutical composition comprising the said compound.
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- Pyrazinothiazole compound and application thereof, and pharmaceutical composition containing pyrazinothiazole compound
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The invention discloses a pyrazinothiazole compound, an application of the pyrazinothiazole compound, and a pharmaceutical composition containing the pyrazinothiazole compound, and provides a pyrazinothiazole compound represented by a formula A or a pharmaceutically acceptable salt of the pyrazinothiazole compound. The pyrazinothiazole compound provided by the invention has relatively good SHP2 inhibitory activity.
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Paragraph 0087-0088; 0089-0092
(2020/11/09)
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- IMIDAZOPYRIMIDINE DERIVATIVES
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The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula I, processes for preparing compounds of Formula I, therapeutic methods for treating cancers.
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Paragraph 0848-0849
(2020/04/29)
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- SHP2 PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF
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The present disclosure relates to novel compounds including formula (X) and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure.
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Paragraph 0175
(2019/10/15)
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- Novel heterocyclic derivative capable of being used as SHP2 inhibitor
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The invention relates to a novel heterocyclic derivative capable of being used as an SHP2 inhibitor, specifically relates to a compound shown by a formula I or pharmaceutically acceptable salts thereof, further relates to a use of the compound shown by the formula I or the pharmaceutically acceptable salts thereof and a pharmaceutical composition thereof in drug preparation, and particularly relates to a use in preparation of drugs for treatment, inhibition or prevention of diseases or discomforts mediated by SHP2 activity.
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Paragraph 0406; 0408-0409
(2019/08/30)
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- NOVEL HETEROCYCLIC DERIVATIVES USEFUL AS SHP2 INHIBITORS
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This invention relates to certain novel pyrazine derivatives (Formula I) as SHP2 inhibitors which is shown as formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, this invention is directed to fused heterocyclic group derivatives useful as inhibitors of SHP2, methods for producing such compounds and methods for treating a SHP2-mediated disorder.
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Page/Page column 82; 83
(2018/10/19)
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- Novel spiropiperidine-based stearoyl-CoA desaturase-1 inhibitors: Identification of 1′-{6-[5-(pyridin-3-ylmethyl)-1,3,4-oxadiazol-2-yl]pyridazin-3-yl}-5-(trifluoromethyl)-3,4-dihydrospiro[chromene-2,4′-piperidine]
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Cyclization of the benzoylpiperidine in lead compound 2 generated a series of novel and highly potent spiropiperidine-based stearoyl-CoA desaturase (SCD)-1 inhibitors. Among them, 1′-{6-[5-(pyridin-3-ylmethyl)-1,3,4-oxadiazol-2-yl]pyridazin-3-yl}-5-(trifluoromethyl)-3,4-dihydrospiro[chromene-2,4′-piperidine] (19) demonstrated the most powerful inhibitory activity against SCD-1, not only in vitro but also in vivo (C57BL/6 J mice). With regard to the pharmacological evaluation, 19 showed powerful reduction of the desaturation index in the plasma of C57BL/6 J mice on a non-fat diet after a 7-day oral administration (q.d.) without causing notable abnormalities in the eyes or skin up to the highest dose (3 mg/kg) in our preliminary analysis.
- Uto, Yoshikazu,Kiyotsuka, Yohei,Ueno, Yuko,Miyazawa, Yuriko,Kurata, Hitoshi,Ogata, Tsuneaki,Deguchi, Tsuneo,Yamada, Makiko,Watanabe, Nobuaki,Konishi, Masahiro,Kurikawa, Nobuya,Takagi, Toshiyuki,Wakimoto, Satoko,Kono, Keita,Ohsumi, Jun
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scheme or table
p. 746 - 754
(2010/06/11)
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- Potent 3-spiropiperidine growth hormone secretagogues
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Systematic SAR studies of the different regioisomers and homologues of the spiro(indane-1,4'-piperidine) moiety in the growth hormone secretagogue L-162,752 are presented. Among them, spiro(3H-1-benzopyran-2,3'-piperidine) was found to afford secretagogue
- Yang, Lihu,Morriello, Greg,Prendergast, Kristine,Cheng, Kang,Jacks, Tom,Chan, Wanda W.-S.,Schleim, Klaus D.,Smith, Roy G.,Patchett, Arthur A.
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p. 107 - 112
(2007/10/03)
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- Spiro piperidines and homologs promote release of growth hormone
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There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.
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