603122-40-3Relevant articles and documents
TYK2 Inhibitor compounds containing alkoxy and amide groups
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Paragraph 0124-0127, (2021/11/21)
The invention belongs to the field of pharmaceutical chemistry, and provides TYK2 inhibitor compounds containing alkoxy and amide groups and a preparation method thereof, and relates to application of the compound in preparation of medicines for treating
METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
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, (2022/01/06)
Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods that restore DNA binding affinity of p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.
CANCER TREATMENTS TARGETING CANCER STEM CELLS
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Paragraph 0331; 0376-0377; 0632; 0635-0636, (2019/11/19)
Disclosed are compounds, methods, compositions, and kits that allow for treating cancer by, e.g., targeting cancer stem cells. In some embodiments, the cancer is colorectal cancer, gastric cancer, gastrointestinal stromal tumor, ovarian cancer, lung cancer, breast cancer, pancreatic cancer, prostate cancer, testicular cancer, or lymphoma. In some embodiments, the cancer is liver cancer, endometrial cancer, leukemia, or multiple myeloma. The compounds utilized in the disclosure are of Formula (0), (O'), and (I):
NOVEL TRICYCLIC COMPOUNDS AS ANTICANCER AGENTS
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Paragraph 0915; 0916, (2016/07/27)
The present invention is directed to tricyclic compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
TRICYCLIC COMPOUNDS AS ANTICANCER AGENTS
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Page/Page column 344; 345, (2015/07/15)
The present invention is directed to tricyclic compounds (I), pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
Design of potent and selective hybrid inhibitors of the mitotic kinase nek2: Structure-activity relationship, structural biology, and cellular activity
Innocenti, Paolo,Cheung, Kwai-Ming J.,Solanki, Savade,Mas-Droux, Corine,Rowan, Fiona,Yeoh, Sharon,Boxall, Kathy,Westlake, Maura,Pickard, Lisa,Hardy, Tara,Baxter, Joanne E.,Aherne, G. Wynne,Bayliss, Richard,Fry, Andrew M.,Hoelder, Swen
, p. 3228 - 3241 (2012/06/01)
We report herein a series of Nek2 inhibitors based on an aminopyridine scaffold. These compounds have been designed by combining key elements of two previously discovered chemical series. Structure based design led to aminopyridine (R)-21, a potent and selective inhibitor able to modulate Nek2 activity in cells.
Discovery of a novel series of biphenyl benzoic acid derivatives as potent and selective human β3-adrenergic receptor agonists with good oral bioavailability. Part I
Imanishi, Masashi,Tomishima, Yasuyo,Itou, Shinji,Hamashima, Hitoshi,Nakajima, Yutaka,Washizuka, Kenichi,Sakurai, Minoru,Matsui, Shigeo,Imamura, Emiko,Ueshima, Koji,Yamamoto, Takao,Yamamoto, Nobuhiro,Ishikawa, Hirofumi,Nakano, Keiko,Unami, Naoko,Hamada, Kaori,Matsumura, Yasuhiro,Takamura, Fujiko,Hattori, Kouji
, p. 1925 - 1944 (2008/12/20)
A novel class of biphenyl analogues containing a benzoic acid moiety based on lead compound 8i have been identified as potent and selective human β3 adrenergic receptor (β3-AR) agonists with good oral bioavailability and long plasma half-life. After further substituent effects were investigated at the terminal phenyl ring of lead compound 8i, we have discovered that more lipophilic substitution at the R position improved potency and selectivity. As a result of these studies, 10a and 10e were identified as the leading candidates with the best balance of potency, selectivity, and pharmacokinetic profiles. In addition, compounds 10a and 10e were evaluated to be efficacious for a carbachol-induced increase of intravesical pressure, such as an overactive bladder model in anesthetized dogs. This represents the first demonstrated result dealing with β3- AR agonists.
AMINO ALCOHOL DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, AND USE OF THESE
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Page/Page column 35, (2008/06/13)
The present invention provides compounds represented by general formula (I): a prodrug thereof, or pharmaceutical acceptable salts thereof, wherein R1 is hydrogen or lower alkyl; each of R2 and R3 is independently hydrogen or lower alkyl; each of R4, R5 and R6 is independently hydrogen, halogen, lower alkyl or lower alkoxy; R7 is hydrogen or lower alkyl; R8 is hydrogen, halogen, lower alkyl, lower alkoxy, etc; R9 is -COR10, -A1-COR10, -O-A2-COR10, etc; Ar is optionally substituted phenyl or heteroaryl; and A is a bond, -OCH2-, etc, which exhibit potent and selective β3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.
PREPARATION AND USE OF BIPHENYL-4-YL-CARBONYLAMINO ACID DERIVATIVES FOR THE TREATMENT OF OBESITY
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Page/Page column 28-29, (2010/11/08)
This invention relates to certain biphenyl-4-yl carbonylamino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.
AMINOALCOHOL DERIVATIVES
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, (2008/06/13)
The present invention relates to a compound formula [I]: wherein Y is bond,--O--(CH2)n--(in which n is 1, 2, 3 or 4), etc., Z is cyano, tetrazolyl, etc., R1 is hydrogen, lower alkyl, etc., R2 is hydrogen or an amino protective group, R3 is hydrogen or lower alkyl, R4 is hydrogen or lower alkyl, R5 and R8 are each independently hydrogen, halogen, hydroxy, lower alkyl, etc., R6 is hydrogen, lower alkyl, etc., R9 is hydrogen or lower alkyl, and i is 1 or 2, or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.