- Benzothiazole derivatives and their uses
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The present invention relates to benzothiazole derivatives and their uses, specifically to compounds shown in formula I or stereoisomers thereof and pharmaceutically acceptable salts, solvates or prodrugs thereof, methods of preparation thereof, and pharmaceutical compositions containing the compounds, wherein the substituentsR1,R2,R8 , X, Y, Z, Q have the meaning given in the instruction manual. The present invention further relates to the application of compounds of formula I in the preparation of drugs for the treatment and / or prevention of sEH-mediated diseases, in particular in the preparation of drugs for the treatment of inflammatory diseases, cardiovascular and cerebrovascular diseases, diabetes mellitus, diabetic complications, diabetes-related diseases, fibrotic diseases, neurological and psychiatric diseases, pain, ulcerative diseases and the like.
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Paragraph 0121; 0234; 0235
(2022/01/05)
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- HERBICIDAL COMPOUNDS
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Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, especially as herbicides.
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Page/Page column 81-82
(2021/04/02)
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- NOVEL COMPOUNDS FOR DIAGNOSIS
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The present invention relates to novel compounds that can be employed in the diagnosis, monitoring of disease progression or monitoring of drug activity of a group of disorders and abnormalities associated with alpha-synuclein (α-synuclein, A-synuclein, aSynuclein, a- synuclein, A-syn, α-syn, aSyn, SNCA, Non-amyloid beta component of Alzheimer's disease (AD) amyloid plaques, Non-A4 component of amyloid precursor, NACP) aggregates including, but not limited to, Lewy bodies and/or Lewy neurites, such as Parkinson's disease (PD). The instant compounds are particularly useful in the diagnosis of the preclinical state of such a disorder, monitoring residual disorder, or predicting the responsiveness of a patient who is suffering from such a disorder to the treatment with a certain medicament.
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- 1, 3, 4, 5-TETRAHYDRO-2H-PYRIDO[4,3-B]INDOLE DERIVATIVES FOR THE TREATMENT, ALLEVIATION OR PREVENTION OF DISORDERS ASSOCIATED WITH TAU AGGREGATES LIKE ALZHEIMER'S DISEASE
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The present invention relates to novel compounds that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neurofibrillary Tangles (NFTs), such as Alzheimer's disease (AD).
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Page/Page column 90
(2019/07/20)
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- TETRAHYDROBENZOFURO[2,3-C]PYRIDINE AND BETA-CARBOLINE COMPOUNDS FOR THE TREATMENT, ALLEVIATION OR PREVENTION OF DISORDERS ASSOCIATED WITH TAU AGGREGATES
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The present invention relates to novel compounds of formula (I) that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neurofibrillary Tangles (NFTs), such as Alzheimer's disease (AD).
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Page/Page column 70
(2019/12/28)
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- COMPOUNDS AND METHODS FOR TREATING CANCER
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Substituted hydrazone compounds, methods of making such compounds and metal complexes thereof, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds and metal complexes to treat, prevent or ameliorate cancer are provided.
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Paragraph 0330
(2018/05/24)
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- TRI-HETEROCYCLIC DERIVATIVES, PREPARATION PROCESS AND USES THEREOF
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The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase.
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Paragraph 0124; 0395
(2014/11/13)
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- 7-HYDROXY-SPIROPIPIPERIDINE INDOLINYL ANTAGONISTS OF P2Y1 RECEPTOR
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The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of Ρ2Y1 receptor and may be used as medicaments in the treatment and/or prophylaxis of thromboembolic disorders.
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- Identification of 1-{2-[4-chloro-1′-(2,2-dimethylpropyl)-7-hydroxy-1, 2-dihydrospiro[indole-3,4′-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3] thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y1 antagonist as an antiplatelet agent
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Spiropiperidine indoline-substituted diaryl ureas had been identified as antagonists of the P2Y1 receptor. Enhancements in potency were realized through the introduction of a 7-hydroxyl substitution on the spiropiperidinylindoline chemotype. SAR studies were conducted to improve PK and potency, resulting in the identification of compound 3e, a potent, orally bioavailable P2Y1 antagonist with a suitable PK profile in preclinical species. Compound 3e demonstrated a robust antithrombotic effect in vivo and improved bleeding risk profile compared to the P2Y12 antagonist clopidogrel in rat efficacy/bleeding models.
- Jeon, Yoon T.,Yang, Wu,Qiao, Jennifer X.,Li, Ling,Ruel, Rejean,Thibeault, Carl,Hiebert, Sheldon,Wang, Tammy C.,Wang, Yufeng,Liu, Yajun,Clark, Charles G.,Wong, Henry S.,Zhu, Juliang,Wu, Dauh-Rurng,Sun, Dawn,Chen, Bang-Chi,Mathur, Arvind,Chacko, Silvi A.,Malley, Mary,Chen, Xue-Qing,Shen, Hong,Huang, Christine S.,Schumacher, William A.,Bostwick, Jeffrey S.,Stewart, Anne B.,Price, Laura A.,Hua, Ji,Li, Danshi,Levesque, Paul C.,Seiffert, Dietmar A.,Rehfuss, Robert,Wexler, Ruth R.,Lam, Patrick Y.S.
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p. 1294 - 1298
(2014/03/21)
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- TRI-HETEROCYCLIC DERIVATIVES, PREPARATION PROCESS AND USES THEREOF
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The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase
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Page/Page column 45; 46
(2013/07/05)
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- CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
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Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
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Page/Page column 22
(2012/10/08)
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- HETEROCYCLIC COMPOUND AND USE THEREOF
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A compound represented by formula (I) or a salt thereof, which has a potent Raf inhibitory activity. In formula (I), R1 represents an optionally substituted C1-6 alkyl, etc.; X represents —O— or —NR2— (wherein R2 represents a hydrogen atom or a C1-6 alkyl); Y represents a group represented by formula 2 (2ii or 2ii) (wherein ring A represents an optionally substituted benzene ring; Z represents a group represented by (1) —NR3CO—W1—, (2) —NR3CO—W1—O—, (3) —NR3CO—W1—O—W2—, (4) —NR3CO—W1—S—, (5) —NR3CO—W1—NR4—, (6) —NR3COO—, (7) —NR3COO—W1—, (8) —NR3CO—CO—, or (9) —NR3CONR4— (wherein R3 and R4 each represents a hydrogen atom, etc., and W1 and W2 each represents an optionally substituted C1-6 alkylene, etc.); and R5 represents an optionally substituted five- or six-membered ring group.
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Page/Page column 37
(2011/10/12)
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- CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
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Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
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Page/Page column 37
(2011/07/30)
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- PYRIMIDINE DERIVATIVES USED AS ITK INHIBITORS
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The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular ltk activity.
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Page/Page column 106
(2010/10/03)
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- BICYCLIC HETEROCYCLIC DERIVATIVES AND METHODS OF USE THEREOF
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The present invention relates to novel Bicyclic Heterocyclic Derivatives, pharmaceutical compositions comprising the Bicyclic Heterocyclic Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a cognitive disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
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Page/Page column 103
(2010/08/05)
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- FUSED BICYCLIC COMPOUNDS AS INHIBITORS FOR PI3 KINASE
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The invention relates to compounds of formula (I) for the regulation of phosphoinositides 3-kinases activity and related diseases.
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Page/Page column 109
(2010/09/18)
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- Synthesis and structure-activity relationships of 2-(1,4′-bipiperidin-1′-yl)thiazolopyridine as H3 receptor antagonists
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A series of 2-(1,4′-bipiperidine-1′-yl)thiazolopyridines was synthesized and evaluated as a new lead of non-imidazole histamine H3 receptor antagonists. Introduction of diversity at the 6-position of the pyridine ring was designed to enhance in vitro potency and decrease hERG activity. The structure-activity relationships for these new thiazolopyridine antagonists are discussed.
- Rao, Ashwin U.,Palani, Anandan,Chen, Xiao,Huang, Ying,Aslanian, Robert G.,West Jr., Robert E.,Williams, Shirley M.,Wu, Ren-Long,Hwa, Joyce,Sondey, Christopher,Lachowicz, Jean
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scheme or table
p. 6176 - 6180
(2010/06/16)
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- Synthesis and antifungal activity of novel thiazole-containing triazole antifungals. II. Optically active ER-30346 and its derivatives
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A series of novel thiazole-containing triazole antifungals was synthesized and evaluated for antifungal activity against a variety of clinically isolated pathogenic fungi in vitro and against systemic candidosis in vivo. These compounds showed potent antifungal activities in vitro and in vivo. In particular, (2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4- difluorophenyl)-1-(1H-1,2,4-triazol-l-yl)-2-butanol (12g; ER-30346) showed potent and well-balanced in vitro activities and potent in vivo efficacy, and had a good safety profile.
- Tsuruoka, Akihiko,Kaku, Yumiko,Kakinuma, Hiroyuki,Tsukada, Itaru,Yanagisawa, Manabu,Nara, Kazumasa,Naito, Toshihiko
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p. 623 - 630
(2007/10/03)
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- THE FIRST BRANCHED BENZOXAZINOPHENOTHIAZINE RING SYSTEM AND ITS AZA-ANALOGUES
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The synthesis of a branched benzoxazinophenotiazine heterocycle is described.The parent compound benzo-benzoxazinophenothiazine (12), was obtained from 2,3-dichloro-1,4-naphthoquinone (6), 2-aminophenol and 2-aminothiophenol.Monoaza-, diaza- and triaza- analogues of this novel heterocycle were also synthesized.The parent compounds, 16-oxa-15-thia-4,5,10,14-tetraazabenzopentaphene (18) and 16-oxa-15-thia-4,5,10,14-tetraazabenzopentaphene (22, R=H) were also synthesized as well as 4-amino-16-oxa-15-thia-4,5,10,14-tetraazabenzopentaphene (24).They are intensely coloured high-melting solids suitable for application as pigments.Their ease of reduction with Na2S2O4 and the ready oxidation of the reduced compounds to applicability also as vat dyes.
- Okafor, Charles O.
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p. 1187 - 1194
(2007/10/02)
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