- Novel 5,6,7,8-tetrahydroimidazo[2′,1′:2,3]thiazolo[5,4-c]pyridine derivatives
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Starting with 4-piperidone, new 5,6,7,8-tetrahydroimidazo[2′,1′:2,3]thiazolo [5,4-c]pyridines were synthesized. Structures of these compounds were confirmed by 1H NMR, 13C NMR, MS and elemental analysis.
- Hou, Xixi,Yang, Jianxue,Mao, Linlin,Lou, Caoxuan,Mao, Longfei
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- 1-[2-(1-Cyclobutylpiperidin-4-yloxy)-6,7-dihydro-4H-thiazolo[5,4-c]pyridin-5-yl]propan-1-one: a Histamine H3 Receptor Inverse Agonist with Efficacy in Animal Models of Cognition
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A series of chemical optimizations, which was guided by in vitro affinity at histamine H3 receptor (H3R), modulation of lipophilicity, ADME properties and preclinical efficacy resulted in the identification of 1-[2-(1-cyclobutylpiperidin-4-yloxy)-6,7-dihydro-4H-thiazolo[5,4-c]pyridin-5-yl]propan-1-one (45 e) as a potent and selective (Ki=4.0 nM) H3R inverse agonist. Dipsogenia induced by (R)-α-methylhistamine was dose dependently antagonized by 45 e, confirming its functional antagonism at H3R. It is devoid of hERG and phospholipidosis issues. Compound 45 e has adequate oral exposures and favorable half-life in both rats and dogs. It has demonstrated high receptor occupancy (ED80=0.22 mg/kg) and robust efficacy in object recognition task and, dose dependently increased acetylcholine levels in brain. The sub-therapeutic doses of 45 e in combination with donepezil significantly increased acetylcholine levels. The potent affinity, selectivity, in vivo efficacy and drug like properties together with safety, warrant for further development of this molecule for potential treatment of cognitive disorders associated with Alzheimer's disease.
- Shinde, Anil Karbhari,Badange, Rajesh Kumar,Reballi, Veena,Achanta, Pramod Kumar,Bojja, Kumar,Manchineella, Sravanthi,Rao Muddana, Nageswara,Subramanian, Ramkumar,Choudary Palacharla, Raghava,Benade, Vijay,Jayarajan, Pradeep,Thentu, Jagadeesh Babu,Lingavarapu, Bujji Babu,Yarra, Sivasekhar,Kagita, Narendra,Rao Doguparthi, Mallikarjuna,Mohammed, Abdul Rasheed,Nirogi, Ramakrishna
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- Identification of novel GPR81 agonist lead series for target biology evaluation
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GPR81 is a novel drug target that is implicated in the control of glucose and lipid metabolism. The lack of potent GPR81 modulators suitable for in vivo studies has limited the pharmacological characterization of this lactate sensing receptor. We performed a high throughput screen (HTS) and identified a GPR81 agonist chemical series containing a central acyl urea scaffold linker. During SAR exploration two additional new series were evolved, one containing cyclic acyl urea bioisosteres and another a central amide bond. These three series provide different selectivity and physicochemical properties suitable for in-vivo studies.
- Davidsson, ?jvind,Nilsson, Kristina,Br?nalt, Jonas,Andersson, Terese,Berggren, Kristina,Chen, Yantao,Fjellstr?m, Ola,Gradén, Henrik,Gustafsson, Linda,Hermansson, Nils-Olov,Jansen, Frank,Johannesson, Petra,Ohlsson, Bengt,Tyrchan, Christian,Wellner, Annika,Wellner, Eric,?lweg?rd-Halvarsson, Maria
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supporting information
(2020/01/22)
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- HMOX1 inducers
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The present invention is related to compounds of structure (I) as heme oxygenase 1 (HMOX 1) inducers. The present invention is also related a method of controlling the activity or the amount, or both the activity and the amount, of heme-oxygenase 1 in a mammalian subject. The definitions of the variables are provided herein.
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Page/Page column 39
(2020/09/18)
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- ANNULATED GLYCOSIDASE INHIBITORS
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Compounds of formula (I) wherein A, R, W1, W2, W3, W4, W5, W6, L, Q, Rx and u have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
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Page/Page column 97
(2019/03/12)
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- Preparation 2 - amino - 5 - CBZ - 4, 5, 6, 7 - tetrahydro-thiazolo [5, 4 - C] pyridine of the new method (by machine translation)
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The invention discloses a process for preparing 2 - amino - 5 - CBZ - 4, 5, 6, 7 - tetrahydro-thiazolo [5, 4 - C] pyridine of the new method, comprises the following steps: N - tert-butoxycarbonyl - 4 - piperidone in pyridine with sulfur and single cyanamide mixed heating reaction→cooling→filtering→washed with an organic solvent, and dried to obtain a pale yellow solid product→in dichloromethane in trifluoroacetic acid is mixed with low-temperature reaction, concentrated→with triethylamine in dichloromethane in the mixed low-temperature drop chlorination benzyl formate, stirring reaction→[...]→dichloromethane extraction, the organic phase water, salt water washing, drying, filtering and concentrated to obtain crude product→ethyl acetate beating, the final product is obtained yellow solid. The invention of cheap price for raw materials to replace the original high price of the raw material for preparing the final product, to avoid the original ring-brominated by-product when many routes, not only the operation is simple, convenient purification, the cost is reduced, high yield, favorable to the industrialized production and cost control. (by machine translation)
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Paragraph 0012; 0014
(2019/01/23)
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- Substituted amide compound and application
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The invention belongs to the field of agricultural bactericidal, insecticidal and acaricidal agents, and relates to a substituted amide compound and an application. The substituted amide compound has a structure as shown in a general formula I in the specification; and in the general formula I, substituents are defined in the specification. The compound provided by the invention has broad-spectrum bactericidal, insecticidal and acaricidal activities, has excellent control effects on diseases like cucumber downy mildew, corn rust, wheat powdery mildew and rice blast, especially has better control effects on the corn rust, also has excellent control effects on aphids and Tetranychus cinnabarinus, and especially can obtain good effects on the Tetranychus cinnabarinus at a low dosage.
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- Substituted tetrahydroisoquinoline compound and application
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The invention discloses a substituted tetrahydroisoquinoline compound and application. The compound has a structure as shown in a general formula I in the specification; and in the general formula I, substituents are defined in the specification. The comp
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- Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation
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Glucokinase (GK) activators are being developed for the treatment of type 2 diabetes mellitus (T2DM). However, existing GK activators have risks of hypoglycemia caused by over-activation of GK in islet cells and dyslipidemia caused by over-activation of intrahepatic GK. In the effort to mitigate risks of hypoglycemia and dyslipidemia while maintaining the promising efficacy of GK activator, we investigated a series of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific partial GK activators, which led to the identification of compound 72 that showed a good balance between in vitro potency and enzyme kinetic parameters, and protected β-cells from streptozotocin-induced apoptosis. Chronic treatment of compound 72 demonstrated its potent activity in regulation of glucose homeostasis and low risk of dyslipidemia with diabetic db/db mice in oral glucose tolerance test (OGTT). Moreover, acute treatment of compound 72 did not induce hypoglycemia in C57BL/6J mice even at 200 mg/kg via oral administration.
- Wang, Zhengyu,Shi, Xiaofan,Zhang, Huan,Yu, Liang,Cheng, Yanhua,Zhang, Hefeng,Zhang, Huibin,Zhou, Jinpei,Chen, Jing,Shen, Xu,Duan, Wenhu
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p. 128 - 152
(2017/08/10)
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- With the biological activity of the tetrahydro-benzothiazole and pyridine hydrochloride salt compound and its preparation method
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The invention discloses a tetrahydro imidazo thieno hydrochloride compound with the biological activity and a preparing method thereof and belongs to the technical field of drug synthesis. The tetrahydro imidazo thiophene pyridine hydrochloride compound with the biological activity is characterized by being provided with the following structure (please see the formula in the specification), and R represents formonitrile phenyl, or tertiary butyl, or phenyl, or trifluoromethyl, or p-chlorophenyl or meta-methoxyphenyl. The invention further discloses the preparing method of the tetrahydro imidazo thiophene pyridine hydrochloride compound with the biological activity. A series of tetrahydro imidazo thiophene pyridine hydrochloride compounds with the biological activity is synthesized through the new method, the reaction process is easy to operate and implement, raw materials are low in price and easy to obtain, the reaction efficiency is high, repeatability is good, and the biological activity effect is obvious.
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Paragraph 0012; 0013; 0014; 0015; 0016; 0017; 0018; 0019
(2017/08/25)
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- Thiazolopyridines Improve Adipocyte Function by Inhibiting 11 Beta-HSD1 Oxoreductase Activity
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Background. Glucocorticoid excess has been linked to clinical observations associated with the pathophysiology of metabolic syndrome. The intracellular glucocorticoid levels are primarily modulated by 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme that is highly expressed in key metabolic tissues including fat, liver, and the central nervous system. Methods. In this study we synthesized a set of novel tetrahydrothiazolopyridine derivatives, TR-01-4, that specifically target 11β-HSD1 and studied their ability to interfere with the glucocorticoid and lipid metabolism in the 3T3-L1 adipocytes. Results. Based on the docking model and structure-activity relationships, tetrahydrothiazolopyridine derivatives TR-02 and TR-04 showed the highest potency against 11β-HSD1 by dose-dependently inhibiting conversion of cortisone to cortisol (IC50 values of 1.8 μM and 0.095 μM, resp.). Incubation of fat cells with 0.1-10 μM TR-01-4 significantly decreased cortisone-induced lipid accumulation in adipocytes and suppressed 11β-HSD1 mRNA expression. Observed reduction in adipocyte fat stores could be partially explained by decreased expression levels of adipogenic markers (PPAR-γ, aP2) and key enzymes of lipid metabolism, including fatty acid synthase (FAS), hormone sensitive lipase (HSL), and lipoprotein lipase (LPL). Conclusions. The tetrahydrothiazolopyridine moiety served as an active pharmacophore for inhibiting 11β-HSD1 and offered a novel therapeutic strategy to ameliorate metabolic alterations found in obesity and diabetes.
- Rathinasabapathy, Thirumurugan,Palatini Jackson, Kimberly Marie,Thor, Yiwen,Buru, Ayuba Sunday,Esposito, Debora,Li, Xu,Pichika, Mallikarjuna Rao,Hamzah, Ahmad Sazali,Komarnytsky, Slavko
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- Heterocyclic compound with Wnt signal path inhibitory activity and application thereof
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The invention provides a heterocyclic compound with Wnt signal path inhibitory activity. The heterocyclic compound and chemically acceptable salt, isotope, isomer and a crystal structure thereof are provided with a structure shown as the general formula I (see the formula in the description). The invention further provides application of the heterocyclic compound with the Wnt signal path inhibitory activity. The heterocyclic compound with the Wnt signal path inhibitory activity serves as effective antagonist of a Wnt signal path, and can be used for treating or preventing diseases caused by abnormity of the Wnt signal path.
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Paragraph 0339; 0340; 0341
(2016/10/08)
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- PRMT5 INHIBITORS AND USES THEREOF
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Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof:wherein Y1 is of formula (?) or formula (y):Ring Y is a 5- to 6-membered heteroaryl ring; and V4, V5, Rx, x, y, and n are as defined herein. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
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Paragraph 00645; 00646
(2016/04/20)
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- ANTI-INFECTIVE COMPOUNDS
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The present invention relates to small molecule compounds having the general formula (I): wherein A is a moiety selected from the group consisting of formulae (A) to (K) and their use in the treatment of bacterial infections, in particular Tuberculosis.
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Page/Page column 64
(2016/06/28)
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- FUSED THIOPHENE AND THIAZOLE DERIVATIVES AS ROR GAMMA MODULATORS
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The present invention provides fused thiophene and thiazole derivatives of formula (I), which may be therapeutically useful, more particularly as RORγ modulators; in which R1, R2, R3, R4, R5, R6, R7, X1, X2, L, m, n and ring A have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in disease(s) or disorder(s) where there is an advantage in modulating RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the fused thiophene and thiazole derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
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Page/Page column 90; 91
(2015/07/16)
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- HEDGEHOG PATHWAY SIGNALING INHIBITORS AND THERAPEUTIC APPLICATIONS THEREOF
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The hedgehog (Hh) signaling pathway is a pathway which regulates patterning, growth and cell migration during embryonic development, but in adulthood is limited to tissue maintenance and repair. Mutational inactivation of the inhibitory pathway components leads to constitutive ligand-independent activation of the Hh signaling pathway, results in cancers such as basal cell carcinoma and medulloblastoma. Ligand-dependent activation of Hh signaling is involved in prostate cancer, pancreatic cancer, breast cancer and blood cancers. Therefore, inhibition of the aberrant Hh signaling represents a promising approach toward novel anticancer therapy. The invention provides novel molecules of formula I that inhibit hedgehog pathway signaling and provides therapeutic applications for the treatment of malignancies (basal cell carcinoma, medulloblastoma, glioblastoma, non-small cell lung cancer, prostate cancer, pancreatic cancer, blood cancers, mesenchymal cancers, etc.), prevention of tumor regrowth, sensitization of radio-chemo therapies, and other diseases (inflammation, fibrosis and immune disorders).
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Paragraph 0124; 0125
(2014/08/06)
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- Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility
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Triazoles with fused-heterocycle nuclei were designed and evaluated for their in vitro activity on the basis of the binding mode of albaconazole using molecular docking, along with SAR of antifungal triazoles. Tetrahydro-[1,2,4] triazolo[1,5-a]pyrazine and tetrahydro-thiazolo[5,4-c]pyridine nuclei were preferable to the other four fused-heterocycle nuclei investigated. Potent in vitro activity, broad spectrum and better water solubility were attained when triazoles containing nitrogen aromatic heterocycles were attached to these two nuclei. The most potent compounds 27aa and 45x, with low hERG inhibition and hepatocyte toxicity, both exhibited excellent activity against Candida, Cryptococcus, and Aspergillus spp., as well as selected fluconazole-resistant strains. A high water-soluble compound 58 (the disulfate salt of 45x) displayed unsatisfactory in vivo activity because of its poor PK profiles. Mice infected with C.alb. SC5314 and C.alb. 103 (fluconazole-resistant strain) and administered with 27aa displayed significantly improved survival rates. 27aa also showed favorable pharmacokinetic (PK) profiles.
- Cao, Xufeng,Sun, Zhaoshuan,Cao, Yongbing,Wang, Ruilian,Cai, Tongkai,Chu, Wenjing,Hu, Wenhao,Yang, Yushe
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supporting information
p. 3687 - 3706
(2014/05/20)
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- 1,2,4 -TRIAZOLES AS ALLOSTERIC MODULATORS OF MGLU5 RECEPTOR ACTIVITY FOR THE TREATMENT OF SCHIZOPHRENIA OF DEMENTIA
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This invention relates to compounds of formula (I) their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
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- NOVEL COMPOUNDS
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This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
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Paragraph 0298;0299; 0300; 0301
(2013/06/26)
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- NOVEL COMPOUNDS
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This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
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Paragraph 0179; 0180; 0181
(2013/06/27)
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- HETEROCYCLYL COMPOUNDS AS HISTAMINE H3 RECEPTOR LIGANDS
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The present invention relates to heterocyclyl compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and th
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Page/Page column 14
(2012/03/26)
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- TETRAHYDROTHIAZOLOPYRIDINE INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE
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The present invention relates to compounds (I) useful as inhibitors of PBK, particularly of PI3K gamma. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders
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Page/Page column 55-56
(2010/09/17)
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- RHO KINASE INHIBITORS
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Substituted amide and urea derivatives useful as inhibitors of Rho kinase are described, which inhibitors can be useful in the treatment of various disorders such as cardiovascular diseases, cancer, neurological diseases, renal diseases, bronchial asthma, erectile dysfunction and glaucoma.
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Page/Page column 127-128
(2008/12/07)
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- TRIAMINE DERIVATIVE
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An object of the present invention is to provide a novel compound which has a potent inhibitory effect on FXa and exhibits an excellent antithrombotic effect when orally administered. The present invention provides a compound represented by the following general formula (1): wherein R 1 and R 2 each independently represent a hydrogen atom, a hydroxy group, an alkyl group or an alkoxy group; Q 1 represents a saturated or unsaturated bicyclic or tricyclic fused hydrocarbon group which may be substituted, a saturated or unsaturated bicyclic or tricyclic fused heterocyclic group which may be substituted, or the like; Q 2 represents a single bond, a straight-chained or branched alkylene group having 1 to 6 carbon atoms, a straight-chained or branched alkenylene group having 2 to 6 carbon atoms, or the like; R 3 and R 4 each represent an alkyl group, or the like; m and n each represent an integer from 0 to 3; Q 4 represents an aryl group; and TDegree and T 1 each represent a carbonyl group or the like, and a medicine containing the compound.
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Page/Page column 57
(2008/06/13)
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- BENZAZOLE DERIVATIVES, COMPOSITIONS, AND METHODS OF USE AS AURORA KINASE INHIBITORS
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The present invention relates to compounds and methods from the treatment of cancer. The invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods for the treatment of cancer using the compounds of the presentation invention or pharmaceutical compositions comprising compounds of the present invention.
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Page/Page column 63-64
(2010/11/28)
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- 3-SULFONYLAMINO-PYRROLIDINE-2-ONE DERIVATIVES AS FACTOR XA INHIBITORS
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The present invention provides at least one chemical entity chosen from compounds of formula (I) wherein: R1 represents a group selected from formula (II), (III), (IV), (V), (VI), (VII), each ring of which optionally contains a further heteroatom N, Z represents an optional substituent halogen, -C1-3alkyl or -NRaRb, alk represents alkylene or alkenylene, T represents S, O or NH; Ra and Rb independently represent hydrogen or -C1-3alkyl; R2 represents a group selected from formula (VIII), (IX), W, X and Y independently represent CH, C-R5 or N; R5 represents halogen or C1-3alkyl; V represents NR3, S or O; R3 represents hydrogen or C1-3alkyl; one of A1 and A2 represents N and the other represents CH; Each R4, R6, R7, R8, R9 independently represents hydrogen or C1-3alkyl; R10 represents hydrogen, -C1-6alkyl, -C1-3alkylCONRaRb, -C1-3alkylCO2C1-4alkyl, -CO2C1-4alkyl or -C1-3alkylCO2H; and pharmaceutically acceptable derivative(s) thereof. The invention also relates to processes for the preparation of compound(s) of formula (I), pharmaceutical compositions containing compound(s) of formula (I) and to the use of compound(s) of formula (I) in medicine, particularly in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.
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Page/Page column 69
(2008/06/13)
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- DIAMINE DERIVATIVES
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A compound represented by formula (1):Q1-Q2-To-N(R1) -Q3-N(R2)-T1-Q4 [wherein R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6- membered cyclic hydrocarbon group which may be substituted, or the like; Q2 is a single bond or the like; Q3 represents the following group: (wherein Q5 is an alkylene group having 1 to 8 carbon atoms, or the like); and T0 and T1 are carbonyl groups or the like], a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after artificial valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.
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Page/Page column 72
(2008/06/13)
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- NOVEL ETHYLENEDIAMINE DERIVATIVES
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A compound represented by the following formula (1):Q-Q-T-N(R)-Q-N(R)-T-Q [wherein, R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6- membered cyclic hydrocarbon group which may have a substituent, or the like; Q2 is a single bond or the like; Q3 represents the following group: -C(R3a)(R4a)-{C(R3b)(R4b)}m1-{C(R3c)(R4c)}m2-{C(R3d)(R4d)}m3-{C(R3e)(R4e)}m4-C(R3f)(R4f)- (in which, R3a to R4e represent hydrogen or the like); T0 represents a carbonyl group or the like; and T1 represents -COCONR- or the like]; or salt thereof, solvate thereof, or N-oxide thereof. The compound is useful as a preventive and/or therapeutic agent for cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.
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Page/Page column 56-57
(2010/02/14)
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- Diamine derivatives
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A compound represented by the general formula (1): Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4??(1) wherein R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Q2 is a single bond or the like; Q3 is a group in which Q5 is an alkylene group having 1 to 8 carbon atoms, or the like; and T0 and T1 are carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.
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- N-SULFONYLAMINOTHIAZOLE
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N-(4,5,6,7-tetrahydro-thiazolo-[5,4-c]pyridin-2-yl)-(C6-18)arylsulfonamides, wherein the nitrogen atom of the pyridine is substituted, and wherein the pyridine ring is optionally bridged, useful as a pharmaceutical related to steroid
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- DIAMINE DERIVATIVES
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A compound represented by the general formula (1):Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4 wherein R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6- membered cyclic hydrocarbon group which may be substituted, or the like; Q2 is a single bond or the like; Q3 is a group in which Q5 is an alkylene group having 1 to 8 carbon atoms, or the like; and T0 and T1 are carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.
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- Facile methods for preparation of thiazolopyridine and tetrahydrothiazolopyridine derivatives
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The improved routes to prepare tetrahydrothiazolo[5,4-c]-pyridine-2- carboxylic acid lithium salts (2 and 3) were developed. Route A is consisted of the improved preparation of thiazolopyridine intermediates, and Route B is applicable for a large scale synthesis of tetrahydrothiazolo[5,4-c]pyridine-2- carboxylic acid derivatives. The methods we developed may serve as facile means for preparing thiazolopyridine and tetrahydrothiazolopyridine derivatives.
- Haginoya, Noriyasu,Komoriya, Satoshi,Osanai, Ken,Yoshino, Toshiharu,Nagata, Tsutomu,Nagamochi, Masatoshi,Muto, Ryo,Yamaguchi, Mitsuhiro,Nagahara, Takayasu,Kanno, Hideyuki
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p. 1555 - 1561
(2007/10/03)
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- ETHYLENEDIAMINE DERIVATIVES
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The invention relates a compound represented by the formula (1):Q1-Q2-C(=O)-N(R1)-Q3-N(R2)-T1-Q4 wherein R1 and R2 represent H or the like; Q1 represents an aromatic ring, heterocyclic ring or the like; Q2 represents a single bond, aromatic ring, heterocyclic ring or the like; Q3 represents a group or the like, Q4 represents an aromatic ring, heterocyclic ring or the like; and T1 represents -CO- or -SO2-, and a medicine which comprises the compound and is useful for thrombosis and embolism.
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