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Synthesis and biological evaluation of novel 5,6,7-trimethoxy flavonoid salicylate derivatives as potential anti-tumor agents
5,6,7-Trimethoxy flavonoid salicylate derivatives were designed by the joining of three important pharmacophores (TMP, flavonoid, and SA) according to the combination principle. A series of novel trimethoxy flavonoid salicylate derivatives were synthesized and their in vitro anti-tumor activities were evaluated. Among these derivatives, compound 7f exhibited excellent antiproliferative activity against HGC-27 cells and MGC-803 cells with IC50 values of 10.26 ± 6.94 μM and 17.17 ± 3.03 μM, respectively. Subsequently, the effects on cell colony formation (clonogenic survival assay), cell migration (wound healing assay), cell cycle distribution (PI staining assay), cell apoptosis (Hoechst 33258 staining assay and annexin V-FITC/PI dual staining assay), lactate level (lactate measurement), microtubules disarrangement (immunofluorescence staining analysis) and docking posture (molecular docking simulation) were determined. Further western blot analysis confirmed that compound 7f could effectively down-regulate the expression of glycolysis-related proteins HIF-1α, PFKM and PKM2 and tumor angiogenesis-related proteins VEGF. Overall, these studies suggested that compound 7f, as the representative compound of those, might be a promising candidate for the treatment of gastric cancer and deserved the further studies.
Deng, Xiangping,Feng, Wanshi,Lei, Xiaoyong,Liu, Renbo,Peng, Yijiao,Tang, Guotao,Xie, Zhizhong,Xiong, Runde,Zheng, Xing,Zou, Yang
(2020/02/13)

METHOD FOR SYNTHESIZING COMPOUND FOR ORGANIC ELECTRONIC ELEMENT AND COMPOUND PRODUCED BY THE SAME
The present invention relates to a method for synthesizing a compound for an organic electronic element, which provides a method for synthesizing a fluorene derivative. Provided in an embodiment of the present invention for achieving the purpose is a meth
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Paragraph 0151-0155

(2020/09/03)

Design, synthesis, and preliminary biological evaluation of 3′,4′,5′-trimethoxy flavonoid salicylate derivatives as potential anti-tumor agents
According to the pharmacophore combination principle, a set of new 3′,4′,5′-trimethoxy flavonoid salicylate derivatives were designed, synthesized, and evaluated for biological activity. The cytotoxicity evaluation revealed that compound 10v exhibited higher potency than 5-Fu against HCT-116 cells. Preliminary biological activity studies showed that compound 10v could inhibit the colony formation and migration of HCT-116 cells. Besides, the Hoechst 33258 staining assay and flow cytometry revealed that treatment with compound 10v induced the apoptosis of HCT-116 cells in a concentration-dependent manner, while it had no effect on their cell cycle. The WB analysis suggested that HIF-1α, tubulin, HK-2, and PFK might be the potential pharmacophore targets of compound 10v. Tubulin was a potential drug target for compound 10v, which was explained by analyzing the crystal structure of compound 10v complexed with tubulin. These results indicated that compound 10v might be a promising anti-tumor agent candidate, deserving further optimization and evaluation.
Deng, Xiangping,Liu, Renbo,Li, Junjian,Li, Zhongli,Liu, Juan,Xiong, Runde,Lei, Xiaoyong,Zheng, Xing,Xie, Zhizhong,Tang, Guotao
p. 1874 - 1884
(2019/01/28)

Microwave-Assisted Synthesis of Benzofuran-3(2H)-ones
A new method for the synthesis of benzofuran-3(2H)-ones under microwave conditions was developed. The reaction conditions were screened, and the scope of benzoate substrates was investigated. The results showed that our method could provide rapid access to these important dihydrobenzofuranones in 43% to 58% yields.
Hu, Xiaojing,Lai, Huimin,Zhao, Fangfei,Hu, Shuyu,Sun, Qianqian,Fang, Lizhen
p. 745 - 750
(2019/10/14)

Development of a synthetic route towards N4,N9-disubstituted 4,9-diaminoacridines: On the way to multi-stage antimalarials
A multi-step synthetic route towards N4,N9-disubstituted 4,9-diaminoacridines that, to the best of our knowledge, has no precedence in the literature, has been developed. The target structures are likely to reveal interesting biological activities in the near future, not only due to their mepacrine-like core, but also because they embed simultaneously the pharmacophores of chloroquine and primaquine, antimalarial drugs that act at different stages of malaria infection.
Fonte, Mélanie,Fagundes, Natália,Gomes, Ana,Ferraz, Ricardo,Prudêncio, Cristina,Araújo, Maria Jo?o,Gomes, Paula,Teixeira, Cátia
supporting information
p. 1166 - 1169
(2019/03/27)

INHIBITORS OF RHO/MRTF/SRF-MEDIATED GENE TRANSCRIPTION AND METHODS FOR USE OF THE SAME
Disclosed herein are inhibitors of Rho/MRTF/SRF-mediated gene transcription, and methods for their use in treating or preventing diseases such as cancer and fibrosis. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically accept
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Paragraph 0067; 0112-0112; 0114; 0115

(2019/10/20)

MODIFIED COMPOUND OF ANDROGRAPHOLIDE
The present disclosure discloses a modified compound of andrographolide, and particularly discloses a compound shown in formula (I) and (II) or a pharmaceutically acceptable salt thereof.
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Paragraph 0199-0201

(2019/01/04)

C-GLUCOSIDE DERIVATIVE CONTAINING FUSED PHENYL RING OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PROCESS FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
The present disclosure relates to C-glycoside derivatives having a fused phenyl ring or pharmaceutical acceptable salts thereof, a method for preparing the same, a pharmaceutical composition comprising the same, a use thereof and a method for dual inhibition of SGLT1 and SGLT2 using the same. A novel compound of the present disclosure has a dual inhibitory activity against SGLT1 and SGLT2, thus being valuably used as a diabetes therapeutic agent.
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Paragraph 0281-0282

(2018/12/04)

Gold promoted arylative cyclization of alkynoic acids with arenediazonium salts
Alkynoic acids derived from salicylic acid and analogues undergo arylative cyclization with arenediazonium salts promoted by gold in the absence of external ligands. The reaction is thermally induced and proceeds even in the absence of light. A difference in regioselectivity has been found compared with that observed in the cycloisomerization process of the same type of compounds.
Carrillo-Arcos, Ulises A.,Porcel, Susana
supporting information
p. 1837 - 1842
(2018/03/23)

C-3 NOVEL TRITERPENONE WITH C-17 REVERSE AMIDE DERIVATIVES AS HIV INHIBITORS
The present invention relates to C-3 novel triterpenone with C-17 reverse amide compounds of Formula (I); and pharmaceutically acceptable salts thereof, wherein ring Formula (II), R1, R2, R3, R4, R5, R6, R7, 'n' and 'm' are as defined in Formula (I). The invention also relates to C-3 novel triterpenone with C-17 reverse amide derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases.
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Page/Page column 53

(2018/03/06)

Chromatography-free, Mitsunobu-triggered heterocyclizations of salicylhydroxamic acids to 3-hydroxybenzisoxazoles
The Mitsunobu reaction has become one of the most powerful tools to alkylate acidic pronucleophiles. A significant caveat of Mitsunobu chemistry, however, is that the reaction mixture is often plagued with purification problems owing to the phosphine oxide and hydrazine dicarboxylate by-products. In addition to the development of more readily separable Mitsunobu reagents, the product's physicochemical properties may be exploited to facilitate purification. In this regard, we present a swift and efficient preparation of 3-hydroxybenzisoxazoles by the Mitsunobu-triggered heterocyclizations of salicylhydroxamic acids, which can be isolated by an acid–base work-up. As expected, a range of functional groups was compatible with the chemistry.
Van Eker, Daniel,Chauhan, Jay,Murphy, William A.,Conlon, Ivie L.,Fletcher, Steven
p. 5301 - 5303
(2016/11/16)

Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof
The present disclosure provides hetero-bicyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by Bruton's tyrosine kinase (Btk) activity, The disclosure also relates to the process of preparation of compounds of Formula (I). These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of Bruton's tyrosine kinase (Btk), such as inflammatory and/or autoimmune disorder, cell proliferation, rheumatoid arthritis, psoriasis, psoriatic arthritis, transplant rejection, graft-versus-host disease, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, B-cell malignancies, systemic lupus, erythematosus or other disorders.
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Paragraph 0115; 0116

(2016/08/23)

Oxidative cyclization of alkenoic acids promoted by AgOAc
Alkenoic acids derived from salicylic acid and analogues undergo an unexpected oxidative cyclization process triggered by AgOAc leading to 4H-benzo[d][1,3]dioxin-4-ones. The process is affected by the substitution on the aryl and the allyl units.
Carrillo-Arcos, Ulises A.,Rojas-Ocampo, Jonathan,Porcel, Susana
supporting information
p. 479 - 483
(2016/01/09)

Aralkylpiperidine (or piperazinecarboxylic) and its derivatives used for treating hypercalcemia schinzopherenia
PROBLEM TO BE SOLVED: To provide an agent for treating schizophrenia and related neuropsychiatric diseases.SOLUTION: This invention provides an aralkylpiperidine (or piperazine) derivative represented by formula (1), where A ring is a 5-7 membered heterocycle including N, with the heterocycle including a hetero atom arbitrarily selected from O, S, N; X is O, an amino group or a substituted amino group; Z is CH, N or C; Y is O, N or S; n is an integer of 1-5; and R1-R6 are H, a C1-C4 alkyl group or the like.
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Paragraph 0068

(2018/12/01)

Substituted Hetero-Bicyclic Compounds, Compositions and Medicinal Applications Thereof
The present disclosure provides hetero-bicyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by Bruton's tyrosine kinase (Btk) activity, The disclosure also relates to the process of preparation of compounds of Formula (I). These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of Bruton's tyrosine kinase (Btk), such as inflammatory and/or autoimmune disorder, cell proliferation, rheumatoid arthritis, psoriasis, psoriatic arthritis, transplant rejection, graft-versus-host disease, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, B-cell malignancies, systemic lupus, erythematosus or other disorders.
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Paragraph 0128

(2015/03/16)

ORGANIC ELECTRONIC ELEMENT USING A COMPOUND FOR ORGANIC ELECTRONIC ELEMENT, AND AN ELECTRONIC DEVICE THEREOF
Provided in the present invention are an organic electronic element using a compound which can improve light emitting efficiency, stability, and life of the element, and an electronic device thereof. The organic electronic device includes: a first electrode; a second electrode; and an organic substance layer located between the first electrode and the second electrode and including at least hole transfer layer and auxiliary light emitting layer, wherein the hole transfer layer includes a compound presented by chemical formula 1, and the auxiliary light emitting layer includes at least one among compounds presented by chemical formula 2 to 4.(110) Substrate(120) Positive electrode(130) Hole injection layer(140) Hole transfer layer(141) Buffer layer(150) Light emitting layer(151) Auxiliary light emitting layer(160) Electron transfer layer(170) Electron injection layer(180) Negative electrodeCOPYRIGHT KIPO 2015
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Paragraph 0268-0271

(2016/10/08)

Silver(I) and gold(I)-promoted synthesis of alkylidene lactones and 2H-chromenes from salicylic and anthranilic acid derivatives
Ag(I) and Au(I) efficiently catalyze the cycloisomerization of terminal alkynoic acids into methylene seven-membered ring lactones. Depending on the metal, divergent reaction pathways were found for non terminal alkynoic acids. While Ag(I) led to lactones, Au(I) led to 2H-chromenes coming from the hydroarylation of the alkyne.
Nolla-Saltiel, Roberto,Robles-Marín, Elvis,Porcel, Susana
supporting information
p. 4484 - 4488
(2014/08/05)

SUBSTITUTED HETERO-BICYCLIC COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF
The present disclosure provides hetero-biclyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by Bruton's tyrosine kinase (Btk) activity, The disclosure also relates to the process of preparation of compounds of Formula (I). These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of Bruton's tyrosine kinase (Btk), such as inflammatory and/or autoimmune disorder, cell proliferation, rheumatoid arthritis, psoriasis, psoriatic arthritis, transplant rejection, graft-versus-host disease, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, B-cell malignancies, systemic lupus, erythematosus or other disorders.
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Page/Page column 42-43

(2013/11/05)

HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
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Page/Page column 90-91

(2012/09/21)

ARALKYL SUBSTITUTED PIPERIDINE OR PIPERAZINE DERIVATIVES AND THEIR USE FOR TREATING SCHIZOPHRENIA
The present invention discloses an aralkyl substituted piperidine or piperazine derivative and the use of the derivative in preparation of medicaments for treating schizophrenia and correlative psychoneuroses. It is shown by pharmacological tests that the derivative of the present invention has better antischizophrenic effect and less toxicity. Said derivative is a free base or salt of the compound having the following general formula.
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Page/Page column 12

(2011/06/10)

Enantioselective bromolactonization of conjugated (2)-enynes
"Chemical equation presented" A catalytic enantioselective syn-1,4-bromolactonization of conjugated (Z)-enynes was reported. Diastereomeric ratios >20:1 and up to 99% enantiomeric excesses were observed. Di-, tri-, and tetra-substituted bromoallenes were prepared together with lactone heterocycles efficiently and stereoselectively. Preliminary investigations suggest that the chiral catalyst may serve as a bifunctional reagent by interacting with both a carboxylic acid nucleophile and NBS electrophile.
Zhang, Wei,Zheng, Suqing,Liu, Na,Werness, Jenny B.,Guzei, Llia A.,Tang, Weiplng
supporting information; experimental part
p. 3664 - 3665
(2010/05/15)

THIOCHROMENE DERIVATIVES AS HIP HYDROXYLASE INHIBITORS
The present invention relates to novel compounds, methods, and compositions capable of decreasing HEF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
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Page/Page column 88

(2010/06/15)

Enzyme-catalysed synthesis and reactions of benzene oxide/oxepine derivatives of methyl benzoates
A series of twelve benzoate esters was metabolised, by species of the Phellinus genus of wood-rotting fungi, to yield the corresponding benzyl alcohol derivatives and eight salicylates. The isolation of a stable oxepine metabolite, from methyl benzoate, allied to evidence of the migration and retention of a carbomethoxy group (the NIH Shift), during enzyme-catalysed ortho-hydroxylation of alkyl benzoates to form salicylates, is consistent with a mechanism involving an initial arene epoxidation step. This mechanism was confirmed by the isolation of a remarkably stable, optically active, substituted benzene oxide metabolite of methyl 2-(trifluoromethyl)benzoate, which slowly converted into the racemic form. The arene oxide was found to undergo a cycloaddition reaction with 4-phenyl-1,2,4-triazoline-3,5-dione to yield a crystalline cycloadduct whose structure and racemic nature was established by X-ray crystallography. The metabolite was also found to undergo some novel benzene oxide reactions, including epoxidation to give an anti-diepoxide, base-catalysed hydrolysis to form a trans-dihydrodiol and acid-catalysed aromatisation to yield a salicylate derivative via the NIH Shift of a carbomethoxy group. This journal is The Royal Society of Chemistry.
Boyd, Derek R.,Sharma, Narain D.,Harrison, John S.,Malone, John. F.,McRoberts, W. Colin,Hamilton, John T. G.,Harper, David B.
experimental part
p. 1251 - 1259
(2008/10/09)

Parallel synthesis of 9-aminoacridines and their evaluation against chloroquine-resistant Plasmodium falciparum
A parallel synthetic strategy to the 9-aminoacridine scaffold of the classical anti-malarial drug quinacrine (2) is presented. The method features a new route to 9-chloroacridines that utilizes triflates of salicylic acid derivatives, which are commercially available in a variety of substitution patterns. The route allows ready variation of the two diversity elements present in this class of molecules: the tricyclic aromatic heterocyclic core, and the disubstituted diamine sidechain. In this study, a library of 175 compounds was designed, although only 93 of the final products had purities acceptable for screening. Impurity was generally due to incomplete removal of 9-acridones (18), a degradation product of the 9-chloroacridine synthetic intermediates. The library was screened against two strains of Plasmodium falciparum, including a model of the drug-resistant parasite, and six novel compounds were found to have IC50 values in the low nanomolar range.
Anderson, Marc O.,Sherrill, John,Madrid, Peter B.,Liou, Ally P.,Weisman, Jennifer L.,DeRisi, Joseph L.,Guy, R. Kiplin
p. 334 - 343
(2007/10/03)

Aminoalcohol derivatives
The present invention relates to a compound formula [I]: wherein R1 is hydrogen or halogen, R2 is hydrogen or an amino protective group, R3 is hydrogen or lower alkyl, X is bond, —CH2— or —O—, and Y is ?in which R4 is lower alkoxycarbonyl, ?in which R5 is carboxy(lower)alkyl, etc., ?in which R6 is hydroxy, etc., and so on, 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.
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Page/Page column 40

(2010/02/07)

AMINOALCOHOL DERIVATIVES AND THEIR USE AS BETA-3 ADRENERGIC RECEPTOR AGONISTS
The present invention relates to a compound formula [I] 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.
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Page/Page column 130

(2010/02/07)

4- AND 5-ALKYNYLOXINDOLES AND 4- AND 5-ALKENYLOXINDOLES
4- and 5-alkynyloxindoles as well as 4- and 5-alkenyloxindoles having formula (I) and (II), wherein R, R, R, R, R, X and z have the meaning indicated in the specification, inhibit or modulate protein kinases, in particular JNK protein kinases and are useful as anti-inflammatory agents, particularly in the treatment of rheumatoid arthritis.
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Page/Page column 36

(2010/02/04)

4-and 5-alkynyloxindoles and 4-and 5-alkenyloxindoles
Disclosed are 4- and 5-alkynyloxindoles as well as 4- and 5-alkenyloxindoles that inhibit or modulate protein kinases, in particular JNK protein kinases. The compounds of the invention and their pharmaceutically acceptable salts, and prodrugs of said compounds, are useful as anti-inflammatory agents, particularly useful in the treatment of rheumatoid arthritis. Also disclosed are pharmaceutical compositions containing the foregoing compounds, methods for the treatment and/or control of inflammation, particularly in the treatment or control of rheumatoid arthritis using these compounds, as well as intermediates useful in the preparation of compounds of the invention.
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(2008/06/13)

Design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine σ ligands as potential antipsychotic drugs
Receptor antagonists may be effective antipsychotic drugs that do not induce motor side effects caused by ingestion of classical drugs such as haloperidol. We obtained evidence that 1-(2-dipropylaminoethyl)-4-methoxy- 6H-dibenzo[b,d]pyran hydrochloride 2a had selective affinity for σ receptor over dopamine D2 receptor. This compound was designed to eliminate two bonds of apomorphine 1 to produce structural flexibility for the nitrogen atom and to bridge two benzene rings with a -CH2O- bond to maintain the planar structure. In light of the evidence, N,Y-dipropyl-2-(4-methoxy-3- benzyloxylphenyl)ethylamine hydrochloride 10b was designed. Since compound 10b had eliminated a biphenyl bond of 6H-dibenzo[b,d]pyran derivative 2a, it might be more released from the rigid structure of apomorphine 1 than compound 2a. The chemical modification of compound 10b led to the discovery that N,N-dipropyl-2-[4-methoxy-3-(2-phenylethoxyl)phenyl]ethylamine hydrochloride 10g (NE- 100), the best compound among arylalkoxyphenylalkylamine derivatives 3, had a high and selective affinity for σ receptor and had a potent activity in an animal model when the drug was given orally. We report here the design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine derivatives 3.
Nakazato, Atsuro,Ohta, Kohmei,Sekiguchi, Yoshinori,Okuyama, Shigeru,Chaki, Shigeyuki,Kawashima, Yutaka,Hatayama, Katsuo
p. 1076 - 1087
(2007/10/03)

The thermal [3, 3] claisen rearrangement of the 3-substituted phenyl allyl and propargyl ethers. The synthesis of 4-halobenzo[b]furans
The thermal [3, 3] Claisen rearrangement of the 3-substituted phenyl allyl and propargyl ethers is regioselective. The major product of the reaction incorporates a 1, 2, 3-trisubstituted benzene ring. The 2-allenylphenol intermediates can be manipulated i
Box, Vernon G. S.,Meleties, Panayiotis C.
p. 2173 - 2183
(2007/10/03)

Substituted benzisoxazole and benzisothiazole herbicidal agents
There are provided substituted benzisoxazole and benzisothiazole compounds having the structural formula I STR1 Further provided are compositions and methods comprising those compounds for the control of undesirable plant species.
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(2008/06/13)

Zatosetron, a Potent, Selective, and Long-Acting 5HT3 Receptor Antagonist: Synthesis and Structure-Activity Relationships
Antagonists of 5HT3 receptors are clinically effective in treating nausea and emesis associated with certain oncolytic drugs, including cisplatin.Moreover, these agents may be useful in pharmacological management of several central nervous system disorders, including anxiety, schizophrenia, dementia, and substance abuse.Our studies on aroyltropanamides led to the discovery that dihydrobenzofuranyl esters and amides are potent 5HT3 receptor antagonists.Simple benzoyl derivatives of tropine and 3α-aminotropane possessed weak 5HT3 receptor antagonist activity, as judged by blockade of bradycardia produced by iv injection of serotonin (5HT) to anesthetized rats.Within this series, use of benzofuran-7-carboxamide as the aroyl moiety led to a substantial increase of 5HT3 receptor affinity.The optimal 5HT3 receptor antagonist identified via extensive SAR studies was endo-5-chloro-2,3-dihydro-2,2-dimethyl-N-(8-methyl-8-azabicyclooct-3-yl)-7-benzofurancarboxamide (Z)-2-butenedioate (zatosetron maleate).The 7-carbamyl regiochemistry, dimethyl substitution, chloro substituent, and endo stereochemistry were all crucial elements of the SAR.Zatosetron maleate was a potent antagonist of 5HT-induced bradycardia in rats (ED50=0.86 μg/kg iv).Low oral doses of zatosetron (30 μg/kg) produced long-lasting antagonism of 5HT3 receptors, as evidenced by blockade of 5HT-induced bradycardia for longer than 6 h in rats.Moreover, this compound did not produce hemodynamic effects after iv administration to rats, nor did it block carbamylcholine-induced bradycardia in doses that markedly blocked 5HT3 receptors.Thus, zatosetron is a potent, selective, orally effective 5HT3 receptor antagonist with a long duration of action in rats.
Robertson, David W.,Lacefield, William B.,Bloomquist, William,Pfeifer, William,Simon, Richard L.,Cohen, Marlene L.
p. 310 - 319
(2007/10/02)

Carboxamides useful as antiemetic or antipsychotic agents
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(2008/06/13)

CARBOXAMIDES USEFUL AS ANTIEMETIC OR ANTIPSYCHOTIC AGENTS
Carboxamides represented by the formula (I): STR1 wherein Z represents the carbon atoms necessary to complete a 5-to 7-membered ring, R 1, R 2, and R 3 may be the same or different and are selected from the group consisting of a hydrogen atom, a lower alkyl group, a cycloalkyl group, a halogen atom, an amino group, a lower alkylamino group, an alkoxy group, an acylamido group, a sulfonamido group, and a nitro group; andA represents an aminoalkyl moiety and acid addition salts thereof.
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(2008/06/13)

Benzofuro[3,2-c]pyrazol-3-amine derivatives
Herein is disclosed benzofuro[3,2-c]pyrazol-3-amine derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are useful for producing analgesia in a mammal. In addition, some of the derivatives are useful for inhibiting gastric acid secretion, convulsions, anxiety and aggression, and producing muscle relaxation, hypnosis and sedation in a mammal.
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(2008/06/13)