cas 76469-88-0, Methyl 4-(cyanomethyl)benzoate

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Preparation method of aryl acetonitrile derivative
The invention relates to a continuous nucleophilic addition and beta-fluorine elimination reaction method of 2,2-difluoroolefin and ammonia water in a catalyst-free and additive-free system. The method comprises the following steps: adding a 2,2-difluoroolefin compound, ammonia water and a solvent into a Schlenk reaction flask, and conducting stirring and reacting at a certain temperature in an air atmosphere to obtain the product aryl acetonitrile derivative.
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Paragraph 0044-0062

(2021/10/20)

Pd/C-Catalyzed methoxycarbonylation of aryl chlorides
A new protocol for the methoxycarbonylation of aryl chlorides has been developed. Various methyl benzoates were produced in good to excellent yields. Several parameters are crucial for the success of this procedure: 1) the usage of LiOMe as the base or co-nucleophile which facilitate the carbonylative transformation; 2) employing Pd/C as the catalyst to prevent the palladium reduced by MeOH and subsequent agglomerate; 3) CO concentration, excessive CO concentration will directly lead to the termination of the reaction.
Ai, Han-Jun,Franke, Robert,Wu, Xiao-Feng
(2020/06/19)

Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation
Histone deacetylase inhibitors (HDACi) have emerged as promising therapeutics for the treatment of neurodegeneration, cancer, and rare disorders. Herein, we report the development of a series of spiroindoline-based HDAC6 isoform-selective inhibitors based on the X-ray crystal studies of the hit 6a. We identified compound 6j as the most potent and selective hHDAC6 inhibitor of the series. Biological investigation of compounds 6b, 6h, and 6j demonstrated their antiproliferative activity against several cancer cell lines. Western blotting studies indicated that they were able to increase tubulin acetylation, without significant variation in histone acetylation state, and induced PARP cleavage indicating their apoptotic potential at the molecular level. 6j induced HDAC6-dependent pSTAT3 inhibition.
Saraswati, A. Prasanth,Relitti, Nicola,Brindisi, Margherita,Osko, Jeremy D.,Chemi, Giulia,Federico, Stefano,Grillo, Alessandro,Brogi, Simone,McCabe, Niamh H.,Turkington, Richard C.,Ibrahim, Ola,O'Sullivan, Jeffrey,Lamponi, Stefania,Ghanim, Magda,Kelly, Vincent P.,Zisterer, Daniela,Amet, Rebecca,Hannon Barroeta, Patricia,Vanni, Francesca,Ulivieri, Cristina,Herp, Daniel,Sarno, Federica,Di Costanzo, Antonella,Saccoccia, Fulvio,Ruberti, Giovina,Jung, Manfred,Altucci, Lucia,Gemma, Sandra,Butini, Stefania,Christianson, David W.,Campiani, Giuseppe
supporting information
p. 2268 - 2276
(2020/12/17)

A Metallaphotoredox Strategy for the Cross-Electrophile Coupling of α-Chloro Carbonyls with Aryl Halides
Here, we demonstrate that a metallaphotoredox-catalyzed cross-electrophile coupling mechanism provides a unified method for the α-arylation of diverse activated alkyl chlorides, including α-chloroketones, α-chloroesters, α-chloroamides, α-chlorocarboxylic acids, and benzylic chlorides. This strategy, which is effective for a wide variety of aryl bromide coupling partners, is predicated upon a halogen atom abstraction/nickel radical-capture mechanism that is generically successful across an extensive range of carbonyl substrates. The construction and use of arylacetic acid products have further enabled two-step protocols for the delivery of valuable building blocks for medicinal chemistry, such as aryldifluoromethyl and diarylmethane motifs.
Chen, Tiffany Q.,MacMillan, David W. C.
supporting information
p. 14584 - 14588
(2019/09/17)

Palladium-Catalyzed, ortho-Selective C-H Halogenation of Benzyl Nitriles, Aryl Weinreb Amides, and Anilides
A palladium-catalyzed, ortho-selective C-H halogenation methodology is reported herein. The highlight of the work is the highly selective C(sp2)-H functionalization of benzyl nitriles in the presence of activated C(sp3)-H bond, which results in good yields of the halogenated products with excellent regioselectivity. Along with benzyl nitriles, aryl Weinreb amides and anilides have been evaluated for the transformation using aprotic conditions. Mechanistic studies yield interesting aspects with respect to the pathway of the reaction and the directing group abilities.
Das, Riki,Kapur, Manmohan
p. 1114 - 1126
(2018/06/18)

SELECTIVE HDAC6 INHIBITORS
The present invention provides hydroxamic acids of the formula described herein, that have activity toward inhibiting histone deacetylases, and in particular HDAC6. Also contemplated are pharmaceutical compositions and methods of use of an effective amount of the hydroxamic acid compounds provided, for treating a disease in a subject. In certain embodiments, the subject is afflicted with cancer, neurodegenerative disease, or HIV infection.
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Page/Page column 51

(2015/07/15)

The Concise Synthesis of Unsymmetric Triarylacetonitriles via Pd-Catalyzed Sequential Arylation: A New Synthetic Approach to Tri- and Tetraarylmethanes
The selective synthesis of multiarylated acetonitriles via sequential palladium-catalyzed arylations of chloroacetonitrile is reported. The three aryl groups are installed via a Pd-catalyzed Suzuki-Miyaura cross coupling reaction followed by back-to-back C-H arylations to afford triarylacetonitriles in three steps with no over-arylation at any step. The triarylacetonitrile products can be converted into highly functionalized species including tetraarylmethanes. This new strategy provides rapid access to a variety of unsymmetrical tri- and tetraarylmethane derivatives from simple, readily available starting materials. (Chemical Presented)
Nambo, Masakazu,Yar, Muhammad,Smith, Joel D.,Crudden, Cathleen M.
supporting information
p. 50 - 53
(2015/07/28)

Alkylations of Arylboronic Acids including Difluoroethylation/Trifluoroethylation via Nickel-Catalyzed Suzuki Cross-Coupling Reaction
An efficient alkylation method of functionalized alkyl halides under mild nickel-catalyzed C(sp3)-(sp2) Suzuki cross-coupling conditions is described. The features of this approach are excellent functional group compatibility, low cost nickel catalyst, and the use of a mild base. This is also the first successful example of the nickel-catalyzed direct 2,2-difluoroethylation or 2,2,2-trifluoroethylation of aryl-/heteroarylboronic acids.
Zhang, Xiaofei,Yang, Chunhao
supporting information
p. 2721 - 2727
(2015/09/01)

Synthesis of α-aryl esters and nitriles: Deaminative coupling of α-aminoesters and α-aminoacetonitriles with arylboronic acids
Transition-metal-free synthesis of α-aryl esters and nitriles using arylboronic acids with α-aminoesters and α-aminoacetonitriles, respectively, as the starting materials has been developed. The reaction represents a rare case of converting C(sp3)-N bonds into C(sp3)-C(sp2) bonds. The reaction conditions are mild, demonstrate good functional-group tolerance, and can be scaled up. Touch base: A transition-metal-free protocol for the synthesis of α-aryl esters and nitriles by deaminative coupling is presented. Strong bases and transition-metal catalysts are not needed. The new synthetic method uses readily available starting materials and demonstrates wide substrate scope.
Wu, Guojiao,Deng, Yifan,Wu, Chaoqiang,Zhang, Yan,Wang, Jianbo
supporting information
p. 10510 - 10514
(2016/02/18)

Rhodium-catalyzed asymmetric hydrogenation of olefins with PhthalaPhos, a new class of chiral supramolecular ligands
A library of 19 binol-derived chiral monophosphites that contain a phthalic acid diamide group (Phthala- Phos) has been designed and synthesized in four steps. These new ligands were screened in the rhodium-catalyzed enantioselective hydrogenation of prochiral dehydroamino esters and enamides. Several members of the library showed excellent enantioselectivity with methyl 2-acetamido acrylate (6 ligands gave >97% ee), methyl (Z)-2- acetamido cinnamate (6 ligands gave >94% ee), and N-(1-phenylvinyl)acetamide (9 ligands gave >95% ee), whilst only a few representatives afforded high enantioselectivities for challenging and industrially relevant substrates N-(3,4-dihydronaphthalen-1- yl)-acetamide (96% ee in one case) and methyl (E)-2-(acetamidomethyl)-3- phenylacrylate (99% ee in one case). In most cases, the new ligands were more active and more stereoselective than their structurally related monodentate phosphites (which are devoid of functional groups that are capable of hydrogen-bonding interactions). Control experiments and kinetic studies were carried out that allowed us to demonstrate that hydrogen-bonding interactions involving the diamide group of the PhthalaPhos ligands strongly contribute to their outstanding catalytic properties. Computational studies carried out on a rhodium precatalyst and on a conceivable intermediate in the hydrogenation catalytic cycle shed some light on the role played by hydrogen bonding, which is likely to act in a substrate-orientation effect.
Pignataro, Luca,Boghi, Michele,Civera, Monica,Carboni, Stefano,Piarulli, Umberto,Gennari, Cesare
supporting information; experimental part
p. 1383 - 1400
(2012/03/27)

HISTONE DEACETYLASE INHIBITORS
Provided herein are isoform selective histone deacetylase inhibitors of the formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, metabolites, prodrugs, solvates, pharmaceutically acceptable salts and compositions thereof. These compounds are isoform selective inhibitors of HDACs and are useful as a therapeutic or ameliorating agent for diseases that are involved in cellular growth such as cancer, malignant tumors, autoimmune diseases, skin diseases, fungal infections, protozoal infections, HIV, inflammation and CNS disorders.
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Page/Page column 37

(2012/09/21)

Phthalaphos: Chiral supramolecular ligands for enantioselective rhodium-catalyzed hydrogenation reactions
Interligand hydrogen bonding of chiral monodentate phosphite ligands bearing H-bond donor and acceptor groups leads to formation of supramolecular bidentate ligands, rhodium complexes of which (see picture) afford excellent enantiomeric excesses in catalyzed hydrogenation of classical benchmark and industrially relevant substrates. cod=1,5-cyclooctadiene.
Pignataro, Luca,Carboni, Stefano,Civera, Monica,Colombo, Raffaele,Piarulli, Umberto,Gennari, Cesare
supporting information; experimental part
p. 6633 - 6637
(2010/10/21)

Paracyclophanes: Extending the bridges. Synthesis
Preparatively satisfactory routes to [3.2]paracyclophane (10), [4.2]paracyclophane (14), [4.3]paracyclophane (19) as well as several derivatives of these compounds - among others the bromides 25, the ester 31, the diesters 40-43 - are described using well-established methods of cyclophane chemistry (ring-closure reactions leading to thiacyclophanes, ring contraction by sulfone pyrolysis). The parent systems and their derivatives are now available in gram quantities allowing a study of their chemical properties. Wiley-VCH Verlag GmbH & Co. KGaA, 2009.
Pechlivanidis, Zissis,Hopf, Henning,Ernst, Ludger
experimental part
p. 223 - 237
(2009/06/21)

AMINOALKYLAZOLE DERIVATIVES AS HISTAMINE-3 ANTAGONISTS
The present invention provides a compound of formula I: and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
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Page/Page column 26

(2009/02/11)

N-substituted-azacyclylamines as histamine-3 antagonists
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
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Page/Page column 31

(2010/11/28)

Multicyclic bis-amide MMP inhibitors
The present invention relates generally to bis-amide group containing pharmaceutical agents, and in particular, to multicyclic bis-amide MMP-13 inhibitor compounds. More particularly, the present invention provides a new class of MMP-13 inhibiting compounds, containing a pyrimidinyl bis-amide group in combination with a heterocyclic moiety, that exhibit an increased potency and solubility in relation to currently known bis-amide group containing MMP-13 inhibitors.
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Page/Page column 118-119

(2008/06/13)

NOVEL ETHYLENEDIAMINE DERIVATIVES
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 117

(2010/02/14)

Novel peripherally functionalized seco-porphyrazines: Synthesis, characterization and spectroscopic evaluation
Co-macrocyclizations of 2,3-dipropylmaleonitrile and 2,3-di-(4- (methoxycarbonyl)phenyl)maleonitrile, respectively, with N,N′-dibenzyl-N, N′-di-(11-tetrahydropyranyloxy-3,6,9-trioxo-undecyl))maleonitrile and N,N,N′,N′-tetramethylmaleonitrile were used to prepare derivatives of the 4,5-diamino-porphyrazine systems including the zinc(II) complexes. Subsequent oxidation of the macrocycles with potassium permanganate gave the corresponding seco-porphyrazines. These were shown to be efficient sensitizers for the production of singlet oxygen (ΦΔ=0.15-0.57) by the determination of their photophysical properties.
Sakellariou, Efstathia G.,Montalban, Antonio Garrido,Beall, Scott L.,Henderson, David,Meunier, Hubert G.,Phillips, David,Suhling, Klaus,Barrett, Anthony G. M.,Hoffman, Brian M.
p. 9083 - 9090
(2007/10/03)

Phenethyl amides as novel noncovalent inhibitors of hepatitis C virus NS3/4A protease: Discovery, initial SAR, and molecular modeling
The discovery of novel, reversible and competitive tripeptide inhibitors of the Hepatitis C virus NS3/4A serine protease is described. These inhibitors are characterized by the presence of a C-terminal phenethyl amide group, which extends into the prime side of the enzyme. Initial SAR together with molecular modeling and data from site-directed mutagenesis suggest an interaction of the phenethyl amide group with Lys-136.
Colarusso, Stefania,Koch, Uwe,Gerlach, Benjamin,Steinkühler, Christian,De Francesco, Raffaele,Altamura, Sergio,Matassa, Victor G.,Narjes, Frank
p. 345 - 348
(2007/10/03)

6-substituted pyrazolo[3,4-d]pyrimidin-4-ones useful as cyclin dependent kinase inhibitors
The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
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(2008/06/13)

Sulfonyl derivatives
Sulfonyl derivatives represented by general formula (I), salts of the same, and solvates of both: and application of them as drugs: [wherein R1is hydrogen, hydroxyl, nitro or the like; R2and R3are each independently hydrogen, halogeno or the like; R4and R5are each dependently hydrogen, halogeno or the like; Q1is an optionally substituted saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group or the like; Q2is a single bond, oxygen or the like; Q3is, e.g., a group represented by formula (a): T1is carbonyl or the like; and X1and X2are each independently methylidyne or nitrogen]. These compounds exhibit potent Fxa inhibiting activities and serve as excellent anticoagulants which speedily exert satisfactory and persistent anti-thrombotic effects through oral administration and little cause adverse effects.
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(2008/06/13)

Synthesis and photophysical characterization of a new, highly hydrophilic caging group
o-Nitrobenzyl-protected bioactive compounds are useful tools in biophysics, allowing controlled photorelease of biologically active compounds with high temporal and spatial precision. Thus, it is possible to study biological processes, such as neurotransmitter-receptor interaction, and many other processes, in much more detail than before. In this respect, these caged compounds have become established as extremely useful tools. In some cases, however, their biological properties (the caged compound should not interact with the biological system), their photochemical properties (quantum yield and kinetics of the photorelease), and their physical properties (high hydrophilicity) are not satisfactory. In order to address the last problem, we examined means to increase the hydrophilicity of caged compounds based on the o-nitrobenzyl moiety. Here, we report the synthesis and the photochemical and biological characterization of a new caged Daspartate derivative with vastly improved hydrophilicity, compared to derivatives reported previously, and satisfactory photophysical properties. Caged compounds with this improved o-nitrobenzyl group may thus represent a valuable new tool for different kinds of biophysical investigations. Wiley-VCH Verlag GmbH, 69451 Weinheim, Germany, 2002.
Schaper, Klaus,Abdollah Madani Mobarekeh,Grewer, Christof
p. 1037 - 1046
(2007/10/03)

6-SUBSTITUTED PYRAZOLO[3,4-D] PYRIMIDIN-4-ONES USEFUL AS CYCLIN DEPENDENT KINASE INHIBITORS
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(2008/06/13)

NAPHTHALENE AMIDES HAVING LEUKOTRIENE-ANTAGONISTIC ACTION
Naphthalene amides of formula (I) wherein the substituent containing A is bound to the 6- or 7- position of the 2-naphthol system; the substituent containing B is bound to the benzene ring at any free position; R is hydrogen or methyl; R is hydrogen, fluorine, chlorine or -OCH3, which is bound to the naphthalene system at any positions except the 2- and the one occupied by the other substituent; R is hydrogen, fluorine, chlorine or bromine; A- is -CO-NR- or -NR-CO- group, wherein R is hydrogen or methyl; B is a 5-tetrazolyl or -COOR group, wherein R is hydrogen, a (C1-C4)-alkyl or a phenylalkyl group of less than 10 carbon atoms; m is 0 or 1; n and p are integers from 0 to 6, with the proviso that n + p is less or equal to 6; as well as the solvates and pharmaceutically acceptable salts thereof, have leukotriene antagonistic action.
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(2008/06/13)

NOVEL SULFONYL DERIVATIVES
Sulfonyl derivatives represented by the following general formula (I): Q1-Q2-T1-Q3-SO2-QA and drugs containing the same (wherein Q1 is an optionally substituted, saturated or unsaturated, five- or six-membered cyclic hydrocarbon group, a five- or six-membered heterocyclic group, or the like; Q2 is a single band, oxygen, sulfur, C1-C6 alkylene or the like; QA is optionally substituted arylalkenyl, heteroarylalkenyl or the like; and T1 is carbonyl or the like). These compounds have potent FXa-inhibitory effects and promptly exert satisfactory and persistent antithrombotic effects through oral administration, thus being useful as anticoagulant agents little accompanied with side effects.
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(2008/06/13)

Potent dibasic GPIIb/IIIa antagonists with reduced prolongation of bleeding time: Synthesis and pharmacological evaluation of 2-oxopiperazine derivatives
A series of 2-oxopiperazine derivatives, possessing basic moieties at the 3- and the 4-positions, were synthesized and evaluated for their abilities to inhibit platelet aggregation and for their effects on bleeding time. Among the compounds, 2-[(3S)-4-[2-[(4-guanidinobenzoyl)amino] acetyl]3-[3-[(4-guanidinobenzoyl)amino]propyl]-2-oxopiperazinyl]acetic acid (12c) showed a potent inhibitory effect on platelet aggregation and good dissociation between the efficacy and the bleeding side effect. Intravenous infusion of compound 12c at 1.6 μg/mL/min. completely prevented arterial thrombus formation induced by endothelial injury in guinea pigs. The dose of 12c that prolonged the bleeding time to three times the control value was 5.8/μg/mL/min. These results suggest that compound 12c might be useful in the clinical treatment of thrombotic diseases, and we selected 12c (TAK-024) as a candidate for the clinical trials.
Kitamura,Fukushi,Miyawaki,Kawamura,Konishi,Terashita,Naka
p. 2438 - 2450
(2007/10/03)

Synthesis and biodistribution of technetiuim-99m-labelled N-(diethylaminoethyl)benzamide via a bis(dithiocarbamate) nitridotechnetium(V) complex.
N-(2-diethylaminoethyl)-4-iodobenzamide has been reported to be an excellent agent for malignant melanoma diagnosis by SPECT. To obtain a 99mTc analogue, we synthesized a sodium {2-[4-(N-diethylaminoethylcarbamoyl)phenyl]ethyl}-N-methyldithiocarbamate ligand in 7 steps from methyl 4-(bromomethyl)benzoate. The corresponding nitridotechnetium complex formed by a ligand exchange method was purified and its biodistribution in mice bearing the B16 murine melanoma was determined.
Auzeloux,Papon,Masnada,Borel,Moreau,Veyre,Pasqualini,Madelmont
p. 325 - 335
(2007/10/03)

Repaglinide and related hypoglycemic benzoic acid derivatives
The structure-activity relationships in two series of hypoglycemic benzoic acid derivatives (5, 6) were investigated. Series 5 resulted from meglitinide (3) when the 2-methoxy was replaced by an alkyleneimino residue. Maximum activity was observed with the cis-3,5-dimethylpiperidino (5h) and the octamethyleneimino (5l) residues. Series 6 resulted from the meglitinide analogon 4 bearing an inversed amido function when the 2-methoxy, the 5- fluoro, and the α-methyl residue were replaced by a 2-piperidino, a 5- hydrogen, and a larger α-alkyl residue, respectively. An alkoxy residue ortho to the carboxy group further increased activity and duration of action in the rat. The most active racemic compound, 6al (R4 = isobutyl; R = ethoxy), turned out to be 12 times more active than the sulfonylurea (SU) glibenclamide (1). Activity was found to reside predominantly in the (S)- enantiomers. Compared with the SUs 1 and 2 (glimepiride), the most active enantiomer, (S)-6al (AG-EE 623 ZW; repaglinide; ED50 = 10 μg/kg po), is 25 and 18 times more active. Repaglinide turned out to be a useful therapeutic for type 2 diabetic patients; approval was granted recently by the FDA and the EMEA. From investigations on the pharmacophoric groups in compounds of type 5 and 6, it was concluded that in addition to the two already known - the acidic group (COOH; S02NH) and the amidic spacer (CONH; NHCO) - the ortho residue R1 (alkyleneimino; alkoxy; oxo) must be regarded as a third one. A general pharmacophore model suitable for hypoglycemic benzoic acid derivatives, SUs, and sulfonamides is proposed (Figure 6). Furthermore, from superpositions of low-energy conformations (LECs) of 1, 2, and (S)-6al, it was concluded that a common binding conformation (LEC II; Figure 10B) may exist and that differences in binding to the SU receptor and in the mechanism of insulin release between repaglinide and the two SUs may be due to specific hydrophobic differences.
Grell, Wolfgang,Hurnaus, Rudolf
p. 5219 - 5246
(2007/10/03)

CARBONYLATION OF p-HALOGENOBENZYL CYANIDES IN THE PRESENCE OF COBALT OCTACARBONYL. TEST FOR RADICAL-ANION MECHANISM
In the reaction of p-halogenobenzyl cyanides with sodium thiophenolate under the conditions of an SRN1 reaction the intermediately formed radical-anion undergoes fragmentation in two concurrent directions, i.e., with elimination of the cyanide ion and with elimination of the halide ion.The presence of the two fragmentation paths was used as evidence for the radical-anion nature of the intermediates in the carbonylation of aryl halides.
Dneprovskii, A. S.,Tuchkin, A. I.
p. 435 - 441
(2007/10/02)

Nitrogenous bicyclic derivatives substituted with benzyl
Novel bicyclic compounds in all possible racemic, enantiomeric and diasteroisomeric forms of the formula STR1 having antagonistic properties for angiotensin II receptors and novel intermediates and process for their preparation.
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(2008/06/13)

Diphosphonic acid derivatives, processes for the preparation thereof and pharmaceutical compositions containing them
Diphosphonate compounds, processes for their preparation and pharmaceutical compositions containing them and being useful for treating calcium metabolism disorders. The diphosphonates are of the formula STR1 wherein R1 and R2 are hydrogen, acyl or alkyl which can be substituted by aryl, R3 and R4 are hydrogen or alkyl or R3 and R4 together represent lower alkylene, R5 is a hydrogen atom or alkyl, X is a valency bond or alkylene, Y is a valency bond, alkylene or substituted alkylene, Z is hydrogen, hydroxyl or amino group optionally substituted by alkyl and n is 1, 2 or 3; and including the pharmacologically acceptable salts thereof.
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(2008/06/13)

Amidine derivatives and cardiotonic compositions
Amidine derivatives of the formula STR1 wherein R1 and R2, which may be the same or different, represent each a hydrogen atom or a lower alkyl group, or R1 and R2 together with an intermediary carbon atom and/or hetero atom may form a ring; X represents STR2 (wherein R8 represents a hydrogen atom, a lower alkyl group, or --CH2 COOR9, where R9 represents a hydrogen atom or a lower alkyl group; Z represents a single bond, --CH2 --, --CH2 CH2 --, or --CH=CH--); R3 represents a hydrogen or chlorine atom, methoxy group, nitro group, or amino group; Y represents --CH2 CH2 --, --CH=CH--, --CH2 O--, or --OCH2 --; R4 represents a hydrogen atom, methoxy group, benzoyl group, nitro group, or amino group; and R5, R6 and R7, which may be the same or different, represent each a hydrogen atom, lower alkyl group, cycloalkyl group, aralkyl group, substituted alkyl group, substituted aralkyl group, or amino group, or R5 and R7 may form a ring, or salts thereof have an excellent cardiotonic activity and can be used as cardiotonics.
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(2008/06/13)

Effects of neutral and anionic substituents on the carbonyl stretching bands of substituted methylbenzoates
Effects of neutral and anionic substituents on frequencies (νCO) and integrated intensities (ACO) of the carbonyl stretching bands of substituted methylbenzoates (solvent dimethyl sulphoxide) have been studied in relation to Hammett's equation: satisfactory correlations have been found between νCO and δ+ constants, as well as by using the dual-parameter equations to Yukawa, Tsuno and Taft; ACO have been found to increase in cases of strong electron-releasing substituents.It has been found that constants of anionic substituents, determined on the basis of nitrile i.r. frequencies and intensities, reflect satisfactorily the effects of these sobstituents on νCO and ACO of methylbenzoates.
Vassileva, P. J.,Binev, I. G.,Juchnovski, I. N.
p. 709 - 712
(2007/10/02)