- ARYL SULFONAMIDES AS SMALL MOLECULE STAT3 INHIBITORS
-
The present disclosure provides pharmaceutical compositions comprising aryl sulfonamide Stat3 small molecule inhibitors and certain pharmaceutically acceptable salts thereof, and methods of their use for treating cancer.
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-
Paragraph 00278; 00280
(2021/01/29)
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- An alternative route for boron phenoxide preparation from arylboronic acid and its application for C[sbnd]O bond formation
-
An efficient synthetic route to benzyl phenyl ether preparation has been successfully developed via a one-pot synthetic protocol utilizing a combination of arylboronic acids, hydrogen peroxide (H2O2), and benzyl halides. The whole procedure consists of two consecutive reactions, formation of boron phenoxide from arylboronic acids and its nucleophilic attack. A simple operation under mild conditions such as room-temperature ionic liquid (choline hydroxide), aerobic environment, and absence of metal- and base-catalysts has been employed. Expansion to utilize benzyl surrogates was also successfully accomplished.
- Joo, Seong-Ryu,Kim, Seung-Hoi,Lim, In-Kyun
-
-
- Preparation method of hydroxyphenylboronic acid
-
The invention discloses a preparation method of hydroxyphenylboronic acid, which belongs to the technical field of boric acid synthesis in medical intermediates. The method comprises the following steps: starting from bromophenol, carrying out BOC, trimethylsilyl or benzyl protection, forming a Grignard reagent, reacting with borate, or carrying out one-pot reaction with borate and n-butyllithium,and hydrolyzing to obtain hydroxyphenylboronic acid. According to the invention, cheap and easily available protecting groups are adopted, so that the protecting groups are easy to remove during boronation reaction hydrolysis, industrial amplification is easy to realize, batch production is carried out on the scale of dozens of kilograms, and the process stability is good.
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Paragraph 0026-0028
(2020/05/08)
-
- Benzo piperidine derivatives for the preparation of (by machine translation)
-
The present invention provides benzo piperidine derivatives of the preparation method. Specifically, under alkaline conditions, type II - e of a compound of formula II - d as shown in the optionally under the action of catalyst reaction of type II - c as
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Paragraph 0166-0168
(2019/07/11)
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- NOVEL MODULATORS OF THE SIGMA-2 RECEPTOR AND THEIR METHOD OF USE
-
Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of sigma- 2 receptor activity.
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Paragraph 0569; 0570
(2018/10/19)
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- 5-HYDROXYTRYPTAMINE RECEPTOR 7 MODULATORS AND THEIR USE AS THERAPEUTIC AGENTS
-
Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity.
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Paragraph 0515; 0516
(2018/10/19)
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- METHOD FOR PRODUCING XANTHENE DERIVATIVE, COMPOUND AND SALT THEREOF
-
PROBLEM TO BE SOLVED: To provide a production method capable of efficiently producing a xanthene derivative at a low cost with fewer production steps compared with conventional production methods in the production of a xanthene derivative, and a compound
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Paragraph 0193-0194
(2019/01/05)
-
- Synthesis and evaluation of small molecules bearing a benzyloxy substituent as novel and potent monoamine oxidase inhibitors
-
A new series of small molecules bearing a benzyloxy substituent have been designed, synthesized and evaluated for hMAO inhibitory activity in vitro. Most of the compounds were potent and selective MAO-B inhibitors, and were weak inhibitors of MAO-A. In particular, compounds 9e (IC50 = 0.35 μM) and 10e (IC50 = 0.19 μM) were the most potent MAO-B inhibitors, and exhibited the highest selectivity for MAO-B (9e, SI > 285.7-fold and 10e, SI = 146.8-fold). In addition, the structure-activity relationships for MAO-B inhibition indicated that electron-withdrawing groups in the open small molecules were more suitable for MAO-B inhibition, and substitutions at the benzyloxy of the open small molecules, particularly with the halogen substituted benzyloxy, were more favorable for MAO-B inhibition. Molecular docking studies have been done to explain the potent MAO-B inhibition of the open small molecules. Furthermore, the representative compounds 9e and 10e showed low neurotoxicity in SH-SY5Y cells in vitro. So the small molecules bearing the benzyloxy substituent could be used to develop promising drug candidates for the therapy of neurodegenerative diseases.
- Lan, Jin-Shuai,Zhang, Tong,Liu, Yun,Zhang, Yong,Hou, Jian-wei,Xie, Sai-Sai,Yang, Jing,Ding, Yue,Cai, Zhen-zhen
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p. 471 - 478
(2017/03/08)
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- Palladium-Catalyzed Synthesis of Pyrayaquinones, Murrayaquinones, and Murrayafoline-B
-
We describe the total synthesis of murrayafoline-B and seven carbazole-1,4-quinone alkaloids. A palladium(II)-catalyzed oxidative cyclization is used to construct the carbazole skeleton. Pyran annulation and oxidation provide pyrayaquinone-A, -B, and -C. DIBAL-H-promoted reductive ring opening of pyrano[3,2-a]carbazole precursors leads to the prenylated and geranylated carbazole-1,4-quinone alkaloids murrayaquinone-B, -C, -D, and -E and to murrayafoline-B.
- Kutz, Sebastian K.,Schmidt, Arndt W.,Kn?lker, Hans-Joachim
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p. 275 - 292
(2016/12/24)
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- TRIAZOLOPYRIDINE INHIBITORS OF MYELOPEROXIDASE
-
The present invention provides compounds of Formula (I): wherein A is as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.
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Paragraph 00245
(2017/03/28)
-
- Opioid Detection
-
An immunoassay method is described which detects O-desmethyltramadol only. This enables an assay of high sensitivity and specificity avoiding false positive results. The unique antibodies incorporated in the immunoassay method can be combined with antibodies which detect mitragynine to provide an assay which increases the possibility of detecting the commonly found drug combination of O-desmethyltramadol and mitragynine.
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Paragraph 0009; 0079
(2017/07/14)
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- TRICYCLIC COMPOUND AND USE THEREOF
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The present invention relates to: a compound selected from the group consisting of a tricyclic compound having the structure of formula I, a pharmaceutically acceptable salt, an isomer, a solvate and a precursor thereof; and a use thereof. The compound effectively controls GPR40, and thus, can be effectively used for the prophylaxis or treatment of diseases associated with GPR40, for example, diabetes and many other diseases.
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Paragraph 1227; 1228; 1229
(2016/01/25)
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- TETRASUBSTITUTED ALKENE COMPOUNDS AND THEIR USE
-
Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.
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Page/Page column 140; 141
(2016/12/22)
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- Effect of Ring Functionalization on the Reaction Temperature of Benzocyclobutene Thermoset Polymers
-
The temperature required to induce cross-linking in typical benzocyclobutene-based thermosets is near 250 °C, which exceeds the use temperature of many chemical components. A new and versatile synthesis of BCB-functionalized monomers has allowed access to monomers that can be incorporated into a variety of macromolecular platforms to enable significantly reduced cure temperatures. Incorporation of BCB-functionalized comonomers in polystyrene and polynorbornene enabled insolublization of thin films by curing at only 120 °C for 1 h.
- Hayes, Colin O.,Chen, Peng-Hao,Thedford, R. Paxton,Ellison, Christopher J.,Dong, Guangbin,Grant Willson
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p. 3706 - 3715
(2016/06/09)
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- With anti-tumor activity of a biphenyl amide compound and its preparation method and application
-
The invention discloses a diphenyl amide compound with anti-tumor activity as well as a preparation method and an application of the diphenyl amide compound. The structural formula of the compound is shown in the specification, wherein R1 is hydrogen or halogen, R2 is alkoxyl which is substituted by tertiary amino at the tail end and has 1-4 carbon atoms and R2 is connected to the para-position of amide through oxygen atoms. The compound has good inhibiting activity to tumor cells in vitro and can be used for preparing anti-tumor medicines, particularly anti-liver cancer medicines and anti-breast cancer medicines. The preparation method of the diphenyl amide compound has the advantages of easily available raw materials, mild reaction condition, simple reaction operation process and cheap used reagents.
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Paragraph 0045; 0046
(2016/10/07)
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- With anti-tumor activity of a biphenyl amide compound and its preparation method and application
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The invention discloses a biphenyl amide compound with antitumor activity as well as a preparation method and application thereof. The structural formula of the compound is shown in the specification, wherein in the structural formula, R1 is hydrogen or halogen; R2 is alkoxy with carbon number of 1-4; the terminal of R2 is replaced by tert-amido; R2 is linked to the para-position of amide via an oxygen atom. The compound has good tumor cell inhibiting activity in vitro and can be used for preparing antitumor drugs, especially anti-hepatoma drugs and anti-breast cancer drugs. The preparation method of the biphenyl amide compound, provided by the invention, has the advantages that the raw materials are accessible, the reaction conditions are mild, the reaction process is simple to operate, and the used reagent is cheap.
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Paragraph 0048; 0049; 0050
(2016/11/24)
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- Discovery of biphenyl-based VEGFR-2 inhibitors. Part 3: Design, synthesis and 3D-QSAR studies
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VEGFR-2 plays an essential role in angiogenesis and is a central target for anticancer drug discovery. In order to develop novel VEGFR-2 inhibitors, we designed and synthesized 33 biphenyl amides based on our previously reported lead compound. The biological results indicated that four compounds (18b, 20e, 20h and 20j) are potent VEGFR-2 inhibitors which are comparable to positive control. Compound 18b displayed the most potent VEGFR-2 inhibition with IC50 value of 2.02 nM. Moreover, it exhibited promising antiproliferative activity against MCF-7 and SMMC-7721 cells with IC50 values of 1.47 μM and 5.98 μM, respectively. Molecular docking and 3D-QSAR studies were also carried out. The results indicated that these biphenyl amides could serve as promising leads for further optimization as novel VEGFR-2 inhibitors.
- Lu, Wen,Li, Pengfei,Shan, Yuanyuan,Su, Ping,Wang, Jinfeng,Shi, Yaling,Zhang, Jie
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p. 1044 - 1054
(2015/03/04)
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- FUROPYRIDINES AS BROMODOMAIN INHIBITORS
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The present invention relates to novel compounds, pharmaceutical compositions containing such compounds and to their use in therapy.
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-
Page/Page column 44
(2014/09/29)
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- PESTICIDE
-
A novel pesticide is provided. The present invention provides a compound represented by the formula (I) or its salt: wherein Q is phenyl or pyridyl which may be substituted; W is an oxygen atom or S(O)m; each of A1 to A5 is -C(R5)= or a nitrogen atom, provided that among A1 to A5, the number of groups which may be nitrogen atoms, is from 0 to 2; each of B1 to B4 is a hydrogen atom, a halogen atom, alkyl or haloalkyl; each of R1 and R2 is a hydrogen atom, a halogen atom, alkyl, haloalkyl, alkoxy, haloalkoxy or cyano; and R3 is alkyl or haloalkyl.
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Page/Page column 21
(2013/03/26)
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- Design, synthesis, and biological activity of a novel series of human sirtuin-2-selective inhibitors
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Selective inhibitors of human sirtuin 2 (SIRT2), a deacetylase, are candidate therapeutic agents for neurodegenerative diseases such as Parkinson's disease and Huntington's disease as well as potential tools for elucidating the biological functions of SIRT2. On the basis of homology models of SIRT1 and SIRT2, we designed and prepared a series of 2-anilinobenzamide analogues. Enzyme assays using recombinant SIRT1 and SIRT2 revealed that 3'-phenethyloxy-2- anilinobenzamide analogues such as 33a and 33i are potent and selective SIRT2 inhibitors, showing more than 3.5-fold greater SIRT2-inhibitory activity and more than 35-fold greater SIRT2-selectivity compared with AGK2 (3), a previously reported SIRT2-selective inhibitor. Compound 33a also induced a dose-dependent selective increase of α-tubulin acetylation in human colon cancer HCT116 cells, indicating selective inhibition of SIRT2 in the cells. These 3'-phenethyloxy-2-anilinobenzamide derivatives represent an entry into a new class of SIRT2-selective inhibitors.
- Suzuki, Takayoshi,Khan, Mohammed Naseer Ahmed,Sawada, Hideyuki,Imai, Erika,Itoh, Yukihiro,Yamatsuta, Katsura,Tokuda, Natsuko,Takeuchi, Jun,Seko, Takuya,Nakagawa, Hidehiko,Miyata, Naoki
-
experimental part
p. 5760 - 5773
(2012/07/28)
-
- The dramatic influence of the location of bend and of lateral fluoro substitution on the mesomorphic properties of angular chiral esters based on a 1,3-disubstituted benzene ring
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The synthesis and mesomorphic properties of a range of 3-ring and 4-ring chiral esters based on a 1,3-disubstituted benzene unit are detailed. These materials all deviate from the usual linear molecular architecture of liquid crystals, and hence are all angular in nature. Some of these materials have the bend right at the end of the molecule where the chain deviates from the normal linear arrangement, and hence a 'hockey stick' molecular architecture is perhaps an accurate description. Other materials have a genuine bent-core construction where the bend is towards the centre of the molecule, and hence are best termed as 'boomerang' shape. In all cases, interesting comparisons of mesophase morphology and transition temperatures were found, both between the various angular materials and with their linear analogues. In particular, the influence on transition temperatures of lateral fluoro substitution in the novel angular materials was found to be wholly different to that found in the known linear analogues. The work forms part of a larger on-going research programme to investigate the mesomorphic and chirality-dependent properties of angular liquid crystals. The research revealed that no mesomorphism in parent compounds is possible when the bend is close to the centre of the molecule, however, lateral fluoro substitution of such compounds facilitates the generation of liquid crystal phases. Where the molecular bend is as a consequence of the terminal unit at the end of the core, then surprisingly high clearing points resulted, and such materials were found to show the potential for a high tilt angle, and a strong tendency towards helical mesophases. Lateral fluoro substitution of these latter examples resulted consistently in significantly higher clearing points, which is in marked contrast to the behaviour reported previously in known liquid crystals of linear molecular architectures. The Royal Society of Chemistry.
- Fergusson, Kenneth M.,Hird, Michael
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supporting information; experimental part
p. 3069 - 3078
(2011/08/03)
-
- Efficient Arndt-Eistert synthesis of selective 5-HT7 receptor antagonist SB-269970
-
This contribution describes a novel Arndt-Eistert approach for the efficient synthesis of the potent and selective 5-HT7-antagonist, (R)-3-(2-(2-(4-methylpiperidin-1-yl)-ethyl)pyrrolidine-1-sulfonyl)phenol (SB-269970), from D-proline. The synthesis was ca
- Schjoth-Eskesen, Christina,Jensen, Henrik Helligso
-
experimental part
p. 3243 - 3253
(2011/03/17)
-
- QUATERNARY ALPHA-AMINOCARBOXAMIDE DERIVATIVE AS MODULATORS OF VOLTAGE-GATED SODIUM CHANNELS
-
The invention relates to quaternary E-aminocarboxyamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, X, q and n are as defined in claim 1, for treating diseases and conditions mediated by modulation of voltage-gated sodium channels.
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Page/Page column 85
(2010/11/27)
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- ORGANIC COMPOUNDS AND THEIR USES
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The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.
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Page/Page column 93
(2010/11/28)
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- Compositions for oxidatively dyeing keratin fibers and methods for using such compositions
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Compositions for dyeing keratin fibers comprise (a) at least one keratin dyeing compound selected from aromatic systems which comprise at least one boronic acid or boronic ester moiety and which are capable of forming upon oxidation a nucleophile or an electrophile, (b) at least one additional keratin dyeing compound selected from the group consisting of auxiliary developers and auxiliary couplers, and (c) a cosmetically suitable medium. Methods for oxidatively dyeing keratin fibers comprise the steps of applying such compositions in the presence of an oxidizing agent and rinsing the hair. A hair coloring product in kit form comprises a first separately packaged container comprising a composition as described above and a second separately packaged container comprising an oxidizing agent.
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Page/Page column 8
(2008/06/13)
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- Synthesis of cage-type molecules with π-cavity and selective gas-phase cation complexation
-
Cage-type molecules composed of phenyl walls and caps were synthesized as hosts for the binding of ammonium and alkali metal cations through cation-π interactions. The synthesis involved a key cyclization step, which was markedly dependent on the capping
- Kim, Jeongryul,Kim, Young Kook,Park, Nokyoung,Hahn, Jong Hoon,Ahn, Kyo Han
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p. 7087 - 7092
(2007/10/03)
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- PHENOXYETHER DERIVATIVES AS PPAR MODULATORS
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The present invention is directed to a compound of formula (I), or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR), such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.
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Page/Page column 123-124; 138
(2008/06/13)
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- Chemoselective Heck arylation of acrolein diethyl acetal catalyzed by an oxime-derived palladacycle
-
A dimeric 4-hydroxyacetophenone oxime-derived palladacycle has been used as a very efficient precatalyst for the chemoselective arylation of acrolein diethyl acetal to give either cinnamaldehyde derivatives or 3-arylpropanoate esters by proper choice of the reaction conditions. The synthesis of cinnamaldehyde derivatives can be performed by Heck reaction of acrolein diethyl acetal with iodo-, bromo- or chloroarenes in N,N-dimethylacetamide (DMA) using K2CO3 as base at 120°C and tetra-n-butylammonium acetate (TBAA) and KCl as additives, followed by acid workup. In the case of 3-arylpropanoate esters the corresponding arylation of acrolein diethyl acetal with iodoarenes can be performed at 90°C in aqueous DMA using (dicylohexyl)methylamine as base, whereas for bromoarenes the reaction has to be performed at 120°C using tetra-n-butylammonium bromide (TBAB) as additive. Alternatively, this process can be performed under microwave irradiation. These couplings take place in good yields and with lower catalyst loading than with palladium(II) acetate as well as in shorter reaction times and with lower excess of acrolein diethyl acetal.
- Nájera, Carmen,Botella, Luis
-
p. 9688 - 9695
(2007/10/03)
-
- Diphenylethylene compounds and uses thereof
-
The present invention relates to Diphenylethylene Compounds and compositions comprising a Diphenylethylene Compound. The present invention also relates to methods for preventing or treating various diseases and disorders by administering to a subject in need thereof one or more Diphenylethylene Compounds. In particular, the invention relates to methods for preventing or treating cancer or an inflammatory disorder by administering to a subject in need thereof one or more Diphenylethylene Compounds. The present invention further relates to articles of manufacture and kits comprising one or more Diphenylethylene Compounds.
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-
- NOVEL BENSOPHENONE DERIVATIVES OR SALTS THEREOF
-
A benzophenone derivative represented by the following formula: whereinR1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl;R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, ???or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.
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-
- Substituted benzoic acid derivatives exhibiting nf-k b inhibiting activity
-
A substituted benzoic acid derivative which is represented by the following formula (I) and has an NF-κB inhibiting action (in the formula, R3, R4 and R5 each independently represents a hydrogen atom, an alkyl group having 1 to 6 carbon(s) or an alkoxy group having 1 to 6 carbon(s); R9 and R10 each independently represents a hydrogen atom, an alkyl group having 1 to 6 carbon(s) or an acyl group having 2 to 11 carbons); R2 represents an optionally-substituted aromatic hydrocarbon group or an optionally-substituted heterocyclic group; and X represents a carboxyl group which may be esterified or amidated).
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Page/Page column 9
(2008/06/13)
-
- Design and synthesis of oxadiazolidinediones as inhibitors of plasminogen activator inhibitor-1
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A novel series of PAI-1 inhibitors containing an oxadiazolidinedione moiety were identified by high through-put screening. Optimization of substituents by parallel synthesis and the iterative design toward understanding structure-activity relationship to improve potency are described.
- Gopalsamy, Ariamala,Kincaid, Scott L.,Ellingboe, John W.,Groeling, Thomas M.,Antrilli, Thomas M.,Krishnamurthy, Girija,Aulabaugh, Ann,Friedrichs, Gregory S.,Crandall, David L.
-
p. 3477 - 3480
(2007/10/03)
-
- NF-KAPPA-B INHIBITOR CONTAINING SUBSTITUTED BENZOIC ACID DERIVATIVE AS ACTIVE INGREDIENT
-
A novel NF-κB inhibitor represented by the following formula (I) is provided.
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-
-
- Inhibitors of prenyl-protein transferase
-
The present invention is directed to macrocyclic compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemothera-peutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
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- Naphthyl compounds and compositions, as estrogen receptor binding agents
-
The invention provides a compound of formula I: STR1 or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions containing a compound of formula I, and methods of using a compound of formula I for inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen dependent cancer.
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-
-
- Naphthyl compounds, compositions, and methods
-
The invention provides naphthyl compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen-dependent cancer.
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-
-
- Benzothiophene compounds, compositions, and method
-
The invention provides benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen-dependent cancer.
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-
-
- Substituted 2,3-aryl-benzothiophene compounds having estrogenic activity
-
The invention provides 2,3-aryl-benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen-dependent cancer.
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-
- Aryl substituted heterocycles
-
The present invention concerns the novel use of aryl substituted heterocycles of formula I, set out below, which antagonize the pharmacological actions of one of ent endogenous neuropeptide tachykinins an the neurokinin 2 (NK2) receptor making them useful whenever such antagonism is desired, such as in the treatment of asthma and related conditions. The invention also provides pharmaceutical compositions containing the aryl substituted heterocycles for use in such treatment. Certain novel aryl substituted heterocycles of formula I and novel intermediates for their manufacture are also provided. STR1
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- Insecticidal 5-substituted-2,4-diaminopyrimidine derivatives
-
An insecticidal composition comprising, in admixture with an agriculturally acceptable carrier, an insecticidally effective amount of a compound of the formula: STR1 wherein R, R1, R2, R3, R7, R8, m, n, and p are as defined herein, and agriculturally acceptable salts thereof, and methods of using the same.
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- Meta-substituted aromatic compounds having six-membered rings, for use in liquid-crystal mixtures
-
Meta-substituted aromatic compounds having six-membered rings, for use in liquid-crystal mixtures Compounds of the formula I STR1 in which X is CH, CF or N, R2 is, for example, an alkyl, ether or ester group, which may also contain a chiral center, and R1 (--A1)a (--M1)b (--A2)c (--M2) d (--A3)e (--M3)f is a mesogenic radical, can advantageously be used as components of liquid-crystal mixtures, in particular ferroelectric liquid-crystal mixtures. The substances of the formula I have a particularly favorable effect on the optical switching angle and the critical pulse area of the mixtures.
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- HETEROCYCLIC DERIVATIVES
-
The invention concerns a heterocyclic derivative of the formula I, or a pharmaceutically-acceptable salt there of. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
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-
- Nucleophilic Substitution of Nitrite in Nitrobenzenes, Nitrobiphenyls and Nitronaphthalenes
-
Aromatic compounds, accessible only by multistep procedures, can be synthesized easily by nucleophilic substitution of nitrite in nitrobenzenes, nitrobiphenyls, and nitronaphthalines.Thus, meta-substituted phenols 3, 4, and 7 are obtained from 1,3-dinitrobenzene (1) and meta-substituted nitrobenzenes 6, as well as 3,5-disubstituted phenols 10 and 5-substituted resorcinol derivatives 11 from 3,5-disubstituted nitrobenzenes 9.The unsymmetrically substituted nitrobiphenyls 13, 15, 17, 19, 23, 24, and 26 are also available by nitrite exchange from the corresponding easily accessible dinitrobiphenyls 16, 18, 20, 22, and 25.A nitrite exchange with nucleophiles is easily possible in the 1,5-disubstituted naphthalenes 29, 34, while in the case of the 1,8-disubstituted naphthalenes 31, 36 only the chloro derivative 36 undergoes this exchange under much stronger conditions in low yield.
- Effenberger, Franz,Koch, Markus,Streicher, Willi
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p. 163 - 173
(2007/10/02)
-