- Method for preparing benzo oxygen-containing aliphatic heterocyclic derivative
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The invention relates to a method for preparing a benzo oxygen-containing aliphatic heterocyclic derivative, which specifically comprises the following steps: (1) carrying out nitration reaction on acompound shown as a formula I-1 to obtain a compound shown as a formula I-2; (2) carrying out reduction reaction on the compound shown in the formula I-2 to obtain a compound shown in a formula I-3; (3) performing halogenation reaction on the compound shown in the formula I-3 to obtain a compound shown in a formula I-4; (4) carrying out diazotization reaction on the compound shown as the formula I-4, and further reacting the obtained product with a halogenated metal salt to generate a compound shown as a formula I;.
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Paragraph 0046-0048
(2021/02/10)
-
- Synthesis of multifunctional metal-organic frameworks and tuning the functionalities with pendant ligands
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A series of multifunctional metal-organic frameworks (MOFs), SNU-170-SNU-176, has been synthesized using ligands, in which various functional pendants such as -NH2, -SMe, -OMe, -OEt, -OPr, and -OBu are attached to the phenyl ring of 4-(2-carboxyvinyl)benz
- Prasad, Thazhe Kootteri,Suh, Myunghyun Paik
-
supporting information
p. 15034 - 15040
(2020/11/11)
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- IRAK4 INHIBITORS AND USES THEREOF
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Compounds of Formula I as IRAK4 inhibitors are disclosed. The pharmaceutical compositions comprising compounds of formula I, methods of synthesis of these compounds, methods of treatment for diseases associated with IRAK-4 such as inflammatory diseases an
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Paragraph 0125
(2019/05/22)
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- Preparation method of intermediate of medicine for treating chronic dry eye
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The invention relates to a preparation method of an intermediate of a medicine for treating chronic dry eye. The method comprises the following steps: (a) adding methyl alcohol, m-hydroxybenzoic acid,NaOH and NaI to a reaction vessel; and dropwise adding
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Paragraph 0011; 0013; 0014; 0015
(2018/09/26)
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- Photopatterning of fluorescent host-guest carriers through pore activation of metal-organic framework single crystals
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Encoded fluorescent particles are fabricated through the selective uptake of dyes in photopatterned metal-organic framework single crystals. The concept is based on spatially controlled photochemical cleavage of pore-blocking pendant groups. Because of the crystalline and porous nature of the host, this approach enables guest uptake that is tunable and can be triggered though controlled irradiation.
- Stassen,Boldog,Steuwe,De Vos,Roeffaers,Furukawa,Ameloot
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supporting information
p. 7222 - 7225
(2017/07/11)
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- ARYLOXYACETYLINDOLES AND ANALOGS AS ANTIBIOTIC TOLERANCE INHIBITORS
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The disclosure provides compounds and pharmaceutical compositions of aryloxyacetylindoles compounds and analogs useful for treating chronic and acute bacterial infections. Certain of the compounds are compounds of general Formula (I) (I) or a pharmaceutically acceptable salt or prodrug thereof. Certain compounds of this disclosure are MvfR inhibitors. MvfR inhibitors reduce the formation of antibiotic tolerant bacterial strains and are useful for treating Gram-negative bacterial infections and reducing the virulence of Pseudomonas aeruginosa. Methods of treating bacterial infections in a subject, including Pseudomonas aeruginosa infections, are also provided by the disclosure.
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Paragraph 0646
(2016/08/10)
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- Three sra topological lanthanide-organic frameworks built from 2,2′-dimethoxy-4,4′-biphenyldicarboxylic acid
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Three 3D lanthanide-organic frameworks (LOFs), [LnL(HCO2)(DMF)]n (Ln = Eu (1), Gd (2), Dy (3); H2L = 2,2′-dimethoxy-4,4′-biphenyldicarboxylic acid), have been prepared by the solvothermal reaction of Ln(NO3)sub
- Wang, Xin,Zhao, Jie,Zhao, Yan,Xu, Heng,Shen, Xuan,Zhu, Dun-Ru,Jing, Su
-
supporting information
p. 9281 - 9288
(2015/05/20)
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- Bicyclic-Fused Heteroaryl or Aryl Compounds
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Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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Paragraph 0398
(2015/10/28)
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- Synthesis and antibacterial evaluation of new, unsymmetrical triaryl bisamidine compounds
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Herein we describe the synthesis and antibacterial evaluation of a new, unsymmetrical triaryl bisamidine compound series, [Am]-[indole]-[linker]-[HetAr/ Ar]-[Am], in which [Am] is an amidine or amino group, [linker] is a benzene, thiophene or pyridine ring, and [HetAr/Ar] is a benzimidazole, imidazopyridine, benzofuran, benzothiophene, pyrimidine or benzene ring. When the [HetAr/Ar] unit is a 5,6-bicyclic heterocycle, it is oriented such that the 5-membered ring portion is connected to the [linker] unit and the 6-membered ring portion is connected to the [Am] unit. Among the 34 compounds in this series, compounds with benzofuran as the [HetAr/Ar] unit showed the highest potencies. Introduction of a fluorine atom or a methyl group to the triaryl core led to the more potent analogs. Bisamidines are more active toward bacteria while the monoamidines are more active toward mammalian cells (as indicated by low CC 50 values). Importantly, we identified compound P12a (MBX 1887) with a relatively narrow spectrum against bacteria and a very high CC50 value. Compound P12a has been scaled up and is currently undergoing further evaluations for therapeutic applications.
- Nguyen, Son T.,Williams, John D.,Butler, Michelle M.,Ding, Xiaoyuan,Mills, Debra M.,Tashjian, Tommy F.,Panchal, Rekha G.,Weir, Susan K.,Moon, Chaeho,Kim, Hwa-Ok,Marsden, Jeremiah A.,Peet, Norton P.,Bowlin, Terry L.
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supporting information
p. 3366 - 3372
(2014/07/22)
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- Control of framework interpenetration for in situ modified hydroxyl functionalised IRMOFs
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By intimate control of reaction conditions, phase-pure crystalline porous metal-organic framework materials [Zn4O(L)3] with interpenetrated and non-interpenetrated structures can be synthesised. Under certain conditions, these reacti
- Rankine, Damien,Avellaneda, Antonio,Doonan, Christian J.,Sumby, Christopher J.,Hill, Matthew R.
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supporting information
p. 10328 - 10330,3
(2020/09/09)
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- NOVEL 3-PHENYL ACRYLIC ACID COMPOUND ACTIVATORS OF TYPE PPAR RECEPTORS AND PHARMACEUTICAL/COSMETIC COMPOSITIONS COMPRISED THEREOF
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Novel 3-phenyl acrylic acid compounds have the following general formula (I): and are formulated into pharmaceutical compositions for administration in human or veterinary medicine (in dermatology, as well as in the field of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or into cosmetic compositions.
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Page/Page column 9
(2010/06/19)
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- NOVEL 3-PHENYLPROPANOIC COMPOUND ACTIVATORS OF RECEPTORS OF PPAR TYPE AND PHARMACEUTICAL/COSMETIC COMPOSITIONS COMPRISED THEREOF
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Novel 3-phenylpropanoic acid compounds have the general formula (I) below: and are formulated into pharmaceutical compositions for administration in human or veterinary medicine (in dermatology, and also in the field of cardiovascular diseases, immune dis
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- Ring strain and total syntheses of modified macrocycles of the isoplagiochin type
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Macrocycles of the bisbibenzyl-type are natural products that are found exclusively in bryophytes (liverworts). The molecular framework of the subtype "isoplagiochin" is of substantial structural interest because of the chirality of the entire molecule, w
- Speicher, Andreas,Backes, Timo,Hesidens, Kerstin,Kolz, Juergen
-
supporting information; experimental part
(2010/04/22)
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- NOVEL BIAROMATIC COMPOUNDS THAT MODULATE PPAR-RECEPTORS
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Novel biaromatic compounds that modulate peroxisome proliferator-activator receptors, known as PPAR, having the formula (I): are formulated into pharmaceutical compositions useful in human or veterinary medicine, or alternatively, in cosmetic compositions.
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Page/Page column 21
(2009/01/23)
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- Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4
-
The series of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-dione and 4-[(pyridylmethyl)aminometh-ylene]isoquinoline-1,3-(2H,4H)-dione derivatives reported here represents a novel class of potential antitumor agents, which potently and selectively inhibit CDK4 over CDK2 and CDK1. In the benzylamino headpiece, a 3-OH substituent is required on the phenyl ring for CDK4 inhibitory activity, which is further enhanced when an iodo, aryl, heteroaryl, t-butyl, or cyclopentyl substituent is introduced at the C-6 position of the isoquinoline-1,3-dione core. To circumvent the metabolic liability associated with the phenolic OH group on the 4-substituted 3-OH phenyl headpiece, we take two approaches: first, introduce a nitrogen o- or p- to the 3-OH group in the phenyl ring; second, replace the phenyl headpiece with N-substituted 2-pyridones. We present here the synthesis, SAR data, metabolic stability data, and a CDK4 mimic model that explains the binding, potency, and selectivity of our CDK4 selective inhibitors.
- Tsou,Liu, Xiaoxiang,Birnberg, Gary,Kaplan, Joshua,Otteng, Mercy,Tran, Tritin,Kutterer, Kristina,Tang, Zhilian,Suayan, Ron,Zask, Arie,Ravi, Malini,Bretz, Angela,Grillo, Mary,Mcginnis, John P.,Rabindran, Sridhar K.,Ayral-Kaloustian, Semiramis,Mansour, Tarek S.
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scheme or table
p. 2289 - 2310
(2010/02/28)
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- Highly stereoselective cobalt-catalyzed allylation of functionalized diarylzinc reagents
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Functionalized diarylzinc reagents react readily with allylic chlorides or phosphates in the presence of Co(acac)2 (10 mol%) to give the S N2 products in high yields and with retention of the double-bond configuration. Functionalities like ester, ketone, or cyano are tolerated. Georg Thieme Verlag Stuttgart.
- Dunet, Guillaume,Knochel, Paul
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p. 1383 - 1386
(2008/02/13)
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- NOVEL BIAROMATIC COMPOUNDS WHICH ACTIVATE RECEPTORS OF PPAR TYPE AND THEIR USE IN COSMETIC OR PHARMACEUTICAL COMPOSITIONS
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The invention relates to novel biaromatic compounds which correspond to the following general formula (I) and to their method of preparation and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology a
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Page/Page column 25-26
(2010/10/20)
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- NOVEL BIAROMATIC COMPOUNDS THAT ACTIVATE PPAR TYPE RECEPTORS, AND USE THEREOF IN COSMETIC OR PHARMACEUTICAL COMPOSITIONS
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The invention relates to novel biaromatic compounds that correspond to the general formula (I) and also to the method for preparing them, and to their use in pharmaceutical compositions for use in human or veterinary medicine (in dermatology, and also in the field of cardiovascular diseases, immune diseases and/or lipid metabolism-related diseases), or alternatively in cosmetic compositions.
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Page/Page column 78
(2010/10/20)
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- NOVEL MCH RECEPTOR ANTAGONISTS
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The present invention relates to a melanin concentrating hormone antagonist compound of formula I: or a pharmaceutically acceptable salt thereof, useful for the treamtment useful fog treating Type H diabetes and/or obesity.
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Page/Page column 56
(2010/02/11)
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- Quinuclidine-substituted hetero-bicyclic aromatic compounds for the treatment of disease
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The invention provides compounds of Formula I: wherein W0 is a bicyclic moiety and is These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful to treat diseases or conditions in which α7 is known to be involved.
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- Azabicyclic compounds for the treatment of disease
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The invention provides compounds of Formula I: 1wherein Azabicyclo is 2These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals in which α7 is known to be involved.
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-
- Rational design, synthesis, and structure-activity relationships of novel factor Xa inhibitors: (2-substituted-4-amidinophenyl)pyruvic and -propionic acids
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An inhibitor of factor Xa (fXa), the m-substituted benzamidine AXC1578 (1a), was structurally modified with the aim of increasing its potency. In particular, pyruvic acid and propionic acid substituents were incorporated into the P1 benzamidine moiety to
- Sagi, Kazuyuki,Nakagawa, Tadakiyo,Yamanashi, Masahiro,Makino, Shingo,Takahashi, Mitsuo,Takayanagi, Masaru,Takenaka, Kaoru,Suzuki, Nobuyasu,Oono, Seiji,Kataoka, Noriyasu,Ishikawa, Kohki,Shima, Sayaka,Fukuda, Yumiko,Kayahara, Takashi,Takehana, Shunji,Shima, Yoichiro,Tashiro, Kazumi,Yamamoto, Hiroshi,Yoshimoto, Ryota,Iwata, Seinosuke,Tsuji, Takashi,Sakurai, Kuniya,Shoji, Masataka
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p. 1845 - 1857
(2007/10/03)
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- Substituted 7-aza[2.2.1]bicycloheptanes for the treatment of disease
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The invention provides compounds of Formula I: which may be in the form of pharmaceutical acceptable salts or compositions, are useful in treating diseases or conditions in which α7 nicotinic acetylcholine receptors (nAChRs) are known to be involved.
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-
- AMIDINOPHENYLPYRUVIC ACID DERIVATIVES
-
An amidinophenylpyruvic acid derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an excellent antagonistic effect against activated blood coagulation factor VII.
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-
- Syntheses of chlorinated bisbibenzyls from bryophytes
-
Chlorinated bisbibenzyls of the isoplagiochin type detected in different bryophyte species were synthesized by an efficient and flexible unit construction system making extensive use of Suzuki and Wittig protocols.
- Speicher, Andreas,Kolz, Juergen,Sambanje, Rufino Paulino
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p. 2503 - 2512
(2007/10/03)
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- New oxybenzamide derivatives useful for inhibiting factor Xa or VIIa
-
The present invention relates to compounds comprising the following formula: R0—Q—X—Q′—W—U—V—G—M??(I) These compounds are useful as pharmacologically active compounds. They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders such as thromboembolic diseases or restenoses. These compounds are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can generally be used to treat, prevent, or cure conditions in which an undesired activity of factor Xa and/or factor VIIa is present, or where inhibition of factor Xa and/or factor VIIa is intended. The invention further relates to processes for the preparation of these compounds, methods of their use (e.g., as active ingredients in pharmaceuticals), and pharmaceutical preparations comprising them.
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-
- Inhibitors of factor Xa and factor VIIa
-
The present invention relates to compounds of the formula I,R0-Q-X-Q'-W-U-V-G-M in which Q; X; Q', U, V, G and M have the meanings indicated in the claims; R0 is aryl or heteroaryl; and W is selected from aryl, heteroaryl, carbocyclic and heterocyclic groups. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa(FXa) and/or factor VIIa(FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
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- BENZAMIDINE DERIVATIVES
-
A benzamidine derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an effect of inhibiting the blood coagulation based on their excellent effect of inhibiting activated blood-coagulation factor X. Thus, a blood-coagulation inhibitor or an agent for preventing or treating thrombosis or embolism, containing one of those compounds as the active ingredient, is provided.
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-
-
- Biphenyl derivatives substituted by an aromatic or heteroaromatic radical and pharamaceutical and cosmetic compositions containing same
-
“Biphenyl derivatives substituted with an aromatic or heteroaromatic radical, and pharmaceutical and cosmetic compositions containing them” in which: Ar represents an aromatic or a heteroaromatic radical optionally substituted, in particular, with an alkyl or a carboxyl group, R2and R3represent, in particular, H or alkyl, or R2and R3, taken together, form a 5- or 6-membered ring, R4and R5represent, in particular, H or halogen, R6represents, in particular, H or lower alkyl, and the salts of the compounds of formula (I). These compounds can be used in particular in the treatment of dermatological complaints associated with a keratinization disorder, and for combating ageing of the skin.
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-
- Benzamidine derivatives
-
Benzamidine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an effect of inhibiting activated blood-coagulation factor X, and they are useful as agents for preventing or treating various diseases caused by thrombi or emboli.
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-
- AMINOISOQUINOLINE DERIVATIVES
-
Aminoisoquinoline derivatives represented by formulae (I and II), analogs thereof or pharmaceutically acceptable salts of the same. Because of having excellent inhibitory effects on activated blood coagulation factor X, these compounds are useful as active ingredients in anticoagulants or preventives/remedies for thrombosis or embolism.
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- Triaromatic compounds and pharmaceutical/cosmetic compositions comprised thereof
-
Novel pharmaceutically/cosmetically-active triaromatic compounds have the structural formula (I): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
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- BENZAMIDINE DERIVATIVES
-
Benzamidine derivatives of the following formulae or analogs thereof, i. e., pharmaceutically acceptable salts thereof, are provided. These compounds or salts thereof have a blood-coagulation inhibiting effect based on an excellent effect of inhibiting the action of activated blood coagulation factor X, and they are useful as anticoagulants.
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- FIQ and FIQ2, New Q-site inhibitors for photosynthetic electron transport: Synthesis and the relationship between stereochemistry and biological activity
-
The synthetic hexahydrofuroisoquinoline 4 has, as a mixture of stereoisomers, been identified as a potent and specific inhibitor of electron transport in photosynthesis. We now report that the biological activity of 4 is, surprisingly, independent of conf
- Pilling, Robert J.,Whiting, Donald A.
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p. 2077 - 2086
(2007/10/03)
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- Synthesis of novel inhibitors of electron transport
-
Molecular modelling comparisons of several known natural and synthetic inhibitors of electron transport, e.g. rotenone, papaverine, and piericidin A, suggested new 'hybrid' structure 8-12, and relatives as potential new inhibitors.Synthetic routes to these targets, some of which display significant biological activity, are outlined.
- Cockerill, G. Stuart,Levett, Philip C.,Whiting, Donald A.
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p. 1103 - 1114
(2007/10/02)
-