- Preparation method of p-vinylsalicylic acid
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The invention discloses a p-vinylsalicylic acid preparation method, which comprises: (1) carrying out a diazotization reaction on p-aminosalicylic acid and nitrous acid in water to generate a diazotization intermediate, and adding a metal iodide to carry
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Paragraph 0036-0038; 0040-0041; 0043-0044; 0046-0047
(2020/12/30)
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- LANTHANIDE CLUSTERS AND METHODS OF USE THEREOF
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The present invention is directed to multinuclear lanthanides chiral clusters, based on phenyl-oxazoline-amide (POxA) ligands, and to methods of use thereof. The chiral clusters of this invention are highly fluorescent with high stability.
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Paragraph 0236; 0237
(2016/01/30)
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- Acetylene Bridged Linkers and Metal-Organic Frameworks (MOFs) Produced Thereof
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Described are acetylene bridged linkers, metal-organic frameworks produced thereof, processes for producing the linkers and the metal-organic frameworks, and the use of the metal-organic frameworks. The metal-organic frameworks possess an enhanced ability to adsorb and desorb high amounts of gases, in particular methane or hydrogen. The metal-organic frameworks have a high porosity and, thus, a high inner surface.
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Paragraph 0145-0149
(2014/04/03)
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- ACETYLENE BRIDGED LINKERS AND METAL-ORGANIC FRAMEWORKS (MOFS) PRODUCED THEREOF
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The present invention relates to acetylene bridged linkers, metal-organic frameworks produced thereof, processes for producing the linkers and the MOFs and their use.
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Page/Page column 16
(2014/04/04)
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- Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists
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A series of acrylic acids and their structurally related compounds were evaluated for their binding affinity to four EP receptor subtypes (EP1-4). Starting from the initial hit 3, which was discovered in our in-house library, compounds 4 and 5 were identified as new chemical leads as candidates for further optimization towards a selective EP3 receptor antagonist. The identification process of these compounds and their pharmacokinetic profiles are presented.
- Asada, Masaki,Obitsu, Tetsuo,Nagase, Toshihiko,Sugimoto, Isamu,Yamaura, Yoshiyuki,Sato, Kazutoyo,Narita, Masami,Ohuchida, Shuichi,Nakai, Hisao,Toda, Masaaki
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experimental part
p. 6567 - 6582
(2009/12/09)
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- Iodination of aryl amines in a water-paste form via stable aryl diazonium tosylates
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The diazotization of aryl amines at room temperature in paste form with NaNO2, p-TsOH and a small amount of water, followed by treatment with KI provides a new, simple, and effective route for the preparation of various aryl iodides. The water-paste and strong acid-free reaction conditions are environmentally friendly and compatible with acid-sensitive functional groups.
- Gorlushko, Dmitry A.,Filimonov, Victor D.,Krasnokutskaya, Elena A.,Semenischeva, Nadya I.,Go, Bong Seong,Hwang, Ho Yun,Cha, Eun Hye,Chi, Ki-Whan
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p. 1080 - 1082
(2008/09/18)
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- Compounds and Compositions as Tpo Mimetics
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The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly disea
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Page/Page column 7
(2008/12/07)
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- FUSED HETEROCYCLIC COMPOUND AND USE THEREOF
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The present invention relates to wherein each symbol is as defined in the specification. The compound has a superior mineral corticoidreceptorantagonistic action and is useful as an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like, a compound having a fused heterocycle, or a prodrug thereof, or a salt thereof; and an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like.
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Page/Page column 320
(2008/06/13)
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- METHODS FOR TREATING HEPATITIS C
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In accordance with the present invention, compounds that inhibit viral replication, preferably Hepatitis C Virus (HCV) replication, have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the treatment
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Page/Page column 445
(2010/10/20)
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- Vitamin D analogues
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The invention concerns novel bi-aromatic compounds having the formula: which are analogs of vitamin D, the process of preparing them, as well as their use in pharmaceutical compositions in human or veterinary medicine, particularly in dermatology, cancer treatment, treatment of auto-immune diseases, and in organ or tissue transplants. Cosmetic compositions and methods of use are also included.
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Page column 30
(2010/02/05)
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- Ligands for expression cloning and isolation of GABAB receptors
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The scope of the plenary lecture at the occasion of the Xth Meeting on Heterocyclic Structures in Medicinal Chemistry, Palermo 2002, is considerably larger than that of the main lecture at the XVIth International Symposium on Medicinal Chemistry, Bologna 2000, described by Froestl et al. in Farmaco 56 (2001) 101. Additional information is presented, in particular, on the reaction conditions for the 31 step synthesis of the combined affinity chromatography and photoaffinity radioligand [125I]CGP84963 and on the recent developments of the molecular biology of GABAB receptors.
- Froestl, Wolfgang,Bettler, Bernhard,Bittiger, Helmut,Heid, Jakob,Kaupmann, Klemens,Mickel, Stuart J.,Strub, Dietrich
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p. 173 - 183
(2007/10/03)
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- Synthesis of a chiral precursor for no-carrier-added (NCA) PET tracer 6- [18F]fluoro-L-dopa based on regio- and enantioselective alkylation of 2,4- bis(chloromethyl)-5-iodoanisole
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(2S,5S)-5-(3-Formyl-6-iodo-4-methoxybenzyl)-1-t-butoxycarbonyl-2-t- butyl-3-methyl-4-imidazolidinone (11), a chiral intermediate towards NCA PET tracer 6-[18F]fluoro-L-dopa (1), was synthesized from 3-iodoanisole in four steps. 3-Iodoanisole was first bischloromethylated to 2,4-bis(chloromethyl)- 5-iodoanisole (14). Regio- and enantio-selective alkylation of 14 with (S)-1- (t-butoxycarbonyl)-2-t-butyl-3-methyl-4-imidazolidinone (12) afforded 33, which was then hydrolyzed and oxidized to the desired intermediate 11.
- Kuroda, Chiaki,Ochi, Atsushi,Nakane, Noritoshi,Umeyama, Takashi,Muto, Nobuko,Niimura, Nami,Teramoto, Yoshiki,Nogami, Hiroyuki,Reddy, Guvvala N.
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p. 417 - 422
(2007/10/03)
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- Polyaromatic heterocyclic compounds and pharmaceutical/cosmetic compositions comprised thereof
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Novel pharmaceutically/cosmetically-active polyaromatic heterocyclic compounds have the structural formula (I): STR1 in which Z is a divalent radical selected from among --O--, --S-- or --Nr'-- and Ar is either a radical having the following structural fo
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- Synthesis and ligand binding studies of 4'-iodobenzyl esters of tropanes and piperidines at the dopamine transporter
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Four analogs and two homologs of cocaine, designed as potent cocaine antagonists, were synthesized. The S(N)2 reaction between ecgonine methyl ester (13) or appropriately substituted piperidinol (19, 21) and appropriately substituted 4-indobenzoyl chloride gave 4-indobenzoyl esters of tropane and piperidines (5-8). 2'-Hydroxycocaine (9) was obtained from 2'- acetoxycocaine (12) by selective transesterification with MeOH saturated with dry HCl gas. 2'-Acetoxycocaine (12) was synthesized from acetylsalicyloyl chloride (23) and ecgonine methyl ester (13). The binding affinities of these compounds were determined at the dopamine transporter for the displacement of ([3H]WIN-35428. An iodo group substitution at the 4'-position of cocaine decreased dopamine transporter binding potency, while a hydroxy or acetoxy group at the 2'-position exhibited increased binding potency for the dopamine transporter compared to cocaine (10- and 3.58-fold, respectively). 2'- Hydroxylation also enhanced the binding potency of 4'-iodococaine (5) by 10- fold. Replacement of the tropane ring with piperidine led to poor binding affinities.
- Singh, Satendra,Basmadjian, Garo P.,Avor, Kwasi S.,Pouw, Buddy,Seale, Thomas W.
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p. 2474 - 2481
(2007/10/03)
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- Kinetics of Iodination of Some Substituted Benzoic Acids by N-Iodosuccinimide
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Iodination of o-amino-, p-amino-, o-hydroxy-, p-hydroxy, o-acetylamino-, p-acetylamino-, o-methoxy- and p-methoxy-benzoic acids by N-iodosuccinimide (NIS) in mixtures of acetic acid and perchloric acid follows first order kinetics with respect to the halo
- Radhakrishnamurti, P. S.,Panda, B. K.
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p. 770 - 773
(2007/10/02)
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