77095-51-3Relevant academic research and scientific papers
Method for preparing benzo oxygen-containing aliphatic heterocyclic derivative
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Paragraph 0053-0055, (2021/02/10)
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;.
Preparation method of benzofuran derivative
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Paragraph 0061; 0064-0066; 0074, (2020/02/06)
The invention discloses a preparation method for synthesizing a benzofuran derivative. The specific implementation method is as shown in the specification. The method has novel synthetic route, simpleand convenient operation, high yield, and good safety, and is suitable for industrial production. A novel synthetic method of an intermediate VI is also designed, a Wittig reaction is carried out, and then ring-closing is carried out to obtain a benzofuran ring.
NOVEL PROCESS FOR THE PREPARATION OF LIFITEGRAST
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Page/Page column 19, (2019/05/02)
The present invention relates to a novel process for the preparation of lifitegrast of Formula (I). The present invention further provides a novel process for the purification of lifitegrast of Formula (I).
Synthesis method of lifitegrast intermediate
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Paragraph 0008; 0017; 0018; 0019, (2018/07/06)
The invention provides a preparation method of a lifitegrast intermediate I. The method comprises steps as follows: 6-bromobenzo[b]furan is taken as a starting raw material and subjected to a halogen-lithium exchange reaction under the action of n-butyllithium, a product is subjected to a reaction with dimethyl carbonate, methyl benzofuran-6-carboxylate is prepared and hydrolyzed, and the lifitegrast intermediate I is obtained. The raw materials are cheap and easily available, few reaction by-products are produced, yield and purity of a final product are high, meanwhile, the step (1) an the step (2) can be subjected to the one-pot reaction, so that steps of the reaction are simplified, furthermore, the reaction conditions are mild, the product does not need separation on columns, and industrialization is easy to realize.
GEMINAL SUBSTITUTED QUINUCLIDINE AMIDE COMPOUNDS AS AGONISTS OF ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTORS
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Paragraph 00319-00320, (2016/07/05)
The present invention relates to novel geminal substituted quinuclidine amide compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of α7- nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.
LFA-1 INHIBITOR AND POLYMORPH THEREOF
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Paragraph 00131; 00132; 00133; 00134; 00135, (2014/02/16)
Methods of preparation and purification of a compound, intermediates thereof, a polymorph thereof, and related compounds are disclosed. Formulations and uses thereof in the treatment of LFA -1 mediated diseases are also disclosed.
Discovery and development of potent LFA-1/ICAM-1 antagonist SAR 1118 as an ophthalmic solution for treating dry eye
Zhong, Min,Gadek, Thomas R.,Bui, Minna,Shen, Wang,Burnier, John,Barr, Kenneth J.,Hanan, Emily J.,Oslob, Johan D.,Yu, Chul H.,Zhu, Jiang,Arkin, Michelle R.,Evanchik, Marc J.,Flanagan, W. Mike,Hoch, Ute,Hyde, Jennifer,Prabhu, Saileta,Silverman, Jeffrey A.,Wright, Jasmin
supporting information; scheme or table, p. 203 - 206 (2012/05/04)
LFA-1/ICAM-1 interaction is essential in support of inflammatory and specific T-cell regulated immune responses by mediating cell adhesion, leukocyte extravasation, migration, antigen presentation, formation of immunological synapse, and augmentation of T-cell receptor signaling. The increase of ICAM-1 expression levels in conjunctival epithelial cells and acinar cells was observed in animal models and patients diagnosed with dry eye. Therefore, it has been hypothesized that small molecule LFA-1/ICAM-1 antagonists could be an effective topical treatment for dry eye. In this letter, we describe the discovery of a potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonist (SAR 1118) and its development as an ophthalmic solution for treating dry eye.
Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5- carboxamide, an agonist of the α7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: Synthesis and structure-activity relationship
Wishka, Donn G.,Walker, Daniel P.,Yates, Karen M.,Reitz, Steven C.,Jia, Shaojuan,Myers, Jason K.,Olson, Kirk L.,Jacobsen, E. Jon,Wolfe, Mark L.,Groppi, Vincent E.,Hanchar, Alexander J.,Thornburgh, Bruce A.,Cortes-Burgos, Luz A.,Wong, Erik H. F.,Staton, Brian A.,Raub, Thomas J.,Higdon, Nicole R.,Wall, Theron M.,Hurst, Raymond S.,Walters, Rodney R.,Hoffmann, William E.,Hajos, Mihaly,Franklin, Stanley,Carey, Galen,Gold, Lisa H.,Cook, Karen K.,Sands, Steven B.,Zhao, Sabrina X.,Soglia, John R.,Kalgutkar, Amit S.,Arneric, Stephen P.,Rogers, Bruce N.
, p. 4425 - 4436 (2007/10/03)
N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide (14, PHA-543,613), a novel agonist of the α7 neuronal nicotinic acetylcholine receptor (α7 nAChR), has been identified as a potential treatment of cognitive deficits in schizophrenia. Compound 14 is a potent and selective a7 nAChR agonist with an excellent in vitro profile. The compound is characterized by rapid brain penetration and high oral bioavailability in rat and demonstrates in vivo efficacy in auditory sensory gating and, in an in vivo model to assess cognitive performance, novel object recognition.
MODULATORS OF CELLULAR ADHESION
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Page/Page column 80-81, (2010/02/11)
The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).
Substituted 7-aza[2.2.1]bicycloheptanes for the treatment of disease
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, (2008/06/13)
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.
