Patents by Inventor Yingjie Lai
Yingjie Lai has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 10487058Abstract: A cyclopropyl unsaturated quinoline compound used as leukotriene receptor antagonist and applications thereof, wherein the structural formula of the compound is as follows: An application of the compound or its pharmaceutically acceptable salts, hydrates, solvates, or prodrugs in preparing a drug for treating and/or preventing and/or delaying and/or providing adjuvant therapy for asthma and/or allergic rhinitis and asthma syndromes is provided. A drug composition includes the cyclopropyl unsaturated quinoline compound or the pharmaceutically acceptable salts, hydrates, solvates, or prodrugs thereof. The compound series has favorable foreground in preparing drugs for treating and/or preventing and/or delaying and/or providing adjuvant therapy for asthma and/or allergic rhinitis and asthma syndromes.Type: GrantFiled: April 23, 2019Date of Patent: November 26, 2019Assignee: Guangdong Moltech Pharma Co. Ltd.Inventor: Yingjie Lai
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Patent number: 10385000Abstract: Disclosed is a new method for synthesizing 2-fluorocyclopropanecarboxylic acid comprising: 1) performing reaction of 1,1-dichloro-1-fluoroethane with thiophenol in the presence of an alkali, to produce a phenyl sulfide intermediate; 2) performing oxidation reaction of the phenyl sulfide intermediate with Oxone; 3) performing elimination reaction of the product of Step 2) in the presence of an alkali, to obtain 1-fluoro-1-benzenesulfonyl ethylene; 4) performing addition reaction of the 1-fluoro-benzenesulfonyl ethylene with ethyl diazoacetate in the presence of a catalyst, to obtain a cyclopropane intermediate; 5) performing elimination reaction of the cyclopropane intermediate in the presence of an alkali before acidification, to obtain 2-fluorocyclopropanecarboxylic acid. Herein, the synthetic route is short, used materials are bulk commodities, and raw materials are inexpensive and readily available. The process can be safely scaled up by replacing commonly used mCPBA reagents with Oxone.Type: GrantFiled: April 25, 2017Date of Patent: August 20, 2019Assignee: CHEN-STONE (GUANGZHOU) CO., LTD.Inventors: Yingjie Lai, Xuyan Wang
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Publication number: 20190248746Abstract: A cyclopropyl unsaturated quinoline compound used as leukotriene receptor antagonist and applications thereof, wherein the structural formula of the compound is as follows: An application of the compound or its pharmaceutically acceptable salts, hydrates, solvates, or prodrugs in preparing a drug for treating and/or preventing and/or delaying and/or providing adjuvant therapy for asthma and/or allergic rhinitis and asthma syndromes is provided. A drug composition includes the cyclopropyl unsaturated quinoline compound or the pharmaceutically acceptable salts, hydrates, solvates, or prodrugs thereof. The compound series has favorable foreground in preparing drugs for treating and/or preventing and/or delaying and/or providing adjuvant therapy for asthma and/or allergic rhinitis and asthma syndromes.Type: ApplicationFiled: April 23, 2019Publication date: August 15, 2019Inventor: Yingjie LAI
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Patent number: 10358417Abstract: The present invention discloses a preparation method for efficient synthesis of sitafloxacin intermediate (7S)-5-azaspiro[2.4]heptane-7-yl-tert-butyl carbamate, comprising the following steps: reacting to obtain reacting to obtain reacting to obtain and reacting to obtain In the present invention, a single compound with a relatively high ee value can be obtained, the unnecessary waste of materials is avoided, the yield is significantly improved, the operation is simple, the industrial scale-up is easy, and the production cost is reduced.Type: GrantFiled: April 25, 2017Date of Patent: July 23, 2019Assignee: Chen-Stone (Guangzhou) Co., Ltd.Inventors: Yingjie Lai, Dabing Ye, Fengrui Lang, Xiangtian Long
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Patent number: 10315997Abstract: A cyclopropyl unsaturated quinoline compound used as leukotriene receptor antagonist and applications thereof, wherein the structural formula of the compound is as follows: An application of the compound or its pharmaceutically acceptable salts, hydrates, solvates, or prodrugs in preparing a drug for treating and/or preventing and/or delaying and/or providing adjuvant therapy for asthma and/or allergic rhinitis and asthma syndromes is provided. A drug composition includes the cyclopropyl unsaturated quinoline compound or the pharmaceutically acceptable salts, hydrates, solvates, or prodrugs thereof. The compound series has favorable foreground in preparing the drugs for treating and/or preventing and/or delaying and/or providing adjuvant therapy for asthma and/or allergic rhinitis and asthma syndromes.Type: GrantFiled: September 10, 2015Date of Patent: June 11, 2019Assignee: GUANGDONG MOLTECH PHARMA CO., LTD.Inventor: Yingjie Lai
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Publication number: 20180370914Abstract: The present invention discloses a preparation method for efficient synthesis of sitafloxacin intermediate (7S)-5-azaspiro[2.4]heptane-7-yl-tert-butyl carbamate, comprising the following steps: reacting to obtain reacting to obtain reacting to obtain and reacting to obtain In the present invention, a single compound with a relatively high ee value can be obtained, the unnecessary waste of materials is avoided, the yield is significantly improved, the operation is simple, the industrial scale-up is easy, and the production cost is reduced.Type: ApplicationFiled: April 25, 2017Publication date: December 27, 2018Inventors: Yingjie Lai, Dabing Ye, Fengrui Lang, Xiangtian Long
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Publication number: 20180370893Abstract: Disclosed is a new method for synthesizing 2-fluorocyclopropanecarboxylic acid comprising: 1) performing reaction of 1,1-dichloro-1-fluoroethane with thiophenol in the presence of an alkali, to produce a phenyl sulfide intermediate; 2) performing oxidation reaction of the phenyl sulfide intermediate with Oxone; 3) performing elimination reaction of the product of Step 2) in the presence of an alkali, to obtain 1-fluoro-1-benzenesulfonyl ethylene; 4) performing addition reaction of the 1-fluoro-benzenesulfonyl ethylene with ethyl diazoacetate in the presence of a catalyst, to obtain a cyclopropane intermediate; 5) performing elimination reaction of the cyclopropane intermediate in the presence of an alkali before acidification, to obtain 2-fluorocyclopropanecarboxylic acid. Herein, the synthetic route is short, used materials are bulk commodities, and raw materials are inexpensive and readily available. The process can be safely scaled up by replacing commonly used mCPBA reagents with Oxone.Type: ApplicationFiled: April 25, 2017Publication date: December 27, 2018Inventors: Yingjie LAI, Xuyan WANG
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Publication number: 20180118687Abstract: A cyclopropyl unsaturated quinoline compound used as leukotriene receptor antagonist and applications thereof, wherein the structural formula of the compound is as follows: An application of the compound or its pharmaceutically acceptable salts, hydrates, solvates, or prodrugs in preparing a drug for treating and/or preventing and/or delaying and/or providing adjuvant therapy for asthma and/or allergic rhinitis and asthma syndromes is provided. A drug composition includes the cyclopropyl unsaturated quinoline compound or the pharmaceutically acceptable salts, hydrates, solvates, or prodrugs thereof. The compound series has favorable foreground in preparing the drugs for treating and/or preventing and/or delaying and/or providing adjuvant therapy for asthma and/or allergic rhinitis and asthma syndromes.Type: ApplicationFiled: September 10, 2015Publication date: May 3, 2018Applicant: Guangdong Moltech Pharma Co., Ltd.Inventor: Yingjie LAI
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Publication number: 20170081320Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted thiadiazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: ApplicationFiled: October 26, 2015Publication date: March 23, 2017Applicant: Roche Palo Alto LLCInventors: Li Chen, Lichun Feng, Minmin Yang, Michael Patrick Dillon, Yingjie Lai
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Patent number: 9309240Abstract: The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy.Type: GrantFiled: May 16, 2013Date of Patent: April 12, 2016Assignee: GENENTECH, INC.Inventors: Toby Blench, Simon Goodacre, Yingjie Lai, Jun Liang, Calum Macleod, Steven Magnuson, Vickie Tsui, Karen Williams, Birong Zhang
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Patent number: 9173861Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted thiadiazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: GrantFiled: January 26, 2012Date of Patent: November 3, 2015Assignee: Roche Palo Alto LLCInventors: Li Chen, Lichun Feng, Minmin Yang, Michael Patrick Dillon, Yingjie Lai
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Publication number: 20140206702Abstract: The invention provides compounds of Formulas Ia-Ib, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, Ra, R1, R2, R4, R5 and R16 are defined herein, a pharmaceutical composition that includes a compound of Formulas Ia-Ib and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy.Type: ApplicationFiled: March 20, 2014Publication date: July 24, 2014Applicant: GENENTECH, INC.Inventors: Yingjie Lai, Jun Liang, Steven R. Magnuson, Kirk D. Robarge, Vickie H. Tsui, Birong Zhang
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Publication number: 20140171408Abstract: Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.Type: ApplicationFiled: February 20, 2014Publication date: June 19, 2014Applicant: Genentech, Inc.Inventors: Toby Jonathan Blench, Charles Ellwood, Simon Charles Goodacre, Yingjie Lai, Jun Liang, Calum MacLeod, Steven R. Magnuson, Vickie Hsiao-Wei Tsui, Karen Williams, Birong Zhang
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Patent number: 8697708Abstract: Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.Type: GrantFiled: September 14, 2011Date of Patent: April 15, 2014Assignee: F. Hoffmann-La Roche AGInventors: Toby Jonathan Blench, Charles Ellwood, Simon Charles Goodacre, Yingjie Lai, Jun Liang, Calum Macleod, Steven R. Magnuson, Vickie H. Tsui, Karen Williams, Birong Zhang
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Publication number: 20130252941Abstract: The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy.Type: ApplicationFiled: May 16, 2013Publication date: September 26, 2013Applicant: F. Hoffmann-La Roche AGInventors: Toby Blench, Simon Goodacre, Yingjie Lai, Jun Liang, Calum Macleod, Steven Magnuson, Vickie Tsui, Karen Williams, Birong Zhang
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Patent number: 8486950Abstract: The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, B, D, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and methods of use thereof.Type: GrantFiled: June 10, 2010Date of Patent: July 16, 2013Assignee: F. Hoffmann-La Roche AGInventors: Simon Charles Goodacre, Yingjie Lai, Jun Liang, Steven R. Magnuson, Kirk D. Robarge, Mark S. Stanley, Vickie Hsiao-Wei Tsui, Karen Williams, Birong Zhang, Aihe Zhou
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Publication number: 20130096104Abstract: The invention provides compounds of Formulas Ia-Ib, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4, R5 and R16 are defined herein, a pharmaceutical composition that includes a compound of Formulas Ia-Ib and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy, as an inhibitor of TYK2 kinase and conditions related, such as inflammatory illnesses, inflammatory bowel disease or psoriasis.Type: ApplicationFiled: March 15, 2011Publication date: April 18, 2013Applicant: GENENTECH, INC.Inventors: Yingjie Lai, Jun Liang, Steven R. Magnuson, Kirk D. Robarge, Vickie H. Tsui, Birong Zhang, Aihe Zhou
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Patent number: 8318719Abstract: This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-II: wherein, variables Q1, Q2, R, X, Y1, Y2, Y2?, Y3, Y4, Y5, m, and p are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-II and at least one carrier, diluent or excipient.Type: GrantFiled: April 23, 2010Date of Patent: November 27, 2012Assignee: Roche Palo Alto LLCInventors: Nolan James Dewdney, Ronald Charles Hawley, Rama Kondru, Yingjie Lai, Yan Lou
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Publication number: 20120202788Abstract: Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.Type: ApplicationFiled: September 14, 2011Publication date: August 9, 2012Inventors: Toby Jonathan Blench, Charles Ellwood, Simon Charles Goodacre, Yingjie Lai, Jun Liang, Calum Macleod, Steven R. Magnuson, Vickie H. Tsui, Karen Williams, Birong Zhang
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Publication number: 20120122886Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted thiadiazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: ApplicationFiled: January 26, 2012Publication date: May 17, 2012Inventors: Li Chen, Lichun Feng, Minmin Yang, Michael Patrick Dillon, Yingjie Lai