The Other Cyclo In The Bicyclo Ring System Is Five-membered Patents (Class 544/280)
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Patent number: 11931412Abstract: The present invention provides methods for treating pruritus having a neurogenic component in a subject in need thereof comprising administering a therapeutically effective amount of a JAK1 inhibitor based on a benzimidazole core, a purine core, or a pyrrolo pyridine core.Type: GrantFiled: February 4, 2021Date of Patent: March 19, 2024Assignee: Washington UniversityInventor: Brian Kim
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Patent number: 11905292Abstract: The present invention is related to processes for preparing ruxolitinib, or a salt thereof, and related synthetic intermediates related thereto.Type: GrantFiled: August 17, 2021Date of Patent: February 20, 2024Assignee: Incyte CorporationInventors: Jiacheng Zhou, Shili Chen, Pingli Liu, David J. Meloni, James M. Parks, Yongchun Pan, Naijing Su, Michael Xia, Weiguo Liu
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Patent number: 11827598Abstract: The present disclosure provides a preparation method of tofacitinib citrate, which comprises the following steps: passing an intermediate TOF-2 into hydrogen at a normal pressure in the presence of a catalyst to obtain an intermediate TOF-3; in the presence of a solvent and a base, under a reduced pressure of ?490 mmHg to ?760 mmHg, and at a temperature of 10° C. to 25° C., reacting TOF-3 with ethyl cyanoacetate to generate an intermediate TOF-4; heating and dissolving TOF-4 and citric acid in a solvent, and performing separation by cooling to obtain tofacitinib citrate. The present disclosure obtains tofacitinib citrate with high yield, high purity and low impurities by changing a gas flow rate and a reaction temperature and pressure of a hydrogenation reaction. Therefore, the preparation method is suitable for industrial production.Type: GrantFiled: September 8, 2022Date of Patent: November 28, 2023Assignee: CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO. LTD.Inventors: Yao-Lung Hsu, Kuang-Chan Hsieh, Hui-Wen Cheng, Zong-Han Yang
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Patent number: 11814388Abstract: Compounds are provided herein. In general, the compounds are substituted pyrrolo[2,3-d]pyrimidines. The compounds can be used as inhibitors for multi-resistant cancers. Also provided herein are methods of forming the compounds, methods for inhibiting aurora kinase A and/or aurora kinase B activity and epidermal growth factor activity, methods of treating, ameliorating, or preventing cancer, and uses of the compounds for inhibiting aurora kinase A and/or aurora kinase B activity and epidermal growth factor receptor kinase activity. The compounds are generally of the formulas as illustrated herein, including those of Formula (I) or a pharmaceutically acceptable salt thereof: wherein: X1 is N; X2 is N; X3 is —NH—; X4 is N or CR2; X5 is CH or CCH3; L1 is —NR4—R1; L2 is NH2 or H; R1 is: R2 is a 5-membered heteroaryl; R4 is H; R5 is as described herein; and m is 1, 2, 3, 4, or 5.Type: GrantFiled: August 27, 2021Date of Patent: November 14, 2023Assignee: Ferris State UniversityInventor: Sonali Raghavan Kunjunni Kurup
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Patent number: 11738027Abstract: The present disclosure relates to new therapeutic uses of MPO inhibitors and methods of treatment involving the same.Type: GrantFiled: December 2, 2021Date of Patent: August 29, 2023Assignee: AstraZeneca ABInventors: Andrew Whittaker, Hitesh Jayantilal Sanganee
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Patent number: 11591333Abstract: The present invention provides a method for preparing a pyrrolopyrimidine compound and application thereof. Specifically, the present invention provides a compound represented by formula I or pharmaceutically-acceptable salts thereof, a pharmaceutical composition containing the compound or its salts, and a method for preparing the pharmaceutical composition and an application of the pharmaceutical composition as an immunosuppressive drug.Type: GrantFiled: February 22, 2017Date of Patent: February 28, 2023Assignees: CINAKATE PHARM TECH (SHANGHAI) CO., LTD., CINKATE PHARMACEUTICAL INTERMEDIATES CO., LTD.Inventors: Na Liu, Lixia Bao, Zhepeng Wei, Yufeng Zhou, Bin Rong, Lihui Zhao, Fei Xiao
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Patent number: 11548895Abstract: The present disclosure provides crystalline forms of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(cyclopropylsulfonyl)azetidin-3-yl)acetonitrile, pharmaceutical compositions comprising the crystalline forms, methods of using the crystalline forms, and processes for making the crystalline forms.Type: GrantFiled: April 22, 2020Date of Patent: January 10, 2023Assignee: Elanco US Inc.Inventors: Jingdan Hu, Timothy Andrew Woods
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Patent number: 11524968Abstract: The present invention provides a novel compound having a protein kinase inhibition activity, a stereoisomer thereof or a pharmaceutically acceptable salt thereof. The compound, the stereoisomer thereof or the pharmaceutically acceptable salt thereof according to the present invention show a protein kinase inhibition activity, thus being effective in preventing or treating diseases related to protein kinase, such as cancer, autoimmune disease, neurological disease, metabolic disease, infection or the like.Type: GrantFiled: October 17, 2018Date of Patent: December 13, 2022Assignee: HK inno.N CorporationInventors: Hyuk Woo Lee, Mi Kyung Ji, Seung Chan Kim, Ha Na Yu, Soo Yeon Jung, Ji-Yeon Park, Ye-Lim Lee, Ho-Youl Lee, So Young Ki, Dongkyu Kim, Myeongjoong Kim
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Patent number: 11440912Abstract: The invention relates to a process for the preparation of ribociclib of formula V or its salts. The invention provides novel crystalline forms of ribociclib succinate and ribociclib trifluoroacetate. The present invention also relates to pharmaceutical compositions comprising a crystalline form of ribociclib succinate and at least a pharmaceutically acceptable carrier. It further relates to the use of such compositions in the treatment of cancer.Type: GrantFiled: October 26, 2018Date of Patent: September 13, 2022Assignee: FRESENIUS KABI ONCOLOGY LTDInventors: Sarbjot Singh Sokhi, Govind Singh, Saswata Lahiri, Maneesh Kumar Pandey, Raj Narayan Tiwari, Sonu Shukla, Sachin Musmade, Heena Dua, Walter Cabri
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Patent number: 11414421Abstract: The present invention relates to an improved process for the preparation of 7-cyclopentyl-N,N-dimethyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide succinate (1/1) compound of formula-1a and its novel crystalline forms.Type: GrantFiled: January 10, 2019Date of Patent: August 16, 2022Assignee: NATCO PHARMA LTDInventors: Arunkumar Thiriveedhi, Swapna Kondaveeti, Sathish Thumati, Naresh Ghanta, Janaki Rama Rao Ravi, Durga Prasad Konakanchi, Pulla Reddy Muddansani, Venkaiah Chowdary Nannapaneni
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Patent number: 11384084Abstract: A compound of the Formula I and optionally a pharmaceutically acceptable salt thereof is provided: Formula I, wherein, R is one selected from the group consisting of H and CH3; n is an integer 4 when X is —CH2— and Ar is 1,4-phenyl, or n is an integer ranging from 1 to 4 when X is —CH2— and Ar is either 2?-fluoro-1,4-phenyl or 2,5-thienyl, or n is an integer ranging from 1 to 4 when X is one selected from the group consisting of O, S, —NH—, —NHCHO—, —NHCOCH3—, and —NHCOCF3— and Ar is one selected from the group consisting of (a) 1,4-phenyl, (b) 2?-fluoro-1,4-phenyl, and (c) 2,5-thienyl, or n is an integer 3 when X is —CH2—, R is CH3 and Ar is 1,4-phenyl.Type: GrantFiled: August 26, 2020Date of Patent: July 12, 2022Assignees: DUQUESNE UNIVERSITY OF THE HOLY SPIRIT, WAYNE STATE UNIVERSITYInventors: Aleem Gangjee, Larry H. Matherly
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Patent number: 11331320Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: March 17, 2020Date of Patent: May 17, 2022Assignees: Incyte Holdings Corporation, Incyte CororationInventors: James D. Rodgers, Stacey Shepard
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Patent number: 11254684Abstract: The present invention relates to a manufacturing process and intermediates for preparing a crystalline or non-crystalline form of N-((1S,3S)-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclobutyl)propane-1-sulfonamide. The present invention also relates to salt forms and pharmaceutical compositions comprising the crystalline form, and to methods for use of the compound prepared from a crystalline form in the treatment of various diseases.Type: GrantFiled: September 29, 2020Date of Patent: February 22, 2022Assignee: Pfizer Inc.Inventors: Kapildev Kashmirilal Arora, Jacob Cole DeForest, Andrew Kevern Hills, Brian Patrick Jones, Kris Nicole Jones, Chad Arthur Lewis, Anil Mahadeo Rane
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Patent number: 11236096Abstract: The present invention provides a novel RET inhibitor comprising, as an active ingredient, a compound or a salt thereof that have not been known for their RET inhibitory activity, and also provides an agent for preventing or treating diseases (e.g., malignant tumors) that can be prevented or treated by RET inhibitory activity. The RET inhibitor comprises, as an active ingredient, a compound represented by Formula (I) below or a salts thereof: wherein A, R1 to R3, X, and n are as defined in the specification.Type: GrantFiled: April 22, 2020Date of Patent: February 1, 2022Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Isao Miyazaki, Tadashi Shimamura, Masanori Kato, Hidenori Fujita
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Patent number: 11236095Abstract: The invention relates to a novel group of compounds of Formula (I) or salts thereof: wherein Y, Z1, Z2, R1, R4, R5 and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I).Type: GrantFiled: April 7, 2020Date of Patent: February 1, 2022Assignee: ASTRAZENECA ABInventors: Paul David Johnson, Andrew Leach, Richard William Arthur Luke, Zbigniew Stanley Matusiak, Jeffrey James Morris
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Patent number: 11225479Abstract: Provided herein are compounds and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of conditions associated with inhibition of HDAC (e.g., HDAC2).Type: GrantFiled: August 31, 2020Date of Patent: January 18, 2022Assignee: Alkermes, Inc.Inventors: Nathan Oliver Fuller, John A. Lowe, III
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Patent number: 11220504Abstract: This invention concerns pyrrolo[3,2-d]pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treatment and/or therapy of diseases.Type: GrantFiled: April 12, 2019Date of Patent: January 11, 2022Assignee: JANSSEN SCIENCES IRELAND UNLIMITED COMPANYInventors: David Craig McGowan, Stefaan Julien Last, Serge Maria Aloysius Pieters, Werner Embrechts, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson
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Patent number: 11213528Abstract: The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: March 2, 2020Date of Patent: January 4, 2022Assignees: Incyte Holdings Corporation, Incyte CorporationInventors: Hui-Yin Li, James D. Rodgers
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Patent number: 11186575Abstract: Methods of treating infections due to Helicobacter pylori (H. pylori), in particular in subjects having a peptic ulcer, are disclosed where the methods comprise administering to the subject an inhibitor of H.Type: GrantFiled: August 7, 2013Date of Patent: November 30, 2021Assignees: Alber Einslein College of Medicine, Victoria Link LimitedInventors: Vern L. Schramm, Shanzhi Wang, Antti Marko Haapalainen, Gary Brian Evans, Richard Hubert Furneaux, Keith Clinch, Peter Charles Tyler, Shivali Ashwin Gulab
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Patent number: 11124519Abstract: The present invention is directed to cocrystal forms of ((1S,2S,4R)-4-{4-[(1S)-2,3-dihydro-1H-inden-1-ylamino]-7H-pyrrolo[2,3-d]pyrimidin-7-yl}-2-hydroxcyclopentyl) methyl sulfamate of formula (I). The invention is also directed to methods of making cocrystal forms of ((1S,2S,4R)-4-{4-[(1S)-2,3-dihydro-1H-inden-1-ylamino]-7H-pyrrolo[2,3-d]pyrimidin-7-yl}-2-hydroxycyclopentyl) methyl sulfamate of formula (I). The invention is also directed to the pharmaceutical use of a cocrystal form as an E1 activating enzyme inhibitor, as well as a pharmaceutical composition comprising a cocrystal form. The invention is further directed to a method of treatment comprising administering a cocrystal form of ((1S,2S,4R)-4-{4-[(1S)-2,3-dihydro-1H-inden-1-ylamino]-7H-pyrrolo [2,3-d]pyrimidin-7-yl}-2-hydroxycyclopentyl)methyl sulfamate of formula (I).Type: GrantFiled: September 20, 2018Date of Patent: September 21, 2021Assignee: Millennium Pharmaceuticals, Inc.Inventors: Patricia Andres, Sarah Bethune, Marianne Langston, Debra L. Mazaik
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Patent number: 11111252Abstract: The present invention discloses a compound of the formula: and optionally comprising a pharmaceutically acceptable salt or hydrate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt or hydrate thereof.Type: GrantFiled: August 11, 2020Date of Patent: September 7, 2021Assignee: Duquesne University of The Holy SpiritInventor: Aleem Gangjee
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Patent number: 11014941Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient a safe and effective amount of a compound represented by any of Formulas I-III, or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a safe and effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.Type: GrantFiled: April 24, 2018Date of Patent: May 25, 2021Assignee: COCRYSTAL PHARMA, INC.Inventors: Irina C. Jacobson, Michael David Feese, Sam S K Lee
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Patent number: 10975085Abstract: The present invention is related to processes for preparing a composition comprising (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile, and related synthetic intermediate compounds. This compound is useful as an inhibitor of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.Type: GrantFiled: June 10, 2019Date of Patent: April 13, 2021Assignees: Incyte Holdings Corporation, Incyte CorporationInventors: Jiacheng Zhou, James D. Rodgers, Haisheng Wang
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Patent number: 10899736Abstract: This invention relates to processes and intermediates for making {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, useful in the treatment of diseases related to the activity of Janus kinases (JAK) including inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: GrantFiled: January 29, 2019Date of Patent: January 26, 2021Assignee: Incyte CorporationInventors: Dengjin Wang, Pingli Liu, Yongzhong Wu, Jiacheng Zhou
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Patent number: 10829450Abstract: The present disclosure is related to an improved and efficient process for preparation of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine which comprises: (a) N-acylation of 3-Amino-4-methyl pyridine; (b) Quarternization of 3-Acetylamino-4-methyl pyridine using benzyl halide; (c) Partial reduction of quarternized 3-Acetylamino-4-methyl pyridine by Sodium borohydride in Methanol or water; (d) Hydrolysis of partially reduced product to 1-Benzyl-4-methylpiperidin-3-one in presence of acid; (e) Reductive amination of 1-Benzyl-4-methylpiperidin-3-one using Methanolic methylamine in presence of Titanium(IV) isopropoxide in Methanol; (f) Resolution of 1-Benzyl-4-methylpiperidin-3-yl)-methylamine using Ditoluoyl (L) tartaric acid to get (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine. The disclosure is also related to novel intermediates: wherein R, R? and X are as described in the specification.Type: GrantFiled: January 11, 2018Date of Patent: November 10, 2020Assignee: UNICHEM LABORATORIES LIMITEDInventors: Dhananjay G. Sathe, Arijit Das, Yogesh Subhash Patil, Nilesh L. Bonde, Ankush Sampat Kekan
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Patent number: 10815240Abstract: The present invention relates to a manufacturing process and intermediates for preparing a crystalline or non-crystalline form of N-((1S,3S)-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclobutyl)propane-1-sulfonamide. The present invention also relates to salt forms and pharmaceutical compositions comprising the crystalline form, and to methods for use of the compound prepared from a crystalline form in the treatment of various diseases.Type: GrantFiled: July 3, 2019Date of Patent: October 27, 2020Assignee: Pfizer Inc.Inventors: Kapildev Kashmirilal Arora, Jacob Cole DeForest, Andrew Kevern Hills, Brian Patrick Jones, Kris Nicole Jones, Chad Arthur Lewis, Anil Mahadeo Rane
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Patent number: 10793572Abstract: Disclosed are novel compounds useful in the treatment of multiple sclerosis and other autoimmune diseases. The present invention describes compounds of formula (I) wherein: R1 is selected from H and CH3 R2 is selected from H, C4H9 alkyl, C6H13 alkyl and C3H6-phenyl, said phenyl optionally substituted by OH or OCH3, (1R,2S,5S)-5-methylcyclopent-3-ene-1,2-diol X is O or S Y is C, N or S.Type: GrantFiled: September 29, 2015Date of Patent: October 6, 2020Assignee: THE PROVOST FELLOWS FOUNDATION SCHOLARS AND THE OTHER MEMBERS OF BOARD OF THE COLLEGE OF THE HOLY AND UNDIVIDED TRINITY OF QUEEN ELIZABETHInventors: John Michael Southern, Stephen J. Connon
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Patent number: 10787457Abstract: The present invention provides a novel RET inhibitor comprising, as an active ingredient, a compound or a salt thereof that have not been known for their RET inhibitory activity, and also provides an agent for preventing or treating diseases (e.g., malignant tumors) that can be prevented or treated by RET inhibitory activity. The RET inhibitor comprises, as an active ingredient, a compound represented by Formula (I) below or a salts thereof: wherein A, R1 to R3, X, and n are as defined in the specification.Type: GrantFiled: November 29, 2018Date of Patent: September 29, 2020Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Isao Miyazaki, Tadashi Shimamura, Masanori Kato, Hidenori Fujita
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Patent number: 10772890Abstract: The present invention relates to the use of myeloperoxidase inhibitors (MPO) inhibitors for the treatment of multiple system atrophy. The present invention also relates to the use of MPO inhibitors for the treatment of Huntington's disease. The present invention also relates to the use of MPO inhibitors for neuroprotection.Type: GrantFiled: August 30, 2018Date of Patent: September 15, 2020Assignee: AstraZeneca ABInventors: Hakan Eriksson, Werner Poewe
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Patent number: 10766901Abstract: Provided are a preparation method for a chiral pyrrolopyrimidine compound and a related intermediate. In the method, a compound of formula A and a compound of formula 6 or a salt thereof are reacted to obtain a compound of formula 7 or a compound of formula 14, and a compound of formula I is prepared from the compound of formula 7 or the compound of formula 14. Also provided are the intermediate used, a preparation method for the intermediate and a use of the intermediate in the preparation of the compound of formula I. The preparation method has characteristics such as brief steps, a high stereoselectivity, a high utilization ratio of atoms, mild reaction conditions and a convenient post-treatment. The method avoids using an expensive asymmetric reaction catalyst, and is suitable for industrial production.Type: GrantFiled: June 15, 2017Date of Patent: September 8, 2020Assignees: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., LIANYUNGANG RUNZHONG PHARMACEUTICAL CO., LTD., CENTAURUS BIOPHARMA CO., LTD.Inventors: Xiquan Zhang, Aiming Zhang, Zhou Zhou, Huadong Yao, Jie Xie
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Patent number: 10759812Abstract: The present invention relates to a thienopyrimidine derivative and use thereof in medicine, and also to a pharmaceutical composition containing the compound. The compound or pharmaceutical composition is used for inhibiting acetyl-CoA carboxylase (ACC). The present invention also relates to a method of preparing such compound and pharmaceutical composition, as well as their use in the treatment or prevention of diseases regulated by acetyl-CoA carboxylase in mammals, especially in humans.Type: GrantFiled: January 22, 2018Date of Patent: September 1, 2020Assignee: Sunshine Lake Pharma Co., Ltd.Inventors: Wanjun Tang, Xinye Yang, Zheng Gu, Chenlu Li, Zongyuan Zhang, Zhifu Wan, Xiaojun Wang, Yingjun Zhang
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Patent number: 10695337Abstract: The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: GrantFiled: June 1, 2018Date of Patent: June 30, 2020Assignees: Incyte Holdings Corporation, Incyte CorporationInventors: Taisheng Huang, Chu-Biao Xue
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Patent number: 10676478Abstract: The present invention relates to a 7-(thiazol-5-yl)pyrrolopyrimidine compound as a TLR7 agonist, and particularly relates to a compound shown in formula (I), pharmaceutically acceptable salt and preparation method thereof, a pharmaceutical composition containing such a compound, and usage thereof in preparing an antiviral drug.Type: GrantFiled: November 4, 2016Date of Patent: June 9, 2020Assignee: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.Inventors: Zhaozhong Ding, Fei Sun, Lifang Wu, Hao Wu, Shuhui Chen, Ling Yang
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Patent number: 10640506Abstract: The present invention provides cyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I: wherein X, Y, Z, L, A, R5, n and m are defined above, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: GrantFiled: July 27, 2018Date of Patent: May 5, 2020Assignees: Incyte Holdings Corporation, Incyte CorporationInventors: James D. Rodgers, Stacey Shepard, Lixin Shao, Joseph Glenn
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Patent number: 10639310Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: November 1, 2018Date of Patent: May 5, 2020Assignee: Incyte CorporationInventors: James D. Rodgers, Stacey Shepard
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Patent number: 10626118Abstract: The present application relates to the field of pharmaceutical chemistry. The application specifically relates to a crystal form A and crystal form B of a pyrrolopyrimidine (formula I) for preparing a JAK inhibitor. The application further relates to a method for preparing the crystal form A and crystal form B, a crystalline composition comprising the crystal form A or crystal form B, a pharmaceutical composition comprising the crystal form A, crystal form B, or crystalline composition, and a pharmaceutical application of the pharmaceutical composition, the crystal form A, and the crystal form B. The crystal form A and crystal form B of the application has the advantages of high purity, high crystallinity, and good stability.Type: GrantFiled: June 15, 2017Date of Patent: April 21, 2020Assignees: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., LIANYUNGANG RUNZHONG PHARMACEUTICAL CO., LTD., CENTAURUS BIOPHARMA CO., LTD.Inventors: Zhou Zhou, Aiming Zhang, Xiquan Zhang, Huadong Yao
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Patent number: 10611765Abstract: Disclosed herein are novel compounds that are Mps1/TTK inhibitors. Also disclosed are compositions comprising the compounds and methods of using the compounds in treating various diseases.Type: GrantFiled: November 5, 2015Date of Patent: April 7, 2020Inventors: Robert Brueggemeier, Harold Fisk, Pui-Kai Li, Chenglong Li, Yasuro Sugimoto
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Patent number: 10610530Abstract: The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: June 8, 2018Date of Patent: April 7, 2020Assignees: Incyte Corporation, Incyte Holdings CorporationInventors: Hui-Yin Li, James D. Rodgers
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Patent number: 10570141Abstract: The present invention belongs to the field of pharmaceutical chemistry, and relates to a substituted pyrrolopyrimidine CDK inhibitor, in particular to a compound as shown in formula I or a pharmaceutically acceptable salt or solvate thereof, as well as a preparation method thereof and a pharmaceutical composition thereof. The present invention also relates to the use of the compound and the pharmaceutical composition thereof in the preparation of a drug for treating diseases associated with CDK inhibition. The compound according to the present invention has a marked inhibitory effect on CDK, excellent drug absorption and significantly superior oral absorption effect.Type: GrantFiled: March 27, 2017Date of Patent: February 25, 2020Assignees: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., CENTAURUS BIOPHARMA CO., LTD., LIANYUNGANG RUNZHONG PHARMACEUTICAL CO., LTD.Inventors: Shulong Wang, Kuncheng Chen, Xijie Liu, Yuandong Hu, Bo Liu, Yong Peng, Hong Luo, Yongxin Han, Shanchun Wang, Mei Liu, Hongjiang Xu
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Patent number: 10562902Abstract: Disclosed are a compound related to inhibiting the activity of an IRAK4 kinase, a pharmaceutical composition thereof, a use thereof in preparing drugs, a method in which same is used for inhibiting the activity of the IRAK4 kinase and a method in which same is used for treating and/or preventing IRAK4 kinase mediated diseases or conditions in mammals (especially humans). The compound has a structural formula I.Type: GrantFiled: August 12, 2016Date of Patent: February 18, 2020Assignee: Beijing Hanmi Pharmaceutical Co., Ltd.Inventors: Jiangcheng Xu, Qinguan Cai, Mi Young Cha, Maengsup Kim
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Patent number: 10472366Abstract: The invention relates to glucuronide prodrug compounds of the Janus kinase (JAK) inhibitor tofacitinib having formula I: where A1 and R1 are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.Type: GrantFiled: March 7, 2018Date of Patent: November 12, 2019Assignee: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Daniel D. Long, Donna A.A. Wilton, Mandy M. Loo
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Patent number: 10420768Abstract: Disclosed are chemical entities of formula I: wherein X, Y, Z, R1, R3, R4, R5 and R6 are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of formula I, and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of formula I.Type: GrantFiled: April 24, 2018Date of Patent: September 24, 2019Assignee: Rugen Holdings (Cayman) LimitedInventor: Gideon Shapiro
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Patent number: 10398699Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: April 23, 2018Date of Patent: September 3, 2019Assignees: Incyte Holdings Corporation, Incyte CorporationInventors: James D. Rodgers, Stacey Shepard
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Patent number: 10364248Abstract: The present invention is related to processes for preparing 4-chloro-7H-pyrollo[2,3,-d]pyrimidine, and related synthetic intermediate compounds. 4-Chloro-7H-pyrrolo[2,3,-d]pyrimidine is an intermediate for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines, which are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.Type: GrantFiled: January 12, 2018Date of Patent: July 30, 2019Assignees: Incyte Corporation, Incyte Holdings CorporationInventors: Jiacheng Zhou, James D. Rodgers, Haisheng Wang
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Patent number: 10328080Abstract: In some embodiments, the invention includes a therapeutic combination of a phosphoinositide 3-kinase (PI3K) inhibitor, including PI3K inhibitors selective for the ?- and ?-isoforms and selective for both ?- and ?-isoforms, and a Bruton's tyrosine kinase (BTK) inhibitor. In some embodiments, the invention includes therapeutic methods of using a BTK inhibitor and a PI3K-? inhibitor to treat solid tumor cancers by modulation of the tumor microenvironment, including macrophages, monocytes, mast cells, helper T cells, cytotoxic T cells, regulatory T cells, natural killer cells, myeloid-derived suppressor cells, regulatory B cells, neutrophils, dendritic cells, and fibroblasts.Type: GrantFiled: December 5, 2014Date of Patent: June 25, 2019Assignee: Acerta Pharma, B.V.Inventors: Ahmed Hamdy, Wayne Rothbaum, Raquel Izumi, Brian Lannutti, Todd Covey, Roger Ulrich, Dave Johnson, Tjeerd Barf, Allard Kaptein
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Patent number: 10259814Abstract: This invention concerns pyrrolo[3,2-d]pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treatment and/or therapy of diseases.Type: GrantFiled: October 25, 2016Date of Patent: April 16, 2019Assignee: Janssen Sciences Ireland UCInventors: David Craig McGowan, Stefaan Julien Last, Serge Maria Aloysius Pieters, Werner Embrechts, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson
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Patent number: 10233174Abstract: The invention relates to thiocarbamate prodrug compounds of the Janus kinase (JAK) inhibitor tofacitinib having formula I: wherein R1, R2, R3, R4 and n are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.Type: GrantFiled: May 22, 2018Date of Patent: March 19, 2019Assignee: THERAVANCE BIOPHARMA R&D IP, LLCInventor: Daniel D. Long
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Patent number: 10220037Abstract: Compounds of the general formula): processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.Type: GrantFiled: June 2, 2017Date of Patent: March 5, 2019Assignee: Pfizer Inc.Inventors: John Howard Tatlock, Indrawan James McAlpine, Michelle Bich Tran-Dube, Eugene Yuanjin Rui, Martin James Wythes, Robert Arnold Kumpf, Michele Ann McTigue, Ryan Patman
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Patent number: 10167287Abstract: This invention provides substituted pyrimidine compounds having the formula: wherein X is absent, CH2, S, or O, and R is an alkyl group having from one to ten carbon atoms, and optionally salts, hydrates, or solvates thereof, that are useful in treating a patient having a disease or cancer. The compounds of this invention are useful as multi-enzyme antifolates selectively targeting the folate receptor (FR). Further, a method of making 5- and 6-substituted cyclopenta[d]pyrimidine for nonclassical and classical antifolates as TS and DHFR inhibitors is provided.Type: GrantFiled: April 5, 2017Date of Patent: January 1, 2019Assignee: Duquesne University of the Holy SpiritInventors: Aleem Gangjee, Larry H. Matherly
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Patent number: 10138250Abstract: The present invention relates to novel crystalline forms of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide (compound I), its salts, and process for preparation thereof. Crystalline forms in the present invention have good stability, low hygroscopicity, good processability, easy treatability and other favorable properties. In addition, the process is simple, low cost, and has an important value for future optimization and development of the drug.Type: GrantFiled: May 21, 2018Date of Patent: November 27, 2018Assignee: Crystal Pharmatech Co., Ltd.Inventors: Minhua Chen, Yanfeng Zhang, Xiaoyu Zhang