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1.发明公开公开(公告)号：US20240239735A1
公开(公告)日：2024-07-18
申请号：US18559891
申请日：2022-05-13
发明人： Liang WANG , Jun LOU , Yi YUAN , Xiaodan GUO , Yongkai CHEN , Yihan ZHANG , Huayun HONG , Wei PENG , Chaodong WANG
IPC分类号： C07C55/07 , A61K31/10 , A61K31/194 , A61K31/4155 , A61K45/06 , C07C51/43 , C07C57/145 , C07C59/255 , C07C315/06 , C07C317/14 , C07D403/04
CPC分类号： C07C55/07 , A61K31/10 , A61K31/194 , A61K31/4155 , A61K45/06 , C07C51/43 , C07C57/145 , C07C59/255 , C07C315/06 , C07C317/14 , C07D403/04 , C07B2200/13
摘要： An acid addition salt of a ROCK inhibitor, and a crystal form, a composition and the pharmaceutical use thereof are provided. The acid addition salt is an acid addition salt of compound A and any one of the following acids: hydrochloric acid, p-toluenesulfonic acid, benzenesulfonic acid, maleic acid, tartaric acid, oxalic acid, fumaric acid, sulfuric acid, methanesulfonic acid, phosphoric acid, succinic acid or citric acid (A). The acid addition salt of compound A and the crystal form thereof have the characteristics of high solubility, good stability, high purity, few impurities and high bioequivalence, and are beneficial for the storage, quality control and druggability of drugs.
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公开(公告)号：US20230050653A1
公开(公告)日：2023-02-16
申请号：US17756079
申请日：2020-11-12
发明人： Jinping LI , Jun LOU , Xiaodan GUO , Xian ZENG , Yongkai CHEN , Yihan ZHANG , Wei PENG , Chaodong WANG
IPC分类号： C07D471/04 , C07D401/04 , C07D403/04 , C07D413/04 , C07D405/14 , C07D513/04 , C07D401/14 , C07D487/04
摘要： The compound represented by formula (I), and racemates, stereoisomers, tautomers, isotopic markers, nitrogen oxides, solvates, polymorphs, metabolites, esters, pharmaceutically acceptable salts, or prodrugs thereof have ROCK inhibitory activity. The compound represented by formula (1) has good safety, good metabolic stability, and a low risk of potential hepatotoxicity. Further, the compound represented by formula (I) has a simple preparation method and is easy to purify, and therefore has good application prospects.
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3.发明授权公开(公告)号：US11161803B2
公开(公告)日：2021-11-02
申请号：US16609190
申请日：2018-04-27
发明人： Bo Zhang , Xiaohua Ding , Dongcheng Dai , Sijun Lei , Xueming Liu , Panpan Duan , Yongkai Chen , Chaodong Wang
IPC分类号： C07D295/027 , C07C229/34 , C07C227/20 , C07C231/02 , C07C231/12
摘要： The present disclosure belongs to the field of chemical synthesis, and in particular relates to an ammonium carboxylate compound, a crystalline form and an amorphous form, and a preparation method thereof. The present disclosure prepares the compound and the crystalline form I and its single crystal, amorphous form and crystalline form II thereof. The compound, the crystalline forms, the single crystal and the amorphous form can stably exist and exhibit good solid forms, suitable for medicine-making. Furthermore, these products possess high purity and less single impurity. Moreover, the preparation methods of the present disclosure are easy to implement due to the simple processes with mild reaction conditions, and could produce products of high yield and high purity without complex purification steps. Furthermore, the preparation methods may facilitate safety, environmental protection, and industrial production.
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公开(公告)号：US11040958B2
公开(公告)日：2021-06-22
申请号：US16486761
申请日：2018-02-08
发明人： Hongwei Tang , Jun Lou , Penggao Yu , Li Liu , Anxiao Zheng , Yongkai Chen , Chaodong Wang
IPC分类号： C07D401/14 , C07D403/06 , C07F9/6558 , C07H13/04 , A61P31/10
摘要： The present disclosure provides a triazole antibacterial derivative and a pharmaceutical composition thereof and a use thereof and in particular relates to a compound represented by the following formula (I), and a racemate, a stereoisomer, a tautomer, an oxynitride or a pharmaceutically acceptable salt thereof: The compound of the present disclosure has a desirable water solubility and can be formulated into an injection for use without adding a cosolvent having a potential safety risk (such as hydroxypropyl-β-cyclodextrin, sulfobutylether-β-cyclodextrin, and the like), facilitating drug administration for patients, and greatly improving clinical safety. The drug can be used even by patients with moderate or severe renal impairment, thereby expanding the application scope of the drug.
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公开(公告)号：US11013736B2
公开(公告)日：2021-05-25
申请号：US16317508
申请日：2017-07-28
发明人： Lei Liang , Yongkai Chen , Liu Hu , Wei Feng , Chaodong Wang
IPC分类号： A61K31/497 , A61P9/12 , A61K9/00 , A61K9/20
摘要： The invention discloses an oral solid preparation containing any one, or a mixture of two or more of crystalline form I, II, III, and IV of the compound represented by formula (A). The oral solid preparation of the present invention disintegrates rapidly, increasing dissolution rate thereof, thereby improving bioavailability. In particular, it is possible to solve the problem that an active material (active ingredient), which is high hygroscopic and becomes sticky after moisture absorption, can not be effectively disintegrated by conventional disintegrants. The present invention further relates to a use of the oral solid preparation in preparing an angiotensin II receptor antagonist or a use thereof in preparing medicine for preventing and/or treating hypertension, chronic heart failure and diabetic nephropathy.
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公开(公告)号：US20190038621A1
公开(公告)日：2019-02-07
申请号：US16075514
申请日：2017-01-26
发明人： Jun LOU , Penggao YU , Li LIU , Hongwei TANG , Anxiao ZHENG , Yongkai CHEN , Chaodong WANG
IPC分类号： A61K31/496 , A61K31/675 , A61P31/10
摘要： The present disclosure provides a posaconazole derivative, a pharmaceutical composition and use thereof, which specifically include a compound represented by the following formula (I), a racemate, stereoisomer, tautomer, oxynitride, or a pharmaceutically acceptable salt thereof: The compounds of the present disclosure have strong antifungal activity, high safety, and good water solubility, without the need for the addition of a cosolvent (such as hydroxypropyl-β-cyclodextrin, sulfobutyl ether-β-cyclodextrin, and the like) with potential safety risks. Furthermore, the formulation process of the compound could have less difficulty and less cost, and therefore can be used to prepare improved antifungal drugs.
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公开(公告)号：US09708306B2
公开(公告)日：2017-07-18
申请号：US15123961
申请日：2015-03-18
发明人： Jian Ge , Jianyi Ma , Guangya Xiang , Wei Wang , Chaodong Wang
IPC分类号： C07D413/10 , A61K31/4245 , A61K31/497 , A61K31/501 , C07D403/14 , C07D493/04 , C07D498/18 , C07D413/14
CPC分类号： C07D413/10 , A61K31/4245 , A61K31/497 , A61K31/501 , C07D403/14 , C07D413/14 , C07D493/04 , C07D498/18
摘要： The invention belongs to the technical field of pharmaceutical chemistry, and particularly pertains to benzimidazole derivatives, and preparation process and pharmaceutical uses thereof. Benzimidazole derivatives include Ligustrazine and NO donor derivatives. The kind of the compounds can rapidly release Ligustrazine or No in vivo, so that they can produce effective synergetic effects with Azilsartan, to enhance the anti-hypertension effect, and reduce adverse effects, and the released Ligustrazine can produce ideal protection to patients' livers and kidneys, thereby filling blanks in the prior art.
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8.发明申请Benzimidazole Derivatives and Preparation Process and Pharmaceutical Uses Thereof 有权苯并咪唑衍生物及其制备方法及药物用途公开(公告)号：US20170022188A1
公开(公告)日：2017-01-26
申请号：US15123961
申请日：2015-03-18
发明人： Jian GE , Jianyi MA , Guangya XIANG , Wei WANG , Chaodong WANG
IPC分类号： C07D413/10 , C07D413/14 , C07D493/04
CPC分类号： C07D413/10 , A61K31/4245 , A61K31/497 , A61K31/501 , C07D403/14 , C07D413/14 , C07D493/04 , C07D498/18
摘要： The invention belongs to the technical field of pharmaceutical chemistry, and particularly pertains to benzimidazole derivatives, and preparation process and pharmaceutical uses thereof. Benzimidazole derivatives include Ligustrazine and NO donor derivatives. The kind of the compounds can rapidly release Ligustrazine or No in vivo, so that they can produce effective synergetic effects with Azilsartan, to enhance the anti-hypertension effect, and reduce adverse effects, and the released Ligustrazine can produce ideal protection to patients' livers and kidneys, thereby filling blanks in the prior art
摘要翻译： 本发明属于药物化学技术领域，特别涉及苯并咪唑衍生物及其制备方法及药物用途。 苯并咪唑衍生物包括Ligustrazine和NO供体衍生物。 这种化合物可以快速释放Ligustrazine或No体内，使他们能够与Azilsartan产生有效的协同作用，增强抗高血压作用，减少不良反应，释放的Ligustrazine可以为患者的肝脏提供理想的保护 和肾脏，从而在现有技术中填充空白
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公开(公告)号：US20230257382A1
公开(公告)日：2023-08-17
申请号：US18014143
申请日：2021-06-23
发明人： Jinping Li , Xiaodan Guo , Feng Zhou , Jun Lou , Li Liu , Xiaoya Chen , Yihan Zhang , Yongkai Chen , Chaodong Wang
IPC分类号： C07D487/04 , A61P1/16
CPC分类号： C07D487/04 , A61P1/16
摘要： Disclosed is a heterocyclic compound as represented by formula (I), a tautomer thereof, or a pharmaceutically acceptable salt thereof. The compound has better inhibitory activity on TRPC5, has good metabolic stability in liver micro-particles, and has good clinical pharmacokinetic properties.
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10.发明申请公开(公告)号：US20230068538A1
公开(公告)日：2023-03-02
申请号：US17417304
申请日：2019-12-27
发明人： Jun LOU , Yongkai CHEN , Junhua LIU , Yihan ZHANG , Xiaodan GUO , Li LIU , Lina QIAN , Chaodong WANG
IPC分类号： C07D471/04 , C07D413/06 , C07D491/048 , C07F5/04 , C07D209/18 , C07D487/04 , A61P11/14
摘要： Disclosed by the invention is a heterocyclic compound, an intermediate, and a preparation method therefor and an application thereof. Provided by the invention are a heterocyclic compound as shown in formula I, and a stereoisomer, a geometric isomer, a tautomer, a nitrogen oxide, a hydrate, a solvate, a metabolite, an ester, a pharmaceutically acceptable salt or a prodrug thereof. The heterocyclic compound has a high P2X3 antagonistic activity, and has good selectivity, low toxicity, good metabolic stability and little taste influence.
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