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1. 发明授权

US10759765B2 Heterocyclic carboxylic acid amide ligand and applications thereof in copper catalyzed coupling reaction of aryl halogeno substitute 有权
公开(公告)号：US10759765B2
公开(公告)日：2020-09-01
申请号：US16093688
申请日：2017-04-14
申请人： CE Pharm CO., LTD.
发明人： Dawei Ma , Wei Zhou , Mengyang Fan , Haibo Wu , Junli Yin , Xi Jiang , Yuntong Zhai , Songtao Niu
IPC分类号： C07D241/02 , B01J31/22 , C07C231/02 , C07C233/00 , C07D207/32 , C07D209/08 , C07D209/12 , C07D213/06 , C07D235/08 , C07D239/02 , C07D277/02 , C07D277/62 , C07D307/02 , C07D307/78 , C07C209/60
摘要： Provided are a heterocyclic carboxylic acid amide ligand and applications thereof in a copper catalyzed coupling reaction. Specifically, provided are uses of a compound represented by formula (I), definitions of radical groups being described in the specifications. The compound represented by formula (I) can be used as the ligand in the copper catalyzed coupling reaction of the aryl halogeno substitute, and is used or catalyzing the coupling reaction for forming the aryl halogeno substitute having C—N, C—O, C—S and other bonds.

2. 发明授权

US09284280B2 Use of form-I crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide 有权
标题翻译：使用2- {4- [N-（5,6-二苯基吡嗪-2-基）-N-异丙基氨基]丁氧基} -N-（甲基磺酰基）乙酰胺
公开(公告)号：US09284280B2
公开(公告)日：2016-03-15
申请号：US14160641
申请日：2014-01-22
申请人： Hideyuki Itou
发明人： Hideyuki Itou
IPC分类号： C07D241/02 , C07D241/20 , A61K31/4965
CPC分类号： C07D241/20 , A61K31/4965 , C07B2200/13
摘要： A method is provided in which Form-I crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide is administered as an active ingredient to a subject for the purpose of treating or preventing certain diseases, disorders, and symptoms, or for promoting angiogenesis or gene therapy. The Form-I crystal exhibits diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2θ when the spectrum is obtained by using Cu Kα radiation: 9.4 degrees, 9.8 degrees, 17.2 degrees, and 19.4 degrees. The targeted diseases and disorders include transient ischemic attack, diabetic neuropathy, diabetic gangrene, peripheral circulatory disturbance, connective tissue disease, reocclusion/restenosis after percutaneous transluminal coronary angioplasty, arteriosclerosis, thrombosis, hypertension, pulmonary hypertension, ischemic disorder, angina, glomerulonephritis, diabetic nephropathy, chronic renal failure, allergy, bronchial asthma, ulcer, pressure ulcer (bedsore), restenosis after coronary intervention, thrombocytopenia by dialysis, the diseases in which fibrosis of organs or tissues is involved, erectile dysfunction, inflammatory bowel disease, and gastritis.
摘要翻译：提供了一种方法，其中将2- {4- [N-（5,6-二苯基吡嗪-2-基）-N-异丙基氨基]丁氧基} -N-（甲基磺酰基）乙酰胺的I型晶体作为活性成分以治疗或预防某些疾病，病症和症状，或用于促进血管发生或基因治疗的目的。 Form-I晶体在X射线粉末衍射光谱中至少在以下衍射角2θ处显示衍射峰; 当通过使用CuKα辐射获得光谱时：9.4度，9.8度，17.2度和19.4度。目标疾病和障碍包括短暂性脑缺血发作，糖尿病性神经病变，糖尿病性坏疽，外周循环障碍，结缔组织病，经皮腔内冠状动脉成形术后再闭塞/再狭窄，动脉硬化，血栓形成，高血压，肺动脉高压，缺血性障碍，心绞痛，肾小球性肾炎，糖尿病肾病，慢性肾衰竭，过敏，支气管哮喘，溃疡，压力性溃疡（褥疮），冠状动脉介入后再狭窄，透析血小板减少症，器官或组织纤维化的疾病，勃起功能障碍，炎症性肠病和胃炎。

3. 发明授权

US09079866B2 Flap modulators 有权
标题翻译：瓣片调制器
公开(公告)号：US09079866B2
公开(公告)日：2015-07-14
申请号：US14169770
申请日：2014-01-31
申请人： JANSSEN PHARMACEUTICA NV
发明人： Genesis M. Bacani , Wendy Eccles , Anne E. Fitzgerald , Steven D. Goldberg , Michael D. Hack , Natalie A. Hawryluk , William M. Jones , John M. Keith , Paul Krawczuk , Alec D. Lebsack , Alice Lee-Dutra , Jing Liu , Kelly J. McClure , Steven P. Meduna , Daniel J. Pippel , Mark D. Rosen , Zachary S. Sales
IPC分类号： A61K31/4965 , C07D241/02 , C07D241/20 , C07D241/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D487/04 , C07F7/08 , C07D405/14 , C07D413/14 , C07D213/73 , C07D401/04 , C07D235/10 , C07D401/10 , C07D403/10 , C07D237/20 , C07D409/12 , C07D413/10 , C07D417/10 , C07D471/04 , C07D487/08 , C07D263/48 , C07D491/10 , C07D498/04 , C07D209/08 , C07D277/62 , C07D285/12
CPC分类号： C07F7/0812 , C07D209/08 , C07D213/73 , C07D235/10 , C07D237/20 , C07D241/20 , C07D241/26 , C07D263/48 , C07D277/62 , C07D285/12 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/10 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10 , C07D491/107 , C07D495/10 , C07D498/04 , C07F5/025 , C07F7/08
摘要： The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, R2, R3, R3′, L, W, and V are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
摘要翻译：本发明涉及式（I）化合物或其形式，其中环A，R 1，R 2，R 3，R 3'，L，W和V如本文所定义，可用作FLAP调节剂。本发明还涉及包含式（I）化合物的药物组合物。制备和使用式（I）化合物的方法也在本发明的范围内。

4. 发明授权

US08969573B2 Compounds for the inhibition of cellular proliferation 有权
标题翻译：用于抑制细胞增殖的化合物
公开(公告)号：US08969573B2
公开(公告)日：2015-03-03
申请号：US13807132
申请日：2011-06-28
申请人： Michael Chorev , Bertal Huseyin Aktas , Jose A. Halperin , Gerhard Wagner
发明人： Michael Chorev , Bertal Huseyin Aktas , Jose A. Halperin , Gerhard Wagner
IPC分类号： C07D417/02 , C07D277/38 , C07D241/02 , A61K31/381 , A61K31/496 , C07D277/84 , C07D233/88 , C07D263/48 , C07D277/50 , C07D417/04 , C07D417/10 , C07D417/12 , C07D277/30 , C07D277/42 , C07D513/04
CPC分类号： C07D277/84 , C07D233/88 , C07D263/48 , C07D277/30 , C07D277/42 , C07D277/50 , C07D417/04 , C07D417/10 , C07D417/12 , C07D513/04
摘要： Compositions and methods for inhibiting translation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, (4) disorders associated with viral infections, and/or (5) non-proliferative metabolic disorders such as type II diabetes where inhibition of translation initiation is beneficial using the compounds disclosed herein.
摘要翻译：提供了用于抑制翻译的组合物和方法。用于治疗（1）细胞增殖性疾病的组合物，方法和试剂盒，（2）非增殖性，退行性疾病，（3）病毒感染，（4）与病毒感染相关的病症和/或（5）非增殖性代谢紊乱例如II型糖尿病，其中使用本文公开的化合物对翻译起始的抑制是有益的。

5. 发明授权

US08859768B2 Heteroaryls and uses thereof 有权
标题翻译：杂芳基及其用途
公开(公告)号：US08859768B2
公开(公告)日：2014-10-14
申请号：US13206671
申请日：2011-08-10
申请人： Courtney A. Cullis , Krista E. Granger , Jianping Guo , Masaaki Hirose , Gang Li , Miho Mizutani , Tricia J. Vos
发明人： Courtney A. Cullis , Krista E. Granger , Jianping Guo , Masaaki Hirose , Gang Li , Miho Mizutani , Tricia J. Vos
IPC分类号： C07D239/02 , C07D241/02 , C07D213/22 , C07D413/00 , C07D401/00 , A61K31/505 , A61K31/44 , A61K31/42 , A61K31/422 , C07D413/14 , C07D417/14 , C07D413/04
CPC分类号： A61K31/422 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04
摘要： This invention provides compounds of formula IA or IB: wherein HY, R1, R2, and G1, are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
摘要翻译：本发明提供式IA或IB的化合物：其中HY，R1，R2和G1如说明书中所述。这些化合物是VPS34和/或PI3K的抑制剂，因此可用于治疗增殖性，炎性或心血管疾病。

6. 发明授权

US08778309B2 Fluorescent pyrazine derivatives and methods of using the same in assessing renal function 有权
标题翻译：荧光吡嗪衍生物及其在肾功能评估中的应用
公开(公告)号：US08778309B2
公开(公告)日：2014-07-15
申请号：US11721186
申请日：2005-12-22
申请人： Raghavan Rajagopalan , Richard B. Dorshow , William L. Neumann , Dennis A. Moore
发明人： Raghavan Rajagopalan , Richard B. Dorshow , William L. Neumann , Dennis A. Moore
IPC分类号： A61B5/20 , C07D241/02
CPC分类号： C07D241/28 , A61K31/4965 , A61K49/0004 , A61K49/0021 , A61K49/0052 , C07D241/20 , C07D241/26
摘要： The present invention relates to pyrazine derivatives represented by Formula I. X1 and X2 of Formula I may be characterized as electron withdrawing groups, while Y1 and Y2 of Formula I may be characterized as electron donating groups. Pyrazine derivatives of the present invention may be utilized in assessing organ (e.g., kidney) function. In a particular example, an effective amount of a pyrazine derivative that is capable of being renally cleared may be administered into a patient's body. The pyrazine derivative may be capable of one or both absorbing and emanating spectral energy of at least about 400 nm (e.g., visible and/or infrared light). At least some of the derivative that is in the body may be exposed to spectral energy and, in turn, spectral energy may emanate from the derivative. This emanating spectral energy may be detected and utilized to determine renal function of the patient
摘要翻译：本发明涉及由式I表示的吡嗪衍生物。式I的X1和X2可以表征为吸电子基团，而式I的Y1和Y2可以表征为给电子基团。本发明的吡嗪衍生物可用于评估器官（例如肾）功能。在具体实例中，有效量的能够被再次清除的吡嗪衍生物可以被施用到患者体内。吡嗪衍生物可以具有至少约400nm的吸收和发射光谱能量（例如可见光和/或红外光）的一种或两种。身体中的至少一些衍生物可能暴露于光谱能量，反过来，光谱能量可能来自衍生物。这种发出的光谱能量可以被检测并用于确定患者的肾功能

7. 发明授权

US08697705B2 Isoindolinone derivatives 失效
标题翻译：异吲哚啉酮衍生物
公开(公告)号：US08697705B2
公开(公告)日：2014-04-15
申请号：US13899885
申请日：2013-05-22
申请人： Hoffmann-La Roche Inc.
发明人： Steven Joseph Berthel , Robert Francis Kester , Lucja Orzechowski
IPC分类号： A61K31/4965 , C07D241/02
CPC分类号： C07D403/12
摘要： The present invention relates to compounds of the formula I, as well as pharmaceutically-acceptable salts thereof, pharmaceutical compositions containing said compounds and methods of using said compounds in the treatment or prophylaxis of diseases and disorders. The compounds and compositions disclosed herein are glucokinase activators useful for the treatment or prophylaxis of metabolic diseases and disorders, for example diabetes mellitus, including type II diabetes mellitus.
摘要翻译：本发明涉及式I化合物及其药学上可接受的盐，含有所述化合物的药物组合物和使用所述化合物治疗或预防疾病和病症的方法。本文公开的化合物和组合物是可用于治疗或预防代谢性疾病和病症（例如糖尿病，包括II型糖尿病）的葡糖激酶活化剂。

8. 发明授权

US08513415B2 Preparation of C-pyrazine-methylamines 失效
标题翻译： C-吡嗪甲胺的制备
公开(公告)号：US08513415B2
公开(公告)日：2013-08-20
申请号：US13265363
申请日：2010-04-19
申请人： Yunyu Mao , Josef A. Rechka , Paula A. Tavares-Greco
发明人： Yunyu Mao , Josef A. Rechka , Paula A. Tavares-Greco
IPC分类号： C07D241/02
CPC分类号： C07D487/04 , C07D241/16
摘要： A process for preparing a compound of formula (I) or a salt thereof: (I) wherein R1 is H or optionally substituted aryl or heteroaryl; comprising reacting 2,3-dichloropyrazine with a suitable diaryl imine followed by hydrolysis.
摘要翻译：制备式（I）化合物或其盐的方法：其中R 1为H或任选取代的芳基或杂芳基的（I）包括使2,3-二氯吡嗪与合适的二芳基亚胺反应，然后水解。

9. 发明授权

US08497373B2 Phosphonic acid compounds as inhibitors of serine proteases 有权
标题翻译：膦酸化合物作为丝氨酸蛋白酶的抑制剂
公开(公告)号：US08497373B2
公开(公告)日：2013-07-30
申请号：US13471876
申请日：2012-05-15
申请人： Michael N. Greco , Harold R. Almond, Jr. , Lawrence de Garavilla , Michael J. Hawkins , Michael J. Humora , Yun Qian , Donald Gilmore Walker , Sergio Cesco-Cancian , Christopher Norman Nilsen , Mitul N. Patel , Kirk Leonard Sorgi , Eugene Powell
发明人： Michael N. Greco , Harold R. Almond, Jr. , Lawrence de Garavilla , Michael J. Hawkins , Michael J. Humora , Yun Qian , Donald Gilmore Walker , Sergio Cesco-Cancian , Christopher Norman Nilsen , Mitul N. Patel , Kirk Leonard Sorgi , Eugene Powell
IPC分类号： C07D241/02 , C07F9/02 , A61K31/4965
CPC分类号： C07F9/65586 , C07F9/3882 , C07F9/572 , C07F9/59 , C07F9/650952 , C07F9/65517 , C07F9/65583 , C07F9/6561
摘要： The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
摘要翻译：本发明涉及可用作丝氨酸蛋白酶抑制剂的膦酸化合物，其组合物和用于治疗炎性和丝氨酸蛋白酶介导的病症的方法。

10. 发明授权

US08343967B2 Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases 有权
公开(公告)号：US08343967B2
公开(公告)日：2013-01-01
申请号：US13458968
申请日：2012-04-27
申请人： Hong Ding , Steven W. Elmore , Laura A. Hexamer , Aaron R. Kunzer , Cheol-Min Park , Andrew J. Souers , Gerard M. Sullivan , Michael D. Wendt
发明人： Hong Ding , Steven W. Elmore , Laura A. Hexamer , Aaron R. Kunzer , Cheol-Min Park , Andrew J. Souers , Gerard M. Sullivan , Michael D. Wendt
IPC分类号： A61K31/5377 , A61K31/5375 , A61K31/435 , A61K31/437 , C07D413/02 , C07D241/02 , C07D295/00 , C07D211/00
CPC分类号： C07D211/58 , C07C311/51 , C07C2601/14 , C07C2603/74 , C07D295/112 , C07D295/195 , C07D417/04
摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

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