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1. 发明授权

US12049461B2 4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections 有权
公开(公告)号：US12049461B2
公开(公告)日：2024-07-30
申请号：US16950654
申请日：2020-11-17
申请人： Gilead Sciences, Inc.
发明人： Ling-Jie Gao , Piet Andre Maurits Maria Herdewijn , Steven Cesar Alfons De Jonghe , William John Watkins , Lee Shun Chong
IPC分类号： A61K31/517 , A61K31/5375 , A61K31/5377 , A61P31/14 , C07D239/72 , C07D239/78 , C07D239/86 , C07D239/88 , C07D239/94 , C07D239/95 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04
CPC分类号： C07D413/04 , A61K31/517 , A61K31/5375 , A61K31/5377 , A61P31/14 , C07D239/72 , C07D239/78 , C07D239/86 , C07D239/88 , C07D239/94 , C07D239/95 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R2 is hydrogen, NR′R″, C1-7alkyl, arylC1-7 alkyl or C3-10 cycloalkyl; R4 is amino, C1-7alkyl, C2-7 alkenyl, C3-10 cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C1-7alkyl or C3-10 cycloalkyl-C1-7 alkyl; R5 is hydrogen or C1-7 alkyl, or R5 and R4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C1-7alkylene, C2-7 alkenylene or C2-7 alkynylene; R6 is halogen, heteroaryl or aryl; R′ and R″ are each independently hydrogen, C1-7 alkyl-carbonyl or C1-7 alkyl; provided that R4 is not phenyl substituted with morpholino when R2 is H and R5 is H, and provided that when NR4R5 is piperazinyl, said NR4R5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.

2. 发明公开

US20230348460A1 ANTI-WOLBACHIA PYRIDO[2,3-d]PYRIMIDINECOMPOUNDS 审中-公开
公开(公告)号：US20230348460A1
公开(公告)日：2023-11-02
申请号：US17956435
申请日：2022-09-29
申请人： Liverpool School of Tropical Medicine , The University of Liverpool , Eisai R&D Management Co., Ltd.
发明人： Stephen A. Ward , Mark J. Taylor , Paul M. O’Neil , Weiqian David Hong , Farid Benayoud
IPC分类号： C07D471/04 , C07D239/86 , C07D495/04
CPC分类号： C07D471/04 , C07D239/86 , C07D495/04
摘要： The present invention relates to compounds of Formulae I and II as defined herein, and salts and solvates thereof.

The present invention also relates to pharmaceutical compositions comprising compounds of Formulae I and II, and to the use of compounds of Formulae I and II in the treatment or prevention of filarial worm infection, as well as other diseases or conditions in which filarial worm infection is implicated.

3. 发明授权

US10626124B2 Activators of autophagic flux and phospholipase D and clearance of protein aggregates including tau and treatment of proteinopathies 有权
公开(公告)号：US10626124B2
公开(公告)日：2020-04-21
申请号：US16027930
申请日：2018-07-05
申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK , NY STATE PSYCHIATRIC INSTITUTE
发明人： Kirsten Alison Rinderspacher , Wai Yu , Karen Duff , Donald Landry , Shi-Xian Deng
IPC分类号： C07D513/04 , C07D403/12 , C07D405/12 , C07D239/86 , C07D239/93 , C07D239/94 , C07D471/04 , C07D491/04 , C07D495/04 , A61K31/517 , C07D217/22 , C07D239/88 , C07D401/12 , C07D491/048 , A61P25/28
CPC分类号： C07D513/04 , A61K31/517 , A61P25/28 , C07D217/22 , C07D239/86 , C07D239/88 , C07D239/93 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04
摘要： The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.

4. 发明申请

US20170304305A1 QUINAZOLINE DERIVATIVES SUBSTITUTED BY ANILINE, PREPARATION METHOD AND USE THEREOF 审中-公开
公开(公告)号：US20170304305A1
公开(公告)日：2017-10-26
申请号：US15645300
申请日：2017-07-10
申请人： XUANZHU PHARMA CO., LTD.
发明人： Yanyan DONG , Shih CHENGKON
IPC分类号： A61K31/517 , A61K45/06 , C07D491/08 , C07D487/10 , C07D487/08 , C07D487/04 , C07D471/10 , C07D471/08 , C07D471/04 , C07D451/06 , C07D451/02 , C07D413/14 , C07D409/12 , C07D405/12 , C07D403/14 , C07D403/12 , C07D401/12 , C07D239/94 , C07D239/86 , C07D491/107 , C07D493/08
CPC分类号： A61K31/517 , A61K31/5377 , A61K45/06 , C07D239/86 , C07D239/94 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D413/14 , C07D451/02 , C07D451/06 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/08 , C07D491/107 , C07D493/08
摘要： The invention relates to quinazoline derivatives substituted by aniline which are represented by the below formula (I), pharmaceutical acceptable salts and stereoisomer thereof, wherein these groups of R1, R2, R3, R4, R5, R6, L and n have the meanings given in the specification. The invention also relates to preparation methods, pharmaceutical compositions, pharmaceutical preparation and the use for preparation of medicine of treating excessive hyperplasia and chronic obstructive pulmonary disease and uses for treating excessive hyperplasia and chronic obstructive pulmonary disease thereof.

5. 发明申请

US20100056517A1 ARYLSULFONAMIDE COMPOUNDS 有权
标题翻译：芳香酰胺化合物
公开(公告)号：US20100056517A1
公开(公告)日：2010-03-04
申请号：US12513835
申请日：2007-11-15
申请人： Jonathan Bayldon Baell , Guillaume Laurent Lessene , Brad Edmund Sleebs , Wayne J. Fairbrother , John A. Flygare , Michael F.T. Koeler
发明人： Jonathan Bayldon Baell , Guillaume Laurent Lessene , Brad Edmund Sleebs , Wayne J. Fairbrother , John A. Flygare , Michael F.T. Koeler
IPC分类号： A61K31/5377 , A61K31/496 , C07D413/14 , C07D239/86 , A61P35/00
CPC分类号： C07D239/94
摘要： The invention relates generally to small molecules that mimic the biological activity of certain peptides and proteins, to compositions containing them and to their use. In particular, the invention relates to compounds of the general formula (I) that mimic the biological activity of BH3-only proteins and are capable of binding to and neutralizing pro-survival Bcl-2 proteins: wherein A1, A2, B1, B2, B3, X, Z, R1, R2, R3 and t are as described herein. The invention also relates to processes of preparing the benzenesulfonamide compounds that mimic portions of peptides and proteins, and to the use of such compounds in the regulation of cell death and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death.
摘要翻译：本发明一般涉及模拟某些肽和蛋白质的生物学活性的小分子，含有它们的组合物及其用途。特别地，本发明涉及模拟仅含BH3蛋白的生物学活性的通式（I）的化合物，并能够结合并中和原生存Bcl-2蛋白：其中A1，A2，B1，B2， B3，X，Z，R1，R2，R3和t如本文所述。本发明还涉及制备模仿肽和蛋白质的一部分的苯磺酰胺化合物的方法，以及这些化合物在调节细胞死亡中的用途以及治疗和/或预防与细胞死亡调节相关的疾病或病症。

6. 发明申请

US20080207614A1 QUINAZOLINE DERIVATIVES FOR THE TREATMENT AND PREVENTION OF DIABETES AND OBESITY 审中-公开
标题翻译：用于治疗和预防糖尿病和肥胖的喹诺酮衍生物
公开(公告)号：US20080207614A1
公开(公告)日：2008-08-28
申请号：US11772098
申请日：2007-06-29
申请人： Nam Kyu Lee , Jun Won Lee , Sukho Lee , Guang-Jin Im , Hye Young Han , Tae Kon Kim , Yong Hyuk Kim , Wie-Jong Kwak , Sang Woong Kim , Joohun Ha , Eon Kyum Kim , Jung Kyu Lee , Choong Yeul Yoo , Dae Yeon Lee
发明人： Nam Kyu Lee , Jun Won Lee , Sukho Lee , Guang-Jin Im , Hye Young Han , Tae Kon Kim , Yong Hyuk Kim , Wie-Jong Kwak , Sang Woong Kim , Joohun Ha , Eon Kyum Kim , Jung Kyu Lee , Choong Yeul Yoo , Dae Yeon Lee
IPC分类号： A61K31/517 , A61P3/10 , C07D239/72 , C07D413/02 , C07D401/02 , C07D239/86 , A61P3/04
CPC分类号： C07D239/91 , C07D239/93 , C07D239/94 , C07D239/95 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to novel quinazoline derivatives effective in lowering blood glucose level and body weight, and a medicine for treatment and/or prevention of diabetes and/or obesity, which comprises the compound as an active ingredient.
摘要翻译：本发明涉及有效降低血糖水平和体重的新型喹唑啉衍生物，以及用于治疗和/或预防糖尿病和/或肥胖症的药物，其包含该化合物作为活性成分。

7. 发明授权

US5576322A Anti-ischemic 2,4-diaminoquinazolines 失效
标题翻译：抗缺血性2,4-二氨基喹唑啉
公开(公告)号：US5576322A
公开(公告)日：1996-11-19
申请号：US196110
申请日：1994-02-18
申请人： Yasutaka Takase , Nobuhisa Watanabe , Makoto Matsui , Hironori Ikuta , Teiji Kimura , Takao Saeki , Hideyuki Adachi , Tadakazu Tokumura , Hisatoshi Mochida , Yasunori Akita , Shigeru Souda
发明人： Yasutaka Takase , Nobuhisa Watanabe , Makoto Matsui , Hironori Ikuta , Teiji Kimura , Takao Saeki , Hideyuki Adachi , Tadakazu Tokumura , Hisatoshi Mochida , Yasunori Akita , Shigeru Souda
IPC分类号： C07D215/42 , A61K31/415 , A61K31/4184 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/454 , A61K31/4706 , A61K31/4709 , A61K31/496 , A61K31/505 , A61K31/517 , A61K31/519 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/06 , A61P37/00 , A61P43/00 , B60S1/16 , B60S1/24 , C07D215/48 , C07D235/06 , C07D235/08 , C07D239/78 , C07D239/84 , C07D239/86 , C07D239/88 , C07D239/90 , C07D239/94 , C07D239/95 , C07D239/96 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/12 , C07D471/04 , C07D491/04 , C07D491/056 , C07D521/00 , F16C7/02 , F16C11/04
CPC分类号： C07D235/06 , C07D215/42 , C07D231/12 , C07D233/56 , C07D239/84 , C07D239/86 , C07D239/88 , C07D239/94 , C07D239/95 , C07D239/96 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10 , C07D413/12 , C07D471/04 , C07D491/04
摘要： The invention is directed to certain 2,4-diaminoquinazoline compounds, their pharmaceutically acceptable salts, the pharmaceutical compositions comprising those compounds and their therapeutic methods of use. The compounds possess anti-ischemic activity.
摘要翻译： PCT No.PCT / JP92 / 01258 Sec。 371日期1994年2月18日 102（e）日期1994年2月18日PCT提交1992年9月30日PCT公布。出版物WO93 / 07124 日期1994年4月15日本发明涉及某些2,4-二氨基喹唑啉化合物，其药学上可接受的盐，包含那些化合物的药物组合物及其治疗方法。该化合物具有抗缺血活性。

8. 发明授权

US5401745A Quinazolinones substituted with phenoxyphenylacetic acid derivatives 失效
标题翻译：喹唑啉酮被苯氧基苯乙酸衍生物取代
公开(公告)号：US5401745A
公开(公告)日：1995-03-28
申请号：US33595
申请日：1993-03-19
申请人： Scott W. Bagley , Prasun K. Chakravarty , Anna Chen , Daljit S. Dhanoa , Kenneth J. Fitch , William J. Greenlee , Elizabeth M. Naylor , James R. Tata , Thomas F. Walsh , David L. Williams, Jr.
发明人： Scott W. Bagley , Prasun K. Chakravarty , Anna Chen , Daljit S. Dhanoa , Kenneth J. Fitch , William J. Greenlee , Elizabeth M. Naylor , James R. Tata , Thomas F. Walsh , David L. Williams, Jr.
IPC分类号： C07D239/91 , C07D405/12 , A61K31/505 , A61K31/54 , C07D239/86 , C07D239/95
CPC分类号： C07D405/12 , C07D239/91
摘要： Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebal and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.
摘要翻译：苯氧基苯基乙酸和一般结构式I的衍生物具有内皮素拮抗剂活性，因此可用于治疗心血管疾病，例如高血压，缺血性肾衰竭，血管痉挛，脑和心脏缺血，心肌梗死，炎性疾病，雷诺氏病，和内毒素性休克和哮喘。

9. 发明授权

US5373011A Substituted quinazoline fungicidal agents 失效
标题翻译：取代喹唑啉杀真菌剂
公开(公告)号：US5373011A
公开(公告)日：1994-12-13
申请号：US121825
申请日：1993-09-14
申请人： Gregory J. Haley
发明人： Gregory J. Haley
IPC分类号： A01N43/54 , A01N47/06 , A01N47/22 , C07D239/86 , C07D239/88 , C07D239/94 , A01N57/00 , A01N57/10 , A01N59/20
CPC分类号： C07D239/86 , A01N43/54 , A01N47/06 , A01N47/22 , C07D239/88 , C07D239/94
摘要： There are provided substituted quinazoline compounds of formula I ##STR1## and their use for the prevention, control or amelioration of diseases caused by phytopathogenic fungi. Further provided are compositions and methods comprising those compounds for the protection of plants from fungal infestations and diseases.
摘要翻译：提供式I的取代喹唑啉化合物（I）及其用于预防，控制或改善由植物病原真菌引起的疾病的用途。进一步提供的是包含用于保护植物免受真菌侵袭和疾病的化合物的组合物和方法。

10. 发明授权

US4147700A Triazolylbenzophenone derivatives and production thereof 失效
标题翻译：三唑基二苯甲酮衍生物及其制备
公开(公告)号：US4147700A
公开(公告)日：1979-04-03
申请号：US861011
申请日：1977-12-15
申请人： Kentaro Hirai , Toshio Fujishita , Teruyuki Ishiba , Hirohiko Sugimoto
发明人： Kentaro Hirai , Toshio Fujishita , Teruyuki Ishiba , Hirohiko Sugimoto
IPC分类号： A61K38/00 , C07D239/86 , C07D239/92 , C07D249/08 , C07K5/06 , C07K5/065 , C07D249/14
CPC分类号： C07D239/86 , C07D239/92 , C07D249/08 , C07K5/06026 , C07K5/06078 , A61K38/00 , Y10S514/906
摘要： Triazolylbenzophenone derivatives of the formula: ##STR1## (wherein R represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 halo-alkyl, the group --(CH.sub.2).sub.n --X--R.sup.5, or the group ##STR2## R.sup.5 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.6 -C.sub.10 aryl, or C.sub.2 -C.sub.8 acyl; X represents sulfur or oxygen; n represents 0, 1, 2, or 3; R.sup.6 and R.sup.7 each represents hydrogen or C.sub.1 -C.sub.6 alkyl; or the group ##STR3## represents pyrrolidino, piperidino, morpholino, or .gamma.-methylpiperazino; R.sup.1 represents hydrogen or halogen; R.sup.2 represents halogen, nitro, or trifluoromethyl; R.sup.3 represents C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 halo-alkyl, C.sub.1 -C.sub.6 azido-alkyl, C.sub.6 -C.sub.10 aryl, C.sub.2 -C.sub.8 acyl, or the group ##STR4## R.sup.4 and R.sup.8 each represents hydrogen, C.sub.1 -C.sub.6 alkyl, or C.sub.7 -C.sub.10 aralkyl; R.sup.9 represents hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.10 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.10 aralkyl, or C.sub.2 -C.sub.11 .alpha.-amino-acyl; or the group ##STR5## represents phthalimido, pyrrolidino, piperidino, morpholino, or .gamma.-methylpiperazino) and their pharmaceutically acceptable acid addition salts, useful as anxiolytics, sedatives, hypnotics, anticonvulsants, muscle relaxants, antidepressants, their synthetic intermediates, and their preparation.
摘要翻译：下式的三唑基二苯甲酮衍生物：其中R表示氢，C1-C6烷基，C1-C6卤代烷基，基团 - （CH2）nX-R5或基团R5表示氢，C1-C6 烷基，C 2 -C 6烯基，C 2 -C 6炔基，C 6 -C 10芳基或C 2 -C 8酰基; X表示硫或氧; n表示0,1,2或3; R 6和R 7各自表示氢或C 1 -C 6 烷基;或者“IMAGE”代表吡咯烷子基，哌啶子基，吗啉代或γ-甲基哌嗪基; R1代表氢或卤素; R2代表卤素，硝基或三氟甲基; R3代表C1-C6烷基，C1-C6卤代烷基，C1 -C 6叠氮基 - 烷基，C 6 -C 10芳基，C 2 -C 8酰基或者R 4和R 8各自表示氢，C 1 -C 6烷基或C 7 -C 10芳烷基; R 9表示氢或C 1 -C 6烷基; R 10 表示氢，C1-C6烷基，C7-C10芳烷基或C2-C11α-氨基酰基;或者“IMAGE”代表苯二甲酰亚氨基，吡咯烷子基，哌啶子基，吗啉代或γ-甲基哌嗪基）及其药学上可接受的酸加成盐，可用作抗焦虑剂，镇静剂，催眠药，抗惊厥药，肌肉松弛剂，抗抑郁药，其合成中间体及其制备。

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