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1. 发明授权

US07511041B2 Fused azole-pyrimidine derivatives 有权
标题翻译：熔融唑 - 嘧啶衍生物
公开(公告)号：US07511041B2
公开(公告)日：2009-03-31
申请号：US10527376
申请日：2003-09-18
申请人： Mitsuyuki Shimada , Toshiki Murata , Kinji Fuchikami , Hideki Tsujishita , Naoki Omori , Issei Kato , Mami Miura , Klaus Urbahns , Florian Gantner , Kevin Bacon
发明人： Mitsuyuki Shimada , Toshiki Murata , Kinji Fuchikami , Hideki Tsujishita , Naoki Omori , Issei Kato , Mami Miura , Klaus Urbahns , Florian Gantner , Kevin Bacon
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D237/26 , C07D237/36 , C07D241/36 , C07D239/00 , C07D471/00 , C07D471/04 , C07D401/04 , C07D401/22 , C07D487/00 , C07D487/04 , C07D491/00 , C07D495/00 , C07D497/00
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention relates to hovel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoixnmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis. The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.
摘要翻译：本发明涉及霍夫唑唑吡啶衍生物，其制备方法和含有它们的药物制剂。本发明的稠合吡唑嘧啶衍生物对于磷脂酰肌醇-3-激酶（PI3K）抑制的效力显着增强，特别是对于PI3K-γ抑制，可用于预防和治疗与PI3K相关的疾病，特别是PI3K-γ活性。更具体地说，本发明的唑类衍生物可用于治疗和预防以下疾病：炎性和免疫调节性疾病，如哮喘，特应性皮炎，鼻炎，过敏性疾病，慢性阻塞性肺病（COPD），脓毒性休克，关节疾病，自身免疫性疾病如类风湿性关节炎，格雷夫斯病，癌症，心肌收缩性疾病，心力衰竭，血栓栓塞，缺血和动脉粥样硬化。本发明的化合物还可用于肺动脉高压，肾衰竭，心脏肥大，以及神经变性疾病如帕金森病，阿尔茨海默病，糖尿病和局灶性缺血，因为这些疾病还涉及人或动物中的PI3K活性学科。

2. 发明授权

US07501418B2 Fused heterocyclic isoxazoline derivatives and their use as anti-depressants 有权
标题翻译：稠合杂环异恶唑啉衍生物及其作为抗抑郁剂的用途
公开(公告)号：US07501418B2
公开(公告)日：2009-03-10
申请号：US10524123
申请日：2003-08-13
申请人： José Ignacio Andrés-Gil , Manuel Jesús Alcázar-Vaca , José Manuel Bartolomé -Nebreda , Francisco Javier Fernández-Gadea , Margaretha Henrica Maria Bakker , Antonius Adrianus Hendrikus Megens
发明人： José Ignacio Andrés-Gil , Manuel Jesús Alcázar-Vaca , José Manuel Bartolomé -Nebreda , Francisco Javier Fernández-Gadea , Margaretha Henrica Maria Bakker , Antonius Adrianus Hendrikus Megens
IPC分类号： A01N43/54 , A01N43/40 , A61K31/445 , A61K31/497 , C07D211/32 , C07D211/68 , C07D211/80 , C07D213/02 , C07D261/20 , C07D239/00 , C07D237/26 , C07D237/36 , C07D413/00 , C07D417/00 , C07D419/00 , C07D471/00 , C07D487/00 , C07D491/00 , C07D495/00 , C07D497/00
CPC分类号： C07D498/14
摘要： The invention concerns fused heterocyclic isoxazoline derivatives of Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular, tetrahydropyranoisoxazole, hexahydroisoxazolopyridine, tetrahydrothiopyrano isoxazole and hexahydrobenzoisoxazole derivatives fused to a heterocyclic ring system via the 6-membered ring of the bicyclic moiety as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherein the variables are defined as in Claim 1. The compounds have surprisingly been shown to have selective serotonine (5-HT) reuptake inhibitor activity as well as α2-adrenoceptor antagonist activity, compounds according to the invention are also suitable for treatment and/or prophylaxis in diseases where either one of the activities alone or the combination of said activities may be of therapeutic use.
摘要翻译：本发明涉及式（I）的稠合杂环异恶唑啉衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构体形式及其N-氧化物形式，更特别是四氢吡喃异恶唑，六氢异恶唑并吡啶，四氢噻喃异恶唑和六氢苯并异恶唑衍生物通过双环部分的6元环以及其制备方法，包含它们的药物组合物及其作为药物的用途，特别是用于治疗抑郁症，焦虑症，运动障碍，精神病，帕金森病和包括神经性厌食症和贪食症的体重紊乱，其中变量如权利要求1中所定义。化合物惊奇地显示具有选择性5-羟色胺（5-HT）再摄取抑制剂活性以及α2-肾上腺素受体拮抗剂活性，根据发明也适用于f 或治疗和/或预防疾病，其中单独的一种活性或所述活性的组合可能具有治疗用途。

3. 发明授权

US07220857B2 Azo dye compound 有权
标题翻译：偶氮染料化合物
公开(公告)号：US07220857B2
公开(公告)日：2007-05-22
申请号：US11280345
申请日：2005-11-17
申请人： Katsumi Kobayashi , Yasuhiro Ishiwata , Kiyoshi Takeuchi
发明人： Katsumi Kobayashi , Yasuhiro Ishiwata , Kiyoshi Takeuchi
IPC分类号： C09B17/00 , C07D237/36 , C07D513/04 , C07D487/04 , C07D471/12
CPC分类号： C07D471/04 , C07D237/36 , C07D471/14 , C07D487/04 , C07D513/04 , C09B37/00
摘要： A compound represented by formula (I):Formula (I) wherein Z1 and Z2 each are atoms necessary for forming an aromatic ring; V1 and V2 each are a substituent W1 or W2; when at least one V1 is W1, at least one V2 is W2, or when at least one V1 is W2, at least one V2 is W1; r is 1 to 4; s is 1 to 4; M1 is a counter ion; m1 is the number necessary for neutralizing charge; W1 is a hydroxyl, primary- or secondary- or tertiary-amino, acylamino, or sulfonamido group; W2 is a nitro, cyano, alkoxycarbonyl, aryloxycarbonyl, alkyl- or aryl-sulfonyl, carbamoyl, sulfamoyl, alkenyl, alkynyl, aryl, heterocyclic, sulfo, carboxyl, heterocyclic oxy, ammonio, alkyl- or aryl-sulfinyl, alkyl- or aryl-sulfonyl, acyl, or aryl- or heterocyclic-azo group; and the aromatic ring may have a substituent other than V1 and V2.
摘要翻译：式（I）表示的化合物：式（I）其中Z 1和Z 2各自为形成芳环所必需的原子; V 1和V 2各自为取代基W 1或W 2; 当至少一个V 1是W 1时，至少一个V 2是W 2 2，或者当在至少一个V 1是W 2，至少一个V 2是W 1; r为1〜4; s是1到4; M 1是抗衡离子; m 1 是中和电荷所需的数量; W 1是羟基，伯或仲或叔氨基，酰氨基或亚磺酰氨基; W 2是硝基，氰基，烷氧基羰基，芳氧基羰基，烷基 - 或芳基 - 磺酰基，氨基甲酰基，氨磺酰基，烯基，炔基，芳基，杂环，磺基，羧基，杂环氧基，氨基，烷基 - 或芳基 - 亚磺酰基，烷基 - 或芳基 - 磺酰基，酰基或芳基 - 或杂环 - 偶氮基; 芳环可以具有除V 1和V 2以外的取代基。

4. 发明授权

US5631254A Dihydropyridazinones, pyridazinones and related compounds as fungicides 失效
标题翻译：二氢哒嗪酮，哒嗪酮和相关化合物作为杀真菌剂
公开(公告)号：US5631254A
公开(公告)日：1997-05-20
申请号：US467384
申请日：1995-06-06
申请人： Enrique L. Michelotti , Anne R. Egan , Ronald Ross, Jr. , Willie J. Wilson
发明人： Enrique L. Michelotti , Anne R. Egan , Ronald Ross, Jr. , Willie J. Wilson
IPC分类号： A01N43/40 , A01N43/42 , A01N43/54 , A01N43/58 , A01N43/60 , A01N43/62 , A01N43/653 , A01N43/72 , A01N43/80 , A01N43/82 , A01N43/88 , B27K3/34 , C07D213/64 , C07D213/85 , C07D215/22 , C07D215/227 , C07D237/04 , C07D237/14 , C07D237/18 , C07D237/26 , C07D237/32 , C07D237/36 , C07D239/36 , C07D243/02 , C07D243/04 , C07D273/04 , C07D285/34 , C07D401/04 , C07D403/04 , C07D405/06 , C07D405/10 , C07D407/06 , C07D409/04 , C07D409/06 , C07D413/06 , C07D521/00 , C07F7/08 , A61K31/50 , C07D295/03
CPC分类号： A01N43/40 , A01N43/42 , A01N43/54 , A01N43/58 , A01N43/60 , A01N43/62 , A01N43/653 , A01N43/80 , A01N43/82 , A01N43/88 , C07D213/64 , C07D213/85 , C07D215/227 , C07D231/12 , C07D233/56 , C07D237/04 , C07D237/18 , C07D237/26 , C07D237/32 , C07D237/36 , C07D239/36 , C07D243/02 , C07D249/08 , C07D273/04 , C07D285/34 , C07D401/04 , C07D403/04 , C07D405/06 , C07D405/10 , C07D409/04 , C07D409/06 , C07D413/06 , C07F7/0812
摘要： This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.
摘要翻译：本发明涉及下式的取代二氢哒嗪酮，哒嗪酮和相关化合物，其中A，Q，D和R 1如含有这些化合物的组合物和控制农业和哺乳动物真菌疾病的方法。

5. 发明授权

US5045541A Fused pyridazine compounds and their pharmaceutical use 失效
标题翻译：稠合哒嗪化合物及其药物用途
公开(公告)号：US5045541A
公开(公告)日：1991-09-03
申请号：US391603
申请日：1989-07-02
申请人： Toru Nakao , Minoru Kawakami , Masao Hisadome , Tetsuya Tahara
发明人： Toru Nakao , Minoru Kawakami , Masao Hisadome , Tetsuya Tahara
IPC分类号： A61K31/50 , A61K31/502 , A61K31/535 , A61P7/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/04 , C07D237/36 , C07D401/04 , C07D405/12 , C07D491/04 , C07D491/052 , C07D495/04
CPC分类号： C07D401/04 , C07D237/36 , C07D491/04 , C07D495/04
摘要： Fused pyridazine compounds ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and respectively hydrogen, a halogen, hydroxy, nitro, amino, cyano, trifluoromethyl, and alkyl, an alkoxy or an alkanoylamino; one of R.sub.a and R.sub.b is a group of the formula--O--Y--NR.sup.5 R.sup.6wherein R.sup.5 and R.sup.6 are the same or different and respectively hydrogen, an alkyl, a phenylalkyl or a substituted phenylalkyl or a group forming a heterocycle together with the adjacent nitrogen atom and Y stands for a straight- or branched-chain alkylene which may have hydroxy group as a substituent on the chain, and the other is hydrogen, or both of R.sub.a and R.sub.b are the same or different and respectively a group of the formula--O--Y--NR.sup.5 R.sup.6wherein R.sup.5 and R.sup.6 are of the same meanings as defined above; W is .dbd.CH-- or .dbd.N; X is CH.sub.2, S, SO, SO.sub.2 or O; and the bond designated by a broken line in its part stands for a single bond or a double bond, or their pharmaceutically acceptable salts or hydrates and their pharmaceutical use.Said compounds possess stimulating effects on phagocytosis of leukocytes and macrophages, restorative effects on leukopenia, protective effects against infection, antitumor actions and the like and thus they are useable for the prophylaxis or therapy of human diseases accompanied by immunodeficiency.

6. 发明授权

US4075074A Method for preparing benzo[C]cinnoline and its derivatives 失效
标题翻译：制备苯并{8 C {9噌啉及其衍生物的方法
公开(公告)号：US4075074A
公开(公告)日：1978-02-21
申请号：US777419
申请日：1977-03-14
申请人： Akira Yabe
发明人： Akira Yabe
IPC分类号： C07D237/26 , C07D237/36 , C07D471/04 , B01J1/10
CPC分类号： C07D237/36 , C07D237/26 , C07D471/04 , Y10S204/912 , Y10S204/914
摘要： Benzo[C]cinnoline or its derivative is prepared by irradiating 2,2'-diazidobiphenyl or its derivative with light in a low-temperature rigid solvent.
摘要翻译：苯并[C]噌啉或其衍生物通过在低温刚性溶剂中用光照射2,2'-二叠氮基联苯或其衍生物来制备。

7. 发明授权

US09096536B2 Asymmetrically substituted anthrapyridazone derivatives as cytostatics 有权
标题翻译：不对称取代的蒽代哒嗪衍生物作为细胞抑制剂
公开(公告)号：US09096536B2
公开(公告)日：2015-08-04
申请号：US14111022
申请日：2012-04-13
申请人： Edward Borowski , Barbara Stefanska , Maria Dzieduszycka , Marcin Cybulski , Wieslaw Szelejewski , Janusz Obukowicz , Maria Bontemps-Gracz , Malgorzata Wysocka , Jan Mazerski , Pawel Punda , Joanna Wietrzyk
发明人： Edward Borowski , Barbara Stefanska , Maria Dzieduszycka , Marcin Cybulski , Wieslaw Szelejewski , Janusz Obukowicz , Maria Bontemps-Gracz , Malgorzata Wysocka , Jan Mazerski , Pawel Punda , Joanna Wietrzyk
IPC分类号： C07D237/26 , C07D487/06 , A61K31/502 , A61K31/5025 , C07D237/36
CPC分类号： C07D237/26 , A61K31/502 , A61K31/5025 , C07D237/36 , C07D487/06
摘要： The invention relates to the new, asymmetrically substituted derivatives of 2,7-dihydro-3H-dibenzo[de,h]cinnoline-3,7-dione and their use as cytostatics exhibiting activity against tumor cells, especially against cells with multidrug resistance (MDR). In particular, the invention concerns derivatives of 2,7-dihydro-3H-dibenzo[de,h]cinnoline-3,7-dione represented by the general formula (I).
摘要翻译：本发明涉及2,7-二氢-3H-二苯并[de，h]噌啉-3,7-二酮的新的不对称取代的衍生物及其作为细胞抑制剂的用途，其表现出对肿瘤细胞的活性，特别是抗多药耐药性细胞 MDR）。特别地，本发明涉及由通式（I）表示的2,7-二氢-3H-二苯并[de，h]噌啉-3,7-二酮的衍生物。

8. 发明授权

US08486946B2 Pyrazolo [4,3-c] cinnolin-3-one M1 receptor positive allosteric modulators 有权
标题翻译：吡唑并[4,3-c]噌啉-3-酮M1受体阳性变构调节剂
公开(公告)号：US08486946B2
公开(公告)日：2013-07-16
申请号：US13201575
申请日：2010-02-12
申请人： Douglas C. Beshore , Scott D. Kuduk
发明人： Douglas C. Beshore , Scott D. Kuduk
IPC分类号： A61K31/50 , C07D237/36
CPC分类号： A61K31/495 , C07D487/04
摘要： The present invention is directed to pyrazolo[4,3-c]cinnolin-3-one compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
摘要翻译：本发明涉及作为M1受体阳性变构调节剂的式（I）的吡唑并[4,3-c]噌啉-3-酮化合物，其可用于治疗涉及M1受体的疾病，例如如阿尔茨海默病，精神分裂症，疼痛或睡眠障碍。本发明还涉及包含该化合物的药物组合物，以及该化合物和组合物在治疗由M1受体介导的疾病中的用途。

9. 发明授权

US08163755B2 Hexahydrooxazinopterine compounds 有权
标题翻译：六氢恶嗪蝶啶化合物
公开(公告)号：US08163755B2
公开(公告)日：2012-04-24
申请号：US12869452
申请日：2010-08-26
申请人： Bohan Jin , Nicholas Scorah , Qing Dong
发明人： Bohan Jin , Nicholas Scorah , Qing Dong
IPC分类号： A61K31/497 , C07D237/36
CPC分类号： C07D498/14
摘要： The present invention provides mTOR inhibitors of the formula wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods of making the compounds and intermediates thereof; and methods of using the compounds.
摘要翻译：本发明提供下式的mTOR抑制剂，其中变量如本文所定义。还提供了包含这些化合物的药物组合物，试剂盒和制品; 制备化合物及其中间体的方法; 和使用该化合物的方法。

10. 发明授权

US07737272B2 Diazaphosphacycle transition metal complexes 有权
标题翻译：二氮磷环过渡金属络合物
公开(公告)号：US07737272B2
公开(公告)日：2010-06-15
申请号：US12032350
申请日：2008-02-15
申请人： Clark R. Landis , Wiechang Jin , Jonathan S. Owen , Thomas P. Clark
发明人： Clark R. Landis , Wiechang Jin , Jonathan S. Owen , Thomas P. Clark
IPC分类号： C07D487/00 , C07D243/00 , C07D255/00 , C07D257/00 , C07D259/00 , C07D487/22 , C07D491/00 , C07D498/00 , C07D237/26 , C07D237/28 , C07D237/36 , C07D293/00 , C07D421/00 , C07D517/00 , C07F3/12
CPC分类号： C07F15/006 , C07F9/6584 , C07F15/0073 , C07F15/008 , C07F15/0086
摘要： Transition metal complexes include a diazaphosphacycle of formula III and a transition metal. The phosphorus atom of the diazaphosphacycle is bonded to the transition metal and the diazaphosphacycle of formula III has the following structure where the variables have the values set forth herein.
摘要翻译：过渡金属络合物包括式III的二氮杂磷酰基和过渡金属。二氮磷杂环磷的磷原子与过渡金属键合，式Ⅲ的二氮磷酰基具有以下结构，其中变量具有本文所述的值。

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