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1. 发明申请

US20180354889A1 NEW PROCESS AND INTERMEDIATES 审中-公开
公开(公告)号：US20180354889A1
公开(公告)日：2018-12-13
申请号：US15780957
申请日：2016-12-08
申请人： Novartis AG
发明人： Florian Karl KLEINBECK-RINIKER , Benjamin MARTIN , Gerhard PENN , Francesco VENTURONI , Thierry SCHLAMA , Thomas RUCH , Thomas ALLMENDINGER , Bernhard WIETFELD , Paolo FILIPPONI
IPC分类号： C07C69/738 , C07C67/035 , C07C59/84 , C07C51/373 , C07C229/34 , C07C251/40 , C07C251/66 , C07C313/06
CPC分类号： C07C69/738 , C07B2200/07 , C07C51/373 , C07C59/84 , C07C67/035 , C07C229/34 , C07C251/40 , C07C251/66 , C07C313/06 , C07D207/36 , C07D265/02
摘要： The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril. It further relates to new intermediate compounds and their use for said new chemical synthesis route.

2. 发明授权

US09884802B2 Substituted aromatic compounds for the treatment pulmonary fibrosis, liver fibrosis, skin fibrosis and cardiac fibrosis 有权
公开(公告)号：US09884802B2
公开(公告)日：2018-02-06
申请号：US14775882
申请日：2014-03-14
申请人： PROMETIC BIOSCIENCES INC.
发明人： Lyne Gagnon , Pierre Laurin , Brigitte Grouix , Lilianne Geerts , François Sarra-Bournet , Martin Leduc , Shaun Abbott , Boulos Zacharie , Jean-François Bienvenu , Valérie Perron
IPC分类号： C07C57/30 , A61K31/192 , C07C59/52 , C07C57/58 , C07C57/42 , C07C57/60 , C07C59/84 , A61K31/4418 , A61K45/06
CPC分类号： C07C57/30 , A61K31/192 , A61K31/4418 , A61K45/06 , C07C57/42 , C07C57/58 , C07C57/60 , C07C59/52 , C07C59/84 , Y02A50/423
摘要： The present invention relates to substituted aromatic compounds for use in prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis and cardiac fibrosis, where the compound has the following formula: or a pharmaceutically acceptable salt thereof, wherein A is C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(O)—(CH2)n—CH3 or CH(OH)—(CH2)n—CH3 wherein n is 3 or 4; R1 is H, OH or F; R2 is H, OH, F or CH2—OH; R3 is H, OH, F or CH2Ph; R4 is H, OH or F; Q is 1) (CH2)mC(O)OH wherein m is 1 or 2, 2) CH(CH3)C(O)OH, 3) C(CH3)2C(O)OH, 4) CH(F)—C(O)OH, 5) CF2—C(O)OH, or 6) C(O)—C(O)OH.

3. 发明授权

US09529259B2 Radiation-sensitive resin composition, resist pattern-forming method, acid diffusion control agent, compound, and method for producing compound 有权
标题翻译：辐射敏感性树脂组合物，抗蚀剂图案形成法，酸扩散控制剂，化合物和化合物的制造方法
公开(公告)号：US09529259B2
公开(公告)日：2016-12-27
申请号：US14827795
申请日：2015-08-17
申请人： JSR CORPORATION
发明人： Hayato Namai
IPC分类号： G03F7/004 , G03F7/039 , G03F7/20 , G03F7/30 , G03F7/32 , C07C59/185 , C07C59/205 , C07C59/84 , C07C59/21 , C07C69/36 , C07C381/12 , C07D307/77 , C07D313/04 , C07D317/46 , C07D317/72 , C07D327/04 , C07D313/10 , C07D307/93 , C07D315/00 , C07C51/41 , C07C327/32 , C07C67/30 , C07C51/02 , C08F212/14 , G03F7/038 , C08F2/38 , C08F4/00 , C07C69/63 , C07C327/06 , C08F12/24
CPC分类号： G03F7/0045 , C07C51/02 , C07C51/41 , C07C59/185 , C07C59/205 , C07C59/21 , C07C59/84 , C07C67/30 , C07C69/36 , C07C69/63 , C07C327/06 , C07C327/32 , C07C381/12 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2603/74 , C07D307/77 , C07D307/93 , C07D313/04 , C07D313/10 , C07D315/00 , C07D317/46 , C07D317/72 , C07D327/04 , C08F2/38 , C08F4/00 , C08F12/24 , C08F212/14 , G03F7/004 , G03F7/0046 , G03F7/038 , G03F7/039 , G03F7/0397 , G03F7/2041 , G03F7/30 , G03F7/322 , G03F7/325 , C07C319/20 , C07C323/52
摘要： A radiation-sensitive resin composition includes a polymer including a structural unit that includes an acid-labile group; and a compound represented by formula (1). R1 represents a monovalent organic group having 1 to 30 carbon atoms. L represents a single bond, an oxygen atom or a sulfur atom. M+ represents a monovalent radioactive ray-labile onium cation. The monovalent organic group represented by R1 is preferably a monovalent hydrocarbon group or a monovalent fluorinated hydrocarbon group, and L preferably represents a single bond. The monovalent organic group represented by R1 is preferably a monovalent hydrocarbon group, a monovalent fluorinated hydrocarbon group, a monovalent aliphatic heterocyclic group or a monovalent fluorinated aliphatic heterocyclic group, and L preferably represents an oxygen atom or a sulfur atom. The monovalent radioactive ray-labile onium cation represented by M+ is preferably represented by the formula (X).
摘要翻译：辐射敏感性树脂组合物包括含有酸不稳定基团的结构单元的聚合物; 和由式（1）表示的化合物。 R1表示碳原子数为1〜30的一价有机基团。 L表示单键，氧原子或硫原子。 M +代表一价放射性不稳定鎓阳离子。由R1表示的一价有机基团优选为一价烃基或一价氟化烃基，L优选表示单键。由R1表示的一价有机基团优选为一价烃基，一价氟化烃基，一价脂族杂环基或一价含氟脂族杂环基，L优选表示氧原子或硫原子。由M +表示的单价放射线不稳定鎓阳离子优选由式（X）表示。

4. 发明授权

US09439882B2 Compounds and compositions for the treatment of cancer 有权
公开(公告)号：US09439882B2
公开(公告)日：2016-09-13
申请号：US14797957
申请日：2015-07-13
申请人： PROMETIC BIOSCIENCES, INC.
发明人： Lyne Gagnon , Brigitte Grouix , Lilianne Geerts , Pierre Laurin , Christopher Penney , Boulos Zacharie
IPC分类号： A01N27/00 , A61K31/015 , A61K31/192 , A61K31/196 , A61K31/22 , A61K31/513 , A61K31/675 , A61K31/7068 , C07C57/46 , C07C57/48 , C07C59/54 , C07C59/84 , C07C62/20 , C07C229/18 , C07C229/42 , C07C323/52
CPC分类号： A61K31/192 , A61K31/196 , A61K31/22 , A61K31/513 , A61K31/675 , A61K31/7068 , C07C57/46 , C07C57/48 , C07C59/54 , C07C59/84 , C07C62/20 , C07C229/18 , C07C229/42 , C07C323/52
摘要： New uses for phenylketone carboxylate compounds and substituted aromatic compounds of Formula I, Formula I.1, Formula I.2, Formula IA, Formula IB, Formula IC and Formula II and their pharmaceutical acceptable salts for the treatment of cancer. The use of a combination of two of these compounds is described and the use of the combination of one of these compounds with an anticancer agent such as decarbazine, doxorubicin, daunorubicin, cyclophosphamide, busulfex, busulfan, vinblastine, vincristine, bleomycin, etoposide, topotecan, irinotecan, taxotere, taxol, 5-fluorouracil, methotrexate, gemcitabine, cisplatin, carboplatin and chlorambucil.

5. 发明申请

US20160122292A1 BASE GENERATOR, BASE-REACTIVE COMPOSITION CONTAINING SAID BASE GENERATOR, AND BASE GENERATION METHOD 审中-公开
标题翻译：基站发生器，含有基站发生器的基板反应组合物和基站生成方法
公开(公告)号：US20160122292A1
公开(公告)日：2016-05-05
申请号：US14901525
申请日：2014-06-25
申请人： WAKO PURE CHEMICAL INDUSTRIES, LTD. , TOKYO UNIVERSITY OF SCIENCE FOUNDATION
发明人： Nobuhiko SAKAI , Kosuke YANABA , Koji ARIMITSU
IPC分类号： C07C279/26 , G03F7/004 , C07C65/28 , C07D209/48 , C07C59/84 , C07D311/86
CPC分类号： C07C279/26 , B01J19/123 , B01J19/127 , B01J19/128 , C07C59/84 , C07C65/28 , C07C2601/14 , C07C2603/24 , C07D209/48 , C07D311/86 , G03F7/0045
摘要： It is a subject of the present invention to provide a base generator which has high solubility to general-purpose organic solvents, can dissolve directly into a base-reactive compound, such as an epoxy-based compound, further is provided with both performance of high heat resistance and low nucleophilicity, and generates a strong base, a base-reactive composition comprising the base generator and a base-reactive compound, as well as a method for generating a base, etc.The present invention relates to a compound represented by the general formula (A), a base generator comprising the compound, a base-reactive composition which comprises the base generator and a base-reactive compound, as well as a method for generating a base, etc. (wherein R1 to R5 each independently represent a hydrogen atom; an alkyl group; an aryl group which may have a substituent; or an arylalkyl group which may have a substituent, R6 represents a hydrogen atom; an alkyl group which may have a substituent; an alkenyl group; an alkynyl group; an aryl group which may have a substituent; or an arylalkyl group which may have a substituent, R7 represents a hydrogen atom; an alkyl group which may have an amino group; an aryl group which may have a substituent; or an arylalkyl group which may have a substituent, and Z− represents an anion derived from a carboxylic acid having a specific structure.)
摘要翻译：本发明的主题是提供一种对通用有机溶剂具有高溶解度的碱发生剂，可以直接溶解在诸如环氧基化合物的碱反应性化合物中，还具有高的性能耐碱性和低亲核性，并且产生强碱，包含碱产生剂和碱反应性化合物的碱反应性组合物，以及产生碱的方法等。本发明涉及由通式（A），包含该化合物的碱发生剂，包含碱发生剂和碱反应性化合物的碱反应性组合物，以及产生碱的方法等（其中R 1至R 5各自独立地表示氢原子;烷基;可具有取代基的芳基;或可具有取代基的芳烷基，R6表示氢原子;可具有取代基的烷基;可具有取代基的烷基甲基炔基; 可以具有取代基的芳基; 或可具有取代基的芳基烷基，R7表示氢原子; 可以具有氨基的烷基; 可以具有取代基的芳基; 或可以具有取代基的芳烷基，Z-表示衍生自具有特定结构的羧酸的阴离子。）

6. 发明授权

US09321775B2 Compositions and methods for the treatment of moderate to severe pain 有权
标题翻译：用于治疗中度至重度疼痛的组合物和方法
公开(公告)号：US09321775B2
公开(公告)日：2016-04-26
申请号：US14399183
申请日：2013-02-04
申请人： Mahesh Kandula
发明人： Mahesh Kandula
IPC分类号： C07D487/04 , C07D333/24 , C07C59/84 , C07C69/738 , C07C59/76 , C07C51/56 , A61K31/215 , A61K31/385 , A61K31/407 , A61K31/192 , A61K31/194 , A61K31/198 , A61K31/202 , A61K31/235
CPC分类号： C07D487/04 , A61K31/192 , A61K31/194 , A61K31/198 , A61K31/202 , A61K31/215 , A61K31/235 , A61K31/385 , A61K31/407 , C07C51/56 , C07C59/76 , C07C59/84 , C07C69/738 , C07D333/24
摘要： The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II, and methods for treating or preventing or modulating moderate to severe pain in a disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of pain, severe pain, chronic pain, chemotherapy induced pain, epilepsy, glaucoma, arthritis, tooth aches, inflammation, musculoskeletal pain, sciatica, radiculopathy pain, migraine, neuropathic pain, post herpetic neuralgia, neuralgia pain, multiple sclerosis, multiple sclerosis, restless legs syndrome (RLS), cluster headache, depression, fibromyalgia, amyotrophic lateral sclerosis (ALS), convulsions, partial seizures, mood-stabilizing agent and bipolar disorder.
摘要翻译：本发明涉及式I和式II化合物或其药学上可接受的盐，以及多晶型物，溶剂合物，对映体，立体异构体和水合物。包含有效量的式I或式II化合物的药物组合物，以及用于治疗或预防或调节疾病中至重度疼痛的方法可以配制用于口服，口腔，直肠，局部，透皮，经粘膜，静脉内，肠胃外给药，糖浆或注射。此类组合物可用于治疗疼痛，剧烈疼痛，慢性疼痛，化学疗法诱导的疼痛，癫痫，青光眼，关节炎，牙齿酸痛，炎症，肌肉骨骼疼痛，坐骨神经痛，神经根痛，偏头痛，神经性疼痛，疱疹后神经痛，神经痛，多发性硬化症，多发性硬化症，不宁腿综合征（RLS），丛集性头痛，抑郁症，纤维肌痛，肌萎缩性侧索硬化（ALS），抽搐，部分发作，情绪稳定剂和双相障碍。

7. 发明申请

US20140323535A1 5-OXO-ETE RECEPTOR ANTAGONIST COMPOUNDS 有权
标题翻译： 5-OXO-ETE受体拮抗剂化合物
公开(公告)号：US20140323535A1
公开(公告)日：2014-10-30
申请号：US14324579
申请日：2014-07-07
申请人： THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING/MCGILL UNIVERSITY , FLORIDA INSTITUTE OF TECHNOLOGY
发明人： William S. POWELL , Joshua ROKACH
IPC分类号： C07D403/06 , C07D209/18 , C07D209/08
CPC分类号： C07D209/18 , C07C59/84 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/24 , C07D215/12 , C07D235/08 , C07D307/79 , C07D403/06
摘要： The present invention relates to novel pharmaceutically-useful compounds which are antagonists of the 5-oxo-ETE receptors, such as the OXE receptor. These compounds have use as therapeutic and/or prophylactic agents for diseases characterized by tissue eosinophilia, such as inflammatory conditions including respiratory diseases. The invention also relates to pharmaceutical compositions, to the use of such compounds and compositions as medicaments, and to therapeutic methods.
摘要翻译：本发明涉及作为5-氧代-ETE受体（如OXE受体）的拮抗剂的新颖的药学上有用的化合物。这些化合物可用作用于组织嗜酸性粒细胞增多症，特别是包括呼吸系统疾病在内的炎性疾病的疾病的治疗和/或预防剂。本发明还涉及药物组合物，使用这些化合物和组合物作为药物，以及治疗方法。

8. 发明授权

US08604114B2 Aromatic acylation with cyclic anhydride for plasticizer production 有权
标题翻译：用环状酸酐进行芳香族酰化，用于增塑剂生产
公开(公告)号：US08604114B2
公开(公告)日：2013-12-10
申请号：US12840715
申请日：2010-07-21
申请人： Jihad Mohammed Dakka , Edmund John Mozeleski , Lisa Saunders Baugh , Karla Schall Colle , Allen David Godwin , Diana S. Smirnova , Jörg Friedrich Wilhelm Weber , Stephen Zushma
发明人： Jihad Mohammed Dakka , Edmund John Mozeleski , Lisa Saunders Baugh , Karla Schall Colle , Allen David Godwin , Diana S. Smirnova , Jörg Friedrich Wilhelm Weber , Stephen Zushma
IPC分类号： C08G73/10 , C08K5/00 , C07C69/76
CPC分类号： C08K5/12 , C07C51/31 , C07C67/08 , C07C67/31 , C07C69/73 , C07C69/732 , C07C69/738 , C07C2602/10 , C08K5/10 , C07C59/84 , C07C59/86
摘要： Provided is a process for making non-phthalate plasticizers, by acylating an aromatic compound with a succinic anhydride to form a keto-acid, and then esterifying the keto-acid with C4-C13 OXO-alcohols to form a plasticizer compound. The aromatic rings of the aromatic compound may also be optionally hydrogenated.
摘要翻译：提供了制备非邻苯二甲酸酯增塑剂的方法，通过用琥珀酸酐酰化芳族化合物以形成酮酸，然后用C4-C13OXO-醇酯化酮酸以形成增塑剂化合物。芳族化合物的芳环也可以任选氢化。

9. 发明申请

US20110160371A1 AROMATIC ACYLATION WITH CYCLIC ANHYDRIDE FOR PLASTICIZER PRODUCTION 有权
标题翻译：用于增塑剂生产的环状非离子表面活性剂
公开(公告)号：US20110160371A1
公开(公告)日：2011-06-30
申请号：US12840715
申请日：2010-07-21
申请人： Jihad Mohammed DAKKA , Edmund John Mozeleski , Lisa Saunders Baugh , Karla Schall Colle , Allen David Godwin , Diana S. Smimova , Jorg Friedrich Wilhelm Weber , Stephen Zushma
发明人： Jihad Mohammed DAKKA , Edmund John Mozeleski , Lisa Saunders Baugh , Karla Schall Colle , Allen David Godwin , Diana S. Smimova , Jorg Friedrich Wilhelm Weber , Stephen Zushma
IPC分类号： C08K5/07 , C07C69/616 , C07C69/612
CPC分类号： C08K5/12 , C07C51/31 , C07C67/08 , C07C67/31 , C07C69/73 , C07C69/732 , C07C69/738 , C07C2602/10 , C08K5/10 , C07C59/84 , C07C59/86
摘要： Provided is a process for making non-phthalate plasticizers, by acylating an aromatic compound with a succinic anhydride to form a keto-acid, and then esterifying the keto-acid with C4-C13 OXO-alcohols to form a plasticizer compound. The aromatic rings of the aromatic compound may also be optionally hydrogenated.
摘要翻译：提供了制备非邻苯二甲酸酯增塑剂的方法，通过用琥珀酸酐酰化芳族化合物以形成酮酸，然后用C4-C13OXO-醇酯化酮酸以形成增塑剂化合物。芳族化合物的芳环也可以任选氢化。

10. 发明授权

US07799954B2 Dicarbonyl derivatives and methods of use 有权
标题翻译：二羰基衍生物和使用方法
公开(公告)号：US07799954B2
公开(公告)日：2010-09-21
申请号：US11939909
申请日：2007-11-14
申请人： Chunlin Tao , Qinwei Wang , Vuong Trieu , Neil Desai , Patrick Soon-Shiong
发明人： Chunlin Tao , Qinwei Wang , Vuong Trieu , Neil Desai , Patrick Soon-Shiong
IPC分类号： C07C49/15 , A61K31/12
CPC分类号： C07C69/738 , C07C49/203 , C07C49/217 , C07C49/223 , C07C49/235 , C07C49/255 , C07C49/553 , C07C49/613 , C07C49/657 , C07C49/67 , C07C49/683 , C07C49/697 , C07C49/747 , C07C49/753 , C07C49/755 , C07C49/784 , C07C59/84 , C07C59/90 , C07C225/22 , C07C233/15 , C07C235/78 , C07C251/40 , C07C251/44 , C07C2601/16 , C07D209/34 , C07D213/74 , C07D261/18 , C07D295/185 , C07D307/33 , C07D311/22 , C07D317/54
摘要： Derivatives of dicarbonyl compounds having antitumor and antibiotic activity which can be used as anticancer agents.
摘要翻译：可用作抗癌剂的具有抗肿瘤和抗生素活性的二羰基化合物的衍生物。

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