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1. 发明申请

US20170334878A1 SYNTHESIS OF 6-ARYL-4-AMINOPICOLINATES AND 2-ARYL-6-AMINOPYRIMIDINE-4-CARBOXYLATES BY DIRECT SUZUKI COUPLING 审中-公开
公开(公告)号：US20170334878A1
公开(公告)日：2017-11-23
申请号：US15599716
申请日：2017-05-19
申请人： Dow AgroSciences LLC
发明人： Jason S. Fisk , Xiaoyong Li , Mark Muehlfeld , Robert S. Bauman , Jossian Oppenheimer , Siyu Tu , Mark A. Nitz , Reetam Chakrabarti , Shawn D. Feist , James W. Ringer , Ronald B. Leng
IPC分类号： C07D401/04 , C07D239/28 , C07D213/90 , B01J35/00 , C07D213/79 , C07D239/32 , C07D239/02
CPC分类号： C07D401/04 , B01J31/00 , B01J35/0046 , B01J2231/4211 , C07D213/79 , C07D213/90 , C07D239/02 , C07D239/28 , C07D239/32
摘要： Improved methods of synthesizing 6-aryl-4-aminopicolinates, such as arylalky and alkyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylates and arylalkyl and alkyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylates, are described herein. The improved methods include a direct Suzuki coupling step, which eliminates the protection/de-protection steps in the current chemical process, and therefore eliminates or reduces various raw materials, equipment and cycle time as well as modification of other process conditions including use of crude AP, use of ABA-diMe, and varying pH, catalyst concentration, solvent composition, and/or workup procedures. This invention was expanded to include synthesis of 2-aryl-6-aminopyrimidine-4-carboxylates.

2. 发明授权

US09556129B2 Phosphatidylcholine transfer protein inhibitors 有权
标题翻译：磷脂酰胆碱转移蛋白抑制剂
公开(公告)号：US09556129B2
公开(公告)日：2017-01-31
申请号：US14812657
申请日：2015-07-29
申请人： The Brigham and Women's Hospital, Inc.
发明人： David Cohen , Neil Wagle , Gregory D. Cuny , Jun Xian , Marcie Glicksman , Ross L. Stein , Ekaterina Y. Shishova
IPC分类号： C07D213/72 , A61K31/44 , A61P1/16 , A61P3/04 , A61P3/10 , A61P9/10 , A61P11/06 , C07D239/69 , C07D239/42 , C07D213/76 , C07C311/21 , C07D213/89 , C07D217/22 , A61K31/505 , C07D213/60 , C07D239/32
CPC分类号： C07D239/69 , A61K31/44 , A61K31/505 , C07C311/21 , C07D213/60 , C07D213/76 , C07D213/89 , C07D217/22 , C07D239/32 , C07D239/42
摘要： This invention relates to compounds of Formulas I, II, and III, and their use as inhibitors of phosphatidylcholine transfer protein (PC-TP). The invention further relates to pharmaceutical compositions and methods of treatment of disorders related to the inhibition of PC-TP using the compounds of Formulas I, II, and III. Such disorders include obesity and disorders associated with obesity.
摘要翻译：本发明涉及式I，II和III的化合物及其作为磷脂酰胆碱转移蛋白（PC-TP）抑制剂的用途。本发明还涉及使用式I，II和III的化合物治疗与PC-TP的抑制相关的病症的药物组合物和方法。这种疾病包括肥胖症和与肥胖相关的疾病。

3. 发明授权

US09447051B2 Diaminopyrimidines and uses thereof 有权
标题翻译：二氨基嘧啶及其用途
公开(公告)号：US09447051B2
公开(公告)日：2016-09-20
申请号：US14379155
申请日：2013-02-15
申请人： AbbVie inc.
发明人： Tatyana Dekhtyar , Arthur Gomtsyan , M-Akhteruzzaman Molla , Anil Vasudevan , Iok Chan Ng , Mikhail Chafeev
IPC分类号： C07D239/32 , A61K31/505 , C07D239/48 , C07D403/12 , C07D401/14 , C07D405/14 , C07D401/12 , C07D409/14 , C07D413/12 , C07D417/14 , A61K45/06 , A61K31/506 , C07D413/14
CPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61K45/06 , C07D239/32 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit RSV infection and/or replication; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.

4. 发明授权

US09126938B2 Phosphatidylcholine transfer protein inhibitors 有权
标题翻译：磷脂酰胆碱转移蛋白抑制剂
公开(公告)号：US09126938B2
公开(公告)日：2015-09-08
申请号：US13390910
申请日：2010-08-17
申请人： David Cohen , Neil Wagle , Gregory D. Cuny , Jun Xian , Marcie Glicksman , Ross L. Stein , Ekaterina Y. Shishova
发明人： David Cohen , Neil Wagle , Gregory D. Cuny , Jun Xian , Marcie Glicksman , Ross L. Stein , Ekaterina Y. Shishova
IPC分类号： C07D239/42 , A61K31/505 , A61P1/16 , A61P3/04 , A61P3/10 , A61P9/10 , A61P11/06 , C07D213/60 , A61K31/44 , C07D239/32
CPC分类号： C07D239/69 , A61K31/44 , A61K31/505 , C07C311/21 , C07D213/60 , C07D213/76 , C07D213/89 , C07D217/22 , C07D239/32 , C07D239/42
摘要： This invention relates to compounds of Formulas I, II, and III, and their use as inhibitors of phosphatidylcholine transfer protein (PC-TP). The invention further relates to pharmaceutical compositions and methods of treatment of disorders related to the inhibition of PC-TP using the compounds of Formulas I, II, and III. Such disorders include obesity and disorders associated with obesity.
摘要翻译：本发明涉及式I，II和III的化合物及其作为磷脂酰胆碱转移蛋白抑制剂（PC-TP）的用途。本发明还涉及使用式I，II和III的化合物治疗与PC-TP的抑制相关的病症的药物组合物和方法。这种疾病包括肥胖症和与肥胖相关的疾病。

5. 发明授权

US08741915B2 Dihydropyrimidin-2(1H)-one compounds as S-nitrosoglutathione reductase inhibitors 失效
标题翻译：二氢嘧啶-2（1H） - 酮化合物，为S-亚硝基谷胱甘肽还原酶抑制剂
公开(公告)号：US08741915B2
公开(公告)日：2014-06-03
申请号：US13496799
申请日：2010-09-24
申请人： Xicheng Sun , Jian Qiu
发明人： Xicheng Sun , Jian Qiu
IPC分类号： A01N43/54 , A61K31/505 , A61K31/513 , A61K31/506 , C07D239/34 , C07D239/38 , C07D239/32
CPC分类号： A61K31/5377 , A61K31/505 , A61K31/506 , A61K31/513 , C07D233/32 , C07D233/42 , C07D239/32 , C07D239/34 , C07D239/36 , C07D239/38 , C07D239/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/10 , C07D417/04
摘要： The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
摘要翻译：本发明涉及可用作S-亚硝基谷胱甘肽还原酶（GSNOR）抑制剂的新型二氢嘧啶-2（1H） - 酮化合物，包含这些化合物的药物组合物及其制备和使用方法。

6. 发明申请

US20100274015A1 SYNTHESIS OF 4/5-PYRIMIDINYLIMIDAZOLES VIA SEQUENTIAL FUNCTIONALIZATION OF 2,4-DICHLOROPYRIMIDINE 有权
公开(公告)号：US20100274015A1
公开(公告)日：2010-10-28
申请号：US12830998
申请日：2010-07-06
申请人： Xiaohu DENG , Neelakandha MANI
发明人： Xiaohu DENG , Neelakandha MANI
IPC分类号： C07D239/32
CPC分类号： C07D239/42 , C07D403/04 , C07D403/14
摘要： This invention relates to methods of making pyrimidinyl-substituted imidazole compounds by sequential substitution of the 4- and 2-chloro groups of 2,4-dichloropyrimidine, nucleophilic substitution to form pyrimidinylalkyne derivatives, oxidation to the corresponding 1,2-diketones, and cyclocondensation reactions.

7. 发明申请

US20100240654A1 HYDRAZIDE DERIVATIVES 审中-公开
标题翻译：氢化衍生物
公开(公告)号：US20100240654A1
公开(公告)日：2010-09-23
申请号：US12791571
申请日：2010-06-01
申请人： Richard CLARK , Shinsuke HIROTA , Hiroshi AZUMA , Kazunobu KIRA , Nobuhisa WATANABE , Tadashi NAGAKURA , Tatsuo HORIZOE
发明人： Richard CLARK , Shinsuke HIROTA , Hiroshi AZUMA , Kazunobu KIRA , Nobuhisa WATANABE , Tadashi NAGAKURA , Tatsuo HORIZOE
IPC分类号： A61K31/5377 , C07C243/22 , A61K31/15 , C07D211/72 , A61K31/4402 , C07D215/38 , A61K31/47 , C07D239/32 , C07D295/28 , A61K31/5375 , C07D413/04 , A61P7/02 , A61P9/10 , A61P9/00 , A61P7/00
CPC分类号： C07D209/48 , C07C257/18 , C07C311/49 , C07C317/14 , C07C317/44 , C07C337/06 , C07D209/08 , C07D213/30 , C07D213/54 , C07D213/71 , C07D213/77 , C07D213/80 , C07D213/82 , C07D213/86 , C07D213/87 , C07D213/89 , C07D215/38 , C07D233/90 , C07D237/20 , C07D239/28 , C07D239/42 , C07D249/18 , C07D257/04 , C07D295/32 , C07D307/68 , C07D333/24 , C07D471/04
摘要： A compound represented by the following general formula (1) or a salt thereof or a hydrate of the foregoing is safe while exhibiting suitable physicochemical stability, and is useful as therapeutic or prophylactic agents for diseases associated with thrombus formation. wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc., R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc., Z1, Z2 and Z3 each independently represent hydrogen, etc., Z4 represents hydrogen, etc. and X represents a single bond or —CO—, etc.
摘要翻译：由下列通式（1）表示的化合物或其盐或其水合物是安全的，同时具有合适的物理化学稳定性，并且可用作与血栓形成相关的疾病的治疗或预防剂。其中R1a，R1b，R1c和R1d各自独立地表示氢等，R2表示任选取代的苯基等，R 3表示任选取代的C 6-10芳基等，Z 1，Z 2和Z 3各自独立地表示氢等， Z4表示氢等，X表示单键或-CO-等。

8. 发明申请

US20080262007A1 Hiv Inhibiting 5-Substituted Pyrimidines 有权
标题翻译： HIF抑制5-取代的嘧啶
公开(公告)号：US20080262007A1
公开(公告)日：2008-10-23
申请号：US11576315
申请日：2005-09-29
申请人： Jerome Emile Georges Guillemont , Jan Heeres , Paulus Joannes Lewi
发明人： Jerome Emile Georges Guillemont , Jan Heeres , Paulus Joannes Lewi
IPC分类号： A61K31/505 , C07D239/32 , A61P31/18
CPC分类号： C07D239/48 , C07D239/50
摘要： HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A is —CH2—CH2—, —CH═CH—, —C≡C—; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, R2 hydroxy, halo, C1-6alkyl, carboxyl, cyano, —C(═O)R6, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl; X1 is —NR1—, —O—, —S—, —S(═O)p—; R3 is H, C1-6alkyl, halo; R4 is H, C1-6alkyl, halo; R5 is nitro, amino, mono- and diC1-4alkylamino, aryl, halo, —CHO, —CO—R6, —COOR7, —NH—C(═O)H, —NH—C(═O)R6, —CH═N—O—R8; R6 is C1-4alkyl, amino, mono- or di(C1-4alkyl)amino or polyhaloC1-4alkyl; R7 is hydrogen, C1-6alkyl, arylC1-6alkyl; R8 is hydrogen, C1-6alkyl, aryl; p is 1 or 2; aryl is optionally substituted phenyl; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.
摘要翻译：式I的N-复合抑制剂N-氧化物，药学上可接受的加成盐，季胺或其立体化学异构形式，其中A为-CH 2 -CH 2 - ，-CH-CH-，-C≡C-; R 1是氢，芳基，甲酰基，C 1-6烷基羰基，C 1-6烷基，C 1-6烷基，烷基氧基羰基，R 2羟基，卤素，C 1-6烷基，羧基，氰基，-C（-O）R 6，，硝基，氨基，一或二（C 1-6烷基）氨基，多卤代甲基; X 1是-NR 1 - ， - O - ， - S - ， - S（-O）p - 。 R 3是H，C 1-6烷基，卤素; R 4是H，C 1-6烷基，卤素; R 5是硝基，氨基，单和二C 1-4烷基氨基，芳基，卤素，-CHO，-CO-R 6， -COOR 7，-NH-C（-O）H，-NH-C（-O）R 6，-CH-NOR 8 >; R 6是C 1-4烷基，氨基，单或二（C 1-4烷基）氨基或多卤代1 -4 烷基; R 7是氢，C 1-6烷基，芳基C 1-6烷基; R 8是氢，C 1-6烷基，芳基; p为1或2; 芳基是任选取代的苯基; 含有这些化合物作为活性成分的药物组合物和制备所述化合物和组合物的方法。

9. 发明申请

US20080104772A1 AGENT FOR DYEING KERATIN-BASED FIBERS 失效
标题翻译：用于染色基于KERATIN的纤维的试剂
公开(公告)号：US20080104772A1
公开(公告)日：2008-05-08
申请号：US11937464
申请日：2007-11-08
申请人： Wibke GROSS , Horst HOFFKES , Doris OBERKOBUSCH , Helmut MULLER , Carsten BRAKE
发明人： Wibke GROSS , Horst HOFFKES , Doris OBERKOBUSCH , Helmut MULLER , Carsten BRAKE
IPC分类号： A61K8/49 , A61Q5/10 , C07D239/32
CPC分类号： A61K8/4946 , A61K8/33 , A61K8/34 , A61K8/35 , A61K8/368 , A61K8/49 , A61K8/4953 , A61Q5/065 , A61Q5/10
摘要： An agent for dyeing keratin-containing fibers, especially human hair, is comprised of a cosmetic carrier, and (A) at least one compound of Formula I, wherein each of R1, R2 and R3 is independently a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a C2-C6 alkenyl group, a hydroxyl group, a C1-C6 alkoxy group, a C1-C6 hydroxyalkyl group, a C2-C6 polyhydroxyalkyl group, a hydroxy C1-C6 alkyloxy group, a sulfonyl group, a carboxyl group, a C1-C6 alkoxycarbonyl group, a hydroxy C2-C6 alkyloxycarbonyl group, a sulfonic acid group, a sulfonamido group, a sulfonamide group, a C2-C6 acyl group, a formyl group, a nitro group, a carbamoyl group —C(O)—NR4R5, or a —(CH2)nNR6R7 group wherein each of R4, R5, R6 and R7 is independently a hydrogen atom, a C1-C6 alkyl group or a C2-C6 hydroxyalkyl group; and n is number from 0 to 6, wherein R1 and R2 can form a 5- or 6-membered aromatic or heteroaromatic ring; and (B) at least one CH-acidic compound.
摘要翻译：用于染色含角蛋白纤维，特别是人发的试剂由化妆品载体组成，和（A）至少一种式I化合物，其中R 1，R 2， R 3和R 3独立地是氢原子，卤素原子，C 1 -C 6烷基，C 1 -C 6烷基， C 1 -C 6烷基，C 1 -C 6亚烷基，C 1 -C 6亚烷基，C 1 -C 6烷基，C 1 -C 6亚烷基， C 1 -C 6羟基烷基，C 2 -C 6多羟基烷基，羟基C 1 C 6 -C 6烷氧基，磺酰基，羧基，C 1 -C 6烷氧基羰基，羟基（C 1 -C 6） C 2 -C 6烷氧基羰基，磺酸基，亚磺酰氨基，磺酰胺基，C 2 -C 3烷氧基羰基，酰基，甲酰基，硝基，氨基甲酰基-C（O）-NR 4 R 5或 - （CH 3）其中每个R R 4，R 5，R 6和R 7独立地是氢原子，C 1〜 C 1 -C 6烷基或C 2 -C 6 -C 6羟烷基; 并且n为0至6的数，其中R 1和R 2可以形成5-或6-元芳族或杂芳族环; 和（B）至少一种CH-酸性化合物。

10. 发明授权

US07314933B2 Vanilloid receptor ligands and their use in treatments 失效
标题翻译：香草素受体配体及其在治疗中的应用
公开(公告)号：US07314933B2
公开(公告)日：2008-01-01
申请号：US11256427
申请日：2005-10-21
申请人： Mark H. Norman , Vassil I. Ognyanov , Robert M. Rzasa
发明人： Mark H. Norman , Vassil I. Ognyanov , Robert M. Rzasa
IPC分类号： C07D213/44 , C07D213/643 , C07D237/10 , C07D237/14 , C07D239/32 , C07D401/12 , C07D403/12 , A61K31/4427 , A61K31/501 , A61K31/506 , A61K25/06 , A61K29/00
CPC分类号： C07D401/04 , C07D403/04 , C07D405/04
摘要： Substituted nitrogen-containing heterocycles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
摘要翻译：取代的含氮杂环和含有它们的组合物，用于治疗急性，炎性和神经性疼痛，牙痛，一般头痛，偏头痛，丛集性头痛，混合血管和非血管性综合征，紧张性头痛，一般炎症，关节炎，风湿疾病，骨关节炎，炎症性肠病，炎症性眼病，炎症性或不稳定性膀胱病，银屑病，皮肤炎症成分炎症，慢性炎性病症，炎性疼痛及相关的痛觉过敏和异常性疼痛，神经性疼痛及相关的痛觉过敏和异常性疼痛，糖尿病性神经病疼痛，咳嗽痛，交感神经痛，交感综合征，哮喘，上皮组织损伤或功能障碍，单纯疱疹，呼吸道内脏运动紊乱，泌尿生殖道，胃肠道或血管区，伤口，烧伤，过敏性皮肤反应，瘙痒，白癜风，一般胃肠道紊乱胃溃疡，十二指肠溃疡，腹泻，坏死因子诱导的胃损伤，毛发生长，血管舒缩或过敏性鼻炎，支气管疾病或膀胱疾病。

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