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1. 发明申请

WO2016044183A1 METHODS OF PREPARING TOLL-LIKE RECEPTOR MODULATORS 审中-公开
标题翻译：制备类似受体调节剂的方法
公开(公告)号：WO2016044183A1
公开(公告)日：2016-03-24
申请号：PCT/US2015/050039
申请日：2015-09-14
申请人： GILEAD SCIENCES, INC.
发明人： ALLEN, Darin , BROWN, Brandon Heath , CHAO, Jessica Jade , HALCOMB, Randall L. , HRVATIN, Paul , MCFADDEN, Ryan , ROETHLE, Paul , RUDIO, Erwina , YANG, Hong , YU, Richard Hung Chiu
IPC分类号： C07D487/04 , C07D207/06 , C07D239/46 , C07D239/47 , C07D239/48 , C07D239/545
CPC分类号： C07D475/06 , C07D207/06 , C07D207/09 , C07D239/46 , C07D239/47 , C07D239/48 , C07D239/545 , C07D487/04
摘要： The present invention provides methods of preparing 4-amino-2-biitoxy-8-(3- (pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one and related compounds.
摘要翻译：本发明提供4-氨基-2-二氧化-8-（3-（吡咯烷-1-基甲基）苄基）-7,8-二氢蝶啶-6（5H）酮及其相关化合物的制备方法。

2. 发明申请

WO2013028832A2 INHIBITORS OF NEDD8-ACTIVATING ENZYME 审中-公开
标题翻译： NEDD8激活酶的抑制剂
公开(公告)号：WO2013028832A2
公开(公告)日：2013-02-28
申请号：PCT/US2012/052007
申请日：2012-08-23
申请人： MILLENNIUM PHARMACEUTICALS, INC. , MCCARRON, Ashley, Sue , SELLS, Todd, B. , STIRLING, Matthew , STROUD, Stephen, G.
发明人： MCCARRON, Ashley, Sue , SELLS, Todd, B. , STIRLING, Matthew , STROUD, Stephen, G.
IPC分类号： C07D487/04 , C07D487/02 , A61K31/519 , A61K31/505 , A61P35/00
CPC分类号： C07D239/47 , C07D239/46 , C07D473/02
摘要： Disclosed are chemical entities which are inhibitors of Nedd8-activating enzyme (NAE), namely, the compound {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyciopentyl}methyl sulfamate and pharmaceutically acceptable salts thereof; solid state forms thereof; and prodrugs thereof. Also disclosed are methods of using the chemical entities to treat disorders such as cancer.
摘要翻译：公开了作为Nedd8激活酶（NAE）抑制剂的化学实体，即化合物{（1S，2S，4R）-4 - [（6 - {[（1R，2S） -5-氯-2-甲氧基-2,3-二氢-1H-茚-1-基]氨基}嘧啶-4-基）氧基] -2-羟基环戊基}甲基氨基磺酸酯及其药学上可接受的盐; 其固态形式; 及其前药。还公开了使用化学实体来治疗诸如癌症的疾病的方法。

3. 发明申请

WO2008104472A1 2, 4 -DIAMINOPYRIMIDINE DERIVATIVES AND THEIR USE AS P2X ANTAGONISTS OR AS PRODRUGS THEREOF 审中-公开
标题翻译： 2,4-二氨基吡啶衍生物及其作为P2X拮抗剂或其作为制剂的用途
公开(公告)号：WO2008104472A1
公开(公告)日：2008-09-04
申请号：PCT/EP2008/051939
申请日：2008-02-18
申请人： F. HOFFMANN-LA ROCHE AG , DILLON, Michael, Patrick , JAHANGIR, Alam
发明人： DILLON, Michael, Patrick , JAHANGIR, Alam
IPC分类号： C07D239/46 , C07D413/12 , A61K31/5377 , A61K31/505 , A61P15/00
CPC分类号： C07D413/12 , C07D239/46 , C07D239/48 , C07D403/12
摘要： Compounds and methods for treating diseases mediated by a P2X 3 and/or a P2X 2/3 receptor antagonist, the compounds being of formula (I): wherein R 1 , R 2 , R 3 and R 4 are as defined herein.
摘要翻译：用于治疗由P2X 3和/或P2X 2/3受体拮抗剂介导的疾病的化合物和方法，所述式（I）的化合物：其中R R 1，R 2，R 3和R 4如本文所定义。

4. 发明申请

WO2007031829A3 NOVEL PYRIMIDINE CARBOXAMIDES 审中-公开
标题翻译：新型吡咯烷酮羧酰胺
公开(公告)号：WO2007031829A3
公开(公告)日：2007-11-08
申请号：PCT/IB2006002461
申请日：2006-09-07
申请人： ORCHID RES LAB LTD , TADIPARTHI RAVIKUMAR , AGGARWAL PAWAN , PARAMESWARAN VENKATESAN , THIRUNAVUKKARASU SAPPANIMUTHU , BARIK RAJIB , RAJAGOPAL SRIRAM , REDDY GADDAM OM
发明人： TADIPARTHI RAVIKUMAR , AGGARWAL PAWAN , PARAMESWARAN VENKATESAN , THIRUNAVUKKARASU SAPPANIMUTHU , BARIK RAJIB , RAJAGOPAL SRIRAM , REDDY GADDAM OM
IPC分类号： C07D239/28
CPC分类号： C07D239/38 , C07D239/46 , C07D239/47 , C07D239/48 , C07D401/04
摘要： The present invention relates to novel compounds of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and compositions, their metabolites and prodrugs thereof. The present invention more particularly relates to novel pyrimidine carboxamides of the general formula (I). Also included is a method of prophylaxis or treatment of a pain disorder, immunological diseases, inflammation, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; ischemic heart disease; atherosclerosis; cancer; ischemic-induced cell damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; adult respiratory distress syndrome (ARDS); psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; cachexia; asthma; bone resorption diseases; ischemia reperfusion injury; brain trauma; multiple sclerosis; sepsis; septic shock; toxic shock syndrome; fever, and myalgias due to infection in a mammal comprising administering an effective amount of a compound of formula (I) as described above.
摘要翻译：本发明涉及通式（I）的新化合物，其衍生物，其类似物，其互变异构形式，其立体异构体，其多晶型物，其水合物，它们的溶剂化物，其药学上可接受的盐和组合物，其代谢物和前药。本发明更具体地涉及通式（I）的新型嘧啶甲酰胺。还包括预防或治疗疼痛障碍，免疫疾病，炎症，类风湿性关节炎的方法; 骨质疏松症; 多发性骨髓瘤 uveititis; 急性和慢性粒细胞白血病; 缺血性心脏病; 动脉粥样硬化; 癌症; 缺血诱导的细胞损伤; 胰腺β细胞破坏; 骨关节炎; 类风湿性脊柱炎; 痛风性关节炎炎症性肠病; 成人呼吸窘迫综合征（ARDS）; 银屑病; 克罗恩病; 过敏性鼻炎; 溃疡性结肠炎过敏性反应; 接触性皮炎; 肌肉退化; 恶病质; 哮喘; 骨吸收疾病; 缺血再灌注损伤; 脑外伤; 多发性硬化症败血症; 败血性休克中毒性休克综合征发热和由于哺乳动物感染引起的肌痛，包括给予有效量的如上所述的式（I）化合物。

5. 发明申请

WO2006053227A3 IL-12 MODULATORY COMPOUNDS 审中-公开
标题翻译： IL-12调控化合物
公开(公告)号：WO2006053227A3
公开(公告)日：2006-07-06
申请号：PCT/US2005040952
申请日：2005-11-10
申请人： SYNTA PHARMACEUTICALS CORP , SUN LIJUN , KOSTIK ELENA , PRZEWLOKA TERESA , NG HOWARD P , CHIMMANAMADA DINESH , DEMKO ZACHARY
发明人： SUN LIJUN , KOSTIK ELENA , PRZEWLOKA TERESA , NG HOWARD P , CHIMMANAMADA DINESH , DEMKO ZACHARY
IPC分类号： A61K31/535 , C07D413/00
CPC分类号： C07D403/12 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/48 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention relates to heterocyclic compounds, compositions including the compounds and methods of using and methods of making thereof. The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12.
摘要翻译：本发明涉及杂环化合物，包含该化合物的组合物和使用方法及其制备方法。这些化合物（和组合物）尤其可用于调节由IL-12介导的IL-12产生和过程。

6. 发明申请

WO2006034473A2 NOVEL PYRIMIDINE COMPOUNDS, PROCESS FOR THEIR PREPARATION AND COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：新的嘧啶化合物，它们的制备方法和含有它们的组合物
公开(公告)号：WO2006034473A2
公开(公告)日：2006-03-30
申请号：PCT/US2005/034243
申请日：2005-09-23
申请人： REDDY US THERAPEUTICS, INC. , KALLEDA, Srinivas , PADAKANTI, Srinivas , KUMAR SWAMY, Nalivela , YELESWARAPU, Koteswar, Rao , ALEXANDER, Christopher, W. , KHANNA, Ish, Kumar , IQBAL, Javed , PILLARISETTI, Sivaram , PAL, Manojit , BARANGE, Deepak
发明人： KALLEDA, Srinivas , PADAKANTI, Srinivas , KUMAR SWAMY, Nalivela , YELESWARAPU, Koteswar, Rao , ALEXANDER, Christopher, W. , KHANNA, Ish, Kumar , IQBAL, Javed , PILLARISETTI, Sivaram , PAL, Manojit , BARANGE, Deepak
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4545 , A61K31/4439 , A61K31/44 , C07D417/02 , C07D403/02 , C07D413/02 , C07D401/02
CPC分类号： C07D405/14 , C07D239/30 , C07D239/40 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/48 , C07D239/50 , C07D239/54 , C07D401/04 , C07D403/12 , C07D405/12
摘要： The present invention provides new heterocyclic compounds, particularly substituted pyrimidines, methods and compositions for making and using these heterocyclic compounds, and methods for treating a variety of diseases and disease states, including atherosclerosis, arthritis, restenosis, diabetic nephropathy, or dyslipidemia, or disease states mediated by the low expression of Perlecan.
摘要翻译：本发明提供了新的杂环化合物，特别是取代的嘧啶，制备和使用这些杂环化合物的方法和组合物，以及治疗多种疾病和疾病状态的方法，包括动脉粥样硬化，关节炎，再狭窄，糖尿病性肾病或血脂异常，或由基底膜蛋白低表达介导的疾病状态。

7. 发明申请

WO2003099771A2 DIARYL UREA DERIVATIVES USEFUL FOR THE TREATMENT OF PROTEIN KINASE DEPENDENT DISEASES 审中-公开
标题翻译：用于治疗蛋白激酶依赖性疾病的二尿嘧啶衍生物
公开(公告)号：WO2003099771A2
公开(公告)日：2003-12-04
申请号：PCT/EP2003/005634
申请日：2003-05-28
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FLOERSHEIMER, Andreas , FURET, Pascal , MANLEY, Paul, William , BOLD, Guido , BOSS, Eugen , GUAGNANO, Vito , VAUPEL, Andrea
发明人： FLOERSHEIMER, Andreas , FURET, Pascal , MANLEY, Paul, William , BOLD, Guido , BOSS, Eugen , GUAGNANO, Vito , VAUPEL, Andrea
IPC分类号： C07C275/00
CPC分类号： C07D213/40 , A61K31/33 , A61K31/395 , C07D213/38 , C07D213/64 , C07D213/68 , C07D213/69 , C07D213/81 , C07D213/84 , C07D213/89 , C07D239/34 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/52 , C07D401/04 , C07D401/12 , C07D403/12
摘要： The invention relates to the use of diaryl urea derivatives in the treatment of protein kinase dependent diseases or for the manufacture of pharmaceutical compositions for use in the treatment of said diseases, methods of use of diaryl urea derivatives in the treatment of said diseases, pharmaceutical preparations comprising diaryl urea derivatives for the treatment of said diseases, diaryl urea derivatives for use in the treatment of said diseases, novel diaryl urea derivatives, pharmaceutical preparations comprising these novel diaryl urea derivatives, processes for the manufacture of the novel diaryl urea derivatives, the use or methods of use of the novel diaryl urea derivatives as mentioned above, and/or these novel diaryl urea derivatives for use in the treatment of the animal or human body.
摘要翻译：本发明涉及二芳基脲衍生物在治疗蛋白激酶依赖性疾病或用于制备用于治疗所述疾病的药物组合物中的用途，二芳基脲衍生物在治疗所述疾病中的应用方法，药物制剂包括用于治疗所述疾病的二芳基脲衍生物，用于治疗所述疾病的二芳基脲衍生物，新型二芳基脲衍生物，包含这些新型二芳基脲衍生物的药物制剂，制备新型二芳基脲衍生物的方法，或使用上述新型二芳基脲衍生物的方法，和/或这些新型二芳基脲衍生物用于动物或人体的治疗。

8. 发明申请

WO00049001A2 PHENOXYPYRIMIDINE INSECTICIDES AND ACARICIDES 审中-公开
标题翻译：苯氧基杀虫剂和杀螨剂
公开(公告)号：WO00049001A2
公开(公告)日：2000-08-24
申请号：PCT/US2000/003180
申请日：2000-02-08
IPC分类号： C07D239/34 , C07D239/38 , C07D239/46 , C07D239/52 , C07D239/56 , C07D403/06 , C07D239/42
CPC分类号： C07D239/34 , C07D239/38 , C07D239/46 , C07D239/52 , C07D239/56 , C07D403/06
摘要： Compounds of Formula (I), and their N-oxides and agriculturally suitable salts, are disclosed which are useful as arthropodicides wherein Q is O, S, NR , OCR R , or NR CR R ; wherein when Q is OCR R or NR CR R , then Q is attached to the pyrimidine through the O or N atom respectively; Q is S, CR R , OCR R , SCR R or NR CR R ; wherein when Q is OCR R , SCR R or NR CR R then Q is attached to the pyrimidine through the O, S or N atom respectively; R and R are each independently H, C1-C4 alkyl, halogen, NR R , C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 alkylthio or nitro; each R is independently H, halogen, C1-C4 alkyl, C1-C4 haloalkoxy, C1-C4 haloalkyl, C1-C4 alkoxy, SF5, S(O)nR , cyano or CO2R ; each R and each R is independently H, halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C4 alkoxy, NR or S(O)nR ; p is 0-4; and J, R , R R , R , R , R , R , R , R and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (I) and a method for controlling arthropods which involves contacting the arthropods or their environment with an effective amount of a compound of Formula (I).
摘要翻译：公开了式（I）化合物及其N-氧化物和农业上合适的盐，其可用作其中Q 1为O，S，NR 17，OCR 18 R 19或NR <17> CR <18> - [R <19>; 其中当Q 1是OCR 18 R 19或NR 17 CR 18 R 19时，则Q 1分别通过O或N原子连接到嘧啶上; Q 2是S，CR 3 R 4，OCR 18 R 19，SCR 18 R 19或NR 17 CR 18 R 19。其中当Q 2是OCR 18 R 19时，SCR 18 R 19或NR 17 CR 18 R然后Q 2通过O连接到嘧啶上，S或N原子; R 1和R 2各自独立地为H，C 1 -C 4烷基，卤素，NR 7 R 8，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4烷硫基或硝基; 每个R 5独立地是H，卤素，C 1 -C 4烷基，C 1 -C 4卤代烷氧基，C 1 -C 4卤代烷基，C 1 -C 4烷氧基，SF 5，S（O）n R 9，氰基或CO 2 R 11; 每个R 6和每个R 22独立地是H，卤素，氰基，C 1 -C 4烷基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，C 1 -C 4烷氧基，NR 17或S（O） 9>; p为0-4; 和R 3，R 4，R 8，R 9，R 11，R 17，R 18，R 19和n分别为在本公开中定义。还公开了含有式（I）化合物和控制节肢动物的方法的组合物，其涉及将节肢动物或其环境与有效量的式（I）化合物接触。

9. 发明申请

WO1995007894A1 SUBSTITUTED PYRIDINES AND PYRIMIDINES, PROCESS FOR PRODUCING THEM AND THEIR USE AS PESTICIDES AND FUNGICIDES 审中-公开
标题翻译：取代的吡啶和嘧啶，其制造方法相同，它们作为杀虫剂和杀菌剂
公开(公告)号：WO1995007894A1
公开(公告)日：1995-03-23
申请号：PCT/EP1994002934
申请日：1994-09-02
申请人： HOECHST SCHERING AGREVO GMBH
发明人： HOECHST SCHERING AGREVO GMBH , REUSCHLING, Dieter, Bernd , LINKIES, Adolf, Heinz , WEHNER, Volkmar , PREUSS, Rainer , SCHAPER, Wolfgang , JAKOBI, Harald , BRAUN, Peter , KNAUF, Werner , SACHSE, Burkhard , WALTERSDORFER, Anna , KERN, Manfred , LÜMMEN, Peter , BONIN, Werner
IPC分类号： C07D239/52
CPC分类号： C09K3/10 , A01N43/40 , A01N43/54 , C05G3/02 , C07D239/34 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/88 , C09D5/14
摘要： The invention relates to compounds of formula (I) in which A is N or CH, R is H, halogen, alkyl or cycloalkyl, R and R are H, halogen or an aliphatic radical or together form a ring, X is O, NH or S(O)q with q=0, 1, 2, R q is 0-4 radicals of halogen, possibly substituted alkyl or alkoxy, cycloalkyl and possibly substituted phenyl, n=0-2, m=1-3 and Y is possibly substituted methylene or imino. The invention also relates to a process for their production and their use as pesticides, especially as insecticides, acaricides and fungicides. The compounds are also suitable for combatting nematodes, helminths and molluscs and endo and ecto-parasites in the field of veterinary medecine.
摘要翻译：本发明涉及式（I）的化合物处于ON或CH，R是H，卤素，烷基或环烷基，R <2>和R <3>是H，卤素或脂肪族残基，或一起形成环，XO ，NH或其中q = 0，1，2 S（O）q，R <4> q被选自卤素的基团0-4，任选地被取代的烷基或烷氧基，环烷基和任选取代的苯基，n = 0-2， m是1-3，Y为任选取代的亚甲基或亚氨基。本发明还涉及它们的制备方法及其作为杀虫剂的用途，特别是作为杀虫剂，杀螨剂和杀真菌剂的方法。所述化合物还适于防治线虫，蠕虫和软体动物，以及用于在兽医领域防治体内和体外寄生虫。

10. 发明申请

WO2015013715A3 C-H FLUORINATION OF HETEROCYCLES WITH SILVER (II) FLUORIDE 审中-公开
标题翻译： C-H氟化物（II）氟化物的杂环化合物
公开(公告)号：WO2015013715A3
公开(公告)日：2015-10-29
申请号：PCT/US2014048472
申请日：2014-07-28
申请人： THR REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： HARTWIG JOHN , FIER PATRICK
IPC分类号： C07D213/61
CPC分类号： C07D213/61 , C07D213/63 , C07D213/65 , C07D213/75 , C07D213/79 , C07D213/80 , C07D213/803 , C07D213/81 , C07D213/82 , C07D215/18 , C07D239/42 , C07D239/46 , C07D401/04 , C07D405/04
摘要： The present invention provides compositions and methods for the selective C-H fluorination of nitrogen-containing heteroarenes with AgF2, which has previously been considered too reactive for practical, selective C-H fluorination. Fluorinated heteroarenes are prevalent in numerous pharmaceuticals, agrochemicals and materials. However, the reactions used to introduce fluorine into these molecules require pre-functionalized substrates or the use of F2 gas. The present invention provides a mild and general method for the C-H fluorination of nitrogen-containing heteroarene compounds to 2-fluoro-heteroarenes with commercially available AgF2. In various embodiments, these reactions occur at ambient temperature within one hour and occur with exclusive selectivity for fluorination at the 2-position. Exemplary reaction conditions are effective for fluorinating diazine heteroarenes to form a single fluorinated isomer.
摘要翻译：本发明提供了含有AgF 2的含氮杂芳烃选择性C-H氟化的组合物和方法，其先前被认为对于实际的选择性C-H氟化反应过大。氟化杂芳烃在许多药物，农药和材料中是普遍存在的。然而，用于将氟引入这些分子的反应需要预功能化的底物或使用F2气体。本发明提供了一种使用市售的AgF2将含氮杂芳烃化合物C-H氟化为2-氟 - 杂芳烃的温和的一般方法。在各种实施方案中，这些反应在环境温度下在1小时内发生，并且以2-位氟化的排他选择性发生。示例性的反应条件对于使二嗪杂芳族化合物氟化以形成单一氟化异构体是有效的。

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