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1. 发明申请

WO02022588A1 NOVEL PYRIMIDINE DERIVATIVE AND NOVEL PYRIDINE DERIVATIVE 审中-公开
标题翻译：新型吡咯烷衍生物和新型吡啶衍生物
公开(公告)号：WO02022588A1
公开(公告)日：2002-03-21
申请号：PCT/JP2001/007841
申请日：2001-09-10
IPC分类号： A61K31/455 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61P1/04 , A61P9/10 , A61P11/06 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/28 , A61P25/30 , A61P43/00 , C07D213/80 , C07D213/82 , C07D239/28 , C07D239/34 , C07D239/38 , C07D239/42 , C07D401/04 , C07D403/04 , C07D409/04 , C07D417/04 , C07D239/08 , C07D401/06 , C07D401/12 , C07D401/14
CPC分类号： C07D213/80 , A61K31/455 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , C07D213/82 , C07D239/28 , C07D239/34 , C07D239/38 , C07D239/42 , C07D401/04 , C07D403/04 , C07D409/04 , C07D417/04
摘要： The achiral pyrimidine derivative and pyridine derivative respectively represented by the formulae or analogues of these. They have selective N-type calcium channel inhibitory activity, and showed analgesic activity upon oral administration. They are useful not only as therapeutic agents for pains but as ones for various diseases in which N-type calcium channels participate.
摘要翻译：分别由这些的式或类似物表示的非手性嘧啶衍生物和吡啶衍生物。它们具有选择性的N型钙通道抑制活性，并且在口服给药时显示镇痛作用。它们不仅用作疼痛的治疗剂，而且用作N型钙通道参与的各种疾病的治疗剂。

2. 发明申请

WO01058880A1 NOVEL TRIAZOLE DERIVATIVES 审中-公开
标题翻译：新型三唑衍生物
公开(公告)号：WO01058880A1
公开(公告)日：2001-08-16
申请号：PCT/JP2000/000668
申请日：2000-02-08
IPC分类号： A61K31/4178 , A61K31/4196 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/551 , A61P7/10 , A61P13/12 , C07D249/08 , C07D239/08 , A61K31/427 , A61K31/4427 , C07D401/04 , C07D403/10 , C07D409/04 , C07D417/10
CPC分类号： C07D249/08 , A61K31/4178 , A61K31/4196 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/551
摘要： Triazole derivatives represented by the general formula (I) or pharmaceutically acceptable salts thereof; and arginine vasopressin V1A receptor antagonists containing both as the active ingredient wherein A is an optionally substituted benzene or thiophene ring; Y is N or CH; R is hydrogen or alkyl; and R and R are each hydrogen, halogeno, amino, or other substituent.
摘要翻译：由通式（I）表示的三唑衍生物或其药学上可接受的盐; 和含有作为活性成分的精氨酸加压素V1A受体拮抗剂，其中A是任选取代的苯或噻吩环; Y为N或CH; R 1是氢或烷基; R 2和R 3各自为氢，卤素，氨基或其它取代基。

3. 发明申请

WO2017066650A1 MASS DEFECT-BASED MULTIPLEX DIMETHYL PYRIMIDINYL ORNITHINE (DIPYRO) TAGS FOR HIGH-THROUGHPUT QUANTITATIVE PROTEOMICS AND PEPTIDOMICS 审中-公开
标题翻译：用于高通量定量蛋白质组学和肽类物质的基于质量缺陷的多重二甲基嘧啶鸟氨酸（DIPYRO）标签
公开(公告)号：WO2017066650A1
公开(公告)日：2017-04-20
申请号：PCT/US2016/057156
申请日：2016-10-14
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION
发明人： LI, Lingjun , FROST, Dustin , BUCHBERGER, Amanda
IPC分类号： C07D239/08 , C07D239/14 , G01N27/62 , G01N33/50 , G01N33/68
CPC分类号： G01N33/6848 , C07D239/42 , G01N2458/15
摘要： The use of mass defect signatures to impart milliDalton mass differences between isotopically labeled peptides at the MS 1 -level allows multiplex quantification without the increased mass spectral complexity that occurs with mass difference approaches. Provided herein is a mass defect-based chemical tag, dimethyl pyrimidinyl ornithine (DiPyrO), that is compact and easy to synthesize at high purity in few steps using commercially available starting materials. The multiplex DiPyrO tags are amine-reactive and can impart a mass difference onto labeled peptides and through calculated substitution of heavy isotopes. DiPyrO offers up to 10-plex quantification on current Orbitrap or FT-ICR platforms without increasing mass spectral complexity. The synthesis of the DiPyrO tag is provided along with viability of the DiPyrO tag for labeling complex proteomics samples using yeast extract digests and its effect on labeled peptides during LC-MS 2 analysis. Labeling and quantification of glycans and metabolites using the DiPyrO tag is also demonstrated.
摘要翻译：使用质量缺陷特征来使MS1 / - 水平上的同位素标记的肽之间的毫当量质量差异允许进行多重定量而不增加质量差异所发生的质谱复杂度方法。本文提供的是基于质量缺陷的化学标签二甲基嘧啶鸟氨酸（DiPyrO），其紧凑且易于使用市售起始材料在几个步骤中以高纯度合成。多元化的DiPyrO标签是胺反应性的，并且可以在标记的肽上产生质量差异，并且通过计算重质同位素的替换。 DiPyrO在当前的Orbitrap或FT-ICR平台上提供高达10倍的量化，而不会增加质谱的复杂性。 DiPyrO标签的合成与DiPyrO标签的生存能力一起提供，用于使用酵母提取物消化物标记复杂的蛋白质组学样品及其在LC-MS 2/2分析期间对标记肽的影响。还证明了使用DiPyrO标签标记和定量聚糖和代谢物。

4. 发明申请

WO2002085867A1 ANTIBIOTICS AA-896 审中-公开
标题翻译：抗生素AA-896
公开(公告)号：WO2002085867A1
公开(公告)日：2002-10-31
申请号：PCT/US2002/013024
申请日：2002-04-25
申请人： AMERICAN CYANAMID COMPANY
发明人： LIN, Yang-I , Li, Zhong , FRANCISCO, Gerardo DelaCruz , MCDONALD, Leonard, Alexander
IPC分类号： C07D239/08
CPC分类号： C07H19/06
摘要： This invention relates to antibiotic compounds AA896 of the formula (I), wherein: R 1 is H, aryl, alkyl(C 1 -C 20 ),-CH 2 -aryl,-C(O)alkyl(C 1 -C 20 ),-C(O)NHalkyl(C 1 -C 20 ), or -C(O)NHaryl; R 2 is H, alkyl(C 1 -C 20 ), -CH 2 aryl,alkyl(C1-C 20 ) or -C(O)alkyl(C 1 -C 20 ); R 3 is -OH; R 2 and R 3 may optionally be taken together to form a moiety (II); R 4 is alkyl(C 1 -C 20 ), or aryl; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及式（I）的抗生素化合物AA896，其中：R1是H，芳基，烷基（C1-C20），-CH2-芳基，-C（O）烷基（C1-C20）， - C ）烷基（C 1 -C 20）或-C（O）NH芳基; R2是H，烷基（C1-C20），-CH2芳基，烷基（C1-C20）或-C（O）烷基（C1-C20）; R3是-OH; R2和R3可以任选地一起形成部分（II）; R4是烷基（C1-C20）或芳基; 或其药学上可接受的盐。

5. 发明申请

WO98031359A1 INTEGRIN ANTAGONISTS 审中-公开
公开(公告)号：WO98031359A1
公开(公告)日：1998-07-23
申请号：PCT/US1998/000617
申请日：1998-01-13
IPC分类号： C07D235/16 , A61K31/198 , A61K31/4184 , A61K31/4375 , A61K31/44 , A61K31/66 , A61K45/06 , A61P9/10 , A61P19/10 , A61P27/02 , A61P29/00 , A61P31/12 , A61P35/00 , A61P43/00 , C07D213/73 , C07D471/04 , A61K31/18 , A61K31/19 , A61K31/195 , A61K31/405 , A61K31/415 , A61K31/425 , A61K31/435 , A61K31/47 , C07C63/00 , C07C307/06 , C07C307/08 , C07C307/10 , C07D209/40 , C07D213/89 , C07D217/08 , C07D233/44 , C07D233/88 , C07D239/08 , C07D239/42
CPC分类号： C07D471/04 , A61K31/66 , A61K31/445 , A61K2300/00
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are alpha v beta 3 antagonists, alpha v beta 5 antagonists or dual alpha v beta 3/ alpha v beta 5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, viral disease, and tumor growth.
摘要翻译：本发明涉及某些新化合物及其衍生物，其合成及其作为玻连蛋白受体拮抗剂的用途。本发明的玻连蛋白受体拮抗剂化合物是可用于抑制骨吸收，治疗和预防骨质疏松症以及抑制再狭窄的糖尿病性视网膜病变的αvβ3拮抗剂，αvβ5拮抗剂或双重αvβ3 /αvβ5拮抗剂，黄斑变性，血管生成，动脉粥样硬化，炎症，病毒性疾病和肿瘤生长。

6. 发明申请

WO2006115895A3 PHENYL ETHYNE COMPOUNDS 审中-公开
公开(公告)号：WO2006115895A3
公开(公告)日：2006-11-02
申请号：PCT/US2006/014517
申请日：2006-04-18
申请人： MERCK & CO., INC. , COSFORD, Nicholas, D. , SEIDERS, Thomas, J.
发明人： COSFORD, Nicholas, D. , SEIDERS, Thomas, J.
IPC分类号： C07C255/50 , C07D239/08 , C07D213/62 , A61K31/275 , A61K31/435 , A61K31/505
摘要： In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted or unsubstituted six membered heterocyclic ring that includes at least two nitrogen atoms. The ring additionally includes four carbon atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon triple bond. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system. Invention compounds may also act as insecticides, and as fungicides. Pharmaceutical compositions containing invention compounds also have wide utility.

7. 发明申请

WO2006102760A1 INHIBITORS OF HISTONE DEACETYLASE 审中-公开
标题翻译： HISTONE DEACETYLASE的抑制剂
公开(公告)号：WO2006102760A1
公开(公告)日：2006-10-05
申请号：PCT/CA2006/000483
申请日：2006-03-31
申请人： METHYLGENE INC. , LEIT DE MORADEI, Silvana, Marcela , TESSIER, Pierre , SMIL, David , WAHHAB, Amal , DÉZIEL, Robert , MANKU, Sukhdev , MANCUSO, John , THERRIEN, Eric , ALLAN, Martin , CHANTIGNY, Yves, Andre , AJAMIAN, Alain , BEAULIEU, Patrick
发明人： LEIT DE MORADEI, Silvana, Marcela , TESSIER, Pierre , SMIL, David , WAHHAB, Amal , DÉZIEL, Robert , MANKU, Sukhdev , MANCUSO, John , THERRIEN, Eric , ALLAN, Martin , CHANTIGNY, Yves, Andre , AJAMIAN, Alain , BEAULIEU, Patrick
IPC分类号： C07D417/04 , A61K31/18 , A61K31/166 , A61K31/195 , A61K31/34 , A61K31/404 , A61K31/4184 , A61K31/4192 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/495 , A61K31/505 , C07C237/38 , C07C311/21 , C07C323/33 , C07C323/60 , C07D207/16 , C07D209/30 , C07D209/42 , C07D211/22 , C07D215/38 , C07D217/12 , C07D235/04 , C07D239/08 , C07D241/40 , C07D277/82 , C07D285/12 , C07D317/46 , C07D319/14 , C07D333/32 , C07D403/06 , C07D409/06 , C07D413/04
CPC分类号： C07D209/14 , C07C237/22 , C07C309/51 , C07C311/13 , C07C311/29 , C07C311/46 , C07C311/51 , C07C311/59 , C07C317/22 , C07C317/32 , C07C317/44 , C07C323/60 , C07C2601/14 , C07C2603/32 , C07D209/42 , C07D209/46 , C07D213/30 , C07D213/32 , C07D213/40 , C07D213/70 , C07D213/89 , C07D215/40 , C07D235/14 , C07D239/38 , C07D241/52 , C07D277/82 , C07D285/12 , C07D285/135 , C07D295/185 , C07D307/42 , C07D307/81 , C07D317/58 , C07D333/16 , C07D333/24 , C07D333/34 , C07D401/06 , C07D405/12 , C07D409/06 , C07D409/12
摘要： This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I); wherein Y, L, Z, W, X, Q, R 1 , R 2 and R 3 are as defined in the specification.
摘要翻译：本发明涉及抑制组蛋白脱乙酰酶的化合物。更具体地，本发明提供式（I）的化合物; 其中Y，L，Z，W，X，Q，R 1，R 2和R 3均如说明书中所定义。

8. 发明申请

WO02098850A3 CHEMICAL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS AS CATHEPSIN S INHIBITORS 审中-公开
标题翻译：化学化合物和药物组合物作为CATHEPSIN S抑制剂
公开(公告)号：WO02098850A3
公开(公告)日：2003-04-24
申请号：PCT/US0217411
申请日：2002-06-03
申请人： AXYS PHARM INC , AVENTIS PHARMA INC , GRAUPE MICHAEL , LI JIAYAO , LINK JOHN O , ZIPFEL SHEILA , TIMM ANDREAS P , ALDOUS DAVID J , THURAIRATNAM SUKANTHINI
发明人： GRAUPE MICHAEL , LI JIAYAO , LINK JOHN O , ZIPFEL SHEILA , TIMM ANDREAS P , ALDOUS DAVID J , THURAIRATNAM SUKANTHINI
IPC分类号： C07D295/18 , A61K31/165 , A61K31/277 , A61K31/341 , A61K31/351 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/423 , A61K31/4245 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/4453 , A61K31/4468 , A61K31/454 , A61K31/495 , A61K31/5375 , A61K31/5377 , A61K31/55 , A61P1/02 , A61P13/12 , A61P19/02 , A61P21/04 , A61P29/00 , A61P33/06 , A61P35/00 , A61P43/00 , C07C233/31 , C07C255/29 , C07C255/44 , C07C255/46 , C07C271/12 , C07C271/16 , C07C271/22 , C07C271/24 , C07C317/44 , C07C317/46 , C07C317/48 , C07D205/04 , C07D207/08 , C07D207/16 , C07D211/66 , C07D223/08 , C07D223/12 , C07D239/08 , C07D263/56 , C07D271/06 , C07D271/10 , C07D277/28 , C07D277/64 , C07D277/82 , C07D295/185 , C07D295/20 , C07D295/205 , C07D307/14 , C07D309/14 , C07D333/24 , C07D413/12 , C07D413/14 , C07D417/12 , C07D498/04 , A61K31/16
CPC分类号： C07D207/08 , C07C233/31 , C07C255/29 , C07C255/44 , C07C255/46 , C07C271/12 , C07C271/16 , C07C271/24 , C07C317/44 , C07C317/46 , C07C2601/02 , C07C2601/14 , C07C2601/18 , C07D205/04 , C07D211/66 , C07D223/08 , C07D223/12 , C07D239/08 , C07D263/56 , C07D271/10 , C07D277/28 , C07D277/64 , C07D277/82 , C07D295/185 , C07D295/205 , C07D307/14 , C07D309/14 , C07D333/24 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to coumponds of formula I in which X1 is-NHCR1R2X3 or -NHX4 and the other variables are as defined in the claims and the pharmaceutically acceptable salts and N-oxides therof, useful as selective cathepsin S inhibitors, their uses as therapeutic agents and the methods for their making. Formula I:
摘要翻译：本发明涉及其中X1为-NHCR1R2X3或-NHX4，其他变量如权利要求中所定义的式I化合物和可用作选择性组织蛋白酶S抑制剂的药学上可接受的盐和N-氧化物，其用途为治疗代理人及其制作方法。公式I：

9. 发明申请

WO2018191166A1 TREATMENT OF ADIPOCYTES 审中-公开
公开(公告)号：WO2018191166A1
公开(公告)日：2018-10-18
申请号：PCT/US2018/026707
申请日：2018-04-09
申请人： MELIOR PHARMACEUTICALS I, INC. , BOARD OF SUPERVISORS OF LOUISIANA STATE UNIVERSITY AND AGRICULTURAL AND MECHANICAL COLLEGE
发明人： REAUME, Andrew G. , CONG, Weina , GREENWAY, Frank , COULTER, Ann
IPC分类号： A61K31/495 , A61K31/505 , A61K31/513 , C07D239/08 , C07D239/10 , C07D239/22
摘要： The present disclosure provides compositions comprising a lyn kinase activator and TRPM8 agonist, and to methods of: reducing blood glucose levels, weight gain, or fat depot levels; treating metabolic syndrome, Syndrome X, obesity, prediabetes, type II diabetes, type I diabetes; treating hypercholesterolemia, hypertension, coronary heart disease, diabetic neuropathy, lipodystrophy, diabetic retinopathy, erectile dysfunction, kidney disease, dyslipidemia, dyslipoproteinemia, a peroxisome proliferator activated receptor-associated disorder, septicemia, a thrombotic disorder, or pancreatitis; inducing the beiging of adipocytes; and preventing pancreatic beta cell degeneration.

10. 发明申请

WO2015094443A1 PYRIMIDINES AND USE THEREOF 审中-公开
标题翻译：吡咯烷酮及其用途
公开(公告)号：WO2015094443A1
公开(公告)日：2015-06-25
申请号：PCT/US2014/056601
申请日：2014-09-19
申请人： PURDUE PHARMA L.P.
发明人： NI, Chiyou , PARK, Jae, Hyun , SHAO, Bin , ZHOU, Xiaoming
IPC分类号： C07D403/12 , C07D239/08 , A61K31/506 , A61K31/505
CPC分类号： C07D403/12 , C07B59/002 , C07B2200/05 , C07D239/28 , C07D401/14 , C07D403/06
摘要： The present disclosure provides pyrimidines of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein A 1 , X, A 2 , G, Y, n, R 2a , R 2b , and R 3 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I and the pharmaceutically acceptable salts and solvates thereof to treat a disorder responsive to the blockade of one or more sodium channels. In one embodiment, compounds of the present disclosure are useful for treating pain.
摘要翻译：本公开内容提供式I的嘧啶及其药学上可接受的盐和溶剂化物，其中A1，X，A2，G，Y，n，R2a，R2b和R3如说明书所述定义。本公开还涉及式I化合物及其药学上可接受的盐和溶剂合物用于治疗对一种或多种钠通道阻断作出反应的病症。在一个实施方案中，本公开的化合物可用于治疗疼痛。

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