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21. 发明申请

US20050283005A1 PNA monomer and precursor 有权
公开(公告)号：US20050283005A1
公开(公告)日：2005-12-22
申请号：US11183034
申请日：2005-07-15
申请人： Sung Kim , Hyunil Lee , Jong Lim , Hoon Choi , Jae Jeon , Sang Ahn , Sung Lee , Won Yoon
发明人： Sung Kim , Hyunil Lee , Jong Lim , Hoon Choi , Jae Jeon , Sang Ahn , Sung Lee , Won Yoon
IPC分类号： C12N15/09 , A61K31/513 , A61K31/52 , C07D277/80 , C07D405/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D473/02 , C07D473/18 , C07D473/32 , C07D473/34
CPC分类号： C07D417/04 , C07B2200/11 , C07D277/80 , C07D417/12 , C07D417/14 , Y02P20/55
摘要： This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R′; J is sulfur or oxygen; R′, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural α-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.

22. 发明申请

US20050250786A1 PNA monomer and precursor 有权
标题翻译： PNA单体和前体
公开(公告)号：US20050250786A1
公开(公告)日：2005-11-10
申请号：US11183025
申请日：2005-07-15
申请人： Sung Kim , Hyunil Lee , Jong Lim , Hoon Choi , Jae Jeon , Sahn Ahn , Sung Lee , Won Yoon
发明人： Sung Kim , Hyunil Lee , Jong Lim , Hoon Choi , Jae Jeon , Sahn Ahn , Sung Lee , Won Yoon
IPC分类号： C12N15/09 , A61K31/513 , A61K31/52 , C07D277/80 , C07D405/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D473/02 , C07D473/18 , C07D473/32 , C07D473/34 , C07D43/14
CPC分类号： C07D417/04 , C07B2200/11 , C07D277/80 , C07D417/12 , C07D417/14 , Y02P20/55
摘要： This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R′; J is sulfur or oxygen; R′, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrite, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural α-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.
摘要翻译：本申请涉及用于制备PNA（肽核酸）寡聚体的通式（I）的单体，并提供合成预定义的序列PNA寡聚体和随机序列PNA寡聚体的方法：其中E为氮或C-R' ; J为硫或氧; R'，R 1，R 2，R 3，R 4独立地为H，卤素，烷基，硝基，亚硝酸根，烷氧基，卤代烷基，卤代烷氧基，苯基或卤代苯基，R 5为H或保护或未保护的天然或非天然α- 氨基酸; 并且B是天然或非天然核碱基，其中当所述核碱基具有环外氨基功能时，所述功能受到在硫醇存在下对酸不稳定但对弱至中碱稳定的保护基保护。

23. 发明申请

US20050182077A1 Xanthine phosphodiesterase V inhibitors 审中-公开
公开(公告)号：US20050182077A1
公开(公告)日：2005-08-18
申请号：US11078999
申请日：2005-03-11
申请人： Samuel Chackalamannil , Yuguang Wang , Craig Boyle , Andrew Stamford
发明人： Samuel Chackalamannil , Yuguang Wang , Craig Boyle , Andrew Stamford
IPC分类号： A61K31/522 , A61K45/00 , A61P1/00 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/00 , A61P13/12 , A61P15/00 , A61P27/06 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D473/02 , C07D473/04 , C07D473/06 , C07D473/08 , C07F7/18
CPC分类号： C07D473/04 , C07D473/06 , C07D473/08
摘要： A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders: For example, a representative compound of the invention is:

24. 发明申请

US20050148606A1 Heterocyclic compounds that are inhibitors of the enzyme DPP-IV 失效
标题翻译：作为DPP-IV酶抑制剂的杂环化合物
公开(公告)号：US20050148606A1
公开(公告)日：2005-07-07
申请号：US11070056
申请日：2005-03-02
申请人： Anders Kanstrup , Christian Sams , Jane Lundbeck , Lise Christiansen , Marit Kristiansen
发明人： Anders Kanstrup , Christian Sams , Jane Lundbeck , Lise Christiansen , Marit Kristiansen
IPC分类号： A61P3/10 , C07D473/00 , C07D473/02 , A61K31/522 , A61K31/55
CPC分类号： C07D473/00 , C07D473/02
摘要： The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV of formula I, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity.
摘要翻译：本发明涉及式I的DPP-IV酶的治疗活性和选择性抑制剂，包含该化合物的药物组合物和这些化合物在制备用于治疗与被灭活的蛋白质相关的疾病的药物中的用途通过DPP-IV，如2型糖尿病和肥胖。

25. 发明申请

US20050130969A1 4'-Thio-L-xyloy furanosyl nucleosides, precursors thereof, preparation and use thereof 有权
标题翻译： 4'-硫代-L-木糖呋喃糖基核苷，其前体，其制备和用途
公开(公告)号：US20050130969A1
公开(公告)日：2005-06-16
申请号：US11045085
申请日：2005-01-31
申请人： John Secrist , Kamal Tiwari , John Montgomery
发明人： John Secrist , Kamal Tiwari , John Montgomery
IPC分类号： C07H19/06 , C07H19/16 , A61K31/53 , A61K31/4436 , A61K31/513 , A61K31/519 , A61K31/522 , C07D473/02 , C07D487/02 , C07D49/02
CPC分类号： C07H19/06 , A61K31/4436 , A61K31/519 , A61K31/522 , A61K31/53 , C07H19/16
摘要： Compounds represented by the formula 1: A is selected from the group consisting of wherein each R individually is H or acyl, Y is X, N3, NH2, monoalkylamino, or dialkylamino; Z is O or S; and X is selected from the group consisting of hydrogen, halo, hydroxy, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, thioaryl, thioalkyl, allylamino, cyano and nitro; tautomers thereof; and pharmaceutically acceptable salts thereof are provided along with methods for their fabrication. Various of these compounds can be used as anticancer agents, or antiviral agents or to inhibit DNA replication.
摘要翻译：由式1：A表示的化合物选自其中每个R各自为H或酰基，Y为X，N 3，NH 2，单烷基氨基，或二烷基氨基; Z是O或S; 烷基，卤代烷基，烯基，卤代烯基，炔基，氨基，一烷基氨基，二烷基氨基，硫代芳基，硫代烷基，烯丙基氨基，氰基和硝基; 互变异构体及其药学上可接受的盐及其制备方法。这些化合物中的各种可以用作抗癌剂，抗病毒剂或抑制DNA复制。

26. 发明授权

US06890926B2 Heteroaryl derivatives and their use as medicaments 失效
公开(公告)号：US06890926B2
公开(公告)日：2005-05-10
申请号：US09910141
申请日：2001-07-20
申请人： Peter Emig , Eckhard Günther , Jürgen Schmidt , Bernd Nickel , Bernhard Kutscher
发明人： Peter Emig , Eckhard Günther , Jürgen Schmidt , Bernd Nickel , Bernhard Kutscher
IPC分类号： C07D401/06 , A61K31/4709 , A61K31/496 , A61K31/513 , A61K31/53 , A61P35/00 , C07D215/50 , C07D219/04 , C07D473/02 , C07D401/14
CPC分类号： C07D401/06 , C07D215/50
摘要： The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.

27. 发明申请

US20050026939A1 Metabolite of xanthine phosphodiesterase 5 inhibitor and derivatives thereof useful for treatment of erectile dysfunction 失效
标题翻译：用于治疗勃起功能障碍的黄嘌呤磷酸二酯酶5抑制剂及其衍生物的代谢物
公开(公告)号：US20050026939A1
公开(公告)日：2005-02-03
申请号：US10901574
申请日：2004-07-29
申请人： Anima Ghosal , Wei Tong , Swapan Chowdhury , Shmuel Zbaida , Mark Wirth , Kevin Alton , James Patrick , Craig Boyle , Andrew Stamford
发明人： Anima Ghosal , Wei Tong , Swapan Chowdhury , Shmuel Zbaida , Mark Wirth , Kevin Alton , James Patrick , Craig Boyle , Andrew Stamford
IPC分类号： C07D473/06 , A61K31/522 , C07D473/02
CPC分类号： C07D473/06
摘要： The present invention is directed to a metabolite of a xanthine Phosphodiesterase type 5 inhibitor having the following structure derivatives, and formulations thereof, and processes for preparing the same. Further disclosed are methods of treating a physiological disorder, symptom or disease in a patient, comprising administering to the patient an effective amount of the above compound, wherein the physiological disorder, symptom or disease is a urogenital, cardiovascular, cerebrovascular or peripheral vascular disorder, angina pectoris, hypertension, restenosis post angioplasty, endarterectomy, stent introduction, cerebral stroke, a respiratory tract disorder such as an allergic condition associated with atopy, pulmonary hypertension, an ischemic heart disorder, impaired glucose tolerance, diabetes and its related complication, insulin resistance syndrome, hyperglycemia, polycystic ovarian syndrome, a glomerular disorder, renal insufficiency, nephritis, a tubular interstitial disorder, an autoimmune disorder, glaucoma, intestinal motility, cachexia or cancer.
摘要翻译：本发明涉及具有以下结构衍生物的黄嘌呤磷酸二酯酶5型抑制剂的代谢物及其制剂及其制备方法。进一步公开的是治疗患者的生理障碍，症状或疾病的方法，包括向患者施用有效量的上述化合物，其中所述生理障碍，症状或疾病是泌尿生殖系统，心血管，脑血管或外周血管疾病，心绞痛，高血压，血管成形术后再狭窄，内膜切除术，支架引入，脑中风，呼吸道疾病如与过敏相关的过敏性疾病，肺动脉高压，缺血性心脏病，糖耐量异常，糖尿病及其相关并发症，胰岛素抵抗综合征，高血糖症，多囊卵巢综合征，肾小球疾病，肾功能不全，肾炎，管状间质性疾病，自身免疫性疾病，青光眼，肠蠕动，恶病质或癌症。

28. 发明申请

US20040229887A1 Novel imidazopyrimidinyl and imidazopyri dinyl derivatives 有权
标题翻译：新型咪唑并嘧啶基和咪唑并二烯基衍生物
公开(公告)号：US20040229887A1
公开(公告)日：2004-11-18
申请号：US09738666
申请日：2000-12-15
发明人： Richard G. Wilde , Rajagopal Bakthavatchalam , James P. Beck , Argyrios Arvanitis
IPC分类号： A61K031/522 , A61K031/4745 , C07D471/02 , C07D473/02
CPC分类号： C07D471/04 , C07D473/00
摘要： Provided herein are compounds of the formula (I): 1 as well as stereoisomers and pharmaceutically acceptable salts thereof. Such compounds are, because of their ability to antagonize CRF, useful in the treatment of a variety of disorders characterized by execssive CRF expression. These include, for example: affective disorder, anxiety, depression, headache, irritable bowel syndrome, post-traumatic stress disorder, supranuclear palsy, immune suppression, Alzheimer's disease, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, gastrointestinal diseases, anorexia nervosa or other feeding disorder, drug addiction, drug or alcohol withdrawal symptoms, inflammatory diseases, cardiovascular or heart-related diseases, fertility problems, human immunodeficiency virus infections, hemorrhagic stress, obesity, infertility, head and spinal cord traumas, epilepsy, stroke, ulcers, amyotrophic lateral sclerosis and hypoglycemia.
摘要翻译：本文提供了式（I）的化合物：及其立体异构体及其药学上可接受的盐。因为这些化合物具有拮抗CRF的能力，其可用于治疗以执行性CRF表达为特征的多种疾病。这些包括例如：情感障碍，焦虑症，抑郁症，头痛，肠易激综合征，创伤后应激障碍，核核性麻痹，免疫抑制，阿尔茨海默病，亨廷顿氏病，帕金森病，肌萎缩性侧索硬化，胃肠道疾病，神经性厌食症或其他喂养障碍，药物成瘾，药物或酒精戒断症状，炎症性疾病，心血管疾病或心脏相关疾病，生殖问题，人体免疫缺陷病毒感染，出血性压力，肥胖症，不育症，头部和脊髓创伤，癫痫，中风，溃疡，肌萎缩性侧索硬化和低血糖。

29. 发明申请

US20040192708A1 Sulfonamide substituted xanthine derivatives 失效
标题翻译：磺酰胺取代黄嘌呤衍生物
公开(公告)号：US20040192708A1
公开(公告)日：2004-09-30
申请号：US10776697
申请日：2004-02-11
发明人： Peter W. Dunten , Louise H. Foley , Nicholas J. S. Huby , Sherrie L. Pietranico-Cole , Weiya Yun
IPC分类号： A61K031/522 , C07D473/02
CPC分类号： C07D473/04 , C07D473/06
摘要： The present invention is a sulfonamide substituted xanthine derivative of formula I 1 or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specification. Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.
摘要翻译：本发明是式I的磺酰胺取代的黄嘌呤衍生物或其药学上可接受的盐，其中R 1，R 2和R 3如说明书中所定义。式I化合物及其药学上可接受的盐或前药显示出作为糖异生的调节剂的活性。

30. 发明申请

US20040180897A1 Novel tyrosine kinase inhibitors 有权
标题翻译：新型酪氨酸激酶抑制剂
公开(公告)号：US20040180897A1
公开(公告)日：2004-09-16
申请号：US10751798
申请日：2004-01-05
发明人： Francis Beaulieu , Carl Ouellet , Kurt Zimmermann , Upender Velaparthi , Mark D. Wittman
IPC分类号： A61K031/522 , A61K031/502 , A61K031/498 , A61K031/4745 , C07D487/02 , C07D473/02
CPC分类号： C07D471/04 , C07D473/32 , C07D487/04
摘要： The present invention provides compounds of formula I 1 and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase enzymes thereby making them useful as anti-cancer agents.
摘要翻译：本发明提供式I化合物及其药学上可接受的盐。式I化合物抑制酪氨酸激酶，从而使其成为抗癌剂。

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