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1. 发明专利

AU2002224064B2 Substituted benzene derivatives or salts thereof 未知
公开(公告)号：AU2002224064B2
公开(公告)日：2005-12-08
申请号：AU2002224064
申请日：2001-11-21
申请人： ASTELLAS PHARMA INC
发明人： SUGASAWA KEIZO , KADOKURA TAKESHI , HIRAYAMA FUKUSHI , SHIGENAGA TAKESHI , ISHIHARA TSUKASA , KOGA YUJI
IPC分类号： A61P7/02 , A61P9/10 , C07D211/26 , C07D401/12 , C07D401/14 , C07H15/203 , C07H15/26 , A61K031/501 , A61K031/4545 , C07D405/12 , A61K031/7052 , C07D417/12 , A61K031/706 , C07H015/26 , A61P007/02 , A61K031/454 , A61K031/551 , C07D413/12 , A61P009/10 , A61K031/506 , C07D405/14 , A61K031/445
摘要： There are provided compounds having an anticoagulant action on the basis of inhibition of activated blood coagulation factor X and being useful as anticoagulants or preventive/therapeutic agents for diseases induced by thrombosis or embolism. Effective ingredients are the compounds such as 4'-bromo-2'-Ä(5-chloro-2-pyridyl)carbamoyl)-6- beta -D-galactopyranosyloxy-1-isopropylpiperidine-4-carboxanilide, 2'-(2-acetamido-2-deoxy- beta -D-glucopyranosyloxy)-4'-bromo-6'-Ä(5-chloro-2-pyridyl)carbamoylÜ-1-is opropylpiperidine-4-carboxanilide, etc. or salts thereof.

2. 发明申请

US20040266997A1 Degradation products of azithromycin, and methods for their indentification 审中-公开
标题翻译：阿奇霉素降解产品及其鉴定方法
公开(公告)号：US20040266997A1
公开(公告)日：2004-12-30
申请号：US10809065
申请日：2004-03-25
发明人： Michael Pesachovich , Sarah Isaacs , Claude Singer , Eduard Schwartz , Edit Berger
IPC分类号： A61K031/7052 , C07H017/08
CPC分类号： C07H17/08
摘要： The invention is directed to degradation products of azithromycin, methods for the preparation and identification of the degradation products which may be produced during storage and/or synthesis of azithromycin.

3. 发明申请

US20040226852A1 Method of stabilizing azithromycin 审中-公开
标题翻译：稳定阿奇霉素的方法
公开(公告)号：US20040226852A1
公开(公告)日：2004-11-18
申请号：US10782047
申请日：2004-02-19
发明人： Michael Pesachovich , Sarah Isaacs , Claude Singer , Eduard Schwartz , Edit Berger
IPC分类号： B65D001/09 , B65D083/04 , B65D085/42 , A61K031/7052
CPC分类号： C07H17/08
摘要： A method of packaging of azithromycin which provides improved stability of azithromycin upon storage.
摘要翻译：包装阿奇霉素的方法，其提供阿奇霉素在储存时的改善的稳定性。

4. 发明申请

US20040214782A1 Treatment or prevention of coccidiosis 审中-公开
标题翻译：治疗或预防球虫病
公开(公告)号：US20040214782A1
公开(公告)日：2004-10-28
申请号：US10437312
申请日：2003-05-13
发明人： Peter C. Canning , Renee L. Hassfurther , Nigel A. Evans
IPC分类号： A61K031/7052
CPC分类号： A61K31/7052 , A61K31/70
摘要： Coccidiosis in a bovine animal is prevented by administration of an effective amount of a macrolide antibiotic.
摘要翻译：通过施用有效量的大环内酯类抗生素来防止牛动物中的球虫病。

5. 发明申请

US20040138171A1 Use of glycyrrhizin and its derivatives as MCP-1 production inhibitors 失效
标题翻译：甘草甜及其衍生物作为MCP-1生产抑制剂的使用
公开(公告)号：US20040138171A1
公开(公告)日：2004-07-15
申请号：US10694616
申请日：2003-10-23
发明人： Fujio Suzuki , Makiko Kobayashi , Tokuichiro Utsunomiya , Hiroatsu Matsumoto , Midori Takeda , Shigemi Iwata
IPC分类号： A61K031/7052 , A61K031/473
CPC分类号： A61K31/473 , A61K31/57 , A61K31/704 , A61K31/7052
摘要： The object of the present invention is to provide the use of glycyrrhizin and its derivatives for inhibition of MCP-1 production. The present invention discloses an MCP-1 production inhibition method and pharmaceutical composition for the same comprising administration of glycyrrhizin and its derivatives in an amount effective for said inhibition to mammals in which migration of monocytes or T lymphocytes is increased, or production of IL-10 is increased, and inhibition of said increase is desired.
摘要翻译：本发明的目的是提供甘草甜素及其衍生物用于抑制MCP-1产生的用途。本发明公开了一种MCP-1产生抑制方法及其药物组合物，其含有对所述抑制单核细胞或T淋巴细胞迁移的哺乳动物有效量的甘草甜素及其衍生物的给药量，或产生IL-10 增加，并且希望抑制所述增加。

6. 发明申请

US20040092460A1 Novel amorphous 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A, process for preparing the same, and uses thereof 失效
标题翻译：新型无定形9-脱氧-9a-氮杂-9a-甲基-9a-高红霉素A，其制备方法及其用途
公开(公告)号：US20040092460A1
公开(公告)日：2004-05-13
申请号：US10624911
申请日：2003-07-21
申请人： Pliva Pharmaceutical Industry, Incorporated
发明人： Miljenko Dumic , Mladen Vinkovic , Marina Oresic , Ernest Mestrovic , Aleksandar Danilovski , Alojz Dumbovic , Knezevic Zdravka , Gorjana Lazarevski , Darko Filic , Dominik Cincic , Katica Lazaric , Dejan-Kresimir Bucar
IPC分类号： C07H017/08 , A61K031/7052
CPC分类号： C07H17/08
摘要： Substantially pure amorphous 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A. In addition, this disclosure is directed to a process for the preparation thereof from crude 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A via orthorhombic isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A, of the general formula I 1 wherein S represents a water-miscible or water-immiscible organic solvent, characterized by the orthorhombic space group P212121, with average unit cell parameters anull8.2 to 9.7 null, bnull11.5 to 13.5 null, cnull44.5 to 47.0 null, nullnullnullnullnullnull90null, wherein a, b and c represent the crystal axes lengths and null, null and null represent the angles between the crystal axes. In addition, pharmaceutical compositions containing the substantially pure amorphous 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A are disclosed, as well as a method for the treatment of bacterial and protozoal infections, and inflammation related diseases in humans and animals by administration of a pharmaceutical composition containing same.
摘要翻译：基本上纯的无定形9-脱氧-9a-氮杂-9a-甲基-9a-高红霉素A.此外，本发明涉及一种由9-脱氧-9a-氮杂-9a-甲基-9a- 通过通式I的9-脱氧-9a-氮杂-9a-甲基-9a-高红霉素A的斜方晶异构体假结构的异红霉素A，其中S表示与水可混溶或水不混溶的有机溶剂，其特征在于斜方形空间群P212121 ，平均晶胞参数a = 8.2至9.7，b = 11.5至13.5，c = 44.5至47.0，α=β=γ= 90°，其中a，b和c表示晶轴长度和α， β和γ表示晶轴之间的角度。此外，公开了含有基本上纯的无定形9-脱氧-9a-氮杂-9a-甲基-9a-高红霉素A的药物组合物，以及用于治疗细菌和原生动物感染以及与人类发生炎症有关的疾病的方法动物通过施用含有它们的药物组合物。

7. 发明申请

US20040053862A1 Macrolide solvates 失效
标题翻译：大环内酯类溶剂化物
公开(公告)号：US20040053862A1
公开(公告)日：2004-03-18
申请号：US10432545
申请日：2003-10-10
发明人： Victor Centellas , Jose Diago , Rafael Garcia , Johannes Ludescher
IPC分类号： A61K031/7052 , C07H017/08
CPC分类号： C07H17/08 , Y10S514/927
摘要： Azithromycin in the form of a monohydrate comprising from 4.0% to 6.5% of water, a process for its preparation and its use in pharmaceutical compositions.
摘要翻译：含有4.0％至6.5％水的一水合物形式的阿奇霉素，其制备方法及其在药物组合物中的应用。

8. 发明申请

US20040053861A1 6,11-Bicyclic erythromycin derivatives 有权
标题翻译： 6,11-双环红霉素衍生物
公开(公告)号：US20040053861A1
公开(公告)日：2004-03-18
申请号：US10436622
申请日：2003-05-13
发明人： Yat Sun Or , Guoqiang Wang , Ly Tam Phan , Deqiang Niu , Yao-Ling Qiu , Nha Huu Vo , Jay Judson Farmer , Ying Hou
IPC分类号： A61K031/7048 , A61K031/7052 , C07H017/08
CPC分类号： C07H17/08
摘要： The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: 1 which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
摘要翻译：本发明公开了式I化合物或其药学上可接受的盐，酯或前药：其表现出抗菌性质。本发明还涉及包含上述化合物的药物组合物，用于给予需要抗生素治疗的受试者。本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的细菌感染的方法。本发明还包括制备本发明化合物的方法。

9. 发明申请

US20040053854A1 Process for preparation of 4,5-Epoxymorphinan-6-oxyglucuronides 审中-公开
标题翻译：制备4,5-环氧吗啡喃-6-氧基葡糖苷酸的方法
公开(公告)号：US20040053854A1
公开(公告)日：2004-03-18
申请号：US10660474
申请日：2003-09-12
申请人： Cenes Limited
发明人： Arie L. Gutman , Genadi Nisnevitch , Lev Yudovitch , Igor Rokhman
IPC分类号： A61K031/7052 , C07H017/02
CPC分类号： C07H17/08
摘要： Conjugation of 4,5-Epoxymorphinan-6-ols with Bromoglucuronides in the presence of Zinc containing compounds as activator under conditions capable of forming 4,5-Epoxymorphinan-6-oxyglucuronides is disclosed. This novel approach provides an efficient method for preparation of both anomers of 4,5-Epoxymorphinan-6-oxyglucuronides. The deprotected end products are useful as analgesic agents.
摘要翻译：公开了在能够形成4,5-环氧基吗啡喃-6-氧基葡糖苷酸的条件下，在含锌化合物作为活化剂的情况下，将4,5-环氧吗啡喃-6-ols与溴葡萄糖苷酸缀合。这种新方法提供了一种制备4,5-环氧吗啡喃-6-氧基葡糖苷酸的两种端基异构体的有效方法。去保护的最终产物可用作止痛剂。

10. 发明申请

US20040029820A1 Derivatives of monosaccharides as cell adhesion inhibitors 失效
标题翻译：单糖衍生物作为细胞粘附抑制剂
公开(公告)号：US20040029820A1
公开(公告)日：2004-02-12
申请号：US10611386
申请日：2003-07-01
发明人： Sudershan K. Arora , Nawal Kishore
IPC分类号： A61K031/7052 , C07H001/00
CPC分类号： C07H9/04
摘要： This invention relates generally to compounds and processes for synthesizing derivatives of 2-3-O-isopropylidene-null-L-xylo-2-hexulofuranosonic acid. The compounds of this invention are useful, inter-alia, for the inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies, including inflammatory and autoimmune diseases, such as bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection and psoriasis. This invention also relates to pharmacological compositions containing derivatives of 2-3-O-isopropylidene-null-L-xylo-2-hexulofuranosonic acid and the methods of treating such pathologies as listed above.
摘要翻译：本发明一般涉及用于合成2-3-O-异亚丙基-α-L-木糖-2-己二硼酸的衍生物的化合物和方法。本发明的化合物尤其用于抑制和预防细胞粘附和细胞粘附介导的病理学，包括炎性和自身免疫性疾病，例如支气管哮喘，类风湿性关节炎，I型糖尿病，多发性硬化，同种异体移植排斥和牛皮癣。本发明还涉及含有2-3-O-异亚丙基-α-L-木糖-2-己二酮酸的衍生物的药理学组合物和治疗上述病理学的方法。

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