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1. 发明授权

US06432980B1 Aliphatic amine substituted piperidyl diaryl pyrrole derivatives as antiprotozoal agents 失效
标题翻译：脂肪族胺取代的哌啶基二芳基吡咯衍生物作为抗原虫剂
公开(公告)号：US06432980B1
公开(公告)日：2002-08-13
申请号：US09710165
申请日：2000-11-10
申请人： Tesfaye Biftu , Danqing D. Feng , Gui-Bai Liang , Mitree M. Ponpipom , Xiaoxia Qian , Narindar Girotra , Michael H. Fischer , Matthew J. Wyvratt
发明人： Tesfaye Biftu , Danqing D. Feng , Gui-Bai Liang , Mitree M. Ponpipom , Xiaoxia Qian , Narindar Girotra , Michael H. Fischer , Matthew J. Wyvratt
IPC分类号： A61K314523
CPC分类号： C07D401/14 , A61K31/4545 , C07D413/14 , Y02A50/491
摘要： Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.
摘要翻译：三取代吡咯是可用于治疗和预防人类和动物中的原生动物疾病的抗原虫剂，包括控制家禽中的球虫病。

2. 发明授权

US5019568A Steroidal glycolipids as host resistance stimulators against viral infection 失效
标题翻译：甾体糖脂作为抗病毒感染的宿主抗性刺激物
公开(公告)号：US5019568A
公开(公告)日：1991-05-28
申请号：US370058
申请日：1989-06-21
申请人： Philippe L. Durette , William K. Hagmann , Mitree M. Ponpipom
发明人： Philippe L. Durette , William K. Hagmann , Mitree M. Ponpipom
IPC分类号： A61K33/24 , A61K35/54
CPC分类号： A61K31/704 , A61K31/70 , A61K33/24
摘要： Disclosed are pharmaceutical compositions for enhancing human host resistance against opportunistic infection in an individual immunocompromised by an AIDS-related virus, consisting essentially of an anti-viral, anti-AIDS drug selected from the group consisting of ansamycin, ribavirin, dideoxycitidine, HPA-23, AL-721, foscarnet, and azidothymidine and a glycolipid compound consisting essentially of the formula: ##STR1## where: R.sup.1 is .alpha. or .beta.-D-1-thiomannopyranoside, .alpha. or .beta.-L-1-thiofucopyranoside.
摘要翻译：公开了用于增强人宿主对由艾滋病相关病毒免疫受损的个体的机体感染抵抗力的药物组合物，其基本上由选自安莎霉素，利巴韦林，双脱氧胞苷，HPA-23的抗病毒，抗艾滋病药物组成，AL-721，膦甲酸和叠氮胸苷和基本上由下式组成的糖脂化合物：其中：R1是α或β-D-1-硫代吗喃吡喃糖苷，α或β-L1-硫代吡喃葡萄糖苷。

3. 发明授权

US4310505A Lipid vesicles bearing carbohydrate surfaces as lymphatic directed vehicles for therapeutic and diagnostic substances 失效
标题翻译：含有碳水化合物表面的脂质囊泡作为治疗和诊断物质的淋巴导向载体
公开(公告)号：US4310505A
公开(公告)日：1982-01-12
申请号：US92342
申请日：1979-11-08
申请人： John D. Baldeschwieler , Ronald C. Gamble , Marcia R. Mauk , Tsung-Ying Shen , Mitree M. Ponpipom
发明人： John D. Baldeschwieler , Ronald C. Gamble , Marcia R. Mauk , Tsung-Ying Shen , Mitree M. Ponpipom
IPC分类号： A61K51/00 , A61K9/127 , A61K47/00 , A61K49/00 , A61K43/00 , B01J13/00
CPC分类号： A61K9/1272 , A61K9/127 , A61K9/1271 , Y10T428/2984
摘要： Lipid vesicles comprising a lipid bilayer which includes analogs of cell-surface receptors such as dicetyl phosphate; stearylamine; 6-(5-cholesten-3.beta.-yloxy) hexyl 1-thio-.beta.-L-fucopyranoside; 6-(5-cholesten-3.beta.-yloxy) hexyl 1-thio-.beta.-D-galactopyranoside; 6-(5-cholesten-3.beta.-yloxy)hexyl 1-thio-.alpha.-D-mannopyranoside; 6-(5-cholesten-3-yloxy)hexyl 2-acetamido-2-deoxy-1-thio-.beta.-D-galactopyranoside; 6-(5-cholesten-3.beta.-yloxy)hexyl 6-amino-6-deoxy-1-thio-.beta.-D-galactopyranoside; or 6-(5-cholesten-3.beta.-yloxy)hexyl 6-amino-6-deoxy-1-thio-.alpha.-D-mannopyranoside; cholesterol and distearoyl phospatidylcholine, and an effective amount of physiologically compatible radioactive tracer, cytotoxic or therapeutic agent as a part of the vesicles. The vesicles of this invention can be administered to the human host and have been found to release the contents of the vesicles in a predetermined manner, i.e., controlled release, and in some cases, to be rapidly concentrated in the lymphatic system and/or liver, lungs or spleen of the host.
摘要翻译：包含脂质双层的脂质囊泡，其包括细胞表面受体的类似物，例如磷酸二鲸蜡酯; 硬脂胺 6-（5-胆甾烯-3β-氧代）己基1-硫代-β-L-吡喃葡萄糖苷; 6-（5-胆甾烯-3β-氧基）己基1-硫代-β-D-吡喃半乳糖苷; 6-（5-胆甾烯-3β-氧基）己基1-硫代-α-D-吡喃甘露糖苷; 6-（5-胆甾烯-3-基氧基）己基2-乙酰氨基-2-脱氧-1-硫代-β-D-吡喃半乳糖苷; 6-（5-胆甾烯-3β-氧基）己基6-氨基-6-脱氧-1-硫代-β-D-吡喃半乳糖苷; 或6-（5-胆甾烯-3β-氧基）己基6-氨基-6-脱氧-1-硫代-α-D-吡喃甘露糖苷; 胆固醇和二硬脂酰磷脂酰胆碱，以及有效量的生理相容的放射性示踪剂，细胞毒性剂或治疗剂作为囊泡的一部分。本发明的囊泡可以施用于人宿主，并且已经被发现以预定的方式（即控制释放）释放囊泡的内容物，并且在一些情况下快速浓缩在淋巴系统和/或肝脏中，肺或脾脏的主机。

4. 发明授权

US4970199A Steroidal glycolipids as host resistance stimulators against viral infection 失效
标题翻译：甾体糖脂作为抗病毒感染的宿主抗性刺激物
公开(公告)号：US4970199A
公开(公告)日：1990-11-13
申请号：US378424
申请日：1989-07-10
申请人： Philippe L. Durette , William K. Hagmann , Mitree M. Ponpipom
发明人： Philippe L. Durette , William K. Hagmann , Mitree M. Ponpipom
IPC分类号： C07J31/00 , C07J41/00
CPC分类号： A61K31/704 , C07J31/006 , C07J41/005 , C07J41/0088 , Y10S514/885
摘要： Disclosed are steroidal derivatives of glycolipids, in which steroids are bridged, via a medium length hydrocarbon chain, to 1-thio-D-mannopyranoses or 1-thio-L-fucopyranoses in combination with an anti-AIDS drug, that protect an immunocomprimised hot, particularly resulting from an AIDS-related virus, against opportunistic infection.
摘要翻译：公开了通过中等长度的烃链将类固醇桥连的糖脂的类固醇衍生物与抗艾滋病药物组合的1-硫代-D-甘露吡喃糖或1-硫代-L-吡喃葡萄糖，保护免疫抑制热特别是与艾滋病相关的病毒引起的机会性感染。

5. 发明授权

US4554349A Aralkyl and aralkenyl glycosides as inhibitors of antigen-specific T-cell proliferation 失效
标题翻译：芳烷基和芳烯基糖苷作为抗原特异性T细胞增殖的抑制剂
公开(公告)号：US4554349A
公开(公告)日：1985-11-19
申请号：US540594
申请日：1983-10-11
申请人： Mitree M. Ponpipom , Tsung-Ying Shen , Robert L. Bugianesi
发明人： Mitree M. Ponpipom , Tsung-Ying Shen , Robert L. Bugianesi
IPC分类号： C07H15/18 , C07H5/06
CPC分类号： C07H15/18
摘要： The invention disclosed herein relates to novel 1-deoxyglycosides, preferably 1-deoxy-D-mannopyranosides and 1-deoxy-L-rhamnopyranosides, having in the 1-position of the pyranose ring an aralkylthio/aralkenylthio, aralkyloxy/aralkenyloxy or aralkanoylamino/aralkenoylamino substituent; and to novel processes for preparing these 1-substituted-1-deoxyglycosides starting with the corresponding tetra-O-acetylglycopyranosyl bromide or amine. The 6-hydroxy group of 1-substituted-1 deoxyglycopyranosides can also be replaced by other functional groups. These aralkylthio/aralkenylthio, aralkyloxy/aralkenyloxy and aralkanoylamino/aralkenoylamino 1-deoxyglycosides are potent inhibitors of antigen-specific T-cell proliferation and are also useful as inhibitors of delayed-type hypersensitivity reactions.
摘要翻译：本文公开的本发明涉及新的1-脱氧糖苷，优选1-脱氧-D-甘露吡喃糖苷和1-脱氧-L-鼠李糖吡喃糖苷，其在吡喃糖环的1-位具有芳烷硫基/芳烯基硫基，芳烷氧基/芳烯基氧基或芳烷酰氨基/芳烯基酰氨基取代基; 以及由相应的四-O-乙酰基吡喃葡糖基溴或胺开始制备这些1-取代-1-脱氧糖苷的新方法。 1-取代-1脱氧吡喃糖苷的6-羟基也可以被其它官能团取代。这些芳烷硫基/芳烯基硫基，芳烷氧基/芳烯基氧基和芳烷酰氨基/芳烯酰氨基-1-脱氧糖苷是抗原特异性T细胞增殖的有效抑制剂，也可用作延迟型超敏反应的抑制剂。

6. 发明授权

US4301152A Immunologic adjuvant 失效
标题翻译：免疫佐剂
公开(公告)号：US4301152A
公开(公告)日：1981-11-17
申请号：US88692
申请日：1979-10-26
申请人： Mitree M. Ponpipom
发明人： Mitree M. Ponpipom
IPC分类号： C07H19/04 , A61K39/39 , C07H15/14 , C07H19/044 , C07J31/00 , C07J41/00 , C07J43/00 , A61K31/575 , C07J9/00
CPC分类号： C07H15/14 , C07H19/044 , C07J41/0055 , C07J41/0088 , C07J43/003
摘要： Immunologic adjuvants are obtained by the synthesis of 6-(5-cholesten-3.beta.-yloxy)hexyl 6-amino-6-deoxy-1-thio-.beta.-D-galactopyranoside and its 6-deoxy-6-oleamido derivative.
摘要翻译：通过合成6-（5-胆甾烯-3β-氧代）己基6-氨基-6-脱氧-1-硫代-β-D-吡喃半乳糖苷及其6-脱氧-6-油酰氨基衍生物获得免疫佐剂。

7. 发明授权

US4228274A 1-Substituted glycopyranosides 失效
标题翻译： 1-取代的吡喃糖苷
公开(公告)号：US4228274A
公开(公告)日：1980-10-14
申请号：US922897
申请日：1978-07-10
申请人： Mitree M. Ponpipom , Robert L. Bugianesi , Philippe L. Durette , Howard M. Katzen , Tsung-Ying Shen
发明人： Mitree M. Ponpipom , Robert L. Bugianesi , Philippe L. Durette , Howard M. Katzen , Tsung-Ying Shen
IPC分类号： C07H13/04 , C07H15/04 , C07H15/14 , C07H5/06 , C07H5/08
CPC分类号： C07H13/04 , C07H15/04 , C07H15/14
摘要： The invention disclosed herein relates to novel 1-deoxy-glycopyranosides, preferably 1-deoxy-D-mannopyranosides, having in the 1-position of the pyranoside ring an .omega.-aminoalkylthio, .omega.-aminoalkyloxy or .omega.-aminoalkanoylamino substituent; and to novel processes for preparing these 1-substituted-1-deoxy-glycopyranosides starting with the corresponding tetra-O-acetyl-glycopyranosyl bromide or amine. These .omega.-amino(alkylthio, alkyloxy or alkanoylamino)-1-deoxy-glycopyranosides, and in particular 1-[(6'-aminohexyl)thio or oxy]-1-deoxy-D-mannopyranosides, possess insulin-like activity.
摘要翻译：本文公开的本发明涉及在吡喃糖苷环的1位具有ω-氨基烷硫基，ω-氨基烷氧基或ω-氨基烷酰基氨基取代基的1-脱氧-D-甘露吡喃糖苷类的新型1-脱氧-D-吡喃甘露糖苷，以及由相应的四-O-乙酰基 - 吡喃葡糖基溴或胺开始制备这些1-取代-1-脱氧 - 糖吡喃糖苷的新方法。这些ω-氨基（烷硫基，烷氧基或烷酰氨基）-1-脱氧 - 糖吡喃糖苷，特别是1 - [（6'-氨基己基）硫代或氧基] -1-脱氧-D-甘露吡喃糖苷类，具有胰岛素样活性。

8. 发明授权

US4977146A 2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists 失效
标题翻译： 2,5-二芳基四氢呋喃及其类似物作为PAF拮抗剂
公开(公告)号：US4977146A
公开(公告)日：1990-12-11
申请号：US505712
申请日：1990-04-11
申请人： Tesfaye Biftu , Mitree M. Ponpipom , Nirindar N. Girotra
发明人： Tesfaye Biftu , Mitree M. Ponpipom , Nirindar N. Girotra
IPC分类号： A61K31/34 , A61K31/341 , A61K31/67 , A61P1/04 , A61P7/02 , A61P9/02 , A61P11/00 , A61P11/08 , A61P29/00 , A61P37/06 , A61P37/08 , C07D20060101 , C07D307/12 , C07F9/09 , C07F9/655
CPC分类号： C07D307/12
摘要： The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group, Y is an alkyl or substituted alkyl group, R.sup.6 is an alkyl or a substituted alkyl group and the substituents at positions 3, 4 or 5 are acyclic.

9. 发明授权

US4761404A Phospholipid analogs useful as PAF synthesis inhibitors 失效
标题翻译：磷脂类似物可用作PAF合成抑制剂
公开(公告)号：US4761404A
公开(公告)日：1988-08-02
申请号：US750435
申请日：1985-07-01
申请人： Robert L. Bugianesi , Mitree M. Ponpipom , Kathleen M. Rupprecht
发明人： Robert L. Bugianesi , Mitree M. Ponpipom , Kathleen M. Rupprecht
IPC分类号： C07D521/00 , A61K31/10 , A61K31/13 , A61K31/16 , A61K31/17 , A61K31/27 , A61K31/275 , A61K31/33 , A61K31/445 , A61K31/575 , A61K31/655 , A61K31/66 , A61K31/675 , A61K31/685 , A61P7/02 , A61P9/08 , A61P9/10 , A61P11/00 , A61P25/04 , A61P29/00 , A61P43/00 , C07C45/29 , C07C49/255 , C07C67/00 , C07C313/00 , C07C317/18 , C07C317/44 , C07C325/00 , C07C381/00 , C07F9/09 , C07F9/10 , C07F9/32 , C07F9/38 , C07F9/40 , C07F9/572 , C07F9/58 , C07F9/6533 , C07J9/00
CPC分类号： C07F9/6533 , C07C45/292 , C07C49/255 , C07F9/091 , C07F9/10 , C07F9/5722 , C07F9/581
摘要： There are disclosed phospholipid analogs which are useful as PAF synthesis inhibitors. These compounds inhibit PAF (platelet-activating factor) biosynthesis and are thereby useful in the treatment of various diseases or disorders mediated by the PAF such as, for example, pain, fever, inflammation, cardiovascular disorder, asthma, lung edema, allergic disorders, skin diseases, psoriasis, and adult respiratory distress syndrome.
摘要翻译：公开了可用作PAF合成抑制剂的磷脂类似物。这些化合物抑制PAF（血小板活化因子）生物合成，从而可用于治疗由PAF介导的各种疾病或病症，例如疼痛，发烧，炎症，心血管疾病，哮喘，肺水肿，过敏性疾病，皮肤病，牛皮癣和成人呼吸窘迫综合征。

10. 发明授权

US4652637A Steroidal glycolipids 失效
标题翻译：类固醇糖脂
公开(公告)号：US4652637A
公开(公告)日：1987-03-24
申请号：US801905
申请日：1985-11-25
申请人： William K. Hagmann , Mitree M. Ponpipom
发明人： William K. Hagmann , Mitree M. Ponpipom
IPC分类号： A61K31/56 , A61P37/04 , C07J31/00 , C07J41/00 , C07J9/00
CPC分类号： A61K31/704 , C07J31/006 , C07J41/0088
摘要： Described are derivatives of glycolipids with substituted steroids bridged via a medium length hydrocarbon chain to 1-thio-D-mannopyranoses or 1-thio-L-fucopyranoses. These compounds protect an immunocompromised human or animal host against opportunistic infection by virtue of their immunostimulant properties.
摘要翻译：描述的是具有通过中等长度烃链桥连到1-硫代-D-甘露吡喃糖或1-硫代-L-吡喃葡萄糖的取代类固醇的糖脂的衍生物。这些化合物通过其免疫刺激性质保护免疫受损的人或动物宿主免受机会性感染。

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