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公开(公告)号：US4082844A
公开(公告)日：1978-04-04
申请号：US696255
申请日：1976-06-15
IPC分类号： C07D241/16 , C07D241/24 , A61K31/495 , C07D241/10
CPC分类号： C07D241/24 , C07D241/16 , Y10S514/91
摘要： The compound 6-chloro-2-(1'-piperazinyl)pyrazine, its N-oxides and acid-addition salts are disclosed having pharmacological activity as anorexic agents.
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公开(公告)号：US4163849A
公开(公告)日：1979-08-07
申请号：US887693
申请日：1978-03-17
IPC分类号： C07D241/20 , A61K31/495 , C07D403/04
CPC分类号： C07D241/20 , Y10S514/91
摘要： Substituted piperazinylpyrazines and pharmaceutically acceptable salts thereof which have pharmacological activity as anorexigenic agents.
摘要翻译： 具有药理活性的取代哌嗪基吡嗪及其药学上可接受的盐作为厌食症剂。
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公开(公告)号：US4091101A
公开(公告)日：1978-05-23
申请号：US806898
申请日：1977-06-15
IPC分类号： C07D241/44 , A61K31/495 , A61P3/04 , A61P25/04 , A61P25/20 , A61P25/24 , A61P25/26 , C07D241/42 , C07D295/135 , C07D241/40
CPC分类号： C07D295/135 , C07D241/42
摘要： 6-(1-Piperazinyl)quinoxaline and pharmaceutically acceptable salts thereof have serotoninmimetic activity. It is prepared by reducing the nitro group of 1-(3-amino-4-nitrophenyl)piperazine followed by treatment with glyoxal.
摘要翻译： {PG，1,6-（1-哌嗪基）喹喔啉及其药学上可接受的盐具有5-羟色胺模拟活性。 通过还原1-（3-氨基-4-硝基苯基）哌嗪的硝基，然后用乙二醛处理制备。
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公开(公告)号：US4082845A
公开(公告)日：1978-04-04
申请号：US790362
申请日：1977-04-25
IPC分类号： A61K31/33 , A61P3/04 , A61P25/04 , A61P25/24 , A61P25/26 , C07D471/04 , A61K31/495 , C07D295/12
CPC分类号： C07D471/04 , Y10S514/91
摘要： 3-(1-Piperazinyl)-pyrido[2,3-b]pyrazines and pharmaceutically acceptable salts thereof have serotoninmimetic activity. They are prepared by treating 3-halo-pyrido[2,3-b]pyrazines with piperazine.
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公开(公告)号：US4078063A
公开(公告)日：1978-03-07
申请号：US726713
申请日：1976-09-24
IPC分类号： C07D213/74 , A61K31/495 , A61K31/50 , A61P3/04 , C07D20060101 , C07D295/12 , C07D401/04
CPC分类号： C07D401/12 , Y10S514/91
摘要： Compounds of the formula: ##STR1## and their N-oxides and acid-addition salts are disclosed having pharmacological activity as anorexic agents.
摘要翻译： 公开了具有下式的化合物：其具有作为厌食剂的药理活性的N-氧化物和酸加成盐。
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公开(公告)号：US5527819A
公开(公告)日：1996-06-18
申请号：US488957
申请日：1995-06-07
申请人： Theresa M. Williams , Terrence M. Ciccarone , Walfred S. Saari , John S. Wai , William J. Greenlee , Suresh K. Balani , Mark E. Goldman , Anthony D. Theoharides, deceased , Jacob M. Hoffman, Jr. , William C. Lumma, Jr. , Joel R. Huff , Clarence S. Rooney , Philip E. Sanderson
发明人： Theresa M. Williams , Terrence M. Ciccarone , Walfred S. Saari , John S. Wai , William J. Greenlee , Suresh K. Balani , Mark E. Goldman , Anthony D. Theoharides, deceased , Jacob M. Hoffman, Jr. , William C. Lumma, Jr. , Joel R. Huff , Clarence S. Rooney , Philip E. Sanderson
IPC分类号： C07D209/12 , C07D209/30 , C07D209/42 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D413/06 , C07D417/12 , C07D521/00 , A61K31/40
CPC分类号： C07D231/12 , C07D209/12 , C07D209/30 , C07D209/42 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D413/06 , C07D417/12
摘要： Novel indole compounds inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译： 新型吲哚化合物抑制HIV逆转录酶，可用于预防或治疗艾滋病毒和艾滋病感染，作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒药物结合使用，抗感染药物 ，免疫调节剂，抗生素或疫苗。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。
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公开(公告)号：US4081542A
公开(公告)日：1978-03-28
申请号：US774565
申请日：1977-03-04
IPC分类号： C07D241/16 , C07D241/20 , C07D241/24 , C07D295/12 , A61K31/495
CPC分类号： C07D241/24 , C07D241/16 , C07D241/20 , Y10S514/91
摘要： Compounds of the formula: ##STR1## and their N-oxides and acid-addition salts are disclosed having pharmacological activity as anorexic agents.
摘要翻译： 公开了具有下式的化合物：其具有作为厌食剂的药理活性的N-氧化物和酸加成盐。
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公开(公告)号：US5183815A
公开(公告)日：1993-02-02
申请号：US839741
申请日：1992-02-19
摘要： Described are new agents for treating bone disorders associated with a reduction in bone mass and abnormalities in bone resportion or bone formation including osteoporosis. Paget's disease, bone metastases and malignant hypercalcemia. The agents are hydroxyl containing steroidal hormones, having bone resportion antagonist or bone formation stimulatory activity, covalently linked through the hydroxyl group via a bond hydrolyzable in the human body, e.g. carbamate or carbonate, which is further covalently linked to an amino, or hydroxy substituted alkylidene-1,1-bisphosphonate, through the respective amino or hydroxy group. The alkyl bisphosphonate moiety confers bone affinity. The agent acts by delivering the steroidal hormone directly to the bone target site where it is released for bone resorption antagonist or bone formation stimulatory action by hydrolysis of the hydrolyzable covalent bond.
摘要翻译： 描述了用于治疗与骨量减少相关的骨疾病和骨代谢或包括骨质疏松症在内的骨形成异常的新药物。 佩吉特氏病，骨转移和恶性高钙血症。 所述试剂是含有甾体激素的羟基，具有骨重排拮抗剂或骨形成刺激活性，通过羟基通过在人体中可水解的键共价连接。 氨基甲酸酯或碳酸酯，其通过相应的氨基或羟基进一步共价连接到氨基或羟基取代的亚烷基-1,1-二膦酸盐。 双膦酸烷基酯部分赋予骨亲和力。 该试剂通过将甾体激素直接递送到其被释放用于骨吸收拮抗剂的骨靶部位或通过水解可共价键的骨形成刺激作用而起作用。
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公开(公告)号：US5028692A
公开(公告)日：1991-07-02
申请号：US343092
申请日：1989-04-25
申请人： Allen I. Oliff , Walfred S. Saari
发明人： Allen I. Oliff , Walfred S. Saari
IPC分类号： C07K7/02 , C07K7/08 , C07K14/575
CPC分类号： C07K7/02 , C07K14/57572 , C07K7/086
摘要： Small cell lung carcinoma cells (SCLC) contain gastrin releasing peptide (GRP) receptors. The response of the cells to GRP is rapid growth. We have found a group of peptide derivatives that act as GRP antagonists by blocking the binding of GRP to its receptor thereby inhibiting the growth of cells that are sensitive to the growth promoting activity of GRP.
摘要翻译： 小细胞肺癌细胞（SCLC）含有胃泌素释放肽（GRP）受体。 细胞对GRP的反应是快速增长。 我们已经发现一组作为GRP拮抗剂的肽衍生物通过阻断GRP与其受体的结合，从而抑制对GRP的生长促进活性敏感的细胞的生长。
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公开(公告)号：US4943561A
公开(公告)日：1990-07-24
申请号：US276985
申请日：1988-11-28
CPC分类号： C07K14/57572 , A61K38/00
摘要： Small cell lung carcinoma (SCLC) cells contain gastrin releasing peptide (GRP) receptors. The response of the cells to GRP is rapid growth. We have found a group of peptide derivatives that act as GRP antagonists by blocking the binding of GRP to its receptor thereby inhibiting the growth of cells that are sensitive to the growth promoting activity of GRP.
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