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1. 发明授权

US4707555A Prostaglandin intermediates 失效
标题翻译：前列腺素中间体
公开(公告)号：US4707555A
公开(公告)日：1987-11-17
申请号：US754101
申请日：1985-07-12
申请人： David L. Coffen , George W. Holland , W. Harry Mandeville , Perry Rosen , Frederick Wong
发明人： David L. Coffen , George W. Holland , W. Harry Mandeville , Perry Rosen , Frederick Wong
IPC分类号： C07C405/00 , C07D307/935 , C07D307/93
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0041
摘要： New optically active intermediates and processes thereto are provided for use in synthesizing therapeutically active prostaglandins of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; from a compound of the formula: ##STR2## wherein R.sup.1 is as above and R.sup.2 is hydrogen or a carboxy blocking group convertible to an acid by hydrolysis.
摘要翻译：提供新的光学活性中间体及其方法用于合成下式的治疗活性的前列腺素：其中R 1是氢或低级烷基; 由下式的化合物：其中R1如上所述，R2是氢或通过水解可转化成酸的羧基封端基团。

2. 发明授权

US4866205A Prostaglandin intermediates 失效
标题翻译：前列腺素中间体
公开(公告)号：US4866205A
公开(公告)日：1989-09-12
申请号：US218427
申请日：1988-07-11
申请人： David L. Coffen , George W. Holland , W. Harry Mandeville , Perry Rosen , Frederick Wong
发明人： David L. Coffen , George W. Holland , W. Harry Mandeville , Perry Rosen , Frederick Wong
IPC分类号： C07C405/00 , C07D307/935
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0041
摘要： New optically active intermediates and processes thereto are provided for use in synthesizing therapeutically active prostaglandins of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; from a compound of the formula: ##STR2## wherein R.sup.1 is as above and R.sup.2 is hydrogen or a carboxy blocking group convertible to an acid by hydrolysis.
摘要翻译：提供新的光学活性中间体及其方法用于合成下式的治疗活性的前列腺素：其中R 1是氢或低级烷基; 由下式的化合物：其中R1如上所述，R2是氢或通过水解可转化成酸的羧基封端基团。

3. 发明授权

US4558140A Cyclopenta[b]furan-2-ones 失效
标题翻译：环戊二烯并[b]呋喃-2-酮
公开(公告)号：US4558140A
公开(公告)日：1985-12-10
申请号：US586586
申请日：1984-03-06
申请人： David L. Coffen , George W. Holland , Perry Rosen , Frederick Wong
发明人： David L. Coffen , George W. Holland , Perry Rosen , Frederick Wong
IPC分类号： C07C405/00 , C07D307/935 , C07D307/93
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0041
摘要： New optically active intermediates and processes thereto are provided for use in synthesizing therapeutically active prostaglandins of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; from a compound of the formula: ##STR2## wherein R.sup.1 is as above and R.sup.2 is hydrogen or a carboxy blocking group convertible to an acid by hydrolysis.
摘要翻译：提供新的光学活性中间体及其方法用于合成下式的治疗活性的前列腺素：其中R 1是氢或低级烷基; 由下式的化合物：其中R1如上所述，R2是氢或通过水解可转化成酸的羧基封端基团。

4. 发明申请

US20120225890A1 COMPOUNDS, COMPOSITIONS AND METHODS FOR THE TREATMENT OF AMYLOID DISEASES AND SYNUCLEINOPATHIES SUCH AS ALZHEIMER'S DISEASE, TYPE 2 DIABETES AND PARKINSON'S DISEASE 失效
标题翻译：化合物，组合物和治疗淀粉样变性疾病和合并症的方法，如阿尔茨海默病，2型糖尿病和帕金森病
公开(公告)号：US20120225890A1
公开(公告)日：2012-09-06
申请号：US13413417
申请日：2012-03-06
申请人： Alan D. Snow , Beth Nguyen , Gerardo Castillo , Virginia Sanders , Thomas Lake , Lesley Larsen , Rex T. Weavers , Stephen Lorimer , David Larsen , David L. Coffen , Charlotte Coffen
发明人： Alan D. Snow , Beth Nguyen , Gerardo Castillo , Virginia Sanders , Thomas Lake , Lesley Larsen , Rex T. Weavers , Stephen Lorimer , David Larsen , David L. Coffen , Charlotte Coffen
IPC分类号： A61K31/495 , C07D211/44 , A61K31/45 , C07D295/10 , C07D241/04 , A61P25/16 , A61K31/44 , C07D213/69 , A61P25/28 , A61P3/10 , A61P29/00 , A61P35/00 , C07D295/096 , C07D213/30
CPC分类号： C07C49/248 , A61K31/047 , C07C39/15 , C07C39/16 , C07C39/17 , C07C45/62 , C07C45/64 , C07C49/83 , C07C49/835 , C07C69/017 , C07C215/50 , C07C231/02 , C07C235/34 , C07C235/38 , C07C235/48 , C07C235/54 , C07C235/56 , C07C237/22 , C07C275/34 , C07D207/16 , C07D211/74 , C07D213/30 , C07D213/69 , C07D213/85 , C07D221/08 , C07D221/18 , C07D231/06 , C07D241/08 , C07D263/38 , C07D265/38 , C07D295/096 , C07D295/192 , C07D311/60 , C07D317/50 , C07D317/54 , C07D317/58 , C07D317/60 , C07D317/66 , C07D317/68 , C07D333/16 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D451/06 , C07D471/04 , C07D487/08 , C07D491/08
摘要： Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
摘要翻译：双 - 和三 - 二羟基芳基化合物及其亚甲二氧基类似物和药学上可接受的酯，它们的合成，含有它们的药物组合物及其在治疗淀粉样蛋白病，尤其是A＆诸如在阿尔茨海默病中观察到的淀粉样变性，诸如在2型糖尿病中观察到的IAPP淀粉样变性和诸如在帕金森病中观察到的突触核蛋白病，以及用于这种治疗的药物的制造。

5. 发明授权

US4483990A Preparation of diketones 失效
标题翻译：二酮的制备
公开(公告)号：US4483990A
公开(公告)日：1984-11-20
申请号：US363333
申请日：1982-03-29
申请人： David L. Coffen
发明人： David L. Coffen
IPC分类号： C07D211/70 , C07D211/78 , C07D217/04 , C07D405/04 , C07D471/04
CPC分类号： C07D405/04 , C07D211/70 , C07D211/78 , C07D217/04 , C07D471/04
摘要： The preparation of bicyclic diketones of the formula ##STR1## wherein R.sub.1 is lower alkyl or ar-lower alkyl, from compounds of the formula ##STR2## wherein R.sub.1 is as set forth above, is described.
摘要翻译：描述了其中R 1如上所述的式Ia的二环二酮的制备，其中R 1是低级烷基或芳 - 低级烷基，其中R 1如上所述。

6. 发明授权

US06452050B1 Synthesis and use of &agr;-ketoamide derivatives and arrays 失效
标题翻译： α-酮酰胺衍生物和阵列的合成和应用
公开(公告)号：US06452050B1
公开(公告)日：2002-09-17
申请号：US09531737
申请日：2000-03-21
申请人： Carmen M. Baldino , David L. Coffen , Stewart D. Chipman , Hong Cheng
发明人： Carmen M. Baldino , David L. Coffen , Stewart D. Chipman , Hong Cheng
IPC分类号： C07C23307
CPC分类号： C40B40/04 , C07C275/40 , C07C335/20 , C07D333/60
摘要： The invention is based on new methods for making and using compounds and arrays of novel &agr;-ketoamides, and the arrays and compounds made by these methods. These novel compounds are potential inhibitors of proteolytic enzymes, particularly cysteine proteases such as cruzain. Application of the new methods has led to the identification of a number of new inhibitors, from amongst an array of about 38,000 &agr;-ketoamide derivatives, having specific activity against three cysteine proteases: cruzain, papain, and cathepsin B. These compounds and other compounds identified by the methods described herein can be useful, for example, in developing pharmaceutical agents for the treatment of diseases (e.g., Chagas' disease) associated with these proteases. Although the disclosed compounds have specific activity for cruzain, papain, cathepsin B, the methods described herein can also be used to identify inhibitors of other proteases.
摘要翻译：本发明基于制备和使用新型α-酮酰胺的化合物和阵列的新方法，以及通过这些方法制备的阵列和化合物。这些新型化合物是蛋白水解酶的潜在抑制剂，特别是半胱氨酸蛋白酶如克鲁津。新方法的应用已经导致了一系列新的抑制剂的鉴定，其中有大约38,000个α-酮酰胺衍生物，具有针对三个半胱氨酸蛋白酶：克鲁津，木瓜蛋白酶和组织蛋白酶B的比活性。这些化合物和其它化合物通过本文所述的方法鉴定可用于例如开发用于治疗与这些蛋白酶相关的疾病（例如恰加斯病）的药剂。虽然所公开的化合物对克鲁津，木瓜蛋白酶，组织蛋白酶B具有比活性，但本文所述的方法也可用于鉴定其它蛋白酶的抑制剂。

7. 发明授权

US06358750B1 Spiro[pyrrolidine-2,3′-oxindole] compounds and method of use 失效
标题翻译：螺[吡咯烷-2,3'-羟吲哚]化合物及其使用方法
公开(公告)号：US06358750B1
公开(公告)日：2002-03-19
申请号：US09535719
申请日：2000-03-27
申请人： Demosthenes Fokas , David L. Coffen , William J. Ryan
发明人： Demosthenes Fokas , David L. Coffen , William J. Ryan
IPC分类号： G01N33566
CPC分类号： C07D487/10 , C40B40/00 , G01N33/573 , G01N33/68 , G01N33/86
摘要： The invention provides spiro[pyrrolidine-2,3′-oxindole] compounds and libraries of these compounds produced by the stereo- and regio-selective reaction of variously substituted isatins, &agr;-amino acids, and dipolarophiles (e.g., trans-chalcones, acrylate esters, or vinyl oxindoles). The new libraries can be assayed using any of many known screening procedures for activity, e.g., biological activity. For example, the libraries can be screened for activity as drugs (e.g., anticancer drugs, antibiotics, antiviral drugs, antiinflammatory drugs, analgesics, immunomodulators, neuroleptics, sedatives, stimulants, or diagnostic aids), bioseparation agents, or pesticides (e.g., herbicides, insecticides, or rodenticides).
摘要翻译：本发明提供了螺[吡咯烷-2,3'-羟吲哚]化合物和这些化合物的文库，其通过各种取代的异头ins素，α-氨基酸和dipolarophicity的立体和区域选择性反应（例如反式查尔酮，丙烯酸酯酯或乙烯基羟吲哚）。可以使用许多已知的活性筛选方法（例如生物活性）来测定新的文库。例如，图书馆可以作为药物（例如，抗癌药物，抗生素，抗病毒药物，抗炎药，止痛剂，免疫调节剂，精神安定药，镇静剂，兴奋剂或诊断辅助剂），生物分离剂或杀虫剂（例如除草剂，杀虫剂或杀鼠剂）。

8. 发明授权

US5008411A Glycidic acid ester and process of preparation 失效
标题翻译：糖苷酸酯及其制备方法
公开(公告)号：US5008411A
公开(公告)日：1991-04-16
申请号：US416295
申请日：1989-10-02
申请人： David L. Coffen , Pradeep B. Madan , Alan Schwartz
发明人： David L. Coffen , Pradeep B. Madan , Alan Schwartz
IPC分类号： C07C319/20 , C07C323/56 , C07D281/08 , C07D281/10
CPC分类号： C07C319/20 , C07D281/08 , C07D281/10 , C07C2101/14
摘要： A process for the preparing a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen, trifluoromethyl or nitro; or R.sub.1 and R.sub.2 taken together with the benzene ring to which they are attached are naphthalene, and Ar is p-lower alkoxy phenyl.which comprises reacting ##STR2## wherein R.sub.1 and R.sub.2 are as described above with the compound of the formula ##STR3## wherein Ar is as described above, in an aromatic organic compound. The intermediates formed by the process of the invention are useful in the production of thiazepin-4(5H)-ones which have activity as calcium channel blockers and accordingly are useful as agents for lowering blood pressure and agents for treating ischemia.
摘要翻译：制备式IV化合物的方法，其中R 1和R 2各自独立地为氢，1至4个碳原子的烷基，1至4个碳原子的烷氧基，卤素，三氟甲基或硝基; 或者R 1和R 2与它们所连接的苯环一起为萘，Ar为对低级烷氧基苯基。其中包括使其中R 1和R 2如上所述的其中Ar如上所述的式IIIa化合物在芳族有机化合物中反应。通过本发明的方法形成的中间体可用于制备具有钙通道阻断剂活性的硫氮平-4（5H）酮，因此可用作降低血压的药剂和用于治疗缺血的药剂。

9. 发明授权

US4879395A Vitamin E intermediate 失效
标题翻译：维生素E中间体
公开(公告)号：US4879395A
公开(公告)日：1989-11-07
申请号：US242382
申请日：1988-09-09
申请人： David L. Coffen , Rudolf Schmid , Mark J. Sebastian
发明人： David L. Coffen , Rudolf Schmid , Mark J. Sebastian
IPC分类号： C07C33/02 , C07C33/025 , C07C45/62 , C07C45/74 , C07C47/02 , C07C49/203 , C07D311/58 , C07D311/72
CPC分类号： C07D311/72 , C07C33/02 , C07C33/025 , C07C45/62 , C07C45/74 , C07C47/02 , C07C49/203 , C07C67/08 , C07C68/02 , C07D311/58
摘要： A process for producing natural vitamin E and intermediates in this process.
摘要翻译：在此过程中生产天然维生素E和中间体的方法。

10. 发明授权

US4247712A Preservation of aqueous systems with 2-chloro-3-oxobutyramide derivatives 失效
标题翻译：用2-氯-3-氧代丁酰胺衍生物保护含水体系
公开(公告)号：US4247712A
公开(公告)日：1981-01-27
申请号：US92599
申请日：1979-11-08
申请人： Harold A. Brandman , Milton Manowitz , David L. Coffen
发明人： Harold A. Brandman , Milton Manowitz , David L. Coffen
IPC分类号： A01N37/42 , A01N47/12 , C02F1/50 , C07C125/04 , C07C103/42
CPC分类号： C02F1/50 , A01N37/42 , A01N47/12
摘要： There is disclosed methods and compositions for inhibiting or preventing the growth of microorganisms in aqueous systems wherein the growth is inhibited or prevented by the presence of an effective amount of a 2-chloro-3-oxobutyramide derivative.
摘要翻译：公开了用于抑制或预防水系统中微生物生长的方法和组合物，其中通过有效量的2-氯-3-氧代丁酰胺衍生物的存在抑制或预防生长。

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