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1. 发明授权

US4406902A Dipeptidase inhibitors 失效
标题翻译：二肽酶抑制剂
公开(公告)号：US4406902A
公开(公告)日：1983-09-27
申请号：US285161
申请日：1981-07-23
申请人： Wallace T. Ashton , Louis Barash , Jeannette E. Brown , Donald W. Graham
发明人： Wallace T. Ashton , Louis Barash , Jeannette E. Brown , Donald W. Graham
IPC分类号： A61K31/40 , C07D213/70 , C07D213/80 , C07D233/84 , C07D239/56 , C07D257/04 , C07D277/36 , C07D477/10 , C07D477/20
CPC分类号： C07D213/70 , A61K31/40 , C07D213/80 , C07D239/56 , C07D257/04 , C07D277/36 , C07D477/10 , C07D477/20
摘要： Novel chemical compounds are provided which selectively inhibit the metabolism of dipeptidase (E.C.3.4.13.11) and therefore are useful in combination with antibacterial products. These chemical compounds are Z-2-(2,2-dimethylcyclo-propanecarboxamido)-.omega.-pyridylthio-2-alkenoic acids (and related arylthio and heterocyclylthio analogs).
摘要翻译：提供了选择性抑制二肽酶代谢（E.C.3.4.13.11）的新型化合物，因此可与抗菌产品组合使用。这些化合物是Z-2-（2,2-二甲基环丙烷甲酰氨基）-ω-吡啶基硫代-2-烯酸（和相关的芳硫基和杂环硫基类似物）。

2. 发明授权

US4079069A 5-Deazariboflavin and its derivatives 失效
标题翻译： 5-deazariboflavin及其衍生物
公开(公告)号：US4079069A
公开(公告)日：1978-03-14
申请号：US794771
申请日：1977-05-09
申请人： Donald W. Graham , Edward F. Rogers , Wallace T. Ashton
发明人： Donald W. Graham , Edward F. Rogers , Wallace T. Ashton
IPC分类号： C07D471/04 , A23K1/16 , A61K31/505 , A61K31/675 , A61P33/02 , C07D521/00
CPC分类号： A61K31/505 , A23K20/116 , A61K31/675
摘要： 5-Deazariboflavin, its phosphate ester and nontoxic salts thereof and its novel bis(loweralkoxymethylene) derivatives have antiprotozoal and antiparasitic activity. They are particularly useful for controlling cecal and/or intestinal coccidiosis when administered in minor quantities to animals, in particular to poultry, usually in admixture with animal sustenance. The compounds are included in compositions useful for the prevention and treatment of coccidiosis in poultry.

3. 发明授权

US4053602A Compositions for treating coccidiosis containing 5-deazariboflavin and its derivatives 失效
标题翻译：用于治疗含有5-二氮唑吗啉及其衍生物的结肠病的组合物
公开(公告)号：US4053602A
公开(公告)日：1977-10-11
申请号：US737890
申请日：1976-11-02
申请人： Donald W. Graham , Edward F. Rogers , Wallace T. Ashton
发明人： Donald W. Graham , Edward F. Rogers , Wallace T. Ashton
IPC分类号： C07D471/04 , A23K1/16 , A61K31/505 , A61K31/675 , A61P33/02
CPC分类号： A61K31/505 , A23K20/116 , A61K31/675
摘要： 5-Deazariboflavin, its phosphate ester and non-toxic salts thereof and its novel bis(loweralkoxymethylene) derivatives have antiprotozoal and antiparasitic activity. They are particularly useful for controlling cecal and/or intestinal coccidiosis when administered in minor quantities to animals, in particular to poultry, usually in admixture with animal sustenance. The compounds are included in compositions useful for the prevention and treatment of coccidiosis in poultry.
摘要翻译： 5-脱氮甲黄蛋白，其磷酸酯和无毒盐及其新型双（低级烷氧基亚甲基）衍生物具有抗原虫和抗寄生虫活性。当少量给予动物，特别是通常与动物饲养物混合的家禽时，它们特别有用于控制盲肠和/或肠球虫病。该化合物包括在用于预防和治疗家禽中的球虫病的组合物中。

4. 发明授权

US4094976A Anticoccidial cyclicamino ethanols and esters thereof 失效
标题翻译：抗焦虑的环磷酰胺及其酯
公开(公告)号：US4094976A
公开(公告)日：1978-06-13
申请号：US755366
申请日：1976-12-29
申请人： Richard A. Dybas , Donald W. Graham , Jeannette E. Brown
发明人： Richard A. Dybas , Donald W. Graham , Jeannette E. Brown
IPC分类号： A61K31/63 , A61K31/635 , A61K31/40 , A61K31/65
CPC分类号： A61K31/63 , A61K31/635
摘要： Novel anticoccidial poultry compositions comprising an anticoccidially effective amount of a compound of the formula: ##STR1## wherein n is 3, 4 or 5 and R is hydrogen or an acyl radical derived from a non-toxic carboxylic acid or a non-toxic acid addition salt thereof methods of combatting poultry coccidiosis, novel compounds and methods of preparing these novel compounds.

5. 发明授权

US4290966A Process for the preparation of traumatin 失效
标题翻译：制备创伤剂的方法
公开(公告)号：US4290966A
公开(公告)日：1981-09-22
申请号：US193790
申请日：1980-10-03
申请人： Jeannette E. Brown , Edward F. Rogers , Donald W. Graham
发明人： Jeannette E. Brown , Edward F. Rogers , Donald W. Graham
IPC分类号： C07C59/76 , C07D317/30 , C11C1/00
CPC分类号： C07D317/30 , C07C59/76
摘要： Traumatin, 12-oxo-trans (E) -10-docecenoic acid, is prepared from 10-oxomethyldecanoate by reaction with (triphenylphosphoranylene)acetaldehyde to form 12-oxomethyldodecenoate; blocking the 12-oxo group; hydrolyzing the ester group; and deblocking the 12-oxo group.
摘要翻译：通过与（三苯基亚磷酰）乙醛反应，由10-氧代甲基癸酸酯制备外消旋，12-氧代 - 反式（E）-10-十六烯酸，形成十二碳烯酸12-氧代甲酯; 封闭了12个氧代基团; 水解酯基; 并将12-氧代基团解封。

6. 发明授权

US5952788A Vacuum fluorescent display filament drive circuit 失效
标题翻译：真空荧光显示灯丝驱动电路
公开(公告)号：US5952788A
公开(公告)日：1999-09-14
申请号：US617173
申请日：1996-03-18
申请人： Donald W. Graham , Stephen S. Otzman
发明人： Donald W. Graham , Stephen S. Otzman
IPC分类号： H05B37/02
CPC分类号： G09G3/22 , G09G2320/0209 , G09G2330/021 , G09G2330/028
摘要： A drive circuit for controlling a vacuum fluorescent display is provided. A charge storage device is connected between signal ground or a voltage supply and a display element. One multiway switch or two single-position switches are connected to the display element opposite the charge storage device. In either configuration, the switch or switches are controlled by an oscillator which, by toggling the switch or switches, alternates the configuration of the circuit to charge or discharge the charge storage device through the display element. The charge storage device and the display element may be connected to a regulated voltage which is maintained at a potential above the grid voltage to reduce cross-talk in the display. The switching operation is break before make and produces an AC voltage across the display element.
摘要翻译：提供一种用于控制真空荧光显示器的驱动电路。电荷存储装置连接在信号地或电压源与显示元件之间。一个多路开关或两个单位开关连接到与电荷存储装置相对的显示元件。在任一配置中，开关或开关由振荡器控制，振荡器通过切换开关或开关来交替电路的配置以通过显示元件对电荷存储装置进行充电或放电。电荷存储装置和显示元件可以连接到保持在电网电压以上的电压的调节电压，以减少显示器中的串扰。切换操作在make之前断开，并在显示元件上产生交流电压。

7. 发明授权

US5741795A 16-substituted-6-aza-androsten-4-ene-3-ones as 5-.alpha.-reductase inhibitors 失效
标题翻译： 16-取代-6-氮杂 - 雄-4-烯-3-酮作为5-α-还原酶抑制剂
公开(公告)号：US5741795A
公开(公告)日：1998-04-21
申请号：US732953
申请日：1996-10-17
申请人： Susan D. Aster , Donald W. Graham , Derek J. Von Langen
发明人： Susan D. Aster , Donald W. Graham , Derek J. Von Langen
IPC分类号： A61K31/58 , A61K31/00 , A61P5/28 , C07D221/18 , C07J31/00 , C07J73/00 , A61K31/715
CPC分类号： A61K31/58 , C07D221/18 , C07J31/006 , C07J73/005
摘要： Compounds of the formula I ##STR1## are inhibitors of 5.alpha.-reductase, and are useful for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, prostatic carcinoma, prostatitis and benign prostatic hyperplasia.
摘要翻译：式I的化合物是5α-还原酶的抑制剂，可用于治疗高雄激素性疾病，如寻常痤疮，皮脂溢，女性多毛症，男性型秃发，前列腺癌，前列腺炎和良性前列腺增生。

8. 发明授权

US5621104A Substituted 3-phenanthridinone derivatives as 5-alpha-reductase inhibitors 失效
标题翻译：取代的3-菲啶酮衍生物作为5-α-还原酶抑制剂
公开(公告)号：US5621104A
公开(公告)日：1997-04-15
申请号：US522350
申请日：1995-09-15
申请人： Donald W. Graham , William K. Hagmann
发明人： Donald W. Graham , William K. Hagmann
IPC分类号： C07D221/12 , C07D401/12
CPC分类号： C07D221/12
摘要： The present invention provides for the preparation of compounds,namely, 3-phenanthridinones and their derivatives and their unique ability to inhibit 5-alpha-reductase or their isozymes thereof in mammals enabling said compounds for treating hyperandrogenic conditions of acne, androgenic alopecia, male pattern baldness,female hirsutism,benign prostatic hyperplasia, prostatitis and prostatic cancer.
摘要翻译： PCT No.PCT / US94 / 03080 Sec。 371 1995年9月15日第 102（e）日期1995年9月15日PCT 1994年3月22日PCT公布。公开号WO94 / 21614 日期1994年9月29日本发明提供化合物的制备，即3-菲啶酮及其衍生物及其在哺乳动物中抑制5-α-还原酶或其同功酶的独特能力，使所述化合物能治疗痤疮的雄激素过多症状，雄激素性脱发，男性型秃发，女性多毛症，良性前列腺增生，前列腺炎和前列腺癌。

9. 发明授权

US07662846B2 Selective spirocyclic glucocorticoid receptor modulators 失效
标题翻译：选择性螺环糖皮质激素受体调节剂
公开(公告)号：US07662846B2
公开(公告)日：2010-02-16
申请号：US10551933
申请日：2004-04-19
申请人： Amjad Ali , James M. Balkovec , Richard Beresis , Steven L. Colletti , Donald W. Graham , Gool F. Patel , Cameron J. Smith
发明人： Amjad Ali , James M. Balkovec , Richard Beresis , Steven L. Colletti , Donald W. Graham , Gool F. Patel , Cameron J. Smith
IPC分类号： C07D487/00 , A01N43/56
CPC分类号： C07D495/10 , C07D487/10 , C07D491/10
摘要： The present invention encompasses compounds of Formula (I) and Formula (II) or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明包括式（I）和式（II）的化合物或其药学上可接受的盐或水合物，其可用作治疗各种自身免疫性和炎性疾病或病症的选择性糖皮质激素受体配体。还包括药物组合物和使用方法。

10. 发明授权

US5843953A 7-substituted 4-aza cholanic acid derivatives and their use 失效
标题翻译： 7-取代的4-氮杂胆酸衍生物及其用途
公开(公告)号：US5843953A
公开(公告)日：1998-12-01
申请号：US809506
申请日：1997-03-24
申请人： Donald W. Graham , Josephine R. Carlin , Richard L. Tolman , Shuet-Hing Lee Chiu
发明人： Donald W. Graham , Josephine R. Carlin , Richard L. Tolman , Shuet-Hing Lee Chiu
IPC分类号： C07D221/18 , A61K31/47 , A61K31/473 , A61K31/58 , C07C69/00 , C07J9/00 , C07J73/00 , A61K31/44 , C07D221/04 , C07D221/22
CPC分类号： C07J73/005 , A61K31/58 , C07J9/00 , C07J9/005 , C07C2103/00
摘要： Compounds of formula (I) wherein: the dotted line indicates that a double bond may be present or absent; R.sup.1 is H, methyl or ethyl; R.sup.2 is .alpha.- or .beta.-C.sub.1-10 straight or branched alkyl; R.sup.3 is CO.sub.2 H, CN, CO.sub.2 R.sup.4, COHNR.sup.4, or CON(R.sup.4).sub.2 ; R.sup.4 is H, C.sub.1-10 straight or branched alky, aryl, heteroaryl, or aralkyl; Aryl is phenyl, substituted phenyl, naphthyl, or biphenyl; Heteroaryl is pyridil, pyrrolyl, thienyl, furanyl or quinolinyl; and Aralkyl is C.sub.1-10 alkyl substituted with one to three phenyl or substituted phenyl moieties; and their pharmaceutically acceptable salts are described. These compounds are 5.alpha.-reductase type 1 inhibitors. They may be used for treating conditions associated with an excess of DHT, either alone or in combination with other 5.alpha.-reductase inhibitors. ##STR1##
摘要翻译： PCT No.PCT / US95 / 13112 Sec。 371日期1997年3月24日 102（e）1997年3月24日PCT PCT 1995年10月20日PCT公布。公开号WO96 / 12705 日期：2002年5月2日式（I）化合物其中：虚线表示双键可能存在或不存在; R1是H，甲基或乙基; R2是α或β-C1-10直链或支链烷基; R3是CO2H，CN，CO2R4，COHNR4或CON（R4）2; R4是H，C1-10直链或支链烷基，芳基，杂芳基或芳烷基; 芳基是苯基，取代的苯基，萘基或联苯基; 杂芳基是吡啶基，吡咯基，噻吩基，呋喃基或喹啉基; 芳烷基是被一至三个苯基或取代的苯基部分取代的C 1-10烷基; 及其药学上可接受的盐。这些化合物是5α-还原酶1型抑制剂。它们可以单独使用或与其他5种α-还原酶抑制剂组合用于治疗与过量DHT相关的病症。（一）

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