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51. 发明授权

US6143887A Process for the stereoselective synthesis of 16-substituted-4-aza-androstanones 失效
标题翻译： 16取代-4-氮杂 - 雄甾烷酮的立体选择性合成方法
公开(公告)号：US6143887A
公开(公告)日：2000-11-07
申请号：US309833
申请日：1999-05-11
申请人： Dominick F. Gratale , Richard L. Tolman , Soumya P. Sahoo
发明人： Dominick F. Gratale , Richard L. Tolman , Soumya P. Sahoo
IPC分类号： C07J73/00 , C07D401/12 , C07D221/18 , C07D241/08 , C07D253/06 , C07D403/12
CPC分类号： C07J73/005
摘要： The novel process of the present invention involves the stereoselective synthesis of certain 16.beta.-substituted 4-aza-5.alpha.-androstan-3-ones and the useful intermediates obtained therein.
摘要翻译：本发明的新方法涉及某些16β-取代的4-氮杂-5α-雄甾烷-3-酮及其中获得的有用的中间体的立体选择性合成。

52. 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）

53. 发明授权

US5817757A Inhibitors of peptide binding to MHO class II proteins 失效
标题翻译：肽结合MHC II类蛋白的抑制剂
公开(公告)号：US5817757A
公开(公告)日：1998-10-06
申请号：US736706
申请日：1996-10-28
申请人： Alan D. Adams , A. Brian Jones , Victoria K. Lombardo , Richard L. Tolman
发明人： Alan D. Adams , A. Brian Jones , Victoria K. Lombardo , Richard L. Tolman
IPC分类号： A61K38/00 , C07K5/02 , C07K5/06 , C07K5/068 , C07K5/083 , C07K5/087 , C07K5/09 , C07K5/097 , C07K5/107 , A61K38/06 , A61K35/14 , A61K39/00 , A61K45/00
CPC分类号： C07K5/0821 , C07K5/0207 , C07K5/06052 , C07K5/06086 , C07K5/0808 , C07K5/0812 , C07K5/0815 , C07K5/1016 , A61K38/00 , Y10S424/81
摘要： Compounds of the formula ##STR1## are inhibitors of peptide binding to major histocompatibility complex type II proteins and are useful in the treatment and prevention of autoimmune diseases including: rheumatoid arthritis, Type I diabetes, multiple sclerosis, lupus erythematosis, Graves disease and pemphigus. The present invention also provides novel compositions, methods of treatment employing the compounds of the present invention and methods of manufacture of the compounds of structural formula (I).
摘要翻译：式（I）的化合物是肽与主要组织相容性复合物II型蛋白质结合的抑制剂，并且可用于治疗和预防自身免疫疾病，包括：类风湿性关节炎，I型糖尿病，多发性硬化，狼疮性疾病和天疱疮。本发明还提供新的组合物，使用本发明化合物的处理方法和结构式（I）化合物的制备方法。

54. 发明授权

US5510351A Delta-17 and delta-20 olefinic and saturated 17 beta-substituted 4-aza-5 alpha-androstan-ones as 5 alpha reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders 失效
标题翻译： Δ-17和δ-20烯属和饱和17β-取代的4-氮杂-5α-雄甾烷酮作为5αα还原酶抑制剂，其可用于预防和治疗高雄激素性疾病
公开(公告)号：US5510351A
公开(公告)日：1996-04-23
申请号：US338490
申请日：1994-11-14
申请人： Donald W. Graham , Susan D. Aster , Richard L. Tolman
发明人： Donald W. Graham , Susan D. Aster , Richard L. Tolman
IPC分类号： A61K8/63 , A61K8/00 , A61K31/58 , A61Q5/00 , A61Q7/00 , A61Q19/00 , C07J73/00
CPC分类号： C07J73/005
摘要： Described are delta 17 and delta 20 olefinic and saturated 17 Beta-substituted 4-aza-5 alpha-androstan-3-ones and related compounds having 5 alpha reductase inhibitors for treatment of benign prostatic hyperplasia and other hyperandrogenic related disorders.
摘要翻译： PCT No.PCT / US93 / 04630 Sec。 371日期：1994年11月14日 102（e）日期1994年11月14日PCT提交1993年5月17日PCT公布。第WO93 / 23051号公报日期为1993年11月25日。描述了δ17和Δ20烯属和饱和的17β-取代的4-氮杂-5α-雄甾烷-3-酮和具有5个α还原酶抑制剂的相关化合物，用于治疗良性前列腺增生和其他高雄激素相关疾病。

55. 发明授权

US5438061A 7-substituted-.delta.4-6-azasteroid derivatives as 5.alpha.-reductase inhibitors 失效
标题翻译： 7-取代-6,6-氮杂甾醇衍生物作为5α-还原酶抑制剂
公开(公告)号：US5438061A
公开(公告)日：1995-08-01
申请号：US93107
申请日：1993-07-16
申请人： Jeffrey P. Bergman , Donald W. Graham , Gary H. Rasmusson , Richard L. Tolman , Derek Von Langen
发明人： Jeffrey P. Bergman , Donald W. Graham , Gary H. Rasmusson , Richard L. Tolman , Derek Von Langen
IPC分类号： C07J1/00 , C07J73/00 , C07D221/18 , A61K31/44
CPC分类号： C07J1/0011 , C07J1/0022 , C07J73/005
摘要： Compounds of the formula I ##STR1## wherein R.sub.1 hydrogen or methyl; R.sub.2 is methyl; R.sub.3 hydrogen, Alk-R.sub.4, X-Alk, C.sub.1-6 -X-Alk, XCO-Alk, CN, CO-Alk, CO-Ar, CO-O-Alk, CO-NH-Alk, CO-NH-Ar, CO-NH-Het and CO-N(Alk).sub.2 ; Alk is C.sub.1-12 straight or branched alkyl; Ar is phenyl, Het is piperidinyl, piperizinyl, pyrrolidinyl, pyrrolyl, furanyl or thienyl and X is O, N or S. Such compounds are useful in the treatment of pathologic conditions that benefit from blockade of isozymes of 5.alpha.-reductase.
摘要翻译：式I的化合物其中R 1为氢或甲基; R2是甲基; R3氢，Alk-R4，X-Alk，C1-6-X-Alk，XCO-Alk，CN，CO-Alk，CO-Ar，CO-O-Alk，CO-NH-Alk，CO-NH-Ar ，CO-NH-Het和CO-N（Alk）2; Alk是C1-12直链或支链烷基; Ar是苯基，Het是哌啶基，哌嗪基，吡咯烷基，吡咯基，呋喃基或噻吩基，X是O，N或S.这些化合物可用于治疗受阻于5α-还原酶同工酶受益的病理状况。

56. 发明授权

US5274122A Acidic derivatives of homocysteine thiolactone 失效
标题翻译：同型半胱氨酸硫内酯的酸性衍生物
公开(公告)号：US5274122A
公开(公告)日：1993-12-28
申请号：US963324
申请日：1992-10-15
申请人： Richard L. Tolman , Stephen Marburg , William J. Leanza
发明人： Richard L. Tolman , Stephen Marburg , William J. Leanza
IPC分类号： C07D333/36 , C07F9/6553
CPC分类号： C07D333/36 , C07F9/655345
摘要： Homocysteine thiolactone derivatives in which the nitrogen is acylated with groups containing acidic functionalities have been synthesized. These include the succinyl, the carboxymethylglutaryl, the 3-phosphonopropionyl and the 3-sulfopropionyl derivatives. These thiolactones can be used to introduce a thiol functionality into proteins such as the outer membrane protein complex of Neisseria meninioitidis (OMPC) allowing conjugation with electrophilic ligands. This chemistry is similar to known N-acetyl-homocysteine thiolactone chemistry, but the pK.sub.a values are such that at pH 7, concomitant negative charge is introduced into the conjugate. Such negative charge neutralizes excess positive charge introduced when arginine- and lysine-rich peptides are bonded as ligands. In the case of OMPC, introduction of positive charge commonly effects irreversible precipitation of the conjugate. Conjugates prepared with the anionic thiolactones have improved solubility.
摘要翻译：已经合成了其中氮与含有酸性官能团的基团进行酰化的同型半胱氨酸硫内酯衍生物。这些包括琥珀酰基，羧甲基葡萄糖基，3-膦酰基丙酰基和3-磺基丙酰基衍生物。可以使用这些硫内酯将硫醇官能团引入蛋白质，例如允许与亲电子配体缀合的奈瑟氏球菌（OMPC）的外膜蛋白复合物。该化学类似于已知的N-乙酰基 - 同型半胱氨酸硫内酯化学，但pKa值使得在pH7时，伴随的负电荷被引入缀合物中。当富含精氨酸和富含赖氨酸的肽作为配体键合时，这种负电荷中和了引入的过量正电荷。在OMPC的情况下，引入正电荷通常会影响缀合物的不可逆沉淀。用阴离子硫醇内酯制备的缀合物具有改善的溶解性。

57. 发明授权

US5196411A 17.beta.-acyl-3-carboxy-androsta-3,5-dienes as testosterone 5.alpha.-reductase inhibitors 失效
标题翻译： 17（BETA）-ACYL-3-CARBOXY-ANDROSTA-3,5-DIENES as TESTOSTERONE 5（ALPHA）-REDUCTASE INHIBITORS
公开(公告)号：US5196411A
公开(公告)日：1993-03-23
申请号：US745679
申请日：1991-08-16
申请人： Gary H. Rasmusson , Richard L. Tolman , Gool F. Patel
发明人： Gary H. Rasmusson , Richard L. Tolman , Gool F. Patel
IPC分类号： A61K31/56 , A61K31/57 , A61K31/575 , A61P13/02 , A61P15/00 , A61P17/00 , A61P43/00 , C07J3/00 , C07J7/00 , C07J9/00 , C07J31/00 , C07J41/00 , C07J43/00 , C07J51/00
CPC分类号： C07J41/0066 , C07J3/005 , C07J31/006 , C07J43/003 , C07J51/00 , C07J9/00 , C07J9/005
摘要： 17.beta.-acyl-3-carboxy-androsta-3,5-dienes as testosterone 5.alpha.-reductase inhibitors of the formula: ##STR1## wherein R is C.sub.3 -C.sub.8 cycloalkyl, which can be substituted with C.sub.1 -C.sub.4 alkoxy or C.sub.6 -C.sub.12 aryl, which can be substituted with one or more of: --OH, --OC.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkyl, --(CH.sub.2).sub.m OH, --(CH.sub.2).sub.n COOH, including protected --OH, where m is 1-4, n is 1-3, and pharmaceutically acceptable salts or esters thereof. Also described is a pharmaceutical formulation. The above compounds are active as testosterone 5.alpha.-reductase inhibitors and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.

58. 发明授权

US5137876A Nucleoside antiviral and anti-inflammatory compounds and compositions and methods for using same 失效
标题翻译：核苷酸抗病毒和抗炎化合物及其组合物及其使用方法
公开(公告)号：US5137876A
公开(公告)日：1992-08-11
申请号：US596846
申请日：1990-10-12
申请人： Malcolm MacCoss , Laura C. Meurer , Richard L. Tolman
发明人： Malcolm MacCoss , Laura C. Meurer , Richard L. Tolman
IPC分类号： A61K31/505 , A61K31/495 , A61K31/675 , A61P29/00 , A61P31/12 , A61P37/00 , C07D487/04 , C07F9/6561 , C07H19/14
CPC分类号： C07D487/04 , C07F9/6561 , C07H19/14
摘要： The compound having the formula: ##STR1## has antiviral activity, specifically in the prevention or treatment of infection by retroviruses, including HIV, and immunosuppressive activity, either as a compound, pharmaceutically acceptable salt, or a pharmaceutical composition ingredient, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing or treating viral infections and modulating immune responses in vivo are also described.

59. 发明授权

US5114925A Renin inhibitors containing the 2-[[(2R,3S)-3-amino-4-cyclohexyl-2-hydroxy-1-butyl]thio)alkanoyl moiety and the corresponding sulfoxide and sulfone derivatives 失效
标题翻译：含有2 - [[（2R，3S）-3-氨基-4-环己基-2-羟基-1-丁基]硫基）烷酰基部分和相应的亚砜和砜衍生物的肾素抑制剂
公开(公告)号：US5114925A
公开(公告)日：1992-05-19
申请号：US756632
申请日：1991-09-09
申请人： Wallace T. Ashton , Christine L. Cantone , Richard L. Tolman
发明人： Wallace T. Ashton , Christine L. Cantone , Richard L. Tolman
IPC分类号： A61K38/00 , C07C317/44 , C07C323/52 , C07D207/46 , C07D233/54 , C07D295/108 , C07D295/13 , C07D303/36 , C07K5/02
CPC分类号： C07D233/64 , C07C317/44 , C07C323/52 , C07D207/46 , C07D295/108 , C07D295/13 , C07D303/36 , C07K5/0227 , A61K38/00
摘要： Compounds of the formula: ##STR1## which are potent inhibitors of human renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory compounds, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these conditions which employ these novel compounds.
摘要翻译：下式的化合物：其是人肾素的有效抑制剂，可用于治疗各种形式的肾素相关性高血压，醛固酮增多症和充血性心力衰竭; 含有这些肾素抑制性化合物的组合物，任选与其它抗高血压药物组合; 以及治疗高血压，醛固酮增多症或充血性心力衰竭的方法，或在使用这些新化合物的这些病症中建立肾素作为致病因子。

60. 发明授权

US5110799A Antiherpetic agents 失效
标题翻译：抗菌剂
公开(公告)号：US5110799A
公开(公告)日：1992-05-05
申请号：US386071
申请日：1989-07-28
申请人： Richard L. Tolman , Wallace T. Ashton , Mu T. Wu
发明人： Richard L. Tolman , Wallace T. Ashton , Mu T. Wu
IPC分类号： A61K38/00 , A61P31/12 , A61P31/22 , C07D233/54 , C07K5/06 , C07K5/072 , C07K5/078 , C07K5/08 , C07K5/097
CPC分类号： C07D233/64 , C07K5/06113 , C07K5/06139 , C07K5/06147 , A61K38/00
摘要： A series of carboxyl-containing N-alkyldipeptides have been found to posess antiviral potency--specifically against herpes simplex virus--by selectively inhibiting the viral ribonucleotide reductase enzyme.

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