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1. 发明授权

US5652235A Method of using spiro piperidines to promote the release of growth hormone 失效
标题翻译：使用螺哌啶促进生长激素释放的方法
公开(公告)号：US5652235A
公开(公告)日：1997-07-29
申请号：US641311
申请日：1996-04-30
申请人： Meng-Hsin Chen , Ravi P. Nargund , David B. R. Johnston , Arthur A. Patchett , James R. Tata , Lihu Yang
发明人： Meng-Hsin Chen , Ravi P. Nargund , David B. R. Johnston , Arthur A. Patchett , James R. Tata , Lihu Yang
IPC分类号： A61K31/435 , A61K31/438 , A61K31/445 , A61K31/47 , A61K38/00 , A61K38/04 , A61P3/00 , A61P19/10 , A61P43/00 , C07D221/20 , C07D401/10 , C07D471/10 , C07D491/10 , C07D491/107 , C07D495/10 , C07D495/20 , C07D519/00 , C07K1/00 , C07K5/02 , C07K5/06 , C07K5/078 , C07K14/00 , A61K31/55 , A61K31/44
CPC分类号： C07D401/10 , C07D471/10 , C07D491/10 , C07D495/10 , C07K5/021 , C07K5/06034 , C07K5/06147 , C07K5/06191 , A61K38/00 , Y02P20/55
摘要： There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.
摘要翻译：已经公开了鉴定为促进人和动物中生长激素释放的螺哌啶和同系物的某些新化合物。这种性质可以用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人类中，用于治疗以生长激素分泌不足为特征的生理或医学病症，例如生长激素缺乏的身材矮小儿童，并且治疗通过生长激素的合成代谢作用改善的医疗状况。还公开了含有作为其活性成分的螺环化合物的生长激素释放组合物。

2. 发明授权

US5578593A Spiro piperidines and homologs promote release of growth hormone 失效
标题翻译： Spiro哌啶和同系物促进生长激素的释放
公开(公告)号：US5578593A
公开(公告)日：1996-11-26
申请号：US146848
申请日：1993-11-03
申请人： Meng-Hsin Chen , David B. R. Johnston , Ravi P. Nargund , Arthur A. Patchett , James R. Tata , Lihu Yang
发明人： Meng-Hsin Chen , David B. R. Johnston , Ravi P. Nargund , Arthur A. Patchett , James R. Tata , Lihu Yang
IPC分类号： A61K38/00 , C07D401/10 , C07D471/10 , C07D491/10 , C07D495/10 , C07D519/00 , C07K5/02 , C07K5/06 , C07K5/078 , A61K31/55 , A61K31/44 , C07D401/00 , C07D471/00
CPC分类号： C07D401/10 , C07D471/10 , C07D491/10 , C07D495/10 , C07K5/021 , C07K5/06026 , C07K5/06034 , C07K5/06147 , C07K5/06191 , A61K38/00 , Y10S514/825
摘要： There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.
摘要翻译：已经公开了鉴定为促进人和动物中生长激素释放的螺哌啶和同系物的某些新化合物。这种性质可以用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人类中，用于治疗以生长激素分泌不足为特征的生理或医学病症，例如生长激素缺乏的身材矮小儿童，并且治疗通过生长激素的合成代谢作用改善的医疗状况。还公开了含有作为其活性成分的螺环化合物的生长激素释放组合物。

3. 发明授权

US5536716A Spiro piperidines and homologs which promote release of growth hormone 失效
标题翻译： Spiro哌啶和促进生长激素释放的同系物
公开(公告)号：US5536716A
公开(公告)日：1996-07-16
申请号：US147226
申请日：1993-11-03
申请人： Meng-Hsin Chen , David B. R. Johnston , Ravi P. Nargund , Arthur A. Patchett , James R. Tata , Lihu Yang
发明人： Meng-Hsin Chen , David B. R. Johnston , Ravi P. Nargund , Arthur A. Patchett , James R. Tata , Lihu Yang
IPC分类号： A61K38/00 , C07D401/10 , C07D471/10 , C07D491/10 , C07D495/10 , C07D519/00 , C07K5/02 , C07K5/06 , C07K5/078 , A61K31/55 , A61K31/44 , C07D401/04 , C07D451/00
CPC分类号： C07D401/10 , C07D471/10 , C07D491/10 , C07D495/10 , C07K5/021 , C07K5/06026 , C07K5/06034 , C07K5/06147 , C07K5/06191 , A61K38/00 , Y10S514/825
摘要： There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.
摘要翻译：已经公开了鉴定为促进人和动物中生长激素释放的螺哌啶和同系物的某些新化合物。这种性质可以用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人类中，用于治疗以生长激素分泌不足为特征的生理或医学病症，例如生长激素缺乏的身材矮小儿童，并且治疗通过生长激素的合成代谢作用改善的医疗状况。还公开了含有作为其活性成分的螺环化合物的生长激素释放组合物。

4. 发明授权

US5389660A Substituted imidazo-fused 5-membered ring heterocycles as angiotensin II antagonists 失效
标题翻译：取代的咪唑稠合的5元环杂环作为血管紧张素II拮抗剂
公开(公告)号：US5389660A
公开(公告)日：1995-02-14
申请号：US957588
申请日：1992-10-07
申请人： William J. Greenlee , David B. R. Johnston , Malcolm MacCoss , Nathan B. Mantlo , Arthur A. Patchett , Prasun K. Chakravarty , Thomas F. Walsh
发明人： William J. Greenlee , David B. R. Johnston , Malcolm MacCoss , Nathan B. Mantlo , Arthur A. Patchett , Prasun K. Chakravarty , Thomas F. Walsh
IPC分类号： A61K31/415 , A61K31/42 , A61K31/425 , A61P9/08 , A61P9/10 , A61P9/12 , A61P27/02 , A61P43/00 , C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04 , C07D521/00 , C07F9/6561 , A61K31/41 , C07D487/02
CPC分类号： C07D487/04 , C07D491/04 , C07D495/04
摘要： There are disclosed new substituted imidazo-fused 5-membered ring heterocyclic compounds and derivatives thereof which are useful as angiotensin II antagonists. These compounds have the general formula: ##STR1##
摘要翻译：公开了可用作血管紧张素II拮抗剂的新的取代的咪唑并稠合的5元环杂环化合物及其衍生物。这些化合物具有通式：（I）

5. 发明授权

US5164407A Substituted imidazo-fused 5-membered ring heterocycles and their use as angiotensin II antagonsists 失效
标题翻译：取代的IMIDAZO-FUSED 5结构环杂交体及其作为ANGIOTENSIN II拮抗剂的使用
公开(公告)号：US5164407A
公开(公告)日：1992-11-17
申请号：US516502
申请日：1990-04-25
申请人： William J. Greenlee , David B. R. Johnston , Malcolm MacCoss , Nathan B. Mantlo , Arthur A. Patchett , Prasun K. Chakravarty , Thomas F. Walsh
发明人： William J. Greenlee , David B. R. Johnston , Malcolm MacCoss , Nathan B. Mantlo , Arthur A. Patchett , Prasun K. Chakravarty , Thomas F. Walsh
IPC分类号： A61K31/415 , A61K31/42 , A61K31/425 , A61P9/08 , A61P9/10 , A61P9/12 , A61P27/02 , A61P43/00 , C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04 , C07D521/00 , C07F9/6561
CPC分类号： C07D487/04 , C07D491/04 , C07D495/04
摘要： There are disclosed new substituted imidazo-fused 5-membered ring heterocyclic compounds and derivatives thereof which are useful as angiotensin II antagonists. These compounds have the general formula: ##STR1##

6. 发明授权

US5157040A Substituted quinolines as angiotensin II antagonists 失效
标题翻译：替代喹诺酮作为ANGIOTENSIN II拮抗剂
公开(公告)号：US5157040A
公开(公告)日：1992-10-20
申请号：US681216
申请日：1991-04-05
申请人： William J. Greenlee , David B. R. Johnston , Malcolm MacCoss
发明人： William J. Greenlee , David B. R. Johnston , Malcolm MacCoss
IPC分类号： A61K31/47 , A61P9/00 , A61P9/12 , A61P25/00 , A61P25/28 , A61P27/02 , A61P43/00 , C07D215/12 , C07D215/38 , C07D215/50 , C07D401/10 , C07D403/10 , C07D413/10
CPC分类号： C07D403/10 , C07D215/50
摘要： Substituted quinolines of the formula (I), are angiotensin II antagonists, ##STR1## and useful in the treatment of hypertension, ocular hypertension and certain CNS disorders.

7. 发明授权

US4347368A 3 -Substituted-6-substituted-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxyl ic acid 失效
标题翻译： 3-取代的6-取代-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸
公开(公告)号：US4347368A
公开(公告)日：1982-08-31
申请号：US207042
申请日：1980-11-14
申请人： Burton G. Christensen , David B. R. Johnston , Susan M. Schmitt
发明人： Burton G. Christensen , David B. R. Johnston , Susan M. Schmitt
IPC分类号： C07D205/08 , C07D477/20 , C07D477/26 , C07D498/04 , C07F7/10 , C07D487/04
CPC分类号： C07D477/26 , C07D205/08 , C07D477/20 , C07F7/10
摘要： Disclosed are 3- and 6-substituted 7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acids having the structure: ##STR1## wherein R.sup.6, R.sup.7 and R.sup.8 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
摘要翻译：公开了具有以下结构的3-和6-取代的7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸：其中R6，R7和R8特别独立地选自由氢，烷基，烯基，芳基和芳烷基组成的组。这些化合物及其药学上可接受的盐，酯和酰胺衍生物可用作抗生素。还公开了制备这些化合物的方法，包含这些化合物的药物组合物和治疗方法，包括当指出抗生素作用时施用这些化合物和组合物。

8. 发明授权

US3943153A (-)(Cis-1,2-epoxy propyl)phosphonic acid amides 失效
标题翻译：（{31}（顺式-1,2-环氧丙基）膦酸酰胺
公开(公告)号：US3943153A
公开(公告)日：1976-03-09
申请号：US848678
申请日：1969-08-08
申请人： Burton G. Christensen , Michael W. Fordice , David B. R. Johnston
发明人： Burton G. Christensen , Michael W. Fordice , David B. R. Johnston
IPC分类号： C07F9/655 , C07F9/6584 , C07D303/46 , C07D303/00
CPC分类号： C07F9/65848 , C07F9/65505
摘要： Amides and thioates of (-)(cis-1,2-epoxypropyl)-phosphonic acid and phosphonothioic acid are prepared by converting (-)(cis-1,2-epoxypropyl)phosphonic acid or phosphonothioic acid or a salt thereof to an acid halide and reacting the acid halide with an amine, and by reacting the phosphonic acid or a salt thereof with an amine in the presence of a carbodiimide. The novel (-)(cis-1,2-epoxypropyl)phosphonic and phosphonothioic amides are active antibacterial agents.
摘要翻译：（ - ）（顺式-1,2-环氧丙基） - 膦酸和膦酰硫酸的酰胺和硫酸盐是通过将（ - ）（顺式-1,2-环氧丙基）膦酸或硫代磷酸或其盐转化成酸卤化物并使酰卤与胺反应，并在碳二亚胺存在下使膦酸或其盐与胺反应。新型（ - ）（顺式-1,2-环氧丙基）膦酸和膦酰基酰胺是活性抗菌剂。

9. 发明授权

US4507299A N-[2-amino-5-halo-6-(substituted)-3-pyrazinyl)-methylene]amine antimicrobial compounds 失效
标题翻译： N- [2-氨基-5-卤代-6-（取代的）-3-吡嗪基） - 亚甲基]胺抗微生物化合物
公开(公告)号：US4507299A
公开(公告)日：1985-03-26
申请号：US453055
申请日：1982-12-27
申请人： David B. R. Johnston
发明人： David B. R. Johnston
IPC分类号： A01N43/60 , C07D241/20 , C07D241/16
CPC分类号： A01N43/60 , C07D241/20
摘要： Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine;R is halo; mono- or di-substituted mono- or diloweralkylamino wherein the loweralkyl substituents are hydroxy or loweralkanoyloxy; 4-morpholino; thiocyano; mercapto; straight or branched chain C.sub.1-8 alkylthio; mono- or di-substituted loweralkylthio wherein the substituents are hydroxy, amino, loweralkanoylamino, or loweralkoxycarbonyl; arylthio; loweralkylsulfoxy; or loweralkylsulfonyl;R.sup.1 is hydrogen; straight or branched C.sub.1-8 alkyl; aryl; aryl substituted with up to two members selected from the group consisting of C.sub.1-3 alkyl, C.sub.1-3 alkoxy, halo, and mono- or di-C.sub.1-3 alkyl substituted amino; heteroaryl; formyl C.sub.2-4 alkenyl; or C.sub.2-4 alkenyl; andR.sup.2 is straight or branched C.sub.1-8 alkyl; loweralkoxy; hydroxy; loweralkoxycarbonylmethyl; benzyl; or benzyl substituted with up to two members selected from the group consisting of halo, loweralkyl, and loweralkoxy; are useful in various agricultural and industrial areas.
摘要翻译：下式的抗微生物化合物：其中：Hal是溴或氯; R为卤素; 单取代或二取代的单 - 或二 - 低级烷基氨基，其中低级烷基取代基是羟基或低级烷酰氧基; 4-吗啉代; 硫氰酸巯基直链或支链C 1-8烷硫基; 单取代或二取代的低级烷硫基，其中取代基是羟基，氨基，低级烷酰基氨基或低级烷氧基羰基; 芳硫基低级烷基亚磺酰基; 或低级烷基磺酰基 R1是氢; 直链或支链C 1-8烷基; 芳基; 被至多两个选自C 1-3烷基，C 1-3烷氧基，卤素和一或二-C 1-3烷基取代的氨基的成员取代的芳基; 杂芳基; 甲酰基C2-4烯基; 或C 2-4链烯基; 并且R 2是直链或支链C 1-8烷基; 低级烷氧基羟基; 低级烷氧羰基甲基苄基; 或被至多两个选自卤素，低级烷基和低级烷氧基的成员取代的苄基; 适用于各种农业和工业领域。

10. 发明授权

US4348320A Substituted azetidiones 失效
标题翻译：取代的氮杂环丁烷
公开(公告)号：US4348320A
公开(公告)日：1982-09-07
申请号：US179922
申请日：1980-08-20
申请人： F. Aileen Bouffard , Burton G. Christensen , David B. R. Johnston
发明人： F. Aileen Bouffard , Burton G. Christensen , David B. R. Johnston
IPC分类号： C07D205/08 , C07D477/04 , C07D477/10 , C07D498/04 , C07F7/18 , C07F9/568 , C07D487/04
CPC分类号： C07D477/04 , C07D205/08 , C07D477/10 , C07F7/186 , C07F9/5683
摘要： Disclosed are substituted azetidinones (1) which are useful in the preparation of 1-carba-2-penem-3-carboxylic acids (I): ##STR1## wherein R is hydrogen or a blocking group and R.sup.1, R.sup.2 and R.sup.3 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, aryl, and aralkyl. Such 1-carba-2-penem-3-carboxylic acids and their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics.
摘要翻译：公开了可用于制备1-碳-2-青霉烯-3-羧酸（I）的取代的氮杂环丁酮（1）：其中R是氢或封闭基团，并且R 1，R 2和R 3是独立地选自氢，烷基，芳基和芳烷基。这种1-咔二-2-青霉烯-3-羧酸及其药学上可接受的盐，酯和酰胺衍生物可用作抗生素。

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