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1. 发明申请

WO8802374A3 RENIN INHIBITORY PEPTIDES HAVING NOVEL C-TERMINAL MOIETIES 审中-公开
标题翻译： RENIN具有新型C端子的抑制性肽
公开(公告)号：WO8802374A3
公开(公告)日：1988-08-11
申请号：PCT/US8702264
申请日：1987-09-10
申请人： UPJOHN CO , SCHOSTAREZ HEINRICH J , HESTER JACKSON B JR , SAWYER TOMI K
发明人： SCHOSTAREZ HEINRICH J , HESTER JACKSON B JR , SAWYER TOMI K
IPC分类号： A61K38/55 , A61K38/00 , A61P5/38 , A61P9/00 , A61P9/12 , C07K5/02 , C07K5/06 , C07K5/065 , C07K14/81 , A61K37/64
CPC分类号： C07K5/0227 , A61K38/00 , C07K5/06078
摘要： Novel renin-inhibiting peptides of formula (I): X-A6-B7-C8-D9-E10-F11-V. More particularly the present invention provides renin-inhibiting peptides of the formula (I), wherein A6, B7, C8 and D9 may represent amino acid residues; E10 and F11 may represent the 1,4-diamino-1,4-disubstituted-3-hydroxybutane or other stable transition state moieties; X is a terminal group and V is a novel terminal group. Such inhibitors are useful for the diagnosis and control of renin-dependent hypertension.

2. 发明申请

WO03006440A8 AMIDE-CONTAINING COMPOUND HAVING IMPROVED SOLUBILITY AND METHOD OF IMPROVING THE SOLUBILITY OF AN AMIDE-CONTAINING COMPOUND 审中-公开
标题翻译：具有改善溶解性的含胺化合物和改善含氨化合物的溶解性的方法
公开(公告)号：WO03006440A8
公开(公告)日：2003-07-10
申请号：PCT/US0222526
申请日：2002-07-12
申请人： UPJOHN CO , HESTER JACKSON B JR
发明人： HESTER JACKSON B JR
IPC分类号： C07D263/22 , A61K31/422 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/554 , A61P25/16 , A61P31/04 , A61P43/00 , C07D263/20 , C07D405/10 , C07D411/10 , C07D413/04 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/10 , C07D521/00 , C07F9/653 , C07F9/6558 , F24C15/10
CPC分类号： C07D263/20 , C07D231/12 , C07D233/56 , C07D249/08 , C07D411/10 , C07D413/04 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/10 , C07F9/653 , C07F9/65586 , F24C15/10

3. 发明申请

WO9854161A9 OXAZOLIDINONE ANTIBACTERIAL AGENTS HAVING A THIOCARBONYL FUNCTIONALITY 审中-公开
标题翻译：具有噻唑啉酮功能的奥沙利坦抗菌药物
公开(公告)号：WO9854161A9
公开(公告)日：1999-04-08
申请号：PCT/US9809889
申请日：1998-05-18
申请人： UPJOHN CO , HESTER JACKSON B JR , NIDY ELDON GEORGE , PERRICONE SALVATORE CHARLES , POEL TONI JO
发明人： HESTER JACKSON B JR , NIDY ELDON GEORGE , PERRICONE SALVATORE CHARLES , POEL TONI-JO
IPC分类号： A61K31/42 , A61K31/422 , A61K31/438 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P31/00 , A61P31/04 , C07D261/04 , C07D263/20 , C07D307/33 , C07D413/04 , C07D413/10 , C07D417/12 , C07D471/10 , C07D521/00 , C07D307/32
CPC分类号： C07D263/20 , C07D231/12 , C07D233/56 , C07D249/08 , C07D261/04 , C07D307/33 , C07D413/04 , C07D413/10 , C07D417/12 , C07D471/10
摘要： The present invention provides compounds of Formula (I) or pharmaceutical acceptable salts thereof wherein A, G and R1 are as defined in the claims which are antibacterial agents.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中A，G和R 1如权利要求中所定义的是抗菌剂。

4. 发明授权

US3694552A 3-(5-phenyl-3h-1,4-benzodiazepin-2-yl) carbazic acid and alkyl esters in therapeutic compositions and method 失效
标题翻译： 3-（5-苯基-3H-1,4-苯并二氮杂-2-YL）卡巴酸和治疗组合物中的烷基酯
公开(公告)号：US3694552A
公开(公告)日：1972-09-26
申请号：US3694552D
申请日：1971-11-18
申请人： UPJOHN CO
发明人： HESTER JACKSON B JR
IPC分类号： B41M5/26 , A61K27/00
CPC分类号： B41M5/26
摘要： This invention is a therapeutic composition for treating humans and animals comprising a benzodiazepine of the Formula 1 and pharmacologically acceptable acid addition salts thereof in combination with a pharmaceutical carrier and a method for therapeutic treatment.
摘要翻译：本发明是一种用于治疗人和动物的治疗组合物，其包含式1的苯并二氮杂与其药学上可接受的酸加成盐与药物载体的组合和治疗性治疗方法。

5. 发明授权

US3642822A Hexahydropyrrolobenzodiazepines 失效
标题翻译：十六烷基二苯并二恶英
公开(公告)号：US3642822A
公开(公告)日：1972-02-15
申请号：US3642822D
申请日：1969-11-03
申请人： UPJOHN CO
发明人： HESTER JACKSON B JR
IPC分类号： C07D209/08 , C07D471/06 , C07D487/06 , C07D53/02
CPC分类号： C07D471/06 , C07D209/08 , C07D487/06
摘要： 1,2,4,5,6,7 - HEXAHYDROPYRROLO(3,2,1-JK)(1,4)BENZODIAZEPINES, 1,2,4,6,7 - HEXAHYDROPYRROLO(1,2,3-EF)(1,5) BENZODIAZEPHINES, PROCESES FOR PREPARING THE SAME AND INTERMEDIATES USED TO PREPARE SAID BENZODIAZEPINES. THE BENZODIAZEPINES HAVE CENTRAL NERVOUS SYSTEM SITIMULANT AND DEPRESSANT ACTIVITY.

6. 发明授权

US3514462A 1 and 2 ethoxy 3,4,5,10 - tetrahydroazepino(3,4-b) and (2,3-b)indoles and corresponding amino derivatives thereof 失效
标题翻译： 1和2乙氧基3,4,5,10-四氢叶酸（3,4-B）和（2,3-B）吲哚及其相应的氨基衍生物
公开(公告)号：US3514462A
公开(公告)日：1970-05-26
申请号：US3514462D
申请日：1966-10-21
申请人： UPJOHN CO
发明人： HESTER JACKSON B JR
IPC分类号： C07D209/88 , C07D487/04 , C07D29/28
CPC分类号： C07D487/04 , C07D209/88 , Y10S514/96

7. 发明授权

US3701782A 1-carbolower alkoxy - 6 - phenyl-4h-s-triazolo(1,4)benzodiazepine compounds 失效
标题翻译： 1-CARBOLOWER ALKOXY-6-PHENYL-4H-S-TRIAZOLO（1,4）BENZODIAZEPINE COMPOUNDS
公开(公告)号：US3701782A
公开(公告)日：1972-10-31
申请号：US3701782D
申请日：1972-02-10
申请人： UPJOHN CO
发明人： HESTER JACKSON B JR
IPC分类号： C07D243/20 , C07D57/02
CPC分类号： C07D243/20
摘要： 6-PHENYL-4H-S-TRIAZOLO(4,3-A)(1,4)BENZODIAZEPINES OF THE FORMULA IV:

1-R,4-R1,6-(R2,R3-PHENYL),R4,R5-4H-1,2,4-TRIAZOLO(4,3-A)

(1,4)BENZODIAZEPINE

WHEREIN R IS~COOR'' IN WHICH R'' IS ALKYL OF 1 TO 4 CARBON ATOMS, INCLUSIVE; WHEREIN R1 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND ALKYL OF 1 TO 3 CARBON ATOMS, INCLUSIVE; AND WHEREIN R2, R3, R4, AND R5 ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL OF 1 TO 3 CARBON ATOMS, INCLUSIVE, HALOGEN, NITRO, CYANO, TRIFLUOROMETHYL, AND ALKOXY, ALKYLTHIO, ALKYLSULFINYL, ALKYLSULFONYL, ALKANOYLAMINO AND DIALKYLAMINO IN WHICH THE CARBON CHAIN MOIETIES ARE OF 1 TO 3 CARBON ATOMS, INCLUSIVE, ARE PRODUCED BY CONDENSING A 1,3-DIHYDRO-5PHENYL-2H-1,4-BENZODIAZEPINE-2-THIONE OF THE FORMULA I:

2-(S=),3-R1,6-(R2,R3-PHENYL),R4,R5-3H-1,2-DIHYDRO-3H-

(1,4)BENZODIAZEPINE

WHEREIN R1, R2, R3, R4, AND R5 ARE DEFINED AS ABOVE WITH AN ORGANIC ACID HYDRAZIDE OF THE FORMULA:

H2N-NH-CO-R

WHEREIN R IS DEFINED AS ABOVE. THE NEW PRODUCTS OF FORMULA IV INCLUDING THEIR PHARMACOLOGICALLY ACCEPTABLE ACID ADDITION SALTS ARE USEFUL AS SEDATIVES, TRANQUILIZERS AND MUSCLE RELAXANTS IN MAMMALS AND BIRDS.

8. 发明授权

US3646055A 2 4-dihydro-6-phenyl-ih-s-triazolo(4 3-a)(1 4) benzodiazepin-1-ones 失效
标题翻译： 2 4-二氢-6-苯基-1H-吡唑并（4,3-A）（14）苯并咪唑-1-酮
公开(公告)号：US3646055A
公开(公告)日：1972-02-29
申请号：US3646055D
申请日：1969-08-21
申请人： UPJOHN CO
发明人： HESTER JACKSON B JR
IPC分类号： A23K1/16 , C07D243/20 , C07D487/04 , C07D53/06 , C07D57/02
CPC分类号： C07D487/04 , C07D243/20
摘要： 2,4-DIHYDRO-6-PHENYL - 1H - S - TRIAZOLO(4,3-A)BENZODIAZEPIN-1-ONES OF THE FORMULA:

1-(O=),2-R5,4-R4,6-(R3-PHENYL),R1,R2-1,4-DIHYDRO-1H-1,2,4-

TRIAZOLO(4,3-A)(1,4)BENZODIAZEPINE

WHEREIN R1, R2, AND R3 ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL OF 1 TO 3 CARBON ATOMS, INCLUSIVE, HALOGEN, NITRO, CYANO, TRIFLUOROMETHYL, AND ALKOXY, ALKYLTHIO, ALKYSULFINYL, ALKYLSULFONYL, ALKANOYLAMINO AND DIALKYLAMINO, IN WHICH THE CARBON CHAIN MOIETIES ARE OF 1 TO 3 CARBON ATOMS, INCLUSIVE, AND WHEREIN R5 AND R6 ARE SELECTED FROM GROUP CONSISTING OF HYDROGEN AND ALKYL, DEFINED AS ABOVE, ARE PRODUCED FROM SELECTED 1,3DIHYLDRO-5-PHENYL-2H-1,4-BENZOLDIAZEPINE-2-THIONES (I) BY CONDENSATION WITH ALKYL CARBAZATE, YIELDING THE CORRESPONDING 3-(5-PHENYL-3H-1,4-BENZODIAZEPIN-2-YL)CARBAZIC ACID ALKYL ESTER (II), AND THEN HEATING II TO AN ELEVATED TEMPERATURE TO OBTAIN COMPOUND III (IN WHICH R5 IS HYDROGEN). ALKYLATION OF THE LATTER YIELDS THE PRODUCTS OF FORMULA III IN WHICH R5 IS LOWER ALKYL. THE COMPOUNDS OF FORMULA III AS WELL AS THE INTERMEDIATES II AND THE PHARMACOLOGICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF ARE USEFUL TO SEDATE AND TRANQUILIZE DOMESTIC AND ZOO ANIMALS, PARTICULARLY MAMMALS AND BIRDS.

9. 发明授权

US3622673A 4-(1,4,5,6-TETRAHYDROZEPINO 4,5-b INDOL-3(2H)-YL-BUTYROPHENON COMPOSITIONS AND PROCESS OF TREATMENT MENTAL OR EMOTIONAL DISORDERS 失效
标题翻译： 4-（1,4,5,6-四氢吡喃并[4,5-b]吲哚-3（2H） - - - - - - - - - - - - - 丁基）组合物和处理精神或情绪障碍
公开(公告)号：US3622673A
公开(公告)日：1971-11-23
申请号：US3622673D
申请日：1968-11-14
申请人： UPJOHN CO
发明人： HESTER JACKSON B JR
IPC分类号： A61K31/55 , A61K27/00
CPC分类号： A61K31/55
摘要： Compounds of the formula

AND THE PHARMACOLOGICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF WHEREIN R and R1 are hydrogen or methoxy; R1 is hydrogen or methyl; and R2 is fluorine prepared in unit dosage form for oral, rectal or parenteral administration having tranquilizing, antipsychotic, sedative, anticonvulsant, antiemetic and anorexigenic activity and a process for treating mental and emotional disorders by administering the foregoing compositions at a dosage of from 0.5 to 50 mg./kg./day.

D R A W I N G

10. 发明授权

US3681343A 6-phenyl-s-triazolo{8 4,3-a{9 {8 1,4{9 {0 benzodiazepines 失效
标题翻译： 6-PHENYL-S-TRIAZOLO {8 4,3-A {9 {8 1,4 {9 {0 BENZODIAZEPINES
公开(公告)号：US3681343A
公开(公告)日：1972-08-01
申请号：US3681343D
申请日：1971-05-11
申请人： UPJOHN CO
发明人： HESTER JACKSON B JR
IPC分类号： C07D249/08 , C07D471/04 , C07D487/04 , C07D498/14 , C07D521/00 , C07D53/06
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D471/04 , C07D487/04
摘要： This invention relates to novel 6-phenyl-s-triazolo (4,3-a) (1,4)benzodiazepines embraced by the formulas

WHEREIN R is selected from the group consisting of hydrogen, lower alkyl of one through three carbon atoms, phenyl, benzyl, nitromethyl, cyanomethyl, lower alkoxymethyl having an alkoxy moiety of one through three carbon atoms IN WHICH N IS AN INTEGER OF 1 THROUGH 2, R'' and R'''' are each selected from the group consisting of hydrogen and alkyl of one through three carbon atoms and when combined is an alkylidene bridge of four through five carbon atoms; R1 is selected from the group consisting of hydroxy and lower acyloxy; R2, R3, R4 and R5 are selected from the group consisting of hydrogen, lower alkyl of one through three carbon atoms, halogen, nitro, cyano, trifluoromethyl, lower alkoxy, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, amino, lower alkanoylamino and lower dialkylamino; and a pharmacologically acceptable acid addition sat thereof. It also relates to novel processes for the preparation of the aforesaid compounds. The new products of Formulas I, II, III and IV are useful as sedatives, hypnotics, tranquilizers, muscle relaxants and anticonvulsants. Also, as feed additives for increasing growth rate and feed efficiency of livestock.
摘要翻译：本发明涉及由式WHEREIN R选自氢，一至三个碳原子的低级烷基，苯基或苯基的苯基二苯并噻吩并[4,3-a] ，苄基，硝基甲基，氰基甲基，具有1至3个碳原子的烷氧基部分的低级烷氧基甲基，其中N是1的整数2，R'和R“各自选自氢和一个至少一个的烷基三个碳原子合并时是四至五个碳原子的亚烷基桥; R1选自羟基和低级酰氧基; R2，R3，R4和R5选自氢，一至三个碳原子的低级烷基，卤素，硝基，氰基，三氟甲基，低级烷氧基，低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基，氨基，低级烷酰基氨基和低级二烷基氨基; 和其药理学上可接受的酸加成。它还涉及制备上述化合物的新方法。式I，II，III和IV的新产品可用作镇静剂，催眠药，镇定剂，肌肉松弛剂和抗惊厥药。另外，作为用于增加牲畜生长速度和饲料效率的饲料添加剂。

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