公开(公告)号：US6362217B2

公开(公告)日：2002-03-26

申请号：US80226401

申请日：2001-03-08

Applicant: SQUIBB BRISTOL MYERS CO

Inventor： KADOW JOHN F ,  SCHWARTZ WENDY S ,  SCOLA PAUL M ,  XUE QIUFEN MAY ,  WITTMAN MARK D ,  WU MU-JEN

IPC: A61K31/337 ,  A61K31/341 ,  A61P35/00 ,  C07D305/14 ,  C07D407/12 ,  A61K31/35

CPC classification number: C07D407/12 ,  C07D305/14

Abstract: The present invention concerns novel 7-deoxy taxane derivatives their use as antitumor agents, and pharmaceutical formulations.

Abstract translation: 本发明涉及其用作抗肿瘤剂的新型7-脱氧紫杉烷衍生物和药物制剂。

公开(公告)号：US6362172B2

公开(公告)日：2002-03-26

申请号：US75743801

申请日：2001-01-10

Applicant: SQUIBB BRISTOL MYERS CO

Inventor： UEDA YASUTSUGU ,  MATISKELLA JOHN D ,  GOLIK JERZY ,  HUDYMA THOMAS W ,  CHEN CHUNG-PIN

IPC: A61K31/661 ,  A61K31/662 ,  A61P31/10 ,  C07D249/08 ,  C07D403/06 ,  C07D417/06 ,  C07F9/09 ,  C07F9/6518 ,  C07F9/6539 ,  C07F9/6558 ,  A61K31/375

CPC classification number: C07F9/65586 ,  C07F9/65181 ,  C07F9/65583

Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formulawherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and R and R1 are as defined in the specification.

Abstract translation: 提供了具有仲羟基或叔羟基的三唑抗真菌化合物的水溶性前药。 更具体地，提供了具有通式化合物的新的水溶性三唑抗真菌化合物，A是包含仲羟基或叔羟基的三唑抗真菌化合物的非羟基部分，R和R 1如说明书中所定义。

公开(公告)号：US3928336A

公开(公告)日：1975-12-23

申请号：US49263674

申请日：1974-07-29

Applicant: BRISTOL MYERS CO

Inventor： ESSERY JOHN MICHAEL ,  CHENEY LEE CANNON

IPC: C07D271/08 ,  C07D501/36

CPC classification number: C07D271/08

Abstract: 7-(D-( Alpha -Amino- Alpha -phenyl-, 2-thienyl- and 3thienylacetamido)-3-(3-methyl-1,2,5-oxadiazol-4yl)carbonylthiomethyl-3 -cephem-4-carboxylic acids and their pharmaceutically acceptable salts are valuable as antibacterial agents, as nutritional supplements in animal feeds, as agents for the treatment of mastitis in cattle and as therapeutic agents in poultry and animals, including man. The compounds are especially useful in the treatment, particularly by oral administration, of infectious diseases caused by many Gram-positive and Gramnegative bacteria. Also included within the invention are easily cleavable esters of the abovementioned acids and pharmaceutically acceptable acid addition salts of said esters.

Abstract translation: 7- [D-（α-氨基-α-苯基 - ，2-噻吩基和3-噻吩基乙酰氨基）-3-（3-甲基-1,2,5-恶二唑-4-基）羰基硫代] -3-头孢烯 -4-羧酸及其药学上可接受的盐作为抗菌剂作为动物饲料中的营养补充剂是有价值的，作为用于治疗牛的乳腺炎的药物和作为包括人在内的家禽和动物中的治疗剂，该化合物特别适用于 特别是通过口服给药由许多革兰氏阳性和革兰氏阴性细菌引起的感染性疾病的治疗，本发明还包括上述酸的容易切割的酯和所述酯的药学上可接受的酸加成盐。

公开(公告)号：US3928334A

公开(公告)日：1975-12-23

申请号：US47697274

申请日：1974-06-06

Applicant: BRISTOL MYERS CO

Inventor： ESSERY JOHN MICHAEL

IPC: C07D501/06 ,  C07D501/04 ,  C07D501/20 ,  C07D501/36

CPC classification number: C07D501/36

Abstract: Cefamandole is produced by the consecutive steps of A. MIXING SUBSTANTIALLY EQUIMOLAR WEIGHTS OF N-ethoxycarbonyl-2ethoxy-1,2-dihydroquinoline and of a derivative of D-mandelic acid having the formula

WHEREIN THE HYDROXYL BLOCKING GROUP R represents dichloroacetyl, silyl, tetrahydropyranyl or formyl is an organic solvent; B. ADDING THERETO, PREFERABLY SLOWLY, A SOLUTION CONTAINING SUBSTANTIALLY THE SAME NUMBER OF MOLES OF 7-AMINO-3-(1METHYLTETRAZOL-5-YL)THIOMETHYL-3-CEPHEM-4-CARBOXYLIC ACID OR A SALT OR AN EASILY HYDROLYZED Schiff base thereof to produce the intermediate acid having the formula

OR A SALT THEREOF AND C. REMOVING SAID HYDROXYL BLOCKING GROUP R by conventional chemical methods to produce said cefamandole or salt thereof.

Abstract translation: 头孢麦醇是通过连续步骤A.制备N-乙氧基羰基-2-乙氧基-1,2-二氢喹啉的主要均衡重量和具有下式的D-扁桃酸的衍生物：其中羟基封端基团R代表二氯乙酰基，甲硅烷基 ，四氢吡喃基或甲酰基是有机溶剂; B.优选地，优选地，缓慢地含有相应数量的7-氨基-3-（1-甲基甲基-5-甲基）硫代-3-氰基-4-羧酸或盐或易溶于水的溶液 席夫碱，通过常规的化学方法制备具有下式的中间体酸或其盐和C。通过常规的化学方法制备所述头孢丹多或其盐。

公开(公告)号：US3910920A

公开(公告)日：1975-10-07

申请号：US41346473

申请日：1973-11-07

Applicant: BRISTOL MYERS CO

Inventor： MENARD MARCEL ,  RIVEST PIERRE

IPC: C07C49/755 ,  C07D221/22 ,  C07D303/36 ,  C01D221/28 ,  A61K31/485 ,  C07D491/08

CPC classification number: C07D221/22 ,  C07C49/755 ,  C07D303/36 ,  Y10S514/823

Abstract: 3,14,17-Substituted-6,7-Tetramethylenemorphinans have been found to possess potent narcotic agonist and/or antagonist activity. In particular, the compounds l-17-cyclopropylmethyl-3,14 Alpha (and14 Beta )-dihydroxy-6,7-tetramethylenemorphinan have been found to possess potent narcotic antagonist activity. These compounds are prepared by total synthesis and are not derived from opium alkaloids.

Abstract translation: 已经发现3,14,17-取代的6,7-四亚甲基脑啡肽具有有效的麻醉剂激动剂和/或拮抗剂活性。 特别地，已经发现化合物1-17-环丙基甲基-3,14α（和-14β） - 二羟基-6,7-四甲基孕酮具有有效的麻醉拮抗剂活性。 这些化合物通过全合成制备而不是来自鸦片生物碱。

公开(公告)号：US3886138A

公开(公告)日：1975-05-27

申请号：US42719973

申请日：1973-12-21

Applicant: BRISTOL MYERS CO

Inventor： NAITO TAKAYUKI ,  NAKAGAWA SUSUMU ,  ABE YOSHIO

IPC: C07H15/234 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61P31/04 ,  B01J23/00 ,  C07B61/00 ,  C07H15/236 ,  C07C47/18

CPC classification number: C07H15/234

Abstract: 4''-Deoxykanamycin A, which is prepared from kanamycin A, possesses improved anti-pseudomonas activity as compared to kanamycin A.

Abstract translation: 与卡那霉素A相比，由卡那霉素A制备的4'-脱氧卡那霉素A具有改善的抗假单胞菌活性。

公开(公告)号：US3876760A

公开(公告)日：1975-04-08

申请号：US27040972

申请日：1972-07-10

Applicant: BRISTOL MYERS CO

Inventor： NERSESIAN ARA ,  HUBNER FRED ,  DURBAK TARAS

IPC: A61K8/39 ,  A61K8/73 ,  A61Q5/06 ,  A61K7/06

CPC classification number: A61K8/39 ,  A61K8/731 ,  A61K2800/5426 ,  A61Q5/06 ,  Y10S424/01 ,  Y10S424/02 ,  Y10S424/04 ,  Y10S514/941

Abstract: A hair dressing composition comprising a hair substantive quaternary resin to impart hair-holding properties to hair when supplied, and a grooming agent; the grooming agent preferably being incompatible with the quaternary resin.

公开(公告)号：US3872122A

公开(公告)日：1975-03-18

申请号：US35121773

申请日：1973-04-16

Applicant: BRISTOL MYERS CO

Inventor： JUBY PETER FREDERICK ,  HUDYMA THOMAS WILLIAM

IPC: C07D487/04 ,  A61K31/55 ,  A61P9/00 ,  A61P29/00 ,  C07D265/26 ,  C07D57/02

CPC classification number: C07D265/26

Abstract: Appropriately substituted 11H-pyrimido(4,5-b)(1,4)benzodiazepines have shown biological activity, e.g., antihypoxic, hypothermic, antipyretic and anti-inflammatory. An example of a potent anti-hypoxic agent is 5,6-dihydro-11-methyl11H-pyrimido(4,5-b)(1,4)-benzodiazepine.

Abstract translation: 适当取代的11H-嘧啶并[4,5-b] - [1,4]苯并二氮杂卓已显示出生物活性，例如抗低氧，低温，解热和抗炎。 有效的抗缺氧剂的实例是5,6-二氢-11-甲基-11H-嘧啶并[4,5-b] [1,4] - 苯并二氮杂。

公开(公告)号：US3863797A

公开(公告)日：1975-02-04

申请号：US30695572

申请日：1972-11-15

Applicant: BRISTOL MYERS CO

Inventor： BERGHAHN WALTER G

IPC: B65D41/04 ,  B65D41/16 ,  B65D50/06 ,  B65D55/02 ,  A61J1/00 ,  B65D85/56

CPC classification number: B65D50/061

Abstract: A safety closure-bottle assembly comprising a snap-on closure and bottle in which the closure is provided with a tab and the bottle neck with a notched flange which registers with said tab.

Abstract translation: 一种安全闭合瓶组件，其包括卡扣式封闭件和瓶子，其中所述封闭件设置有突片，并且所述瓶颈具有与所述突出部对准的带凹口的凸缘。

公开(公告)号：US3860574A

公开(公告)日：1975-01-14

申请号：US37419173

申请日：1973-06-27

Applicant: BRISTOL MYERS CO

Inventor： NAITO TAKAYUKI ,  NAKAGAWA SUSUMU ,  OKA MASAHISA

IPC: C07C271/22 ,  C07H15/232 ,  C07C95/04

CPC classification number: C07H15/232 ,  C07C271/22

Abstract: Derivatives of neomycin B and C have been prepared which possess substantially improved antibacterial activity. An example of such an agent is 1-(L-(-)- gamma -amino- Alpha -hydroxybutyryl)neomycin B (IVa, BB-K77).

Abstract translation: 已经制备出具有显着改善的抗菌活性的新霉素B和C的衍生物。 这种试剂的实例是1- [L - （ - ） - γ-氨基-α-羟基丁酰] - 霉素B [IVa，BB-K77]。