| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 161 | CHEMOKINE RECEPTOR ANTAGONISTS AND METHODS OF USE THEREFOR | US09362837 | 1999-07-28 | US20020119973A1 | 2002-08-29 | JAY R. LULY; YOSHISUKE NAKASATO; ETSUO OHSHIMA; HIROKI SONE; OSAMU KOTERA; GERALDINE C.B. HARRIMAN |
| Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: 1 and physiologically acceptable salts thereof. 2 | ||||||
| 162 | Derivatives of amide analogs of certain methano bridged quinolizines | US181888 | 1998-10-29 | US5955470A | 1999-09-21 | Maurice W. Gittos |
| This invention relates to novel amide derivatives of certain 2,6-methano-2H-quinolizine-type compounds, to the intermediates and processes for their preparation, to their ability to antagonize the effects of serotonin at the 5HT.sub.3 receptors, and to their end-use application in the treatment of chemotherapeutically-induced nausea and vomiting, as anti-anxiety agents, in the symptomatic treatment of pain associated with migraine, as anti-arrhythmic agents, in the treatment of cognitive disorders, in treating hallucinatory endogenous psychoses of the type manifested in patients suffering from schizophrenia, and mania, in the treatment of glaucoma, for stimulating gastric motility, to combat drug abuse, to treat sleep apnea and to treat irritable bowel syndrome. | ||||||
| 163 | Substituted phenyl sulfonamides as selective .beta. 3 agonists for the treatment of diabetes and obesity | US168105 | 1993-12-15 | US5451677A | 1995-09-19 | Michael H. Fisher; Robert J. Mathvink; Hyun O. Ok; Emma R. Parmee; Ann E. Weber |
| Substituted phenylsulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted alkyl epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed. | ||||||
| 164 | Stilbene derivatives as anticancer agents | US81755 | 1993-06-23 | US5430062A | 1995-07-04 | Mark S. Cushman; Ernest Hamel |
| The present invention relates to stilbene derivatives which possess utility as anti-cancer agents. The compounds can be used to treat cancers which are susceptible to treatment therewith, and can be utilized in a method of treating such cancers. Pharmaceutical compositions containing the compounds are disclosed. Three preferred compounds among those disclosed are (Z)-1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene, (Z)-1-(4-methylphenyl)-2-(3,4,5-trimethoxyphenyl)ethene, and 4-methyl-3',4',5'-trimethoxybenzylaniline hydrochloride. | ||||||
| 165 | Multicyclic tertiary amine polyaromatic squalene synthase inhibitors | US959898 | 1992-10-13 | US5385912A | 1995-01-31 | Kent Neuenschwander; Dilip Amin; Anthony C. Scotese; Robert L. Morris |
| This invention relates to polycyclic compounds containing two mono- and/or bicyclic rings and a basic tertiary amino group capable of forming an ammonium ion at biological pH and which reduces levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.The compounds of this invention are described by the formula ##STR1## where Ar I is phenylene or naphthylene, Ar II is phenyl or naphthyl and A is 1-azabicyclo[2.2.2]octan-3-yl. | ||||||
| 166 | Medicaments for treatment on prevention of withdrawal syndrome | US246550 | 1988-09-09 | US4948803A | 1990-08-14 | Michael B. Tyers |
| The treatment of withdrawal symptoms from drugs using azabicyclo indazole-3-carboxamides. | ||||||
| 167 | .alpha..sub.2 -adrenoceptor antagonistic arylquinolizines | US90641 | 1987-08-28 | US4824849A | 1989-04-25 | John J. Baldwin; Joel R. Huff; Joseph P. Vacca; Steven D. Young; Jane deSolms; James P. Guare, Jr. |
| Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, platelet aggregation inhibitors, antiobesity agents, and modifiers of gastrointestinal motility. | ||||||
| 168 | Quinolizinone compounds, and pharmaceutical composition comprising the same, useful as anti-ulcerative and anti-allergic agents | US770953 | 1985-08-30 | US4698349A | 1987-10-06 | Yoshihiko Kitaura; Teruo Oku; Hideo Hirai; Tosiyuki Yamamoto; Masashi Hashimoto |
| The invention relates to novel quinolizinone compounds, of inhibitory activity on allergies and ulcers, of the formula: ##STR1## wherein R.sup.1 is carboxy, carbamoyl Y.sup.1, phenylcarbamoyl which may have hydroxy, cyano or thiocarbamoyl,R.sup.7 is hydrogen or aryl selected from phenyl, tolyl, xylyl, cumenyl, naphthyl and biphenylyl;R.sup.2 is hydrogen, hydroxy, lower alkyl or lower alkoxy; andR.sup.3 is hydrogen, hydroxy, lower alkyl, lower alkoxy, lower alkenyloxy, phenyl, naphthyl, biphenylyl, phenyl having one or more substituent(s) selected from halogen, lower alkyl and lower alkoxy, arylthio selected from phenylthio, tolylthio, xylylthio, cumenylthio, naphthylthio and biphenylylthio, aroyl selected from benzoyl, toluoyl and naphthoyl, ar(lower)alkyl selected from phenyl(lower)alkyl, tolyl(lower)alkyl, xylyl(lower)alkyl, cumenyl(lower)alkyl, naphthyl(lower)alkyl and biphenylyl(lower)alkyl, arenesulfonyl selected from benzenesulfonyl and p-toluenesulfonyl, arylamino selected from phenylamino, naphthylamino, biphenylylamino, phenylamino having lower alkyl on the nitrogen atom or aryloxy selected from phenoxy and tolyloxy; or pharmaceutically acceptable salts thereof. | ||||||
| 169 | Reversing amnesia with saturated tricyclic nitrogen-containing diones | US687182 | 1985-01-07 | US4562195A | 1985-12-31 | Donald E. Butler; Yvon J. L'Italien |
| A class of novel saturated, fused-ring, tricyclic, nitrogen-containing diones are useful as agents in treating electro-convulsive shock-induced amnesia. A method of preparing the compounds, pharmaceutical compositions including the compounds, and a method of treating amnesia are disclosed. | ||||||
| 170 | Process for the preparation of vincaminic acid esters | US425866 | 1982-09-28 | US4464534A | 1984-08-07 | Csaba Szantay; Lajos Szabo; Gyorgy Kalaus; Janos Kreidl; Andras Nemes; Maria Farkas nee Kirjak; Gyorgy Visky; Laszlo Czibula |
| The invention relates to a new process for the preparation of apovincaminic acid esters. More particularly, the invention concerns a process for preparing racemic and optionally active vincaminic acid esters of the formula (I) ##STR1## in which R.sup.1 and R.sup.2 independently stand for alkyl having from one to 6 carbon atoms, and 14-epimers thereof.According to the invention an octahydroindolo[2,3-a]quinolizine-oxime ester of the formula (II) ##STR2## in which R.sup.1 and R.sup.2 have the same meaning as defined above, is reacted with an aqueous solution of sulfurous acid or a salt thereof at a temperature of 80.degree. to 110.degree. C. and the 14-epimeric mixture obtained is epimerized or separated in a known manner and if desired, the racemic vincaminic acid esters are resolved.The valuable, pharmaceutically active compounds of the formula (I) can be prepared according to the invention in a considerably improved yield and the undesired side reactions can be suppressed and/or the by-products can easily be converted into other pharmaceutically active materials. | ||||||
| 171 | Process and intermediates for preparing 3-[4-(disubstituted-amino)phenyl] o r | US69979 | 1979-08-27 | US4255577A | 1981-03-10 | Paul J. Schmidt; William M. Hung |
| 3-[4-(Disubstituted-amino)phenyl] or (9-julolidinyl)-3-(diphenylamino)phthalides useful as color formers in pressure-sensitive and thermal marking systems are prepared by reaction of 2-[4-(disubstituted-amino)benzoyl] or (9-julolidinyl-carbonyl)benzoic acids with diphenylamines. | ||||||
| 172 | 세파코스포린 유도체의 제조 방법 | KR1019810000527 | 1981-02-19 | KR1019830005245A | 1983-08-03 | 위르겔블룸바하 |
| 내용없음 | ||||||
| 173 | 세파피린의 아미노산염 제조 방법 | KR1019810001076 | 1981-03-31 | KR1019830005244A | 1983-08-03 | 마르코팔시아니 |
| 내용없음 | ||||||
| 174 | 아미노산 세파드록실염의 제조 방법 | KR1019810001077 | 1981-03-31 | KR1019830005239A | 1983-08-03 | 마르코팔시아니 |
| 내용없음 | ||||||
| 175 | 리파마이신 유도체의 제조 방법 | KR1019810000443 | 1981-02-13 | KR1019830005227A | 1983-08-03 | 레오나르도바르실리 |
| 내용없음 | ||||||
| 176 | 이미다조(4,5-6) 피리딘 유도체의 제조 방법 | KR1019810000983 | 1981-03-23 | KR1019830005216A | 1983-08-03 | 죠오지요어레샤외3인 |
| 내용없음 | ||||||
| 177 | 1-R-5-PY-6-Q-1H-피라졸로[3, 4-b] 피리딘-3-아민 또는 그의 산부가염의 제조 방법 | KR1019810000800 | 1981-03-12 | KR1019830005214A | 1983-08-03 | 죠오지요어레셔어몬테디이그루엣트 |
| 내용없음 | ||||||
| 178 | 샌드위신의 4급 유도체의 제조방법 | KR1019770000629 | 1977-03-16 | KR100010324B1 | 1981-09-02 | 피터펫트; 미카엘쉬나이더 |
| 179 | 샌드위신의 4급 유도체의 제조방법 | KR1019770000629 | 1977-03-16 | KR1019810000658B1 | 1981-06-16 | 피터펫트; 미카엘쉬나이더 |
| Quaternary sandwicin derivs.(I; R = C1-5 normal or side chain alkyl; X = anion of inorganic or organic acid), having anti-adrenalin activity, were prepd. by reacting sandwicinum halide with alkali followed by reacting with organic or inorganic acid. The sandwicinum halide was prepd. by reacting sandwicin with alkylhalide which was constituted with C1-5 normal chain or side chain alkyl group. | ||||||
| 180 | Compositions and methods for making terpenoid indole alkaloids | US16081645 | 2017-03-02 | US11072613B2 | 2021-07-27 | Vincenzo De Luca; Yang Qu |
| Methods that may be used for the manufacture of a class of chemical compounds known as terpenoid indole alkaloids, including tabersonine and catharanthine are provided. Compositions useful for the synthesis of terpenoid indole alkaloids, including tabersonine and catharanthine are also provided. The provided compounds are useful in the manufacture of chemotherapeutic agents. | ||||||
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