| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 1 | 抗癌药物及将其用于治疗恶性黑色素瘤及其它癌症 | CN201080016304.7 | 2010-04-26 | CN102438449B | 2014-06-18 | G·R·古卡拉吉; S·卡斯娜; R·R·古卡拉吉; V·K·R·R·古卡拉吉; V·索门帕利; T·吉拉考提; K·布湖帕瑟拉吉; K·森古卜他; V·K·R·阿鲁瑞 |
| 将硒酚三氮烯类似物，它们的组合物，互变异构体，立体异构体，多晶型，水合物，溶剂和药学可接受的盐及其混合物用于治疗转移性恶性黑色素瘤及其它癌症。所述的硒酚三氮烯类似物具有通式(I)或(II)：其中如说明书所述地取代R1、R2、R3、R6和R7。这些化合物能够治疗的其它癌症非限制性地包括恶性黑色素瘤，白血病，淋巴瘤(霍奇金和非霍奇金)，肉瘤(尤文氏肉瘤)，脑肿瘤，中枢神经系统(CNS)的转移，脑胶质瘤，如乳房癌等癌症，前列腺癌，肺癌(小细胞和非小细胞)癌，结肠癌癌，胰腺癌，头颈部肿瘤及口咽部鳞状细胞癌。 | ||||||
| 2 | α－酮酰胺多元催化蛋白酶抑制剂 | CN98809973.X | 1998-10-07 | CN1172672C | 2004-10-27 | 桑卡尔·查特吉; 约翰·P·马拉姆 |
| 本发明涉及多元催化蛋白酶(MCP)的α-酮酰胺抑制剂、含有这些抑制剂的组合物和这些MCP抑制剂的应用方法。本发明提供的MCP抑制剂适用于例如减少多种生理状态中肌肉质量损失的发生率。 | ||||||
| 3 | 环烷基酮基哌啶速激肽受体拮抗剂 | CN200580039784.8 | 2005-11-18 | CN101061096A | 2007-10-24 | R·J·德维塔; S·G·米尔斯; R·埃德; J·R·杨 |
| 本发明涉及用作神经激肽－1(NK－1)受体拮抗剂和速激肽尤其是P物质的抑制剂的某些哌啶化合物。本发明还涉及包含这些作为活性成分的化合物的药用制剂和化合物及其制剂在治疗包括呕吐、尿失禁、抑郁和焦虑的某些病症中的应用。 | ||||||
| 4 | 改良的水溶性药物制剂 | CN00805399.5 | 2000-03-20 | CN1156461C | 2004-07-07 | D·F·埃尔科波尼; R·S·小弗拉德卡; P·R·斯泰约斯 |
| 本发明描述了一种微溶于水的结晶态药物活性剂制剂，其中活性剂被转化成它的非晶态即通常疏水性载体的固溶体形式，并在该状态下稳定。非晶态通过制剂的组分来稳定，使改良后的组合物储藏期限长。该稳定的制剂其活性剂的溶解度和生物利用度增加。活性剂溶液由其组分来稳定，防止了微溶性结晶态的活性剂从它的水溶液中重结晶和沉淀。 | ||||||
| 5 | 改良的水溶性药物制剂 | CN00805399.5 | 2000-03-20 | CN1379768A | 2002-11-13 | D·F·埃尔科波尼; R·S·小弗拉德卡; P·R·斯泰约斯 |
| 本发明描述了一种微溶于水的结晶态药物活性剂制剂,其中活性剂被转化成它的非晶态即通常疏水性载体的固溶体形式,并在该状态下稳定。非晶态通过制剂的组分来稳定,使改良后的组合物储藏期限长。该稳定的制剂其活性剂的溶解度和生物利用度增加。活性剂溶液由其组分来稳定,防止了微溶性结晶态的活性剂从它的水溶液中重结晶和沉淀。 | ||||||
| 6 | α－酮酰胺多元催化蛋白酶抑制剂 | CN98809973.X | 1998-10-07 | CN1274285A | 2000-11-22 | 桑卡尔·查特吉; 约翰·P·马拉姆 |
| 本发明涉及多元催化蛋白酶(MCP)的α－酮酰胺抑制剂、含有这些抑制剂的组合物和这些MCP抑制剂的应用方法。本发明提供的MCP抑制剂适用于例如减少多种生理状态中肌肉质量损失的发生率。 | ||||||
| 7 | 一种以芴为核心的化合物、制备方法及其应用 | CN201811159106.0 | 2018-09-30 | CN110964021A | 2020-04-07 | 李崇; 庞羽佳; 王芳; 张兆超 |
| 本发明公开了一种以芴为核心的化合物、制备方法及其应用，属于半导体技术领域。本发明提供的化合物的结构如通式(I)所示： 本发明还公开了上述以芴为核心的化合物的制备方法和应用。本发明的化合物含有芴类衍生物及六元环并环衍生物结构，具有较高的玻璃化温度和分子热稳定性，合适的HOMO和LUMO能级，较高Eg，通过器件结构优化，可有效提升OLED器件的光电性能以及OLED器件的寿命。 | ||||||
| 8 | 环烷基哌啶速激肽受体拮抗剂 | CN200580039546.7 | 2005-11-18 | CN101061095A | 2007-10-24 | R·J·德维塔; S·G·米尔斯; R·埃德; J·R·杨 |
| 本发明涉及某些可以用作神经激肽－1(NK－1)受体拮抗剂和速激肽(并且特别是P物质)抑制剂的哌啶化合物。本发明还涉及含有这些化合物作为活性成分的药物制剂，和这些化合物和它们的制剂在治疗某些疾病中的用途，所述疾病包括呕吐、尿失禁、抑郁和焦虑。 | ||||||
| 9 | HIV整合酶抑制剂 | CN200580006996.6 | 2005-03-04 | CN101014574A | 2007-08-08 | M·M·莫里塞特; P·D·威廉斯; J·S·维; T·E·费希尔; T·A·利尔 |
| 式I的化合物是HIV整合酶的抑制剂和HIV复制的抑制剂，其中Z、R1、R2、R3、R4、R5、R6、R7、R8和R9在说明书中定义。该化合物可用于预防和治疗HIV感染以及预防、延迟AIDS的发病和治疗AIDS。该化合物以化合物本身的形式或者药用可接受盐的形式用于抗HIV感染和AIDS。该化合物和其盐可以作为药物组合物的成分，任选的与其它抗病毒剂、免疫调节剂、抗生素或疫苗结合使用。 | ||||||
| 10 | 治疗感冒或过敏性鼻炎的方法 | CN97194611.6 | 1997-03-17 | CN1218368A | 1999-06-02 | K·W·约翰逊; D·L·G·纳尔逊; L·A·菲布斯 |
| 本发明提供了一种治疗或缓解感冒或过敏性鼻炎症状的方法,包括对需要治疗的哺乳动物给予5－HT2拮抗剂。 | ||||||
| 11 | Silver halide color photographic sensitive material | JP26533987 | 1987-10-22 | JPS63314544A | 1988-12-22 | FUJIWARA MITSUTO; UCHIDA TAKU |
| PURPOSE:To improve the graininess of a color image by incorporating a component capable of being oxidized to give an oxidation product which permits an oxidation-reduction reaction with an oxidant of a color developing main agent, or a compd. capable of releasing a precursor of said component by reaction with the oxidant of the color developing main agent. CONSTITUTION:The emulsion layer is composed of a component capable of being oxidized in a process of color development processing, and the oxidation product of said component contains a component (a useful component) capable of causing an oxidation-reduction reaction with the oxidant of a color developing main agent or the compd. (compd.) capable of releasing a precursor of said component by reaction with said oxidant. Namely, as said oxidant is produced at a short distance from a reaction site by using a compd. which is subjected to the oxidation-reduction reaction with the color developing main agent after the photographic useful component is oxidized, and the color matter is formed by coupling reaction of the coupler, the space between the coloring matter clouds is buried whereby the gradation effect of the color image generates, and the graininess of said image is improved. | ||||||
| 12 | Pharmaceutical formulations with improved aqueous solubility | JP2000606587 | 2000-03-20 | JP2003531099A | 2003-10-21 | エフ アーコボニ，デビッド; アール スタジオス，パメラ; エス ジュニア ブラディカ，ロナルド |
| (57)【要約】 【課題】 常態で殆ど水不溶性の結晶状の製薬上活性な薬剤の改良された水溶解度をもつ医薬製剤を提供するものである。 【解決手段】 （ａ）疎水性賦形剤を、該疎水性賦形剤が融解する温度以上の温度であり且つ溶融した疎水性賦形剤に製薬上活性な薬剤が溶解する温度に加熱し、（ｂ）製薬上活性な薬剤を溶融した賦形剤に溶解し、疎水性賦形剤中に製薬上活性な薬剤の溶融溶液を作り、（ｃ）製薬上活性な薬剤と疎水性賦形剤との溶融溶液に安定剤の安定有効量を加え、次いで（ｄ）工程（ｃ）からの溶融混合物を冷却した崩壊剤及び任意成分としての結合剤と共に３０°Ｃ以下の温度で粒状化し、疎水性賦形剤中に無定形の形態で安定した製薬上活性な薬剤の固溶体を含む粒状化粒子を形成する、各工程から製造する。 【効果】 無定形状態で製剤組成物によって安定化され、そして改良された組成物の長期貯蔵寿命を提供する。 この安定化製剤はまた活性薬剤の溶解度及び生物学的利用能を増加する。 活性薬剤の溶液はこの組成物によって安定化され、その水溶液において活性薬剤が殆ど溶解しない結晶性形態への再結晶及び沈殿を防止する。 | ||||||
| 13 | Salt of a weak base | JP2006507175 | 2004-03-12 | JP2006519852A | 2006-08-31 | タパン サングビ，; サミュエル エイチ． ヤルコースキー， |
| 薬学的組成物であって、以下の式：
【化１】 の弱塩基化合物の塩であって、Ｘは、水素、ハロゲン、７個未満の炭素原子のアルキルもしくは７個未満の炭素原子のアルコキシであり；ｎは、４未満の正の整数であり；Ｙは、水素、塩素、ニトロ、メチル、エチルまたはオキシクロロであり；Ｒは、水素、アルキル基が３〜６個の炭素原子を有するアルキルアミノカルボニルまたは１〜８個の炭素原子を有するアルキル基であり、Ｒ２は、４−チアゾリル、Ｒが７個未満の炭素原子の脂肪族炭化水素であるＮＨＣＯＯＲ１、または７個未満の炭素原子のアルキル基である、弱塩基化合物の塩；１つ以上の遊離の酸；ならびに任意の薬学的添加物を含む、薬学的組成物が提供される。 |
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| 14 | Radiation-sensitive composition | JP9280188 | 1988-04-15 | JPH07117695B2 | 1995-12-18 | 剛希 中村; 圭三 古屋; 當昌 坪井 |
| 15 | Radiation sensitive composition | JP9280188 | 1988-04-15 | JPH01263648A | 1989-10-20 | NAKAMURA TAKEKI; TSUBOI MASAAKI; FURUYA KEIZO |
| PURPOSE: To realize the prescribed various kind of the functions of the title composition by irradiating radiation rays to the composition by incorporating a specified compd. and a photoreducing agent capable of forming an oxidation- reduction coupling with said compd. in the composition. CONSTITUTION: The compd. shown by formula I and the photoreducing agent capable of forming the oxidation-reduction coupling with the compd. are incorporated in the composition. In formula I, N is nitrogen atom, X is a group contg. oxygen, sulfur or nitrogen atom, R 1, R 2, R 3 and R 4 bound to a group contg. nitrogen atom. are each a single bond or a substd. or an unsatd. alkyl group or a sulfonyl group having a substd. or an unsubstd. alkyl or aryl group. And UG is a group capable of being released by cleavaging a N-X binding caused by forming the oxidation-reduction coupling with the photoreducing agent by irradiating the radiation rays, as a trigger. R 1, R 2, R 3 and R 4 are bound with each other through full lines and at least one of the groups is bound with the group UG through a broken line. COPYRIGHT: (C)1989,JPO&Japio | ||||||
| 16 | HYDROXAMIC ACID DERIVATIVES AS METALLOPROTEASE INHIBITORS | PCT/US2005013434 | 2005-04-19 | WO2005117882A9 | 2007-03-01 | BURNS DAVID M; YAO WENQING; HE CHUNHONG |
| The present invention provides compounds of Formula (I ) or (II), salt form or prodrug thereof, wherein variables are defined herein, that are modulators of metalloproteases such as matrix metalloproteases (MMPs) and ADAMs. The compounds or compositions described herein can be used to treat diseases associated with metalloprotease activity including, for example, arthritis, cancer, cardiovascular disorders, skin disorders, inflammation or allergic conditions. | ||||||
| 17 | METHODS FOR SYNTHESIZING 2-SUBSTITUTED IMIDAZOLES | PCT/US1998/007614 | 1998-04-17 | WO98046571A1 | 1998-10-22 | |
| The present invention is a method of preparing 2-substituted imidazoles from readily available imidazoles having a leaving group in the 2-position, by alkylating the imidazole under mild conditions to afford a 3-N-alkylated imidazolium salt; and coupling the imidazolium salt with a nucleophile also under mild conditions to afford a 2-substituted 3-N-alkylated imidazolium salt. The reaction product can optionally be isolated and purified. The 2-substituted 3-N-alkylated imidazolium salt is hydrolyzed to afford a 2-substituted imidazole. Alternatively, the imidazole is coupled with a nucleophile in the presence of fluoride ion to provide a 2-substituted imidazole. | ||||||
| 18 | NOVEL COMPOUNDS HAVING A BENZISOSELEN-AZOLINE AND -AZINE STRUCTURE, METHOD FOR PREPARING SAME AND THERAPEUTIC USES THEREOF | CA2164642 | 1995-04-07 | CA2164642C | 2008-03-25 | ERDELMEIER IRENE; CHAUDIERE JEAN; MOUTET MARC; YADAN JEAN-CLAUDE |
| The invention concerns novel benzisoselen-azoline and -azine derivatives. These novel derivatives have the following general formula (II): |
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| 19 | GRANULAR PARTICLE, SOLID DOSAGE FORM COMPRISING IT, AND METHOD FOR PREPARING THE SAME | IL14514001 | 2001-08-27 | IL145140A | 2006-08-20 | |
| 20 | CYCLOALKYL KETO PIPERIDINE TACHYKININ RECEPTOR ANTAGONISTS | CA2587195 | 2005-11-18 | CA2587195A1 | 2006-07-13 | YOUNG JONATHAN R; DEVITA ROBERT J; EID RONSAR; MILLS SANDER G |
| The present invention is directed to certain piperidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety. | ||||||
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