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1. 发明申请

WO99031054A2 NOVEL P-AMINOPHENOL DERIVATIVES AND THE USE THEREOF 审中-公开
标题翻译：新的对氨基苯酚衍生物及其
公开(公告)号：WO99031054A2
公开(公告)日：1999-06-24
申请号：PCT/EP1998/007961
申请日：1998-12-08
IPC分类号： A61K8/00 , A61K8/33 , A61K8/41 , A61K8/46 , A61K8/49 , A61Q5/10 , C07C215/76 , C07C217/76 , C07C317/18 , C07C317/28 , C07C323/27 , D06P3/10 , C07C317/00
CPC分类号： A61Q5/10 , A61K8/415 , C07C215/76
摘要： Compounds of general formula (I), wherein A, B,C and D represent, independently from each other, an -OH- or -NHR- group, wherein R stands for a hydrogen atom or a C1-4 alkyl radical, with the proviso that A, B, C or D respectively stands for a hydroxy group, X stands for oxygen, sulphur, a sulfoxy or sulfoxyl group, R and R represent, independently from each other, hydrogen, fluorine, chlorine, a C1-4 alkyl or hydroxyalkyl group or a C2-4-dihydroxy-alkyl group, preferably a C2-dihydroxy alkyl group, and the physically acceptable salts of these compounds are highly suitable for use as developer components in oxidation coloring agents.
摘要翻译：通式（I），其中A，B，C和D独立地表示-OH或-NHR基团，其中R代表氢原子或C 1-4烷基，条件的化合物作为每个A或B和C或D是羟基时，X代表氧，硫，亚砜一个或一个亚砜基团，R <1>和R <2>独立地是Wassserstoff，氟，氯，C1一 1-4烷基或羟烷基或C 2-4二羟基烷基，优选C2二羟基烷基，以及这些化合物的生理上可接受的盐是特别适合作为在氧化显影剂的部件。

2. 发明申请

WO03066572B1 POLYAMINE COMPOUNDS AND COMPOSITIONS FOR USE IN CONJUNCTION WITH CANCER THERAPY 审中-公开
标题翻译：聚氨酯化合物和组合物与癌症治疗相结合
公开(公告)号：WO03066572B1
公开(公告)日：2003-11-20
申请号：PCT/US0303607
申请日：2003-02-07
申请人： WISCONSIN ALUMNI RES FOUND , FAHL WILLIAM E , COPP RICHARD R , OCHSNER CYNTHIA E , PEEBLES DANIEL D , FAHL KATHLEEN L
发明人： FAHL WILLIAM E , COPP RICHARD R , OCHSNER CYNTHIA E , PEEBLES DANIEL D , FAHL KATHLEEN L
IPC分类号： A61P1/00 , A61K31/132 , A61K31/133 , A61K31/145 , A61P17/00 , A61P17/14 , A61P29/00 , C07C211/14 , C07C211/22 , C07C215/18 , C07C215/24 , C07C323/25 , C07C323/27
CPC分类号： C07C323/25 , C07C211/14 , C07C211/22 , C07C215/18 , C07C215/24 , C07C323/27
摘要： The invention provides novel polyamine compounds and pharmaceutical compositions for administration in conjunction with cancer chemotherapy or radiation therapy. The compounds are administered locally to provide protection against the adverse side-effects of chemotherapy or radiation therapy, such as alopecia, mucositis and dermatitis. Pharmaceutical preparations comprising one or more chemoprotective polyamines formulated for topical or local delivery to epithelial or mucosal cells are disclosed. Methods of administering the pharmaceutical preparations are also disclosed.
摘要翻译：本发明提供新的多胺化合物和用于与癌症化学疗法或放射治疗相结合的药物组合物。化合物在局部施用以提供防止化学疗法或放射治疗（例如秃发，粘膜炎和皮炎）的不良副作用的保护。公开了包含一种或多种配制用于局部或局部递送至上皮或粘膜细胞的化学保护性多胺的药物制剂。还公开了施用药物制剂的方法。

3. 发明申请

WO00075105A1 VALENCY PLATFORM MOLECULES COMPRISING AMINOOXY GROUPS 审中-公开
标题翻译：包含AMINOOXY组的VALENCY PLATFORM分子
公开(公告)号：WO00075105A1
公开(公告)日：2000-12-14
申请号：PCT/US2000/015968
申请日：2000-06-08
IPC分类号： C07D295/18 , A61K47/48 , C07C271/16 , C07C271/20 , C07C271/22 , C07C323/27 , C07C323/60 , C07D295/185 , C07D295/205 , C08G65/329 , C08G65/333 , C08G83/00 , C07C323/57 , C07D295/20
CPC分类号： C07D295/185 , A61K47/54 , A61K47/60 , C07C251/60 , C07C271/16 , C07C271/20 , C07C323/60 , C07D295/205 , C07K14/775 , C08B37/0012 , C08G65/329 , C08G65/33396 , C08G83/003
摘要： Molecules comprising aminooxy groups are provided, wherein the aminooxy groups provide attachment sites for the covalent attachment of other molecules. In one embodiment, polyoxyethylene molecules comprising aminooxy groups are provided that can be conjugated to wide variety of biologically active molecules including poly(amino acids). In another embodiment, valency platform molecules comprising aminooxy groups are provided. The aminooxy groups can be used to form covalent bonds with biological molecules such as poly(amino acids). The aminooxy groups can, for example, react with poly(amino acids) modified to contain carbonyl groups, such as glyoxyl groups, to form a conjugate of the valency platform molecule and the biologically active molecule via an oxime bond. The valency platform molecules comprising aminooxy groups are advantageously reactive in the formation of conjugates, and they also can be readily synthesized to form a composition with very low polydispersity.
摘要翻译：提供包含氨基氧基的分子，其中氨基氧基为其它分子的共价连接提供附着位点。在一个实施方案中，提供了包含氨基氧基的聚氧乙烯分子，其可与多种生物活性分子（包括聚（氨基酸））缀合。在另一个实施方案中，提供了包含氨基氧基的化合物平台分子。氨基氧基可用于与生物分子如聚（氨基酸）形成共价键。例如，氨基氧基可以与经修饰以含有羰基（例如乙醛基）的聚（氨基酸）反应，以通过肟键形成价态平台分子和生物活性分子的缀合物。包含氨基氧基的价态平台分子在缀合物的形成中有利地是反应性的，并且它们也可以容易地合成以形成具有非常低的多分散性的组合物。

4. 发明申请

WO01005742A1 QUATERNARY BIS-AMMONIUM SALT PRECURSORS AND THEIR USES AS PRODRUGS HAVING AN ANTIPARASITIC ACTIVITY 审中-公开
标题翻译：季铵盐钠盐前驱物及其作为具有抗生素活性的原料
公开(公告)号：WO01005742A1
公开(公告)日：2001-01-25
申请号：PCT/FR2000/002122
申请日：2000-07-21
IPC分类号： C07D295/08 , A61K31/132 , A61K31/16 , A61K31/39 , A61K31/4025 , A61K31/444 , A61K31/4453 , A61K31/5377 , A61P33/00 , A61P33/02 , A61P33/06 , A61P43/00 , C07C209/74 , C07C211/09 , C07C319/24 , C07C323/41 , C07C327/30 , C07C327/34 , C07D207/09 , C07D277/22 , C07D277/24 , C07D277/30 , C07D277/587 , C07D295/12 , C07D295/14 , C07D295/155 , C07D327/06 , A61K31/14 , A61K31/145 , A61K31/425 , C07C323/27 , C07C323/59
CPC分类号： C07D295/155 , A61K47/541 , C07C211/09 , C07C323/41 , C07C327/30 , C07C327/34 , C07D277/24 , C07D277/30
摘要： The invention concerns drug precursors with antimalarial effect, characterised in that it consists in quaternary bis-ammonium salts of general formula (I) wherein A and A', identical or different, are respectively either a group A1 and A'1 of formula (1) wherein n = 2 to 4; R'1 is hydrogen, C1-C5 alkyl, optionally substituted by an aryl, a hydroxy, an alkoxy, wherein the alkyl comprises 1 to 5 C, or aryloxy and W is halogen or a nucleofuge group; or a group A2 which represents formyl-CHO, or acetyl-COCH3. B and B', identical or different, represent respectively either the group B1 and B'1, if A and A' respectively represent A1, A'1, B1, B'1 representing a group R1 which has the same definition as R'1 above, but cannot be a hydrogen atom; or respectively the groups B2 and B'2, if A and A' represent A2, B2 or B'2 being the group R1 as defined above, or a group of formula (2) wherein -Ra is RS- or RCO-, wherein R is a C1-C6 alkyl, substituted if required, a phenyl or benzyl, wherein the phenyl is substituted if required, the latter being optionally substituted; R2 is hydrogen, C1-C5 alkyl, or a -CH2-COO- (C1-C5)alkyl group; and R3 is hydrogen, C1-C5 alkyl or alkenyl, substituted if required, a phosphate, an alkoxy wherein the alkyl is a C1-C3 alkyl, or aryloxy; or an alkyl (or aryl) carbonyloxy; or R2 and R3 form together a cycle with 5 or 6 C; R and R3 can be bound to form a cycle. alpha represents: either a single bond when A and A' represent A1 and A'1: or when A and A' represent A2, and B2 and B'2 Represent (3) either, when A and A' are -CHO or -COCH3 and B2 and B'2 are R1, a group of formula (4) or a group of formula (5) wherein (a) represents a bond towards Z and (b) a bond towards the nitrogen atom. Z is a C9-C21 alkyl, if required with insertion of one or several bonds, and/or one or several heteroatoms O and/or S and/or several aromatic cycles, and the pharmaceutically acceptable salts of said compounds. Said precursors and cyclized thiazolium derivatives are useful as antiparasitic medicines in particular antimalarial and antibabesiosis.
摘要翻译：本发明涉及具有抗疟作用的药物前体，其特征在于其由通式（I）的季铵盐，其中A和A'分别相同或不同，分别为式（1）的基团A1和A'1 ）其中n = 2至4; R 1是氢，任选地被芳基，羟基，烷氧基取代的C 1 -C 5烷基，其中烷基包括1至5个C，或芳氧基，W是卤素或核离去基团; 或代表甲酰基-YC或乙酰基-COCH 3的基团A2。 B和B'相同或不同，分别表示组B1和B'1，如果A和A'分别表示A1，A'1，B1，B'1，表示具有与R'相同定义的基团R1， 1，但不能是氢原子; 或分别为基团B2和B'2，如果A和A'表示A2，B2或B'2是如上所定义的基团R 1或式（2）的基团，其中-R a是RS-或RCO-，其中 R是C1-C6烷基，如果需要，被取代，苯基或苄基，其中如果需要，苯基被取代，后者任选被取代; R2是氢，C1-C5烷基或-CH2-COO-（C1-C5）烷基; 并且R 3是氢，C 1 -C 5烷基或链烯基，如果需要，被取代，磷酸酯，烷基是C 1 -C 3烷基或芳氧基的烷氧基; 或烷基（或芳基）羰基氧基; 或R 2和R 3与5或6个碳原子一起形成一个循环; R和R3可以结合形成一个循环。 α表示：当A和A'表示A1和A'1时，单键或当A和A'表示A2时，或B2和B'2表示（3）当A和A'为-CHO或 - COCH 3和B 2和B'2是R 1，式（4）或式（5）的基团，其中（a）代表朝向Z的键和（b）朝向氮原子的键。 Z是C9-C21烷基，如果需要，插入一个或多个键，和/或一个或多个杂原子O和/或S和/或若干芳族循环，以及所述化合物的药学上可接受的盐。所述前体和环化噻唑衍生物可用作抗寄生虫药物，特别是抗疟疾和抗生素。

5. 发明申请

WO00016766A1 MEDICAL COMPOSITION CONTAINING NITROETHENEAMINE DERIVATIVE OR SALT THEREOF AS ACTIVE CONSTITUENT 审中-公开
标题翻译：含有硝基苯胺衍生物或其盐作为活性成分的医药组合物
公开(公告)号：WO00016766A1
公开(公告)日：2000-03-30
申请号：PCT/JP1999/005148
申请日：1999-09-21
IPC分类号： A61K31/00 , A61K31/428 , C07C243/16 , C07C243/20 , C07C243/22 , C07C243/28 , C07C243/38 , C07C251/76 , C07C251/80 , C07C251/86 , C07C257/06 , C07C281/02 , C07C311/49 , C07C311/51 , C07C323/36 , C07C327/58 , C07D213/40 , C07D213/53 , C07D213/74 , C07D213/77 , C07D215/38 , C07D231/38 , C07D231/56 , C07D233/52 , C07D239/42 , C07D239/52 , C07D239/94 , C07D241/44 , C07D251/46 , C07D263/58 , C07D277/82 , C07D295/125 , C07D295/30 , C07D307/40 , C07D307/52 , C07D307/88 , C07D317/58 , C07D317/66 , C07D319/18 , C07D333/20 , C07D333/22 , C07D401/12 , C07D405/12 , C07D471/04 , C07D495/04 , A61K31/135 , A61K31/195 , A61K31/22 , A61K31/335 , A61K31/36 , A61K31/365 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , C07C323/27 , C07C323/48 , C07D213/38 , C07D213/42 , C07D213/76 , C07D215/42 , C07D253/06 , C07D295/12 , C07D295/22 , C07D319/14 , C07D407/12
CPC分类号： C07D495/04 , A61K31/00 , A61K31/428 , C07C243/16 , C07C243/20 , C07C243/22 , C07C243/28 , C07C243/38 , C07C251/76 , C07C251/80 , C07C251/86 , C07C257/06 , C07C281/02 , C07C311/49 , C07C311/51 , C07C323/36 , C07C327/58 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D213/40 , C07D213/53 , C07D213/74 , C07D213/77 , C07D215/38 , C07D231/38 , C07D231/56 , C07D233/52 , C07D239/42 , C07D239/52 , C07D239/94 , C07D241/44 , C07D251/46 , C07D263/58 , C07D277/82 , C07D295/125 , C07D295/30 , C07D307/40 , C07D307/52 , C07D307/88 , C07D317/58 , C07D317/66 , C07D319/18 , C07D333/20 , C07D333/22 , C07D401/12 , C07D405/12 , C07D471/04
摘要： A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by formula (I) wherein R is a hydrogen atom, an optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, aryl or heterocyclic group, or a cyano group; R and R may be each a hydrogen atom, an optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, aryl or heterocyclic group, or -A-R (wherein A is S, SO, SO2, SO3, CO or CO2, and R is a hydrogen atom, an optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, aryl or heterocyclic group), or may form N=CR R (wherein R and R are each a hydrogen atom, an optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, aryl or heterocyclic group, an alkoxy or aryloxy group, a cyano group, a nitro group, or -A-R ); R and R may be each a hydrogen atom, an optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, aryl or heterocyclic group, an alkoxy group, an amino group, an aryloxy group, -A-R , a cyano group, an ester group or a hydroxyl group, or may form N=CR R ; R is a hydrogen atom, a nitro group, a cyano group, -A-R , an optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, aryl or heterocyclic group, an alkoxy group, an amino group, or a halogen atom; and further R , R , R , R and R may form a ring containing or not containing a heteroatom, or a salt thereof as an active constituent.
摘要翻译：含有作为活性成分的式（I）表示的硝基乙烯胺衍生物的化合物，其中R 1为氢原子，任意取代的烷基，烯基，炔基，环烷基，环烯基，芳基或杂环基或氰基组; R 2和R 3可以各自为氢原子，任选取代的烷基，烯基，炔基，环烷基，环烯基，芳基或杂环基或-AR 7（其中A为S，SO，SO 2， SO 3，CO或CO 2，R 7是氢原子，任选取代的烷基，烯基，炔基，环烷基，环烯基，芳基或杂环基），或可以形成N = CR 8 R 9 R 8和R 9各自为氢原子，任选取代的烷基，烯基，炔基，环烷基，环烯基，芳基或杂环基，烷氧基或芳氧基，氰基，硝基或-AR <7>）; R 4和R 5可以各自为氢原子，任选取代的烷基，烯基，炔基，环烷基，环烯基，芳基或杂环基，烷氧基，氨基，芳氧基，-AR 7 或氰基，酯基或羟基，或者可以形成N = CR 8 R 9; R 6是氢原子，硝基，氰基，-AR 7，任选取代的烷基，烯基，炔基，环烷基，环烯基，芳基或杂环基，烷氧基，氨基或卤素原子; 并且进一步的R 1，R 2，R 3，R 4和R 5可以形成含有或不含有杂原子的环或其盐作为活性成分。

6. 发明申请

WO2005014524A2 AMINO THIOL COMPOUNDS AND COMPOSITIONS FOR USE IN CONJUNCTION WITH CANCER THERAPY 审中-公开
标题翻译：氨基硫酚化合物和组合物与癌症治疗相结合
公开(公告)号：WO2005014524A2
公开(公告)日：2005-02-17
申请号：PCT/US2004026535
申请日：2004-08-09
申请人： WISCONSIN ALUMNI RES FOUND , FAHL WILLIAM E , PEEBLES DANIEL D , COPP RICHARD R
发明人： FAHL WILLIAM E , PEEBLES DANIEL D , COPP RICHARD R
IPC分类号： C07C211/14 , C07C211/22 , C07C215/18 , C07C215/24 , C07C323/25 , C07C323/27 , A61K31/132 , A61K31/133 , A61K31/145
CPC分类号： C07C323/25 , C07C211/14 , C07C211/22 , C07C215/18 , C07C215/24 , C07C323/27
摘要： The invention provides novel polyamine and amino thiol compounds and pharmaceutical compositions for administration in conjunction with cancer chemotherapy or radiation therapy. The compounds are administered locally to provide protection against the adverse side-effects of chemotherapy or radiation therapy, such as alopecia, mucositis and dermatitis. Pharmaceutical preparations comprising one or more chernoprotective polyamines or amino thiols formulated for topical or local delivery to epithelial or mucosal cells are disclosed. Methods of administering the pharmaceutical preparations are also disclosed.
摘要翻译：本发明提供新的多胺和氨基硫醇化合物和用于与癌症化学疗法或放射治疗相结合的药物组合物。化合物在局部施用以提供防止化学疗法或放射治疗（例如秃发，粘膜炎和皮炎）的不良副作用的保护。公开了包含一种或多种配制用于局部或局部递送至上皮或粘膜细胞的切尔诺保护性多胺或氨基硫醇的药物制剂。还公开了施用药物制剂的方法。

7. 发明申请

WO99067206A1 NOVEL COMPOUNDS USEFUL IN PAIN MANAGEMENT 审中-公开
标题翻译：新的化合物有助于疼痛管理
公开(公告)号：WO99067206A1
公开(公告)日：1999-12-29
申请号：PCT/SE1999/001077
申请日：1999-06-16
IPC分类号： C07C211/27 , C07C273/18 , C07C275/28 , C07C279/12 , C07C323/27 , C07D207/42 , C07D213/89 , C07D237/20 , C07D295/215 , A61K31/17 , A61K31/535 , A61K49/00 , A61K51/00 , C07D295/182
CPC分类号： C07D213/89 , C07C211/27 , C07C273/1854 , C07C275/28 , C07C279/12 , C07C323/27 , C07C2601/12 , C07C2601/14 , C07D207/42 , C07D237/20 , C07D295/215
摘要： Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
摘要翻译：通式（I）的化合物在本申请中公开和要求保护，以及它们的药学上可接受的盐，包含新化合物的药物组合物及其在治疗中的用途，特别是在治疗疼痛中的用途。

8. 发明申请

WO9931054A3 NOVEL P-AMINOPHENOL DERIVATIVES AND THE USE THEREOF 审中-公开
标题翻译：新的对氨基苯酚衍生物及其用途
公开(公告)号：WO9931054A3
公开(公告)日：1999-09-10
申请号：PCT/EP9807961
申请日：1998-12-08
申请人： HENKEL KGAA , ROSE DAVID , MEINIGKE BERND , HOEFFKES HORST
发明人： ROSE DAVID , MEINIGKE BERND , HOEFFKES HORST
IPC分类号： A61K8/00 , A61K8/33 , A61K8/41 , A61K8/46 , A61K8/49 , A61Q5/10 , C07C215/76 , C07C217/76 , C07C317/18 , C07C317/28 , C07C323/27 , D06P3/10 , A61K7/13
CPC分类号： A61Q5/10 , A61K8/415 , C07C215/76
摘要： Compounds of general formula (I), wherein A, B,C and D represent, independently from each other, an -OH- or -NHR- group, wherein R stands for a hydrogen atom or a C1-4 alkyl radical, with the proviso that A, B, C or D respectively stands for a hydroxy group, X stands for oxygen, sulphur, a sulfoxy or sulfoxyl group, R and R represent, independently from each other, hydrogen, fluorine, chlorine, a C1-4 alkyl or hydroxyalkyl group or a C2-4-dihydroxy-alkyl group, preferably a C2-dihydroxy alkyl group, and the physically acceptable salts of these compounds are highly suitable for use as developer components in oxidation coloring agents.
摘要翻译：其中A，B，C和D相互独立的通式（I）化合物代表-OH或-NHR基团，其中R代表氢原子或C 1-4 - 烷基，条件是 A或B以及C或D中的每一个表示羟基，X表示氧，硫，亚砜基或亚砜基，R 1和R 2独立地表示氢，氟，氯，C1 4-烷基或羟烷基或C2-4-二羟烷基，优选C2-二羟烷基，并且这些化合物的生理学上可接受的盐非常适合作为氧化染料中的显色剂组分。

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