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1. 发明申请

WO9704783A3 BIS-1-OXAQUINOLIZIDINE ALKALOIDS FROM A MARINE SPONGE WITH ANTITUMOR ACTIVITY 审中-公开
标题翻译：来自具有抗肿瘤活性的海洋海绵中的BIS-1-氧杂喹喔啉酸
公开(公告)号：WO9704783A3
公开(公告)日：1997-04-17
申请号：PCT/GB9601852
申请日：1996-07-29
申请人： PHARMA MAR SA , RUFFLES GRAHAM KEITH , TANAKA JUN ICHI , HIGA TATSUO , GARCIA GRAVALOS DOLORES
发明人： TANAKA JUN-ICHI , HIGA TATSUO , GARCIA GRAVALOS DOLORES
IPC分类号： A61K31/5365 , C07D498/22 , A61K31/535
CPC分类号： C07D498/22 , A61K31/5365
摘要： Compounds of general formula (II), or a pharmaceutically acceptable salt thereof, are of use as antitumor agents, where R and R are the same or different, and each group is -H or -OH; the group R is -H or -CH3; and the group R is -H or -CH3; and can be isolated from marine sponges.

2. 发明申请

WO0160810B1 OXY-AND AMINO-SUBSTITUTED TETRAHYDROFURYL DERIVATIVES WITH ANTITUMOUR ACTIVITY 审中-公开
标题翻译：含氧和氨基取代的四氢呋喃衍生物的抗肿瘤活性
公开(公告)号：WO0160810B1
公开(公告)日：2001-11-29
申请号：PCT/GB0100655
申请日：2001-02-16
申请人： PHARMA MAR SA , RUFFLES GRAHAM KEITH , HIGA TATSUO , TANAKA JUNICHI , GARCIA GRAVALOS DOLORES
发明人： HIGA TATSUO , TANAKA JUNICHI , GARCIA GRAVALOS DOLORES
IPC分类号： A61K31/341 , A61K35/56 , A61P35/00 , A61P35/02 , A61P43/00 , C07D307/22
CPC分类号： C07D307/22
摘要： Compounds of formula (I) wherein the substituent groups defined by R1, R2, R3 and R4 are each independently selected of H, C(=O) R,P(=O)R'R",S(=O)R'R", substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl; wherein each of the R', R" groups is independently selected from the group consisting of H, OH, NO2, NH2, SH, CN, halogen, =O, C(=O)H, C(=O)CH 3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstitued aryl; wherein R1, R2, R3 could form part of a heterocyclic ring; R2 can be independently an internal salt; wherein X1, X2 and X3 on formula (I) are independently placed in any particular position of the chain and independently selected of H, OH, OR', SH, SR', SOR', SO2R', NO2, NH2, NHR', N(R')2, NHC(O)R', CN, halogen, =O, C(=O)H, C(=O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic; wherein substituent groups defined by R' are each independently selected from the group consisting of H, OH, OR', SH, SR', SOR', SO2R', NO2, NH2, NHR', N(R')2, NHC(O)R', CN, halogen, =O, C(=O)H, C(=O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic; wherein x can be between 6 and 20; and wherein the dotted line is one or several double bonds placed in any particular position of the side chain; are useful as antitumor compounds and include compound IK-8-73-4 of structure (a) which was isolated from a sponge Pachastrissa sp.
摘要翻译：其中由R 1，R 2，R 3和R 4定义的取代基各自独立地选自H，C（= O）R，P（= O）R'R“，S（= O）R' 取代或未取代的C 1 -C 18烷基，取代或未取代的C 2 -C 18烯基，取代或未取代的C 2 -C 18炔基，取代或未取代的芳基; 其中每个R'，R“基团独立地选自H，OH，NO 2，NH 2，SH，CN，卤素，= O，C（= O）H，C（= O）CH 3， CO2H，CO2CH3，取代或未取代的C1-C18烷基，取代或未取代的C2-C18烯基，取代或未取代的C2-C18炔基，取代或未取代的芳基;其中R1，R2，R3可以形成杂环的一部分; R2可以是其中式（I）中的X 1，X 2和X 3独立地位于链的任何特定位置并且独立地选自H，OH，OR'，SH，SR'，SOR'，SO 2 R'，NO 2， NH2，NHC（O）R'，CN，卤素，= O，C（= O）H，C（= O）CH3，CO2H，CO2CH3，取代或未取代的C1-C18 烷基，取代或未取代的C 2 -C 18烯基，取代或未取代的C 2 -C 18炔基，取代或未取代的芳基，取代或未取代的杂芳族基团;其中由R'定义的取代基各自独立地选自H，OH，O R'，SH，SR'，SOR'，SO2R'，NO2，NH2，NHR'，N（R'）2，NHC（O）R'，CN，卤素，= O，C（= O）（= O）CH3，CO2H，CO2CH3，取代或未取代的C1-C18烷基，取代或未取代的C2-C18烯基，取代或未取代的C2-C18炔基，取代或未取代的芳基，取代或未取代的杂芳族; 其中x可以在6和20之间; 并且其中虚线是放置在侧链的任何特定位置中的一个或多个双键; 作为抗肿瘤化合物是有用的，并且包括从海绵Pachastrissa sp分离的结构（a）的化合物IK-8-73-4。

3. 发明专利

CA2114777A1 CYTOTOXIC COMPOUNDS 未知
公开(公告)号：CA2114777A1
公开(公告)日：1994-08-04
申请号：CA2114777
申请日：1994-02-02
申请人： TANAKA JUN ICHI , HIGA TATSUO , SUWANOBORIRUX KHANIT , JEFFORD CHARLES W , BERNARDINELLI GERALD , GRAVALOS DOLORES G
发明人： TANAKA JUN-ICHI , HIGA TATSUO , SUWANOBORIRUX KHANIT , JEFFORD CHARLES W , BERNARDINELLI GERALD , GRAVALOS DOLORES G
IPC分类号： A61K31/19 , A61K31/215 , A61K31/335 , A61K31/357 , A61K35/56 , A61P31/12 , A61P35/00 , C07C59/11 , C07C69/675 , C07C69/708 , C07D319/02
摘要： Compounds isolated from a marine sponge, and derivatives thereof, have the formulae: or (II) in which R1 is H or lower alkyl; R2 ia OH or CH3; R3 is OH or CH3, and R4 H or MPTA. The compounda have antitumor and antiviral activity. The invention also provides pharmaceutical compositions containing the compounds and methods of treatment employing them.

4. 发明专利

JPH0769884A CYTOTOXIC COMPOUND 失效
公开(公告)号：JPH0769884A
公开(公告)日：1995-03-14
申请号：JP4302394
申请日：1994-02-03
申请人： PHARMA MAR SA
发明人： TANAKA JUNICHI , HIGA TATSUO , KAANITSUTO SUWANOBORIRIYUU , CHIYAARUZU UIRIAMU JIEFUOODO , JIERARUDO BERUNARUDEINERI , DORORESU JII GURABUAROSU
IPC分类号： A61K31/19 , A61K31/215 , A61K31/335 , A61K31/357 , A61K35/56 , A61P31/12 , A61P35/00 , C07C59/11 , C07C69/675 , C07C69/708 , C07D319/02
摘要： PURPOSE: To obtain a new compound useful as an antitumor agent or an antiviral agent. CONSTITUTION: A compound of the formula (R is H or a lower alkyl; R is OH or CH3 ; R is OH or CH3 ), e.g. mycaperoxide A methyl ester. A compound of the formula is obtained by dipping a marine sponge such as Mycal-sp-sponge in methanol, concentrating the extract and extraction-treating the residue with methylene chloride.

5. 发明专利

MXPA02007995A DERIVADOS DE TETRAHIDROFURILO SUSTITUIDOS POR OXY Y AMINO CON ACTIVIDAD ANTITUMORAL. 未知
公开(公告)号：MXPA02007995A
公开(公告)日：2003-05-23
申请号：MXPA02007995
申请日：2001-02-16
申请人： RUFFLES GRAHAM KEITH
发明人： HIGA TATSUO
IPC分类号： A61K31/341 , A61K35/56 , A61P35/00 , A61P35/02 , A61P43/00 , C07D307/22
摘要： Compuestos de la formula (I) en donde los grupos substituyentes definidos por R1, R2, R3 y R4 son seleccionados cada uno en forma independiente de H, C(=O)R', P(=O)R'R", S(=O)R'R", alquilo C1-C18 substituido o no substituido, alquenilo C2-C18 substituido o no substituido, alquinilo C2-C18 substituido o no substituido, arilo substituido o no substituido; en donde cada uno de los grupos R', R" es seleccionado independientemente del grupo que consiste de H, OH, NO2, NH2, SH, CN, halogeno, =O, C(=O)H, C(=O)CH3, C02H, C02CH3, alquilo C1-C18 substituido o no substituido, alquenilo C2-C18 substituido o no substituido, alquinilo C2-C18 substituido o no substituido, arilo substituido o no substituido; en donde R1, R2, R3 podrian formar parte de un anillo heterociclico, R2 puede ser de forma independiente una sal interna; en donde X1, X2 y X3 de la formula (I) son colocados en forma independiente en cualquier lugar en particular de la cadena y seleccionada independientemente de H, OH, OR', SH, SR', SOR', SO2R', NO2, NH2, NHR', N(R')2, NHC(O)R', CN, halogeno, =O, C(=O)H, C(=O)CH3, CO2H, CO2CH3, alquilo C1-C18 substituido o no substituido, alquenilo C2-C18 substituido o no substituido, alquinilo C2-C18 substituido o no substituido, arilo substituido o no substituido, heteroaromatico substituido o no substituido; en donde los grupos substituyentes definidos por R' son seleccionados cada uno independientemente del grupo que consiste de H, OH, OR', SH, SR', SOR', SO2R', NO2, NH2, NHR', N(R')2, NHC(O)R', CN, halogeno, =O, C(=O)H, C(=O)CH3, CO2H, CO2CH3, alquilo C1-C18 substituido o no substituido, alquenilo C2-C18 substituido o no substituido, alquinilo C2-C18 substituido o no substituido, arito substituido o no substituido, heteroaromatico substituido o no substituido; en donde x puede ser entre 6 y 20; y en donde la linea punteada es uno o varios enlaces dobles colocados en cualquier lugar particular de la cadena lateral; son utiles como compuestos antitumorales e incluyen compuestos IK-8-73-4 de la estructura (a) la cual fue aislada a partir de la esponja Pachastissa sp.

6. 发明专利

MXPA02009273A COMPUESTOS ANTI-TUMORALES DE ESPONJA. 未知
公开(公告)号：MXPA02009273A
公开(公告)日：2003-05-23
申请号：MXPA02009273
申请日：2001-03-20
申请人： RUFFLES GRAHAM KEITH
发明人： HIGA TATSUO
IPC分类号： A61P35/00 , A61K31/11 , A61K31/13 , C07C47/225 , C07C47/273 , C07C251/18 , C07C271/68
摘要： Nuevos compuestos anti-tumorales aislados de una esponja son de las formulas (l), (2), (3) y (4).

7. 发明申请

WO8701279A3 ANTITUMOR CHAMIGRENE DERIVATIVES AND THEIR METHODS OF USE 审中-公开
标题翻译：抗肿瘤药物衍生物及其使用方法
公开(公告)号：WO8701279A3
公开(公告)日：1987-07-30
申请号：PCT/US8601746
申请日：1986-08-22
申请人： SNADER KENNETH M , HIGA TATSUO
发明人： SNADER KENNETH M , HIGA TATSUO
IPC分类号： C07C69/145 , A61K31/025 , A61K31/045 , A61K31/075 , A61K31/095 , A61K31/12 , A61K31/13 , A61K31/22 , A61K31/34 , C07C49/653 , C07C49/693 , C07C49/743 , C07D307/00
CPC分类号： A61K31/075 , A61K31/025 , A61K31/045 , A61K31/095 , A61K31/12 , A61K31/13 , A61K31/22 , A61K31/34
摘要： Antitumor compositions, and a method for inhibiting, remitting or controlling the growth of tumors or tumor cells utilizing antitumor compositions. More particularly, the antitumor compositions comprise, as active ingredient, an antitumor effective amount of halogenated chamigrenes extracted and derived from red alga and sea hares which diet upon red alga.

8. 发明专利

ES2256199T3 DERIVADOS DE TETRAHIDROFURILOXI- Y AMINO-SUSTITUIDOS CON ACTIVIDAD ANTITUMORAL. 未知
公开(公告)号：ES2256199T3
公开(公告)日：2006-07-16
申请号：ES01905903
申请日：2001-02-16
申请人： PHARMA MAR SA
发明人： HIGA TATSUO , TANAKA JUNICHI , GARCIA GRAVALOS DOLORES
IPC分类号： A61K31/341 , A61K35/56 , A61P35/00 , A61P35/02 , A61P43/00 , C07D307/22
摘要： El uso en la preparación de un medicamento para el tratamiento de un tumor de un compuesto de fórmula (I): en donde los grupos sustituyentes definidos por R1, R2, R3 y R4 están cada uno de ellos independientemente seleccionados entre H, C(=O)R¿, P(=O)R¿R¿¿, S(=O)R¿R¿¿, alquilo de C1-C18 sustituidos o no sustituidos, alquenilo de C2-C18 sustituidos o no sustituidos, alquinilo de C2-C18 sustituidos o no sustituidos, arilo sustituido o no sustituido; en donde cada uno de los grupos R¿, R¿¿ está seleccionado de forma independiente entre el grupo que consiste en H, OH, NO2, NH2, SH, CN, halógeno, =O, C(=O)H, C(=O)CH3, CO2H, CO2CH3, alquilo de C1-C18 sustituido o no sustituido, alquenilo de C2-C18 sustituido o no sustituido, alquinilo de C2-C18 sustituido o no sustituido, arilo sustituido o no sustituido; en donde R1, R2, R3 pueden formar parte de un anillo heterocíclico; R2 puede ser de forma independiente una sal interna; en donde X1, X2 y X3 en la fórmula I están independientemente situados encualquier posición particular de la cadena incluyendo cerca del anillo en cualquier carbono con la línea de puntos y seleccionados de forma independiente entre H, OH, OR¿, SH, SR¿, SOR¿, SO2R¿, NO2, NH2, NHR¿, N(R¿)2, NHC(O)R¿, CN, halógeno, =O, C(=O)H, C(=O)CH3, CO2H, CO2CH3, alquilo de C1- C18 sustituido o no sustituido, alquenilo de C2-C18 sustituido o no sustituido, alquinilo de C2-C18 sustituido o no sustituido, arilo sustituido o no sustituido, heteroaromático sustituido o no sustituido; en donde los grupos sustituyentes definidos por R¿ están cada uno de ellos seleccionados de forma independiente entre el grupo que consiste en H, OH, OR¿, SH, SR¿, SOR¿, SO2R¿, NO2, NH2, NHR¿, N(R¿)2, NHC(O)R¿, CN, halógeno, =O, C(=O)H, C(=O)CH3, CO2H, CO2CH3, alquilo de C1-C18 sustituido o no sustituido, alquenilo de C2-C18 sustituido o no sustituido, alquinilo de C2-C18 sustituido o no sustituido, arilo sustituido o no sustituido, heteroaromático sustituido o no sustituido; en donde x puede estar comprendido entre 6 y 20; y en donde la línea de puntos está ausente o es uno o varios dobles enlaces situados en cualquier posición particular de la cadena lateral.

9. 发明专利

BR0109394A 未知
公开(公告)号：BR0109394A
公开(公告)日：2003-06-03
申请号：BR0109394
申请日：2001-03-20
申请人： PHARMA MAR SA
发明人： TANAKA JUNICHI , HIGA TATSUO
IPC分类号： A61P35/00 , A61K31/11 , A61K31/13 , C07C47/225 , C07C47/273 , C07C251/18 , C07C271/68 , A61K31/325
摘要： New antitumor compounds isolated from a sponge are of the formulae (1), (2), (3) and (4).

10. 发明专利

CA2400612A1 OXY-AND AMINO-SUBSTITUTED TETRAHYDROFURYL DERIVATIVES WITH ANTITUMOUR ACTIVITY 未知
公开(公告)号：CA2400612A1
公开(公告)日：2001-08-23
申请号：CA2400612
申请日：2001-02-16
申请人： PHARMA MAR SA
发明人： GARCIA GRAVALOS DOLORES , TANAKA JUNICHI , HIGA TATSUO
IPC分类号： A61K31/341 , A61K35/56 , A61P35/00 , A61P35/02 , A61P43/00 , C07D307/22
摘要： Compounds of formula (I) wherein the substituent groups defined by R1, R2, R 3 and R4 are each independently selected of H, C(=O) R,P(=O)R'R",S(=O)R'R", substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C 18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl; wherein each of the R', R" groups is independently selected from the group consisting of H, OH, NO2, NH2, SH, CN, halogen, =O, C(=O)H, C(=O)CH 3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2 - C18 alkynyl, substituted or unsubstitued aryl; wherein R1, R2, R3 could form part of a heterocyclic ring; R2 can be independently an internal salt; where in X1, X2 and X3 on formula (I) are independently placed in any particular position of the chain and independently selected of H, OH, OR', SH, SR', SOR ', SO2R', NO2, NH2, NHR', N(R')2, NHC(O)R', CN, halogen, =O, C(=O)H, C(=O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic; wherein substituent groups defined by R' are each independently selected from the group consisting of H, OH, OR', SH, SR', SOR ', SO2R', NO2, NH2, NHR', N(R')2, NHC(O)R', CN, halogen, =O, C(=O)H, C(=O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic; wherein x can be between 6 and 20; and wherein the dotted li ne is one or several double bonds placed in any particular position of the side chain; are useful as antitumor compounds and include compound IK-8-73-4 of structure (a) which was isolated from a sponge Pachastrissa sp.

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