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公开(公告)号：US08785424B2
公开(公告)日：2014-07-22
申请号：US13321440
申请日：2010-05-20
CPC分类号： C07J53/004 , C07J71/0005
摘要： The present invention relates to a compound of following formula (I): or to a pharmaceutically acceptable salt thereof, as well as to pharmaceutical compositions including same and to the use thereof as a drug, in particular for treating a proliferative disease such as cancer.
摘要翻译： 本发明涉及下式（I）的化合物或其药学上可接受的盐，以及包含其的药物组合物及其作为药物的用途，特别是用于治疗增殖性疾病例如癌症。
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公开(公告)号：US20120077777A1
公开(公告)日：2012-03-29
申请号：US13321440
申请日：2010-05-20
IPC分类号： A61K31/575 , C07J71/00 , A61P35/00 , A61K31/695 , A61K31/585 , C07J53/00 , A61K31/58
CPC分类号： C07J53/004 , C07J71/0005
摘要： The present invention relates to a compound of following formula (I): or to a pharmaceutically acceptable salt thereof, as well as to pharmaceutical compositions including same and to the use thereof as a drug, in particular for treating a proliferative disease such as cancer.
摘要翻译： 本发明涉及下式（I）的化合物或其药学上可接受的盐，以及包含其的药物组合物及其作为药物的用途，特别是用于治疗增殖性疾病例如癌症。
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3.发明授权Retro-.alpha.-retinol (4,14-retro-retinol) derivatives and uses of retro-.alpha.-retinol 失效复方α-吗啉醇（4,14-反 - 视黄醇）衍生物及其用途
公开(公告)号：US5521221A
公开(公告)日：1996-05-28
申请号：US682909
申请日：1991-04-09
IPC分类号： A01N37/18 , A01N37/34 , A61K31/07 , A61K31/23 , A61K31/70 , C07C403/08 , C07D303/14 , C07D317/20 , C07F7/18 , C12N1/38 , C12N5/078 , C12N5/0783 , C12N15/67 , C12P17/02 , C12P23/00 , C07C35/18 , C07C37/68
CPC分类号： C12P23/00 , C07C403/08 , C07C403/10 , C07C403/12 , C07D303/14 , C07F7/184 , C12N15/67 , C12N5/065 , C07B2200/09 , C07C2101/14 , C07C2101/16 , C12N2501/385
摘要： This invention provides a purified retro-retinoid compound characterized by a molecular mass of about 302 daltons. Also provided by this invention is a method of enhancing the growth of a cell in a vitamin A reduced environment which comprises contacting the cell with an effective growth enhancing amount of a compound having a structure: ##STR1## wherein the configuration of the C6, C8, C10 and C12 double bond independently is Z or E and the absolute configuration at C-14 is independently R or S; wherein R.sub.1 is alkyl, alkyl halide, alcohol, ester, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, acid halide, amide, nitrile, or amine; and wherein R.sub.2 is hydroxyl, halide, alkoxy, ester, alkyl, alcohol, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, nitrile, amine, azide, alkyl halide, acid halide, acid azide, or amide; or wherein R.sub.1 and R.sub.2 are replaced by a 14, 15-oxirane group; and wherein the retro structure is alpha or gamma. Further provided are a method for enhancing transcription of a gene regulated by retinoid in a cell, or a method for enhancing an immune response in a subject.
摘要翻译： 本发明提供了一种以分子质量为约302道尔顿为特征的纯化的后视色素化合物。 本发明还提供了增强维生素A还原环境中细胞生长的方法，其包括使细胞与有效生长增加量的具有以下结构的化合物接触：其中C6，C8的构型 ，C10和C12双键独立地为Z或E，C-14的绝对构型独立地为R或S; 其中R1是烷基，烷基卤，醇，酯，醚，醛，酮，羧酸，羧酸酯，酰卤，酰胺，腈或胺; 烷基，醇，醚，醛，酮，羧酸，羧酸酯，腈，胺，叠氮化物，烷基卤，酰卤，叠氮化物或酰胺; 或其中R 1和R 2被14,15-环氧乙烷基团取代; 并且其中所述复古结构是α或γ。 还提供了增强细胞中类视黄醇调节基因转录的方法，或增强受试者的免疫应答的方法。
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4.发明授权Treatment of estrogen-receptor positive breast cancer and estrogen-receptor negative breast cancer with retinoid with CH.sub.2 OH at the side chain terminal position 失效用侧链末端位置的CH2OH处理类视黄醇对雌激素受体阳性乳腺癌和雌激素受体阴性乳腺癌的治疗
公开(公告)号：US6150421A
公开(公告)日：2000-11-21
申请号：US88770
申请日：1998-06-02
申请人： Lorraine Gudas , Fadila Derguini
发明人： Lorraine Gudas , Fadila Derguini
IPC分类号： A61K31/07 , A61K31/122 , A61K31/12 , A61K31/11
CPC分类号： A61K31/07 , A61K31/122
摘要： Certain retinoids with CH.sub.2 OH at the side chain terminal position, preferably 4-oxoretinol, inhibit growth of estrogen-receptor positive and estrogen-receptor negative breast cancer tumor cell lines and have utility for adjuvant therapy and treatment of metastatic disease.
摘要翻译： 在侧链末端具有CH2OH的某些类维生素A优选4-氧代索醇抑制雌激素受体阳性和雌激素受体阴性乳腺癌肿瘤细胞系的生长，并且可用于辅助治疗和治疗转移性疾病。
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5.发明授权Regulating gene expression using retinoids with Ch.sub.2 OH or related groups at the side chain terminal position 失效调节基因表达，使用类视黄醇与Ch2OH或相关基团在侧链末端位置
公开(公告)号：US5786391A
公开(公告)日：1998-07-28
申请号：US371535
申请日：1995-01-11
申请人： Lorraine J. Gudas , Charles Achkar , Jochen Buck , Alexander W. Langston , Fadila Derguini , Koji Nakanishi
发明人： Lorraine J. Gudas , Charles Achkar , Jochen Buck , Alexander W. Langston , Fadila Derguini , Koji Nakanishi
IPC分类号： A61K31/07 , A61K31/075 , A61K31/122 , A61K31/203 , A61K31/232 , A61K31/115 , A61K31/045 , A61K31/08
CPC分类号： A61K31/07 , A61K31/075 , A61K31/122 , A61K31/203 , A61K31/232
摘要： For the first time, certain retinoids with a side chain terminal CH.sub.2 OH group or ester or ether thereof or aldehyde rather than a side chain terminal COOH group and substitution at the 4-position have been indicated to bind to nuclear receptors and to be biologically active in inducing cell differentiation of normal and tumor cells. These compounds activate gene expression through binding to nuclear receptor proteins. These compounds induce differentiation in normal and cancer cells and are useful for treating leukemias, and lymphomas, squamous cell carcinomas, deep (cystic) acne, psoriasis and photodamaged or aging skin. These compounds have stability and in vitro half-life advantages over and solubility differences from all-trans-retinoic acid and activity advantages over 13-cis retinoic acid.
摘要翻译： 具有侧链末端CH 2 OH基团或其酯或醚或具有侧链末端COOH基团的某些类维生素A和第4位的取代已被表明与核受体结合并具有生物学活性 诱导正常和肿瘤细胞的细胞分化。 这些化合物通过结合核受体蛋白激活基因表达。 这些化合物在正常和癌细胞中诱导分化，并且可用于治疗白血病，淋巴瘤，鳞状细胞癌，深（囊性）痤疮，牛皮癣和光损伤或衰老皮肤。 与13-顺式视黄酸相比，这些化合物具有超过全反式视黄酸的稳定性和体外半衰期优点和与全反式视黄酸的溶解度差异和活性优势。
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公开(公告)号：US5908868A
公开(公告)日：1999-06-01
申请号：US331627
申请日：1995-06-05
IPC分类号： A61K31/07 , C07D303/14 , C07F7/18 , C12N5/078 , C12N5/0783 , C12N15/67 , C12P23/00 , A61K31/045 , A61K31/075
CPC分类号： C12P23/00 , A61K31/045 , A61K31/07 , A61K31/075 , C07C403/08 , C07C403/10 , C07C403/12 , C07C403/20 , C07D303/14 , C07F7/184 , C12N15/67 , C12N5/0636 , C12N5/065 , C07B2200/07 , C07B2200/09 , C07C2101/16 , C12N2501/385
摘要： The present invention provides a purified retinoid compound characterized by a molecular mass of about 320 daltons and an atomic composition of C.sub.20 H.sub.32 O.sub.3. The present invention also provides a purified retinoid compound having the following structure: ##STR1## wherein the configuration of C7, C9, and C11 double bond independently is Z or E and the absolute configuration at C13 and C14 is independently R or S; wherein R1 is hydroxyl, alkyl, alkyl halide, alcohol, ester, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, acyl halide, amide, nitrile, or amine; wherein R2 and R3 are independently hydroxyl, halide, alkoxy, ester, alkyl, alcohol, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, nitrile, amine, azide, alkyl halide, acid halide, acid azide, or amide; or wherein R2 and R3, or R1 and R2 are replaced by a 13,14-oxirane or a 14,15-oxirane group, respectively. Also provided by this invention is a pharmaceutical composition which comprises the compound above and a pharmaceutically acceptable carrier. This invention further provides a growth medium comprising the compound above at a concentration effective to enhance cell growth. Additionally, the present invention provides a method of enhancing the growth of a cell, a method for enhancing an immune response in a subject, and a method for enhancing transcription of a gene regulated by a retinoid in a cell.
摘要翻译： PCT No.PCT / US93 / 04323 Sec。 371日期：1995年5月6日 102（e）日期1995年5月6日PCT提交1993年5月6日PCT公布。 公开号WO93 / 22267 日期：1993年11月11日本发明提供一种纯化的类视黄醇化合物，其特征在于分子量为约320道尔顿，原子组成为C20H32O3。 本发明还提供具有以下结构的纯化类视黄醇化合物：其中C7，C9和C11双键独立的构型是Z或E，C13和C14的绝对构型独立地是R或S; 其中R1是羟基，烷基，烷基卤，醇，酯，醚，醛，酮，羧酸，羧酸酯，酰基卤，酰胺，腈或胺; 其中R2和R3独立地是羟基，卤素，烷氧基，酯，烷基，醇，醚，醛，酮，羧酸，羧酸酯，腈，胺，叠氮化物，烷基卤，酰卤，叠氮化物或酰胺; 或其中R2和R3，或R1和R2分别被13,14-环氧乙烷或14,15-环氧乙烷基团取代。 本发明还提供了包含上述化合物和药学上可接受的载体的药物组合物。 本发明进一步提供包含上述化合物的生物培养基，其浓度有效地增强细胞生长。 此外，本发明提供增强细胞生长的方法，增强受试者的免疫应答的方法，以及增强细胞中类视黄醇调节基因转录的方法。
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公开(公告)号：US5814612A
公开(公告)日：1998-09-29
申请号：US880041
申请日：1992-05-06
IPC分类号： A01N37/18 , A01N37/34 , A61K31/07 , A61K31/16 , A61K31/23 , A61K31/70 , C07C43/15 , C07C47/21 , C07C49/203 , C07C233/09 , C07C235/28 , C07C403/00 , C07C403/08 , C07D303/12 , C07D303/14 , C07D317/20 , C07F7/18 , C07F9/06 , C12N1/38 , C12N5/078 , C12N5/0783 , C12N15/67 , C12P17/02 , C12P23/00 , A61K37/22 , C07D317/74
CPC分类号： C07F7/184 , C07C403/08 , C07C403/10 , C07C403/12 , C07C403/20 , C07D303/14 , C12N15/67 , C12N5/065 , C12P23/00 , C07B2200/09 , C07C2101/14 , C07C2101/16 , C12N2501/385
摘要： The present invention provides a purified retinoid compound characterized by a molecular mass of about 320 daltons and an atomic composition of C.sub.20 H.sub.32 O.sub.3. The present invention also provides a purified retinoid compound having the structure: ##STR1## wherein the configuration of the C7, C9, and C11 double bond independently is Z or E and the absolute configuration at C13 and C14 is independently R or S; wherein R1 is alkyl, alkyl halide, alcohol, ester, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, acyl halide, amide, nitrile, or amine; R2 and R3 are independently hydroxyl, halide, alkoxy, ester, alkyl, alcohol, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, nitrile, amine, azide, alkyl halide, acid halide, acid azide, or amide; or wherein R2 and R3, or R1 and R2 are replaced by a 13,14-oxirane or a 14,15-oxirane group, respectively.
摘要翻译： 本发明提供一种纯化的类视色素化合物，其特征在于分子量为约320道尔顿，原子组成为C20H32O3。 本发明还提供了具有以下结构的纯化的类视黄醇化合物：单独的独立地为Z或E，且C13和C14的绝对构型独立地为R或S; 其中R1是烷基，烷基卤，醇，酯，醚，醛，酮，羧酸，羧酸酯，酰卤，酰胺，腈或胺; R2和R3独立地是羟基，卤素，烷氧基，酯，烷基，醇，醚，醛，酮，羧酸，羧酸酯，腈，胺，叠氮化物，烷基卤，酰卤，酸叠氮化物或酰胺; 或其中R2和R3，或R1和R2分别被13,14-环氧乙烷或14,15-环氧乙烷基团取代。
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8.发明授权Anhydroretinol and derivatives thereof as antagonists of immune responses and inhibitors of cancer cell growth 失效作为免疫反应的拮抗剂和癌细胞生长抑制剂的脱氢解蛋白及其衍生物
公开(公告)号：US5883136A
公开(公告)日：1999-03-16
申请号：US478411
申请日：1995-06-07
IPC分类号： A61K31/015 , A61K31/045 , A61K31/07 , A61K31/075 , A61K31/22 , A61K31/23
CPC分类号： A61K31/07 , A61K31/015 , A61K31/045 , A61K31/075 , A61K31/22 , A61K31/23
摘要： This invention provides methods of inhibiting the growth of cells, of treating a subject having a disease characterized by an uncontrolled growth of cells and of blocking an immune response as well as related inflammatory responses in a subject which comprises administering a compound having the structure: ##STR1##
摘要翻译： 本发明提供了抑制细胞生长的方法，该方法包括给予具有以下结构的化合物：治疗患有特征在于细胞不受控生长并且阻断免疫应答以及相关炎症反应的疾病的受试者， 图像>
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公开(公告)号：US5648563A
公开(公告)日：1997-07-15
申请号：US481913
申请日：1995-06-07
IPC分类号： A01N37/18 , A01N37/34 , A61K31/07 , A61K31/23 , A61K31/70 , C07C403/08 , C07D303/14 , C07D317/20 , C07F7/18 , C12N1/38 , C12N5/078 , C12N5/0783 , C12N15/67 , C12P17/02 , C12P23/00 , C07C35/18 , C07C37/68
CPC分类号： C07D303/14 , C07C403/08 , C07C403/10 , C07C403/12 , C07F7/184 , C12N15/67 , C12N5/0636 , C12N5/065 , C12P23/00 , C07B2200/09 , C07C2101/14 , C07C2101/16 , C12N2501/385
摘要： This invention provides a homogeneous retro-retinoid compound, a method of enhancing the growth of a cell in a vitamin A reduced environment, a method for enhancing transcription of a gene regulated by retinoid in a cell, and a method for enhancing an immune response in a subject, wherein the compound has the structure: ##STR1##
摘要翻译： 本发明提供均匀的类维生素A化合物，增强维生素A还原环境中细胞生长的方法，增强细胞中类视黄醇调节基因转录的方法和增强免疫应答的方法 对象，其中化合物具有以下结构：
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10.发明授权Regulating gene expression using retinoids with CH.sub.2 OH or related groups at the side chain terminal position 失效调节基因表达使用维甲酸与CH2OH或相关基团在侧链末端位置
公开(公告)号：US5962534A
公开(公告)日：1999-10-05
申请号：US887633
申请日：1997-07-03
申请人： Lorraine J. Gudas , Charles Achkar , Jochen Buck , Alexander W. Langston , Fadila Derguini , Koji Nakanishi
发明人： Lorraine J. Gudas , Charles Achkar , Jochen Buck , Alexander W. Langston , Fadila Derguini , Koji Nakanishi
IPC分类号： A61K31/07 , A61K31/075 , A61K31/122 , A61K31/203 , A61K31/232 , A61K31/12 , A61K31/11
CPC分类号： A61K31/07 , A61K31/075 , A61K31/122 , A61K31/203 , A61K31/232
摘要： For the first time, certain retinoids with a side chain terminal CH.sub.2 OH group or ester or ether thereof or aldehyde rather than a side chain terminal COOH group and substitution at the 4-position have been indicated to bind to nuclear receptors and to be biologically active in inducing cell differentiation of normal and tumor cells. These compounds activate gene expression through binding to nuclear receptor proteins. These compounds induce differentiation in normal and cancer cells and are useful for treating leukemias, and lymphomas, squamous cell carcinomas, deep (cystic) acne, psoriasis and photodamaged or aging skin. These compounds have stability and in vitro half-life advantages over and solubility differences from all-trans-retinoic acid and activity advantages over 13-cis retinoic acid.
摘要翻译： 具有侧链末端CH 2 OH基团或其酯或醚或具有侧链末端COOH基团的某些类维生素A和第4位的取代已被表明与核受体结合并具有生物学活性 诱导正常和肿瘤细胞的细胞分化。 这些化合物通过结合核受体蛋白激活基因表达。 这些化合物在正常和癌细胞中诱导分化，并且可用于治疗白血病，淋巴瘤，鳞状细胞癌，深（囊性）痤疮，牛皮癣和光损伤或衰老皮肤。 与13-顺式视黄酸相比，这些化合物具有超过全反式视黄酸的稳定性和体外半衰期优点和与全反式视黄酸的溶解度差异和活性优势。
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