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71. 发明申请

US20060233814A1 Elimination of heterogeneous or mixed cell population in tumors 审中-公开
公开(公告)号：US20060233814A1
公开(公告)日：2006-10-19
申请号：US11404001
申请日：2006-04-14
申请人： Viktor Goldmakher , Robert Lutz , Ravi Chari , Yelena Kovtun , John Lambert , Rita Steeves , Hans Erickson
发明人： Viktor Goldmakher , Robert Lutz , Ravi Chari , Yelena Kovtun , John Lambert , Rita Steeves , Hans Erickson
IPC分类号： A61K39/395 , A61K31/5383 , C07K16/46 , A61K31/58 , A61K38/19
CPC分类号： C07K16/3046 , A61K31/5383 , A61K31/58 , A61K47/6803 , A61K47/6849 , A61K2039/505 , C07D498/18 , C07K2317/24
摘要： Methods of killing or inhibiting tumors comprising of heterogeneous or mixed cell populations is described. The killing or inhibition of tumors is achieved by selectively targeting a unique ligand suspected of being expressed on a particular cell population to also kill a cell population lacking the unique ligand. These conjugates have therapeutic use as they are delivered to a specific cell population to kill these cells and the cytotoxic drug is released to kill non-targeted cells, thereby eliminating the tumor.

72. 发明申请

US20060233811A1 Compositions and methods for treating cancer using immunoconjugates and chemotherapeutic agents 有权
公开(公告)号：US20060233811A1
公开(公告)日：2006-10-19
申请号：US11453008
申请日：2006-06-15
申请人： Ravi Chari
发明人： Ravi Chari
IPC分类号： A61K39/395 , C07K16/46
CPC分类号： A61K31/337 , A61K47/6803 , A61K47/6849 , Y02A50/423 , Y02A50/491 , A61K2300/00
摘要： The present invention is based on the discovery that the administration of at least one immunoconjugate and at least one chemotherapeutic agent provides an unexpectedly superior treatment for cancer. The present invention is directed to compositions comprising at least one immunoconjugate and at least one chemotherapeutic agent and to methods of treating cancer using at least one immunoconjugate and at least one chemotherapeutic agent. The present invention also provides methods of modulating the growth of selected cell populations, such as cancer cells, by administering a therapeutically effective amount of at least one chemotherapeutic agent and at least one immunoconjugate.

73. 发明授权

US07097840B2 Methods of treatment using anti-ErbB antibody-maytansinoid conjugates 有权
公开(公告)号：US07097840B2
公开(公告)日：2006-08-29
申请号：US09811123
申请日：2001-03-16
申请人： Sharon Erickson , Ralph Schwall , Mark Sliwkowski , Walter Blattler
发明人： Sharon Erickson , Ralph Schwall , Mark Sliwkowski , Walter Blattler
IPC分类号： A61K39/40
CPC分类号： C07K16/3015 , A01K67/0271 , A01K67/0275 , A01K67/0278 , A01K2207/15 , A01K2217/00 , A01K2217/05 , A01K2217/052 , A01K2227/105 , A01K2267/0331 , A61K9/0019 , A61K39/39558 , A61K47/6803 , A61K47/6855 , A61K47/6871 , A61K2039/505 , C07K16/2863 , C07K16/32 , C07K2317/24 , C12N15/8509
摘要： The application concerns methods of treatment using anti-ErbB receptor antibody-maytansinoid conjugates, and articles of manufacture suitable for use in such methods. In particular, the invention concerns ErbB receptor-directed cancer therapies, using anri-ErbB receptor antibody-maytansinoid conjugates.

74. 再颁专利

USRE39151E1 Process for the preparation and purification of thiol-containing maytansinoids 有权
标题翻译：用于制备和纯化含硫醇的美登木素生物碱的方法
公开(公告)号：USRE39151E1
公开(公告)日：2006-06-27
申请号：US10410143
申请日：2003-04-10
申请人： Ravi Vankeepuram Jagannatha Chari , Wayne Charles Widdison
发明人： Ravi Vankeepuram Jagannatha Chari , Wayne Charles Widdison
IPC分类号： C07D491/12 , C07D498/06
CPC分类号： C07D498/18 , A61K47/6803
摘要： The present invention provides a process for the preparation and purification of thiol-containing maytansinoids comprising the steps of: (1) reductive hydrolysis of a maytansinoid C-3 ester with a reducing agent selected from the group consisting lithium trimethoxyaluminum hydride (LiAl (OMe)3H), lithium triethoxyaluminum hydride (LiAl(OEt)3H), lithium tripropoxyaluminum hydride (LiAl (OPr)3H), sodium trimethoxyaluminum hydride (NaAl (OMe)3H), sodium triethoxyaluminum hydride (NaAl(OEt)3H) and sodium tripropoxyaluminum hydride (NaAl(OPr)3H) to yield a maytansinol; (2) purifying the maytansinol to remove side products when present; (3) esterifying the purified maytansinol with a carboxylic acid to yield a mixture of an L- and a D-aminoacyl ester of maytansinol; (4) separating the L-aminoacyl ester of maytansinol from the reaction mixture in (3); (5) reducing the L-aminoacyl ester of maytansinol to yield a thiol-containing maytansinoid; and (5) purifying the thiol-containing maytansinoid.
摘要翻译：本发明提供了一种制备和纯化含硫醇的美登木素生物碱的方法，包括以下步骤：（1）用选自三氯化铝氢化铝（LiAl（OMe））的还原剂还原水解美登木素生物碱C-3酯， H 3），三乙氧基氢化铝锂（LiAl（OEt）3 H），三丙氧基氢化铝锂（LiAl（OPr）3 H），钠氢化三乙氧基铝（NaAl（OMe）3 H），三乙氧基氢化铝钠（NaAl（OEt）3 H）和三氢氧化铝氢化钠（NaAl（OPr）3） / H），得到美登素; （2）当存在时，净化美登素以除去副产物; （3）用羧酸酯化纯化的美登醇，得到美登素的L-和D-氨酰基酯的混合物; （4）从（3）中的反应混合物中分离出美登素的L-氨基酰基酯; （5）还原美登素的L-氨基酰基酯以产生含硫醇的美登木素生物碱; 和（5）纯化含硫醇的美登木素生物碱。

75. 发明申请

US20050272729A1 Cytotoxic agents comprising taxanes and their therapeutic use 失效
标题翻译：包含紫杉烷及其治疗用途的细胞毒素
公开(公告)号：US20050272729A1
公开(公告)日：2005-12-08
申请号：US11203960
申请日：2005-08-16
申请人： Ravi Chari , Walter Blattler
发明人： Ravi Chari , Walter Blattler
IPC分类号： C07D305/08 , A61K31/337 , A61K31/452 , A61K31/496 , A61K31/5377 , A61K47/48 , A61P35/00 , A61P43/00 , C07D305/14 , C07D413/02 , C07K16/28 , C07K16/32 , C07D45/02 , C07D35/14
CPC分类号： C07D305/14 , A61K31/337 , A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K47/6881 , A61K2039/505 , C07K16/2863 , C07K16/32 , Y02A50/423 , Y02A50/491
摘要： A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.
摘要翻译：包含与细胞结合剂连接的一种或多种紫杉烷类的细胞毒性剂。一种用于杀死所选细胞群的治疗组合物，其包含：（A）细胞毒性量的一种或多种通过连接基团与细胞结合剂共价结合的紫杉烷，和（B）药学上可接受的载体，稀释剂或赋形剂。一种杀死所选细胞群体的方法，包括使含有目标细胞的靶细胞或组织与有效量的细胞毒性剂接触，所述细胞毒剂包含与细胞结合剂连接的一种或多种紫杉烷类。新型含硫紫杉烷。

76. 发明申请

US20050118183A1 Anti-CD33 antibodies and method for treatment of acute myeloid leukemia using the same 有权
标题翻译：抗CD33抗体及其治疗急性骨髓性白血病的方法
公开(公告)号：US20050118183A1
公开(公告)日：2005-06-02
申请号：US10700632
申请日：2003-11-05
申请人： Mary Hoffee , Daniel Tavares , Robert Lutz
发明人： Mary Hoffee , Daniel Tavares , Robert Lutz
IPC分类号： A61K20060101 , A61K39/395 , A61K39/40 , A61K39/42 , A61K39/44 , C07H21/04 , C07K16/28 , C07K16/46 , C12N5/06 , C12N5/16 , C12N15/00 , G01N33/574
CPC分类号： C07K16/2803 , A61K39/3955 , A61K47/6803 , A61K47/6849 , A61K2039/505 , C07K16/2896 , C07K2317/24 , C07K2317/56 , C07K2317/565 , C07K2317/70 , C07K2317/92
摘要： The present invention relates to antibodies that bind CD33. More particularly, the invention relates to anti-CD33 antibodies, fragments and homologues of said antibodies, humanized and resurfaced versions of said antibodies, functional equivalents and improved versions of said antibodies, immunoconjugates and compositions comprising said antibodies, and the uses of same in diagnostic, research and therapeutic applications. The invention also relates to a polynucleotide encoding the antibodies, vectors comprising the polynucleotides, host cells transformed with polynucleotides and methods of producing the antibodies.
摘要翻译：本发明涉及结合CD33的抗体。更具体地说，本发明涉及抗CD33抗体，所述抗体的片段和同系物，所述抗体的人源化和表面化形式，所述抗体的功能等同物和改进形式，免疫偶联物和包含所述抗体的组合物及其在诊断中的用途，研究和治疗应用。本发明还涉及编码抗体的多核苷酸，包含多核苷酸的载体，用多核苷酸转化的宿主细胞和产生抗体的方法。

77. 发明申请

US20050003513A1 Mutant actinosynnema pretiosum strain with increased maytansinoid production 有权
标题翻译：突变型Actinosynnema preysum菌株与美登木素生产增加
公开(公告)号：US20050003513A1
公开(公告)日：2005-01-06
申请号：US10898169
申请日：2004-07-26
申请人： Johnson Chung , Graham Byng
发明人： Johnson Chung , Graham Byng
IPC分类号： C12P17/14 , C12N1/20 , C12P17/18
CPC分类号： C12P17/188
摘要： A microorganism that is a mutant bacterial strain of the species Actinosynnema pretiosum, designated PF4-4, (ATCC PTA-3921), being capable of producing maytansinoid ansamitocins such as ansamitocin P-3 in improved yield compared to previous known strains, and capable of growth under varied culture conditions, and methods of producing maytansinoid ansamitocins by culturing PF4-4 in a suitable growth medium.
摘要翻译：一种微生物，其是与以前已知的菌株相比，能够以提高的产量生产美登木素类粘虫霉素如安曲霉素P-3，称为PF4-4，（ATCC PTA-3921）的Actinosynnema preiosum种突变细菌菌株，并且能够在不同的培养条件下生长，以及通过在合适的生长培养基中培养PF4-4来生产美登木素生物素生物霉素的方法。

78. 发明申请

US20040039176A1 Cross-linkers with high reactivity and solubility and their use in the preparation of conjugates for targeted delivery of small molecule drugs 失效
标题翻译：具有高反应性和溶解性的交联剂及其在制备用于靶向递送小分子药物的缀合物中的用途
公开(公告)号：US20040039176A1
公开(公告)日：2004-02-26
申请号：US10633616
申请日：2003-08-05
申请人： Immunogen, Inc.
发明人： Wayne Charles Widdison
IPC分类号： C07K016/46
CPC分类号： A61K47/6803 , A61K47/6889
摘要： Disclosed is a method of making conjugates of cell binding agents and small molecule drugs comprising reacting a cell binding agent with a bifunctional cross-linking moiety to thereby provide the cell binding agent with a reactive disulfide group and then reacting the modified cell binding agent with a small molecule drug comprising a free thiol group. Bifunctional cross-linking moieties are also disclosed.
摘要翻译：公开了一种制备细胞结合剂和小分子药物的缀合物的方法，包括使细胞结合剂与双功能交联部分反应，从而向细胞结合剂提供活性二硫基团，然后使修饰的细胞结合剂与包含游离巯基的小分子药物。还公开了双功能交联部分。

79. 发明授权

US5834234A Apoptosis associated protein Bbk 失效
标题翻译：凋亡相关蛋白Bbk
公开(公告)号：US5834234A
公开(公告)日：1998-11-10
申请号：US632514
申请日：1996-05-29
申请人： Gregory J. Gallo
发明人： Gregory J. Gallo
IPC分类号： C12N15/02 , A61K31/00 , A61K31/70 , A61K31/7088 , A61K35/76 , A61K38/00 , A61K48/00 , A61P35/00 , A61P37/00 , A61P37/06 , C07K7/00 , C07K14/47 , C07K16/18 , C12N5/10 , C12N15/09 , C12P21/02 , C12P21/08 , C07K7/08 , C12N1/00 , C12N5/02
CPC分类号： C07K14/4747 , A61K38/00
摘要： The present invention is directed to an isolated Bbk protein, nucleotide sequences coding for and regulating expression of the protein, antibodies directed against the protein, and recombinant vectors and host cells containing the genetic sequences coding for and regulating the expression of the protein sequence. The invention is also directed to genomic DNA, cDNA, and RNA encoding the Bbk protein sequence and to corresponding antisense RNA sequences. Antibodies can be used to detect Bbk in biological specimens, including, for example, human tissue samples. The present invention is further directed to methods of treating degenerative disorders characterized in inappropriate cell proliferation or inappropriate cell death. The present invention is further directed to methods for diagnosing degenerative disorders characterized in inappropriate cell proliferation or inappropriate cell death, as well as methods for monitoring the progress of such degenerative disorders.
摘要翻译：本发明涉及分离的Bbk蛋白，编码和调节蛋白质表达的核苷酸序列，针对蛋白质的抗体，以及含有编码和调节蛋白质序列表达的基因序列的重组载体和宿主细胞。本发明还涉及编码Bbk蛋白序列的基因组DNA，cDNA和RNA以及相应的反义RNA序列。抗体可用于检测生物标本中的Bbk，包括例如人组织样品。本发明进一步涉及以不适当的细胞增殖或不适当的细胞死亡为特征的退行性疾病的治疗方法。本发明还涉及用于诊断特征为不适当的细胞增殖或不适当的细胞死亡的退行性疾病的方法，以及用于监测这种退行性疾病进展的方法。

80. 发明公开

US20240299571A1 ANTI-FOLR1 IMMUNOCONJUGATES AND ANTI-PD-1 ANTIBODY COMBINATIONS 审中-公开
公开(公告)号：US20240299571A1
公开(公告)日：2024-09-12
申请号：US18489292
申请日：2023-10-18
申请人： ImmunoGen, Inc. , Merck Sharp & Dohme LLC
发明人： Rodrigo R. RUIZ SOTO
IPC分类号： A61K47/68 , A61K9/00 , A61K31/57 , A61K39/00 , A61K39/395 , A61K45/06 , A61P35/04 , C07K16/28
CPC分类号： A61K47/6803 , A61K9/0019 , A61K31/57 , A61K39/3955 , A61K39/39558 , A61K45/06 , A61K47/6849 , A61K47/6869 , A61K47/6889 , A61P35/04 , C07K16/28 , C07K16/2818 , C07K16/2827 , A61K2039/505 , A61K2039/507 , A61K2039/545 , A61K2300/00
摘要： Therapeutic combinations of immunoconjugates that bind to FOLR1 (e.g., IMGN853) with anti-PD-1 antibodies or antigen-binding fragments thereof (e.g., pembrolizumab) are provided. Methods of administering the combinations to treat cancers, e.g., ovarian, peritoneal, or fallopian tube cancers, with greater clinical efficacy and/or decreased toxicity are also provided.

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