- CANCER VACCINE
-
The invention relates to a combination of a TLR-9 agonist and a conjugate of Formula (I) or pharmaceutically acceptable salt thereof. (Formula (I))
- -
-
Page/Page column 50
(2021/03/13)
-
- ANTIBODY-DRUG CONJUGATE
-
Provided herein is an antibody-drug conjugate (ADC) especially a PEGylated mono or bispecific antibody-drug conjugate (BsADC) prepared with site-specific conjugation to provide homogeneous conjugate with high potency and low toxicity. It also relates to a
- -
-
Page/Page column 55-56; 58-59
(2021/10/22)
-
- LINKERS AND CONJUGATES
-
A conjugate comprising a protein or a peptide, a linker and an active agent, wherein the linker comprises the moiety of formula (III): (III) wherein two of A1, A2 and A3 are N and the other of A1, A2
- -
-
-
- GLYCOPEPTIDE VACCINE
-
The present invention generally relates to a glycopeptide conjugate compound of Formula (I):, as described herein, compositions comprising the conjugate compound and to the use of such a compound to as a vaccine.
- -
-
Page/Page column 50
(2020/11/30)
-
- SULFOMALEIMIDE-BASED LINKERS AND CORRESPONDING CONJUGATES
-
The present invention relates to a linker of the following formula (I) or a salt thereof: (I). The present invention relates to a linker-drug conjugate of the following formula (II) or a salt thereof: (II). The present invention relates also to a binding unit-drug conjugate, such as an antibody- drug conjugate, of the following formula (III) or (IV) or a salt thereof: (III), (IV), as well as a pharmaceutical composition comprising such a binding unit-drug conjugate and its use in the treatment of cancer.
- -
-
Page/Page column 131; 137-138
(2020/05/12)
-
- Amatoxins antibody conjugate
-
The invention discloses an amatoxins antibody conjugate. The compound of the type is conjugated with a corresponding binding group with a special chemical structure, and the structure is stable in plasma and can be cracked into an active component in a special biological environment, and thus the target cell destruction is maximized, and the toxic, harmful and side effects of non-target cell can be minimized; and the amatoxins antibody conjugate is applicable to treatment of various malignant tumors.
- -
-
Paragraph 0071; 0090; 0091-0092
(2019/03/29)
-
- Bifunctional cytotoxic agents
-
Cytotoxic dimers comprising CBI-based and/or CPI-based sub-units, antibody drug conjugates comprising such dimers, and to methods for using the same to treat cancer and other conditions.
- -
-
Page/Page column 209-213
(2018/11/02)
-
- BENZOSELNOPHENE-BASED COMPOUND AND ANTIBODY-DRUG CONJUGATE CONTAINING THE SAME
-
The present invention relates to a benzoselnophene-based compound, and a preparation method thereof, and antibody-drug conjugate (ADC) containing the benzoselnophene-based compound. The present invention provides the benzoselnophene-based compound or a sa
- -
-
-
- A water-soluble nucleolin aptamer-paclitaxel conjugate for tumor-specific targeting in ovarian cancer
-
Paclitaxel (PTX) is among the most commonly used first-line drugs for cancer chemotherapy. However, its poor water solubility and indiscriminate distribution in normal tissues remain clinical challenges. Here we design and synthesize a highly water-solubl
- Li, Fangfei,Lu, Jun,Liu, Jin,Liang, Chao,Wang, Maolin,Wang, Luyao,Li, Defang,Yao, Houzong,Zhang, Qiulong,Wen, Jia,Zhang, Zong-Kang,Li, Jie,Lv, Quanxia,He, Xiaojuan,Guo, Baosheng,Guan, Daogang,Yu, Yuanyuan,Dang, Lei,Wu, Xiaohao,Li, Yongshu,Chen, Guofen,Jiang, Feng,Sun, Shiguo,Zhang, Bao-Ting,Lu, Aiping,Zhang, Ge
-
-
- BIFUNCTIONAL CYTOTOXIC AGENTS CONTAINING THE CTI PHARMACOPHORE
-
The present invention is directed to novel bifunctional CTI-CTI and CBI-CTI dimers of the formula: [in-line-formulae]F1-L1-T-L2-F2 [/in-line-formulae] where F1, L1, T, L2 and F2 are as defined herein, useful for the treatment for proliferative diseases, where the inventive dimers can function as stand-alone drugs, payloads in antibody-drug-conjugates (ADCs), and linker-payload compounds useful in connection with the production or administration of such ADCs; and to compositions including the aforementioned dimers, linker-payloads and ADCs, and methods for using these dimers, linker-payloads and ADCs, to treat pathological conditions including cancer.
- -
-
-
- FUNCTIONALIZED MORPHOLINYL ANTHRACYCLINE DERIVATIVES
-
The present invention relates to new functionalized morpholinyl anthracycline derivatives which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds, or the pharmaceutical compositions containing them. The invention also relates to the use of these derivatives in the preparation of conjugates. The morpholinyl anthracycline derivatives are of the formula Ant-L-W-Z-RM (I) wherein RM is null or a reactive moiety; Z is null or a peptidic, non peptidic or hybrid - peptidic and non peptidic - linker; W is null or a self-immolative system, comprising one or more self-immolative groups; L is null or a conditionally-cleavable moiety; Ant is an anthracycline moiety selected from the formulas (II), (III), (IV) and (V), wherein the wavy line indicates the attachment to the conditionally-cleavable moiety L, or to the self-immolative system W, or to the linker Z, or to the reactive moiety RM; provided that at least one of L, W, Z and RM is not null; R1 is halogen or NR4R5; R2 is OR6, NR7R8 or an optionally substituted group selected from straight or branched C1C4alkyl-, NR7R8-C1C4alkyl- and R60-C1C4alkyl-; R4 and R5 are independently hydrogen, a monosubstituted-benzyl, a disubstituted-benzyl, or an optionally substituted group selected from straight or branched C1-C6alkyl, NR7R8-C1-C6alkyl-, R60-C1-C6alkyl-, R7R8N-C1-C6alkylcarbonyl-, R60-C1-C6alkylcarbonyl-, R7R8N-C1-C6alkoxycarbonyl- and R60-C1-C6alkoxycarbonyl-; or R4 and R5, taken together with the nitrogen atom to which they are bound, form a heterocyclyl substituted with R4', wherein R4' is hydrogen or a group selected from straight or branched C1-C6alkyl and NR7R8-C1-C6alkyl-; R15 is null or an optionally substituted bivalent group selected from -NR7-C1-C6alkyl*, -O-C1-C6alkyl*, -NR7-C1-C6alkylcarbonyl*, -O-C1-C6alkylcarbonyl*, -NR7-C1-C6alkoxycarbonyl* and -O-C1-C6alkoxycarbonyl*, wherein * indicates the point of attachment to -NH-Ant; R6, R7 and R8 are independently hydrogen or an optionally substituted straight or branched C1-C6alkyl; or a pharmaceutically acceptable salt thereof.
- -
-
Page/Page column 66; 67
(2016/06/01)
-
- TUBULYSIN ANALOGS AND METHODS OF MAKING AND USE
-
Tubulysin analogs of the formula (I) where R1, R2 R3, R4, R5, R6, R7, and Y are as defined herein, are anti-mitotic agents that can be used in the treatment of cancer, especially when conjugated to a targeting moiety.
- -
-
Paragraph 0321
(2016/06/06)
-
- THIENO[2,3-e]INDOLE DERIVATIVES AS NEW ANTITUMOR AGENTS
-
The present invention relates to a novel class of alkylating agents comprising a thieno[2,3-e]indole moiety tethered to a DNA-binding moiety, which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds or the pharmaceutical composition containing them. The invention also relates to the use of this novel class of alkylating agents in the preparation of conjugates.
- -
-
Page/Page column 39
(2015/04/15)
-
- CONJUGATE COMPOUNDS
-
The invention relates to sphingoglycolipid analogues and peptide derivatives thereof, which are useful in treating or preventing diseases or such as those relating to infection, atopic disorders, autoimmune diseases or cancer.
- -
-
Page/Page column 88; 89
(2014/06/24)
-
- ANTI-CD70 ANTIBODY DRUG CONJUGATES
-
This invention relates to anti-CD70 antibodies and antibody drug conjugates comprising at least one non-naturally-encoded amino acid. Disclosed herein are αCD70 antibodies with one or more non-naturally encoded amino acids and further disclosed are antibody drug conjugates wherein the αCD70 antibodies of the invention are conjugated to one or more toxins. Further disclosed are methods for using such non-natural amino acid antibody drug conjugates, including therapeutic, diagnostic, and other biotechnology uses.
- -
-
Paragraph 00495
(2014/01/09)
-
- PROSTATE-SPECIFIC MEMBRANE ANTIGEN ANTIBODY DRUG CONJUGATES
-
This invention relates to prostate-specific membrane antigen (PSMA) antibodies and antibody drug conjugates comprising at least one non-naturally-encoded amino acid. Disclosed herein are αPSMA antibodies with one or more non-naturally encoded amino acids and further disclosed are antibody drug conjugates wherein the αPSMA antibodies of the invention are conjugated to one or more toxins. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid antibody drug conjugates, dolastatin analogs, and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology uses.
- -
-
Paragraph 00481
(2014/01/08)
-
- COMPOSITIONS CONTAINING, METHODS INVOLVING, AND USES OF NON-NATURAL AMINO ACID LINKED DOLASTATIN DERIVATIVES
-
Disclosed herein are non-natural amino acids and dolastatin analogs that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The dolastatin analogs can include a wide range of possible functionalities, but typically have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid dolastatin analogs and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology use.
- -
-
Page/Page column 172
(2013/02/28)
-
- Novel cathepsin B-sensitive paclitaxel conjugate: Higher water solubility, better efficacy and lower toxicity
-
In order to realize the targeted delivery of paclitaxel (PTX) to tumor through an environment-sensitive mechanism, increase its solubility in water and reformulate without toxic excipients, a novel PTX conjugate, PEG-VC-PABC-PTX was designed and synthesiz
- Liang, Liang,Lin, Song-Wen,Dai, Wenbing,Lu, Jing-Kai,Yang, Ting-Yuan,Xiang, Yu,Zhang, Yang,Li, Run-Tao,Zhang, Qiang
-
p. 618 - 629
(2012/10/07)
-
