- Mio- and Dio-Fmoc - Two modified Fmoc protecting groups promoting solubility
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Two novel Fmoc-derived protecting groups, Mio-Fmoc and Dio-Fmoc, were developed, which cause dramatically enhanced solubility of the corresponding derivatives in most organic solvents. Furthermore, the suitability of these groups in solid-phase peptide synthesis was highlighted. Georg Thieme Verlag Stuttgart.
- Wessig, Pablo,Czapla, Sylvia,M?llnitz, Kristian,Schwarz, Jutta
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- ANTI-CD25 ANTIBODY-MAYTANSINE CONJUGATES AND METHODS OF USE THEREOF
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The present disclosure provides anti-CD25 antibody-maytansine conjugate structures. The disclosure also encompasses methods of production of such conjugates, as well as methods of using the same.
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Paragraph 00389-00392
(2021/04/10)
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- ANTI-CD37 ANTIBODY-MAYTANSINE CONJUGATES AND METHODS OF USE THEREOF
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The present disclosure provides anti-CD37 antibody-maytansine conjugate structures. The disclosure also encompasses methods of production of such conjugates, as well as methods of using the same.
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Paragraph 00396-00399
(2021/05/07)
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- ANTI-CD22 ANTIBODY-MAYTANSINE CONJUGATES, COMBINATIONS, AND METHODS OF USE THEREOF
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The present disclosure provides methods for treating a cancer or resistant cancer with a combination of an anti-CD22 antibody-maytansine conjugate and one or more anti-cancer agents. The disclosure also encompasses methods for sensitizing a cancer with such combinations. Also provided are pharmaceutical compositions including such combinations.
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Paragraph 0550-0553
(2019/07/15)
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- ANTI-CD22 ANTIBODY-MAYTANSINE CONJUGATES AND METHODS OF USE THEREOF
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The present disclosure provides anti-CD22 antibody-maytansine conjugate structures. The disclosure also encompasses methods of production of such conjugates, as well as methods of using the same.
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Paragraph 00389; 00390; 00391; 00392
(2017/08/24)
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- ANTI-HER2 ANTIBODY-MAYTANSINE CONJUGATES AND METHODS OF USE THEREOF
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The present disclosure provides anti-HER2 antibody-maytansine conjugate structures. The disclosure also encompasses methods of production of such conjugates, as well as methods of using the same.
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Paragraph 00537; 00538; 00539; 00540
(2015/12/24)
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- HYDRAZINYL-PYRROLO COMPOUNDS AND METHODS FOR PRODUCING A CONJUGATE
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The present disclosure provides conjugate structures and hydrazinyl-pyrrolo compound structures used to produce these conjugates. The disclosure also encompasses methods of production of such conjugates, as well as methods of using the same. Aspects of the present disclosure include a pharmaceutical composition. The pharmaceutical composition includes a conjugate as described herein and a pharmaceutically acceptable excipient. Aspects of the present disclosure include a method of delivering a conjugate to a subject. The method includes administering to the subject an effective amount of a conjugate as described herein. Aspects of the present disclosure include a method of treating a condition in a subject.
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Paragraph 00117; 00978; 00979
(2015/06/11)
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- Novel N-substituted 4-hydrazino piperidine derivative as a dipeptidyl peptidase IV inhibitor
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A novel class of N-substituted 4-hydrazino piperidine derivatives were designed, synthesized and evaluated for DPP IV inhibition. The SAR studies on the N-substituted piperidine led to the discovery of compound 22e as a potent DPP IV inhibitor (IC50 88 nM), which is highly selective over other peptidases. In vivo efficacy indicates that compound 22e stimulates insulin release in response to glucose load and improves glucose tolerance in n5-STZ and Zucker Diabetic Fatty (ZDF) rats.
- Gupta, Ramesh C.,Chhipa, Laxmikant,Mandhare, Appaji B.,Zambad, Shitalkumar P.,Chauthaiwale, Vijay,Nadkarni, Sunil S.,Dutt, Chaitanya
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scheme or table
p. 5021 - 5025
(2010/03/24)
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- Oligospiroketals as novel molecular rods
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A modular approach for the synthesis of molecular rods based on oligospiroketals has been developed. The strategy relies on different terminal and intermediate segments, which are joined by ketal formation between ketones and diols. For this purpose it was necessary to develop a new ketalization method to circumvent some problems related with the established methods. The terminal segments are either derived from 4-piperidinone or from 4-oxocyclohexane carboxylic acid whereas the intermediate segments rest on pentaerythritol and cyclohexane-1,4-dione. A series of trispiro (14-18), hexaspiro (19) and nonaspiro (20) compounds have been prepared and characterized. From these we realized that it is imperative to use solubility enhancing groups if more than seven rings are joined.
- Wessig, Pablo,Moellnitz, Kristian,Eiserbeck, Christiane
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p. 4859 - 4872
(2008/02/03)
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- AZOLIDINECARBONITRILES AND THEIR USE AS DPP-IV INHIBITORS
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The invention discloses a novel heterocyclic compounds that falls within f the ambit of general formula (I), its stereoisomers, pharmaceutically acceptable salts or solvates wherein X, n,k,z, R1, R2, R3, R4, R5 and R6 are as defined in the specification that are useful in (i) normalizing elevated blood pglucose levels in diabetes, (ii) treating disorders related to glucose intolerance and (iii) for scavenging free radicals of mammals. The invention also discloses pharmaceutically acceptable composition comprising these compounds, method for preparation of the compounds as defined bove and method of treating mammals including human beings by administering an effective amount of said compounds to a subject in need thereof. The invention further discloses use of these compounds in the manufacture of a medicament useful for treatment of different disease conditions as stated above.
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Page/Page column 61
(2008/06/13)
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