Abstract: The present application provides an improved process for the preparation of sugammadex which comprises the halogenation of ?-cyclodextrin in a suitable organic solvent to give 6-per-deoxy-6-per-halo-?-cyclodextrin, wherein halo is bromo or chloro, reacting the halogenated ?-cyclodextrin with 3-mercaptopropionic acid in the presence of alkoxide base to obtain sugammadex of formula I. This application also provides isolation of 6-per-deoxy-6-per-chloro-?-cyclodextrin as a crystalline compound and its use for the preparation of sugammadex of formula (I).

Abstract: The present application provides an improved process for the preparation of sugammadex which comprises the halogenation of ?-cyclodextrin in a suitable organic solvent to give 6-per-deoxy-6-per-halo-?-cyclodextrin, wherein halo is bromo or chloro, reacting the halogenated ?-cyclodextrin with 3-mercaptopropionic acid in the presence of alkoxide base to obtain sugammadex of formula I. This application also provides isolation of 6-per-deoxy-6-per-chloro-?-cyclodextrin as a crystalline compound and its use for the preparation of sugammadex of formula (I).

Abstract: A process for the preparation of a thiol functionalized hydroxyalkyl starch derivative comprising (i) providing a reaction mixture comprising a solvent, hydroxyalkyl starch, cysteamine and/or cystamine, and a reductive amination agent; (ii) subjecting the reaction mixture provided in (i) to reductive amination conditions, and (iii) subjecting the mixture obtained from (ii) to reducing conditions.

Abstract: The present invention relates to a hydroxyalkyl starch (HAS) derivative of formula (I) wherein F1 is a functional group comprising the group —NR?—, with R? being H or alkyl; L is a spacer bridging F1 and S; wherein HAS? is the remainder of the HAS molecule, Rb and Rc are —[(CR1R2)mO]n—H and are the same or different from each other; Ra is —[(CR1R2)mO]n—H with HAS? being the remainder of the hydroxyalkyl starch molecule, or Ra is HAS? with HAS? and HAS? together being the remainder of the hydroxyalkyl starch molecule; R1 and R2 are independently hydrogen or an alkyl group having from 1 to 4 carbon atoms, m is 2 to 4, wherein R1 and R2 are the same or different from each other in the m groups CR1R2; n is from 0 to 6.

Abstract: The present invention relates to a hydroxyalkyl starch conjugate and a method for preparing the same, said hydroxyalkyl starch conjugate comprising a hydroxyalkyl starch derivative and a cytotoxic agent, the cytotoxic agent comprising at least one secondary hydroxyl group, wherein the hydroxyalkyl starch is linked via said secondary hydroxyl group to the cytotoxic agent. The conjugate according to the present invention has a structure according to the following formula HAS?(-L-M)n wherein M is a residue of the cytotoxic agent, L is a linking moiety, HAS? is the residue of the hydroxyalkyl starch derivative, and n is greater than or equal to 1, and wherein the hydroxyalkyl starch derivative has a mean molecular weight (MW) above the renal threshold.

Abstract: The present invention relates to a hydroxyalkyl starch conjugate and a method for preparing the same, said hydroxy-yalkyl starch conjugate comprising a hydroxyalkyl starch derivative and a cytotoxic agent, the cytotoxic agent comprising at least one secondary hydroxyl group, wherein the hydroxyalkyl starch is linked via said secondary hydroxyl group to the cytotoxic agent. The conjugate according to the present invention has a structure according to the following formula HAS?(-L-M)n wherein M is a residue of the cytotoxic agent, L is a linking moiety, HAS? is the residue of the hydroxyalkyl starch derivative, and n is greater than or equal to 1, and wherein the hydroxyalkyl starch derivative has a mean molecular weight (MW) above the renal threshold.

Abstract: The present invention relates to hydroxyalkyl starch conjugates, a method for preparing the same, the hydroxyalkyl starch conjugate comprising a hydroxyalkyl starch derivative and a cytotoxic agent and the cytotoxic agent comprising at least one tertiary hydroxyl group, wherein the hydroxyalkyl starch is linked via said tertiary hydroxyl group to the cytotoxic agent. The conjugates according to the present invention have a structure according to the following formula HAS?(-L-M)n wherein M is a residue of the cytotoxic agent, L is a linking moiety, HAS? is the residue of the hydroxyalkyl starch derivative, and n is greater than or equal to 1, and wherein the hydroxyalkyl starch derivative has a mean molecular weight (MW) above the renal threshold.

Abstract: The present invention relates to nitric oxide delivering hydroxyalkyl starch derivatives, methods of preparing the same, and specific uses of these hydroxyalkyl starch derivatives.

Abstract: The present invention relates to a hydroxyalkyl starch conjugate and a method for preparing the same, said hydroxyalkyl starch conjugate comprising a hydroxyalkyl starch derivative and a cytotoxic agent, the cytotoxic agent comprising at least one secondary hydroxyl group, wherein the hydroxyalkyl starch is linked via said secondary hydroxyl group to the cytotoxic agent. The conjugate according to the present invention has a structure according to the following formula HAS?(-L-M)n wherein M is a residue of the cytotoxic agent, L is a linking moiety, HAS? is the residue of the hydroxyalkyl starch derivative, and n is greater than or equal to 1, and wherein the hydroxyalkyl starch derivative has a mean molecular weight (MW) above the renal threshold.

Abstract: The present invention relates to hydroxyalkyl starch conjugates and a method for preparing the same, the hydroxyalkyl starch conjugate comprising a hydroxyalkyl starch derivative and a cytotoxic agent, the cytotoxic agent comprising at least one primary hydroxyl group, wherein the hydroxyalkyl starch is linked via said primary hydroxyl group to the cytotoxic agent. The conjugates according to the present invention have a structure according to the following formula HAS?(-L-M)n wherein M is a residue of the cytotoxic agent, L is a linking moiety, HAS? is the residue of the hydroxyalkyl starch derivative, and n is greater than or equal to 1, and wherein the hydroxyalkyl starch derivative has a mean molecular weight (MW) above the renal threshold and a molar substitution (MS) in the range of from 0.6 to 1.5.

Abstract: The present invention relates to a hydroxyalkyl starch conjugate and a method for preparing the same, said hydroxy-yalkyl starch conjugate comprising a hydroxyalkyl starch derivative and a cytotoxic agent, the cytotoxic agent comprising at least one secondary hydroxyl group, wherein the hydroxyalkyl starch is linked via said secondary hydroxyl group to the cytotoxic agent. The conjugate according to the present invention has a structure according to the following formula HAS?(-L-M)n wherein M is a residue of the cytotoxic agent, L is a linking moiety, HAS? is the residue of the hydroxyalkyl starch derivative, and n is greater than or equal to 1, and wherein the hydroxyalkyl starch derivative has a mean molecular weight (MW) above the renal threshold.

Abstract: The present invention relates to a hydroxyalkyl starch conjugate and a method for preparing the same, said hydroxyalkyl starch conjugate comprising a hydroxyalkyl starch derivative and a cytotoxic agent, the cytotoxic agent comprising at least one secondary hydroxyl group, wherein the hydroxyalkyl starch is linked via said secondary hydroxyl group to the cytotoxic agent. The conjugate according to the present invention has a structure according to the following formula HAS?(-L-M)n wherein M is a residue of the cytotoxic agent, L is a linking moiety, HAS? is the residue of the hydroxyalkyl starch derivative, and n is greater than or equal to 1, and wherein the hydroxyalkyl starch derivative has a mean molecular weight (MW) above the renal threshold.

Abstract: The present invention relates to nitric oxide delivering hydroxyalkyl starch derivatives, methods of preparing the same, and specific uses of these hydroxyalkyl starch derivatives.

Abstract: The present invention relates to hydroxyalkyl starch conjugates, a method for preparing the same, the hydroxyalkyl starch conjugate comprising a hydroxyalkyl starch derivative and a cytotoxic agent and the cytotoxic agent comprising at least one tertiary hydroxyl group, wherein the hydroxyalkyl starch is linked via said tertiary hydroxyl group to the cytotoxic agent. The conjugates according to the present invention have a structure according to the following formula HAS?(-L-M)n wherein M is a residue of the cytotoxic agent, L is a linking moiety, HAS? is the residue of the hydroxyalkyl starch derivative, and n is greater than or equal to 1, and wherein the hydroxyalkyl starch derivative has a mean molecular weight (MW) above the renal threshold.

Abstract: The present invention relates to hydroxyalkyl starch (HAS) conjugates and to a method for preparing the hydroxyalkyl starch (HAS) conjugates, the hydroxyalkyl starch (HAS) conjugates comprising a hydroxyalkyl starch derivative and a cytotoxic agent, said conjugate having a structure according the following formula HAS?(-M)n wherein M is a residue of a cytotoxic agent, the cytotoxic agent comprising a carbonyl group, HAS? is a residue of the hydroxyalkyl starch derivative comprising at least one functional group X, n is greater than or equal to 1, and wherein the cytotoxic agent is linked via the carbonyl function present in the cytotoxic agent to the functional group X comprised in the hydroxyalkyl starch derivative, wherein the linkage via the carbonyl function is a cleavable linkage, which is capable of being cleaved in vivo so as to release the cytotoxic agent.