Patents by Inventor Dragan Grabulovski
Dragan Grabulovski has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Publication number: 20230372525Abstract: The present invention relates to a method for generating an antibody-payload conjugate by means of a microbial transglutaminase (MTG). The method comprises a step of conjugating a linker comprising or having the structure (shown in N—>C direction) Aax-(Sp1)-B1-(Sp2) via a primary amine in the N-terminal residue Aax to a glutamine (Gln) residue comprised in the heavy or light chain of an antibody, wherein Aax is an amino acid having the structure NH2—Y—COOH, wherein Y comprises a substituted or unsubstituted alkyl or heteroalkyl chain; (Sp1) is a chemical spacer or is absent; (Sp2) is a chemical spacer or is absent; and B1 is a linking moiety or a payload. Further the present invention relates to antibody-linker conjugates that have been generated with the method of the invention and uses thereof.Type: ApplicationFiled: March 2, 2023Publication date: November 23, 2023Inventors: Romain BERTRAND, Isabella ATTINGER-TOLLER, Dragan GRABULOVSKI, Philipp SPYCHER
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Publication number: 20230263904Abstract: The present invention relates to a method for generating an antibody-payload conjugate by means of a microbial transglutaminase (MTG). The method comprises a step of conjugating a linker comprising the structure (shown in N->C direction) (Sp1)-RK-(Sp2)-B-(Sp3) or (Sp1)-B-(Sp2)-RK-(Sp3) to a Gln residue comprised in an antibody, wherein (Sp1) is a chemical spacer or is absent; (Sp2) is a chemical spacer or is absent; (Sp3) is a chemical spacer or is absent; R is arginine or an arginine derivative or an arginine mimetic; K is lysine or a lysine derivative or a lysine mimetic; B is a linking moiety or a payload; and wherein the linker is conjugated to the Gin residue comprised in the antibody via a primary amine comprised in the side chain of the lysine residue, the lysine derivative or the lysine mimetic. Further, the invention relates to antibody-linker conjugates, antibody-drug conjugates and linker constructs comprising an RK motif.Type: ApplicationFiled: March 23, 2023Publication date: August 24, 2023Inventors: Philipp SPYCHER, Philipp PROBST, Isabella ATTINGER-TOLLER, Romain BERTRAND, Ramona STARK, Dragan GRABULOVSKI
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Patent number: 11351267Abstract: The present invention relates to a polypeptide binding to fibroblast growth factor receptor 3 isoforms 3b and 3c (FGFR3b and FGFR3c), wherein the polypeptide comprises an amino acid sequence selected from the group consisting of: (a) GVTLFVALYDYEVYGPTPMLSFHKGEKFQIL(X1)(X2)(X3) (X4)GPYWEARSL(X5)TGETG(X6)IPSNYVAPVDSIQ (SEQ ID NO: 1), wherein amino acid positions (X1) to (X6) may be any amino acid sequence; (b) an amino acid sequence which is at least 95% identical to the amino acid sequence of (a), wherein the identity determination excludes amino acid positions (X1) to (X6) and provided that the amino acid sequence EVYGPTPM (SEQ ID NO: 2) in amino acid positions 12 to 19 of SEQ ID NO: 1 is conserved and the amino acids P and Y in amino acid positions 37 and 38 of SEQ ID NO: 1 are conserved; (c) GVTLFVALYDYEVMSTTALSFHKGEKF QILSQSPHGQYWEARSLTTGETG(X6)IPSNYVAPVDSIQ (SEQ ID NO: 19), wherein the amino acid position (X6) may be any amino acid; and (d) an amino acid sequence which is at least 95% identical to the amiType: GrantFiled: June 15, 2020Date of Patent: June 7, 2022Assignee: Cilag GMBH InternationalInventors: Michela Silacci Melkko, Richard Woods, Patricia Henne, Barbara Zubler, Elena Kage, Dragan Grabulovski, Julian Bertschinger
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Patent number: 10996226Abstract: A library is provided having a plurality of recombinant derivatives of the SH3 domain of the Fyn kinase of SEQ ID NO: 1, where one or more of the derivatives have a specific binding affinity to a protein or peptide that is not a natural SH3 binding ligand. Substantially each of the derivatives of the SH3 domain of the Fyn kinase of SEQ ID NO: 1 has an amino acid sequence with at least 80% sequence identity to the amino acid sequence of SEQ ID NO: 1, and at least 90% identity to the amino acid of SEQ ID NO: 1 outside the src and RT loops. Additionally, the amino acid sequence has at least one amino acid in or positioned up to two amino acids adjacent to the RT loop or the src loop of SEQ ID NO: 1 which is substituted, deleted or added.Type: GrantFiled: April 10, 2018Date of Patent: May 4, 2021Assignee: EIDGENOESSISCHE TECHNISCHE HOCHSCHULE ZURICHInventors: Dragan Grabulovski, Dario Neri
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Publication number: 20200345859Abstract: The present invention relates to a polypeptide binding to fibroblast growth factor receptor 3 isoforms 3b and 3c (FGFR3b and FGFR3c), wherein the polypeptide comprises an amino acid sequence selected from the group consisting of: (a) GVTLFVALYDYEVYGPTPMLSFHKGEKFQIL(X1)(X2)(X3) (X4)GPYWEARSL(X5)TGETG(X6)IPSNYVAPVDSIQ (SEQ ID NO: 1), wherein amino acid positions (X1) to (X6) may be any amino acid sequence; (b) an amino acid sequence which is at least 95% identical to the amino acid sequence of (a), wherein the identity determination excludes amino acid positions (X1) to (X6) and provided that the amino acid sequence EVYGPTPM (SEQ ID NO: 2) in amino acid positions 12 to 19 of SEQ ID NO: 1 is conserved and the amino acids P and Y in amino acid positions 37 and 38 of SEQ ID NO: 1 are conserved; (c) GVTLFVALYDYEVMSTTALSFHKGEKF QILSQSPHGQYWEARSLTTGETG(X6)IPSNYVAPVDSIQ (SEQ ID NO: 19), wherein the amino acid position (X6) may be any amino acid; and (d) an amino acid sequence which is at least 95% identical to the amiType: ApplicationFiled: June 15, 2020Publication date: November 5, 2020Applicant: Covagen AGInventors: Michela Silacci Melkko, Richard Woods, Patricia Henne, Barbara Zubler, Elena Kage, Dragan Grabulovski, Julian Bertschinger
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Publication number: 20200348309Abstract: The present invention relates to a method for the production of a library comprising recombinant derivatives of the SH3 domain of the Fyn kinase of SEQ ID NO: 1 as well as a method for selecting from a library comprising recombinant derivatives of the SH3 domain of the Fyn kinase of SEQ ID NO: 1 one or more of said derivatives having a specific binding affinity to a protein or peptide.Type: ApplicationFiled: April 10, 2018Publication date: November 5, 2020Inventors: Dragan GRABULOVSKI, Dario NERI
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Patent number: 10722589Abstract: The present invention relates to a polypeptide binding to fibroblast growth factor receptor 3 isoforms 3b and 3c (FGFR3b and FGFR3c), wherein the polypeptide comprises an amino acid sequence selected from the group consisting of: (a) GVTLFVALYDYEVYGPTPMLSFHKGEKFQIL(X1)(X2)(X3) (X4)GPYWEARSL(X5)TGETG(X6)IPSNYVAPVDSIQ (SEQ ID NO: 1), wherein amino acid positions (X1) to (X6) may be any amino acid sequence; (b) an amino acid sequence which is at least 95% identical to the amino acid sequence of (a), wherein the identity determination excludes amino acid positions (X1) to (X6) and provided that the amino acid sequence EVYGPTPM (SEQ ID NO: 2) in amino acid positions 12 to 19 of SEQ ID NO: 1 is conserved and the amino acids P and Y in amino acid positions 37 and 38 of SEQ ID NO: 1 are conserved; (c) GVTLFVALYDYEVMSTTALSFHKGEKF QILSQSPHGQYWEARSLTTGETG(X6)IPSNYVAPVDSIQ (SEQ ID NO: 19), wherein the amino acid position (X6) may be any amino acid; and (d) an amino acid sequence which is at least 95% identical to the amiType: GrantFiled: April 2, 2018Date of Patent: July 28, 2020Assignee: Covagen AGInventors: Michela Silacci Melkko, Richard Woods, Patricia Henne, Barbara Zubler, Elena Kage, Dragan Grabulovski, Julian Bertschinger
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Patent number: 10364419Abstract: The present invention relates to a polypeptide binding to human serum albumin and comprising or consisting of an amino acid sequence selected from the group consisting of: (a) GVTLFVALYDY(X1)(X2)(X3)(X4)(X5)(X6)D(X7)SFHKGEKFQIL(X8)(X9)(X10)(X11)(X12)G(X13)(X14)W(X15)(X16)RSLTTG(X17)(X18)G(X19)IPSNYVAPVDSIQ (SEQ ID NO: 1), wherein (X1) is A, V, I, L, M, G, P, S, T, N, Q, C, R, H, K, D or E; (X2) is R, H, K, A, V, I, L, M, G, P, S, T, N, Q or C; (X3) is R, H, K, S, T, N, Q, C, F, Y, W, A, V, I, L, M, G or P; (X4) is S, T, N, Q, C, A, V, I, L, M, G, P, R, H, K, F, Y, W, D or E; (X5) is S, T, N, Q, C, D, E, F, Y, W, A, V, I, L, M, G, P, R, H or K; (X6) is F, Y, W, A, V, I, L, M, G, P, R, H, K, S, T, N, Q or C; (X7) is A, V, I, L, M, G, P, R, H or K; (X8) is S, T, N, Q, C, D or E; (X9) is S, T, N, Q, C, D, E, A, V, I, L, M, G, P, F, Y or W; (X10) is A, V, I, L, M, G or P; (X11) is F, Y, W, R, H or K; (X12) is S, T, N, Q, C, F, Y or W; (X13) is F, Y, W, R, H, K, S, T, N, Q, C, D, E, A, V, I, L, M, G or P; (X14) isType: GrantFiled: September 25, 2017Date of Patent: July 30, 2019Assignee: Covagen AGInventors: Fabian Buller, Ulrich Wüllner, Irene Zbinden, Isabella Attinger-Toller, Ulrike Von Der Bey, Susann König-Friedrich, Julian Bertschinger, Dragan Grabulovski, Patricia Henne
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Patent number: 10323095Abstract: Provided is a bi-specific fusion polypeptide comprising a fynomer sequence that binds to interleukin-17a (IL-17a) and is conjugated to an antibody or subsequence thereof that binds to interleukin-6 receptor (IL-6R). The fusion polypeptide can bind to both IL-17a and IL-6R thereby suppresses, reduces, decreases, inhibits or blocks both IL-17a and IL-6R activities.Type: GrantFiled: March 16, 2015Date of Patent: June 18, 2019Assignee: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Roland Newman, Steve Granger, Michael Lyman, Dragan Grabulovski, Richard Woods, Michela Silacci, Wenjuan Zha, Isabella Attinger-Toller
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Publication number: 20190169581Abstract: The present invention relates to a polypeptide binding to human serum albumin and comprising or consisting of an amino acid sequence selected from the group consisting of: (a) GVTLFVALYDY(X1)(X2)(X3)(X4)(X5)(X6)D(X7)SFHKGEKFQIL(X8)(X9)(X10)(X11)(X12)G(X13)(X14)W(X15)(X16)RSLTTG(X17)(X18)G(X19)IPSNYVAPVDSIQ (SEQ ID NO: 1), wherein (X1) is A, V, I, L, M, G, P, S, T, N, Q, C, R, H, K, D or E; (X2) is R, H, K, A, V, I, L, M, G, P, S, T, N, Q or C; (X3) is R, H, K, S, T, N, Q, C, F, Y, W, A, V, I, L, M, G or P; (X4) is S, T, N, Q, C, A, V, I, L, M, G, P, R, H, K, F, Y, W, D or E; (X5) is S, T, N, Q, C, D, E, F, Y, W, A, V, I, L, M, G, P, R, H or K; (X6) is F, Y, W, A, V, I, L, M, G, P, R, H, K, S, T, N, Q or C; (X7) is A, V, I, L, M, G, P, R, H or K; (X8) is S, T, N, Q, C, D or E; (X9) is S, T, N, Q, C, D, E, A, V, I, L, M, G, P, F, Y or W; (X10) is A, V, I, L, M, G or P; (X11) is F, Y, W, R, H or K; (X12) is S, T, N, Q, C, F, Y or W; (X13) is F, Y, W, R, H, K, S, T, N, Q, C, D, E, A, V, I, L, M, G or P; (X14) isType: ApplicationFiled: September 25, 2017Publication date: June 6, 2019Applicant: COVAGEN AGInventors: Fabian Buller, Ulrich Wüllner, Irene Zbinden, Isabella Attinger-Toller, Ulrike Von Der Bey, Susann König-Friedrich, Julian Bertschinger, Dragan Grabulovski, Patricia Henne
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Publication number: 20190153096Abstract: Advantageous bispecific binding molecules that comprise a CD3 binding and a CD33 binding part are provided. The CD3 binding part comprises an antibody that has variations in the Fc region with reduced binding to C1q and Fc gamma receptors. The bispecific binding molecules can be used in the treatment of cancer.Type: ApplicationFiled: September 25, 2018Publication date: May 23, 2019Applicant: Covagen AGInventors: Simon Brack, Kristina Klupsch, Isabella Attinger-Toller, Fabian Buller, Adrian Zumsteg, Julian Bertschinger, Dragan Grabulovski, Vanessa Baeriswyl, Joana Roquette, Roland Scholz, Roger Santimaria, David Senn, Elena Kage, Clara Albani
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Publication number: 20190100587Abstract: Antibody and other Fc-containing molecules with variations in the Fc region with reduced binding to C1q and Fc gamma receptors are provided, which can be used in the treatment of various diseases and disorders.Type: ApplicationFiled: September 24, 2018Publication date: April 4, 2019Applicant: Covagen AGInventors: Simon Brack, Isabella Attinger-Toller, Fabian Buller, Dragan Grabulovski, Julian Bertschinger, Adrian Zumsteg
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Publication number: 20180280527Abstract: The present invention relates to a polypeptide binding to fibroblast growth factor receptor 3 isoforms 3b and 3c (FGFR3b and FGFR3c), wherein the polypeptide comprises an amino acid sequence selected from the group consisting of: (a) GVTLFVALYDYEVYGPTPMLSFHKGEKFQIL(X1)(X2)(X3) (X4)GPYWEARSL(X5)TGETG(X6)IPSNYVAPVDSIQ (SEQ ID NO: 1), wherein amino acid positions (X1) to (X6) may be any amino acid sequence; (b) an amino acid sequence which is at least 95% identical to the amino acid sequence of (a), wherein the identity determination excludes amino acid positions (X1) to (X6) and provided that the amino acid sequence EVYGPTPM (SEQ ID NO: 2) in amino acid positions 12 to 19 of SEQ ID NO: 1 is conserved and the amino acids P and Y in amino acid positions 37 and 38 of SEQ ID NO: 1 are conserved; (c) GVTLFVALYDYEVMSTTALSFHKGEKF QILSQSPHGQYWEARSLTTGETG(X6)IPSNYVAPVDSIQ (SEQ ID NO: 19), wherein the amino acid position (X6) may be any amino acid; and (d) an amino acid sequence which is at least 95% identical to the amiType: ApplicationFiled: April 2, 2018Publication date: October 4, 2018Applicant: Covagen AGInventors: Michela Silacci Melkko, Richard Woods, Patricia Henne, Barbara Zubler, Elena Kage, Dragan Grabulovski, Julian Bertschinger
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Patent number: 9989536Abstract: The present invention relates to a method for the production of a library comprising recombinant derivatives of the SH3 domain of the Fyn kinase of SEQ ID NO: 1 as well as a method for selecting from a library comprising recombinant derivatives of the SH3 domain of the Fyn kinase of SEQ ID NO: 1 one or more of said derivatives having a specific binding affinity to a protein or peptide.Type: GrantFiled: May 22, 2017Date of Patent: June 5, 2018Assignee: EIDGENOESSISCHE TECHNISCHE HOCHSCHULE ZURICHInventors: Dragan Grabulovski, Dario Neri
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Publication number: 20170307628Abstract: The present invention relates to a method for the production of a library comprising recombinant derivatives of the SH3 domain of the Fyn kinase of SEQ ID NO: 1 as well as a method for selecting from a library comprising recombinant derivatives of the SH3 domain of the Fyn kinase of SEQ ID NO: 1 one or more of said derivatives having a specific binding affinity to a protein or peptide.Type: ApplicationFiled: May 22, 2017Publication date: October 26, 2017Inventors: Dragan GRABULOVSKI, Dario NERI
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Patent number: 9790475Abstract: The present invention relates to a polypeptide binding to human serum albumin and comprising or consisting of an amino acid sequence selected from the group consisting of: (a) GVTLFVALYDY(X1)(X2)(X3)(X4)(X5) (X6)D(X7)SFHKGEKFQIL(X8)(X9)(X10)(X11)(X12)G(X13)(X14)W(X15)(X16)RSLTTG(X17)(X18)G(X19)IPSNYVAPVDSIQ (SEQ ID NO: 1), wherein (X1) is A, V, I, L, M, G, P, S, T, N, Q, C, R, H, K, D or E; (X2) is R, H, K, A, V, I, L, M, G, P, S, T, N, Q or C; (X3) is R, H, K, S, T, N, Q, C, F, Y, W, A, V, I, L, M, G or P; (X4) is S, T, N, Q, C, A, V, I, L, M, G, P, R, H, K, F, Y, W, D or E; (X5) is S, T, N, Q, C, D, E, F, Y, W, A, V, I, L, M, G, P, R, H or K; (X6) is F, Y, W, A, V, I, L, M, G, P, R, H, K, S, T, N, Q or C; (X7) is A, V, I, L, M, G, P, R, H or K; (X8) is S, T, N, Q, C, D or E; (X9) is S, T, N, Q, C, D, E, A, V, I, L, M, G, P, F, Y or W; (X10) is A, V, I, L, M, G or P; (X11) is F, Y, W, R, H or K; (X12) is S, T, N, Q, C, F, Y or W; (X13) is F, Y, W, R, H, K, S, T, N, Q, C, D, E, A, V, I, L, M, G or P; (X14) isType: GrantFiled: December 18, 2013Date of Patent: October 17, 2017Assignee: Covagen AGInventors: Fabian Buller, Ulrich Wüllner, Irene Zbinden, Isabella Attinger-Toller, Ulrike Von Der Bey, Susann König-Friedrich, Julian Bertschinger, Dragan Grabulovski, Patricia Henne
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Publication number: 20170281768Abstract: The present invention relates to a binding molecule that specifically binds to two different epitopes of an antigen expressed on tumor cells, wherein the binding molecule comprises: (a) a first binding (poly)peptide that specifically binds to a first epitope of said antigen expressed on tumor cells, wherein said first binding (poly)peptide is a Fyn SH3-derived polypeptide; and (b) a second binding (poly)peptide that specifically binds to a second epitope of said antigen expressed on tumor cells. The present invention further relates to a nucleic acid molecule encoding the binding molecule of the invention, a vector comprising said nucleic acid molecule as well as a host cell or a non-human host transformed with said vector. The invention further relates to a method of producing a binding molecule of the invention as well as to pharmaceutical and diagnostic composition.Type: ApplicationFiled: March 9, 2017Publication date: October 5, 2017Inventors: Simon Sebastian BRACK, Frédéric MOURLANE, Isabella TOLLER, Richard WOODS, Julian BERTSCHINGER, Dragan GRABULOVSKI, Babette SCHADE, Kristina KLUPSCH, Helen HACHEMI
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Patent number: 9689879Abstract: The present invention relates to a method for the production of a library comprising recombinant derivatives of the SH3 domain of the Fyn kinase of SEQ ID NO: 1 as well as a method for selecting from a library comprising recombinant derivatives of the SH3 domain of the Fyn kinase of SEQ ID NO: 1 one or more of said derivatives having a specific binding affinity to a protein or peptide.Type: GrantFiled: August 31, 2016Date of Patent: June 27, 2017Assignee: EIDGENOESSISCHE TECHNISCHE HOCHSCHULE ZURICHInventors: Dragan Grabulovski, Dario Neri
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Publication number: 20170081412Abstract: Provided is a bi-specific fusion polypeptide comprising a fynomer sequence that binds to interleukin-17a (IL-17a) and is conjugated to an antibody or subsequence thereof that binds to interleukin-6 receptor (IL-6R). The fusion polypeptide can bind to both IL-17a and IL-6R thereby suppresses, reduces, decreases, inhibits or blocks both IL-17a and IL-6R activities.Type: ApplicationFiled: March 16, 2015Publication date: March 23, 2017Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Roland NEWMAN, Steve GRANGER, Michael LYMAN, Dragan GRABULOVSKI, Richard WOODS, Michela SILACCI, Wenjuan ZHA, Isabella ATTINGER-TOLLER
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Patent number: 9593314Abstract: The present invention relates to a binding molecule that specifically binds to two different epitopes of an antigen expressed on tumor cells, wherein the binding molecule comprises: (a) a first binding (poly)peptide that specifically binds to a first epitope of said antigen expressed on tumor cells, wherein said first binding (poly)peptide is a Fyn SH3-derived polypeptide; and (b) a second binding (poly)peptide that specifically binds to a second epitope of said antigen expressed on tumor cells. The present invention further relates to a nucleic acid molecule encoding the binding molecule of the invention, a vector comprising said nucleic acid molecule as well as a host cell or a non-human host transformed with said vector. The invention further relates to a method of producing a binding molecule of the invention as well as to pharmaceutical and diagnostic composition.Type: GrantFiled: March 8, 2013Date of Patent: March 14, 2017Assignee: Covagen AGInventors: Simon Brack, Frédéric Mourlane, Isabella Toller, Richard Woods, Julian Bertschinger, Dragan Grabulovski, Babette Schade, Kristina Klupsch, Helen Hachemi