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Last Updated: March 28, 2024

Claims for Patent: 9,745,360


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Summary for Patent: 9,745,360
Title:Dual GLP1/GIP or trigonal GLP1/GIP/glucagon agonists
Abstract: The present invention relates to exendin-4 derivatives and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as reduction of excess food intake.
Inventor(s): Haack; Torsten (Frankfurt am Main, DE), Wagner; Michael (Frankfurt am Main, DE), Henkel; Bernd (Frankfurt am Main, DE), Stengelin; Siegfried (Frankfurt am Main, DE), Evers; Andreas (Frankfurt am Main, DE), Lorenz; Martin (Frankfurt am Main, DE), Lorenz; Katrin (Frankfurt am Main, DE)
Assignee: SANOFI (Paris, FR)
Application Number:14/136,061
Patent Claims:1. A peptidic compound having the formula (I): R.sup.1--Z--R.sup.2 (I), or a salt or solvate thereof, wherein Z is a peptide moiety having the formula (II): Tyr-Aib-X3-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-X12-Gln-X14-X15-X16-X17-X18-X1- 9-X20-X21-Phe-Ile-Glu-Trp-Leu-Lys-X28-X29-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-- Pro-Ser-X40 (II), wherein: X3 is an amino acid residue selected from Gln, Glu, and His, X12 is Ile, X14 is an amino acid residue having a side chain with a functionalized --NH.sub.2 group, wherein the functionalized --NH.sub.2 side chain group is functionalized by --C(O)--R.sup.5, wherein R.sup.5 is a moiety comprising up to 100 carbon atoms and optionally heteroatoms independently selected from halogen, N, O, S and P, X15 is an amino acid residue selected from Asp and Glu, X16 is an amino acid residue selected from Ser, Lys, Glu, and Gln, X17 is an amino acid residue selected from Arg, Lys, Glu, Gln, Leu, Aib, Tyr, and Ala, X18 is an amino acid residue selected from Ala, Arg, Aib, Leu, and Tyr, X19 is an amino acid residue selected from Ala, Val, and Aib, X20 is an amino acid residue selected from Pip, (S)MeLys, (R)MeLys, and (S)MeOrn, X21 is an amino acid residue selected from Asp, Glu, and Leu, X28 is an amino acid residue selected from Asn, Ala, Aib, and Ser, X29 is an amino acid residue selected from Gly, Thr, Aib, D-Ala, and Ala, X40 is either absent or is Lys, R.sup.1 is --NH.sub.2, and R.sup.2 is the C-terminal group of the peptidic compound and is selected from --OH and --NH.sub.2.

2. The compound, salt, or solvate of claim 1, wherein X14 is an amino acid residue with a functionalized --NH.sub.2 side chain group selected from functionalized Lys, Orn, Dab and Dap, wherein at least one H atom of the --NH.sub.2 side chain group is replaced by --C(O)--R.sup.5, which is selected from the group consisting of (S)-4-Carboxy-4-hexadecanoylamino-butyryl-, (S)-4-Carboxy-4-octadecanoylamino-butyryl-, 4-Hexadecanoylamino-butyryl-, 4-{3-[(R)-2,5,7,8-tetramethyl-2((4R,8R)-4,8,12-trimethyl-tridecyl)-chroma- n-6-yloxycarbonyl]-propionylamino}-butyryl-, 4-octadecanoylamino-butyryl-, 4-((Z)-octadec-9-enoylamino)-butyryl-, 6-[(4,4-Diphenyl-cyclohexyloxy)-hydroxy-phosphoryloxy]-hexanoyl-, Hexadecanoyl-, (S)-4-Carboxy-4-(15-carboxy-pentadecanoylamino)-butyryl-, (S)-4-Carboxy-4-{3-[3-((2S,3R,4S,5R)-5-carboxy-2,3,4,5-tetrahydroxy-penta- noylamino)-propionylamino]-propionylamino}-butyryl, (S)-4-Carboxy-4-{3-[(R)-2,5,7,8-tetramethyl-2((4R,8R)-4,8,12-trimethyl-tr- idecyl)-chroman-6-yloxycarbonyl]-propionylamino}-butyryl-, (S)-4-Carboxy-4-((9Z,12Z)-octadeca-9,12-dienoylamino)-butyryl-, (S)-4-Carboxy-4-[6-((2S,3R,4S,5R)-5-carboxy-2,3,4,5-tetrahydroxy-pentanoy- lamino)-hexanoylamino]-butyryl-, (S)-4-Carboxy-4-((2S,3R,4S,5R)-5-carboxy-2,3,4,5-tetrahydroxy-pentanoylam- ino)-butyryl-, (S)-4-Carboxy-4-tetradecanoylamino-butyryl-, (S)-4-(11-Benzyloxycarbonyl-undecanoylamino)-4-carboxy-butyryl-, (S)-4-Carboxy-4-[11-((2S,3R,4R,5R)-2,3,4,5,6-pentahydroxy-hexylcarbamoyl)- -undecanoylamino]-butyryl-, (S)-4-Carboxy-4-((Z)-octadec-9-enoylamino)-butyryl-, (S)-4-Carboxy-4-(4-dodecyloxy-benzoylamino)-butyryl-, (S)-4-Carboxy-4-henicosanoylamino-butyryl-, (S)-4-Carboxy-4-docosanoylamino-butyryl-, (S)-4-Carboxy-4-((Z)-nonadec-10-enoylamino)-butyryl-, (S)-4-Carboxy-4-(4-decyloxy-benzoylamino)-butyryl-, (S)-4-Carboxy-4-[(4'-octyloxy-biphenyl-4-carbonyl)-amino]-butyryl-, (S)-4-Carboxy-4-(12-phenyl-dodecanoylamino)-butyryl-, (S)-4-Carboxy-4-icosanoylamino-butyryl-, (S)-4-Carboxy-4-((S)-4-carboxy-4-hexadecanoylamino-butyrylamino)-butyryl-- , (S)-4-Carboxy-4-((S)-4-carboxy-4-octadecanoylamino-butyrylamino)-butyryl- -, 3-(3-Octadecanoylamino-propionylamino)-propionyl-, 3-(3-Hexadecanoylamino-propionylamino)-propionyl-, 3-Hexadecanoylamino-propionyl-, (S)-4-Carboxy-4-[(R)-4-((3R,5S,7R,8R,9R,10S,12S,13R,14R,17R)-3,7,12-trihy- droxy-8,10,13-trimethyl-hexadecahydro-cyclopenta[a]phenanthren-17-yl)-pent- anoylamino]-butyryl-, (S)-4-Carboxy-4-[(R)-4-((3R,5R,8R,9S,10S,13R,14S,17R)-3-hydroxy-10,13-dim- ethyl-hexadecahydro-cyclopenta[a]phenanthren-17-yl)-pentanoylamino]-butyry- l-, (S)-4-Carboxy-4-((9S,10R)-9,10,16-trihydroxy-hexadecanoylamino)-butyry- l-, tetradecanoyl-, 11-Carboxy-undecanoyl-, 11-Benzyloxycarbonyl-undecanoyl-, (S)-4-Carboxy-4-((S)-4-carboxy-4-tetradecanoylamino-butyrylamino)-butyryl- -, 6-[Hydroxy-(naphthalen-2-yloxy)-phosphoryloxy]-hexanoyl-, 6-[Hydroxy-(5-phenyl-pentyloxy)-phosphoryloxy]-hexanoyl-, 4-(Naphthalene-2-sulfonylamino)-4-oxo-butyryl-, 4-(Biphenyl-4-sulfonylamino)-4-oxo-butyryl-, (S)-4-Carboxy-4-{(S)-4-carboxy-4-[2-(2-{2-[2-(2-{2-[(S)-4-carboxy-4-(17-c- arboxy-heptadecanoylamino)-butyrylamino]-ethoxy}-ethoxy)-acetylamino]-etho- xy}-ethoxy)-acetylamino]-butyrylamino}-butyryl-, (S)-4-Carboxy-4-[2-(2-{2-[2-(2-{2-[(S)-4-carboxy-4-(17-carboxy-heptadecan- oylamino)-butyrylamino]-ethoxy}-ethoxy)-acetylamino]-ethoxy}-ethoxy)-acety- lamino]-butyryl-, (S)-4-Carboxy-2-{(S)-4-carboxy-2-[2-(2-{2-[2-(2-{2-[(S)-4-carboxy-4-(17-c- arboxy-heptadecanoylamino)-butyrylamino]-ethoxy}-ethoxy)-acetylamino]-etho- xy}-ethoxy)-acetylamino]-butyrylamino}-butyryl-, (S)-4-Carboxy-2-[2-(2-{2-[2-(2-{2-[(S)-4-carboxy-4-(17-carboxy-heptadecan- oylamino)-butyrylamino]-ethoxy}-ethoxy)-acetylamino]-ethoxy}-ethoxy)-acety- lamino]-butyryl-, (S)-4-Carboxy-4-{(S)-4-carboxy-4-[2-(2-{2-[(S)-4-carboxy-4-(17-carboxy-he- ptadecanoylamino)-butyrylamino]-ethoxy}-ethoxy)-acetylamino]-butyrylamino}- -butyryl-, (S)-4-Carboxy-4-[2-(2-{2-[(S)-4-carboxy-4-(17-carboxy-heptadeca- noylamino)-butyrylamino]-ethoxy}-ethoxy)-acetylamino]-butyryl-,(S)-4-Carbo- xy-2-{(S)-4-carboxy-2-[2-(2-{2-[(S)-4-carboxy-4-(17-carboxy-heptadecanoyla- mino)-butyrylamino]-ethoxy}-ethoxy)-acetylamino]-butyrylamino}-butyryl-, (S)-4-Carboxy-2-[2-(2-{2-[(S)-4-carboxy-4-(17-carboxy-heptadecanoylamino)- -butyrylamino]-ethoxy}-ethoxy)-acetylamino]-butyryl-, 2-(2-{2-[2-(2-{2-[(S)-4-Carboxy-4-(17-carboxy-heptadecanoylamino)-butyryl- amino]-ethoxy}-ethoxy)-acetylamino]-ethoxy}-ethoxy)-acetyl-, 2-(2-{2-[(S)-4-Carboxy-4-(17-carboxy-heptadecanoylamino)-butyrylamino]-et- hoxy}-ethoxy)-acetyl-, (S)-4-Carboxy-4-((S)-4-carboxy-4-{(S)-4-carboxy-4-[(S)-4-carboxy-4-(19-ca- rboxy-nonadecanoylamino)-butyrylamino]-butyrylamino}-butyrylamino)-butyryl- -, 2-(2-{2-[2-(2-{2-[(S)-4-Carboxy-4-(16-1H-tetrazol-5-yl-hexadecanoylamin- o)- butyrylamino]-ethoxy}-ethoxy)-acetylamino]-ethoxy}-ethoxy)-acetyl-, 2-(2-{2-[2-(2-{2-[(S)-4-Carboxy-4-(16-carboxy-hexadecanoylamino)-butyryla- mino]-ethoxy}-ethoxy)-acetylamino]-ethoxy}-ethoxy)-acetyl-, (S)-4-Carboxy-4-{(S)-4-carboxy-4-[(S)-4-carboxy-4-(17-carboxy-heptadecano- ylamino)-butyrylamino]-butyrylamino}-butyryl-, (S)-4-Carboxy-4-((S)-4-carboxy-4-{2-[2-(2-{2-[2-(2-{(S)-4-carboxy-4-[10-(- 4-carboxy-phenoxy)-decanoylamino]-butyrylamino}-ethoxy)-ethoxy]-acetylamin- o}-ethoxy)-ethoxy]-acetylamino}-butyryl-, (S)-4-Carboxy-4-{(S)-4-carboxy-4-[2-(2-{2-[2-(2-{2-[(S)-4-carboxy-4-(7-ca- rboxy-heptanoylamino)- butyrylamino]-ethoxy}-ethoxy)-acetylamino]-ethoxy}-ethoxy)-acetylamino]-b- utyrylamino}-butyryl-, (S)-4-Carboxy-4-{(S)-4-carboxy-4-[2-(2-{2-[2-(2-{2-[(S)-4-carboxy-4-(11-c- arboxy-undecanoylamino)-butyrylamino]-ethoxy}-ethoxy)-acetylamino]-ethoxy }-ethoxy)-acetylamino]-butyrylamino}-butyryl-, (S)-4-Carboxy-4-{(S)-4-carboxy-4-[2-(2-{2-[2-(2-{2-[(S)-4-carboxy-4-(13-c- arboxy-tridecanoylamino)-butyrylaminol]-ethoxy}-ethoxy)-acetylamino]-ethox- y}-ethoxy)-acetylamino]-butyrylamino}-butyryl-, (S)-4-Carboxy-4-{(S)-4-carboxy-4-[2-(2-{2-[2-(2-{2-[(S)-4-carboxy-4-(15-c- arboxy-pentadecanoylamino)-butyrylamino]-ethoxy}-ethoxy)-acetylamino]-etho- xy}-ethoxy)-acetylamino]-butyrylamino}-butyryl-, and (S)-4-Carboxy-4-{(S)-4-carboxy-4-[2-(2-{2-[2-(2-{2-[(S)-4-carboxy-4-(19-c- arboxy-nonadecanoylamino)-butyrylamino]-ethoxy}-ethoxy)-acetylamino]-ethox- y}-ethoxy)-acetylamino]-butyrylamino}-butyryl-.

3. The compound, salt, or solvate of claim 1, wherein X14 is Lys, wherein the --NH.sub.2 side chain group is functionalized by one of the groups selected from the group consisting of (S)-4-Carboxy-4-hexadecanoylamino-butyryl-, (S)-4-Carboxy-4-octadecanoylamino-butyryl-, 4-octadecanoylamino-butyryl-, Hexadecanoyl-, (S)-4-Carboxy-4-henicosanoylamino-butyryl-, (S)-4-Carboxy-4-((S)-4-carboxy-4-octadecanoylamino-butyrylamino)-butyryl-- , and 3-(3-Octadecanoylamino-propionylamino)-propionyl-.

4. The compound, salt, or solvate according to claim 1, wherein X14 is Lys functionalized by one of the groups selected from the group consisting of (S)-4-carboxy-4-hexadecanoylamino-butyryl (.gamma.E-x53) and (S)-4-carboxy-4-octadecanoylamino-butyryl (.gamma.E-x70).

5. The compound, salt, or solvate of claim 1, wherein R.sup.2 is --NH.sub.2.

6. The compound, salt, or solvate of claim 1, wherein X14 is Lys, wherein the --NH.sub.2 side chain group is functionalized by one of the groups selected from the group consisting of (S)-4-Carboxy-4-hexadecanoylamino-butyryl-, and (S)-4-Carboxy-4-octadecanoylamino-butyryl-.

7. The compound, salt, or solvate of claim 1, wherein X3 is an amino acid residue selected from Gln, His, and Glu, X12 is Ile, X14 is Lys, wherein the --NH.sub.2 side chain group is functionalized by one of the groups selected from the group consisting of (S)-4-Carboxy-4-hexadecanoylamino-butyryl-, and (S)-4-Carboxy-4-octadecanoylamino-butyryl-, X15 is an amino acid residue selected from Glu and Asp, X16 is Glu, X17 is an amino acid residue selected from Arg and Gln, X18 is an amino acid residue selected from Ala and Arg, X19 is Ala, X20 is an amino acid residue selected from Pip, (S)MeLys, (R)MeLys, and (S)MeOrn, X21 is Glu, X28 is an amino acid residue selected from Asn, Ser, and Ala, X29 is an amino acid residue selected from Gly and Thr, and X40 is absent.

8. The compound, salt, or solvate of claim 1, wherein X19 is Ala.

9. The compound, salt, or solvate of claim 1, wherein X16 is Glu.

10. The compound, salt, or solvate of claim 1, wherein: X28 is Ala, and X29 is Gly.

11. The compound, salt, or solvate of claim 1, wherein: X28 is Asn, and X29 is Thr.

12. The compound, salt, or solvate of claim 1, wherein: X3 is an amino acid residue selected from Gln and Glu, X12 is Ile, X14 is Lys, wherein the --NH.sub.2 side chain group is functionalized by one of the groups selected from the group consisting of (S)-4-Carboxy-4-hexadecanoylamino-butyryl- (.gamma.E-x53), and (S)-4-Carboxy-4-octadecanoylamino-butyryl- (.gamma.E-x70), X15 is an amino acid residue selected from Asp and Glu, X16 is Glu, X17 is an amino acid residue selected from Arg and Gln, X18 is an amino acid residue selected from Ala and Arg, X19 is Ala, X20 is an amino acid residue selected from Pip, (S)-MeLys, (R)-MeLys, and (S)-MeOrn, X21 is Glu, X28 is an amino acid residue selected from Asn, Ala, and Ser, X29 is an amino acid residue selected from Gly and Thr, and X40 is absent.

13. The compound of claim 1, wherein the compound is selected from those of SEQ ID NOs: 8-11, and 13-16, or a salt or solvate thereof.

14. The compound of claim 1, wherein the compound is selected from those of SEQ ID NOs: 8-11, 13 and 15, or a salt or solvate thereof.

15. A pharmaceutical composition comprising a peptidic compound having the formula (I): R.sup.1--Z--R.sup.2 (I), or a salt or solvate thereof, wherein Z is a peptide moiety having the formula (II): Tyr-Aib-X3-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-X12-Gln-X14-X15-X16-X17-X18-X1- 9-X20-X21-Phe-Ile-Glu-Trp-Leu-Lys-X28-X29-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-- Pro-Ser-X40 (II), wherein: X3 is an amino acid residue selected from Gln, Glu, and His, X12 is Ile, X14 is an amino acid residue having a side chain with a functionalized --NH.sub.2 group, wherein the functionalized --NH.sub.2 side chain group is functionalized by --C(O)--R.sup.5, wherein R.sup.5 is a moiety comprising up to 100 carbon atoms and optionally heteroatoms independently selected from halogen, N, O, S and P, X15 is an amino acid residue selected from Asp and Glu, X16 is an amino acid residue selected from Ser, Lys, Glu, and Gln, X17 is an amino acid residue selected from Arg, Lys, Glu, Gln, Leu, Aib, Tyr, and Ala, X18 is an amino acid residue selected from Ala, Arg, Aib, Leu, and Tyr, X19 is an amino acid residue selected from Ala, Val, and Aib, X20 is an amino acid residue selected from Pip, (S)MeLys, (R)MeLys, and (S)MeOrn, X21 is an amino acid residue selected from Asp, Glu, and Leu, X28 is an amino acid residue selected from Asn, Ala, Aib, and Ser, X29 is an amino acid residue selected from Gly, Thr, Aib, D-Ala, and Ala, X40 is either absent or is Lys, R.sup.1 is --NH.sub.2, and R.sup.2 is the C-terminal group of the peptidic compound and is selected from --OH and --NH.sub.2.

16. The pharmaceutical composition according to claim 15, wherein the compound having the formula (I), or a salt or solvate thereof, is present as an active agent, and wherein the pharmaceutical composition further comprises at least one pharmaceutically acceptable carrier.

17. The pharmaceutical composition according to claim 15, further comprising at least one additional therapeutically active agent, wherein the additional therapeutically active agent is a GLP-1 agonist and/or insulin or an insulin analogue and/or a gastrointestinal peptide.

18. A solvate of a compound of claim 1.

19. A hydrate of a compound of claim 1.

20. The peptidic compound, salt, or solvate of claim 1, wherein R.sup.5 is a moiety comprising up to 50 carbon atoms and optionally heteroatoms selected from halogen, N, O, S and P.

21. A peptidic compound with reduced relative activity, the compound having the formula (I): R.sup.1--Z--R.sup.2 (I), or a salt or solvate thereof, wherein Z is a peptide moiety having of the formula (II): Tyr-Aib-X3-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-X12-Gln-X14-X15-X16-X17-X18-X1- 9-X20-X21-Phe-Ile-Glu-Trp-Leu-Lys-X28-X29-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-- Pro-Ser-X40 (II), wherein: X3 is an amino acid residue selected from Gln, Glu, and His, X12 is Ile, X14 is an amino acid residue having a side chain with a functionalized --NH.sub.2 group, wherein the functionalized --NH.sub.2 side chain group is functionalized by --C(O)--R.sup.5, wherein R.sup.5 is a moiety comprising up to 100 carbon atoms and optionally selected heteroatoms independently selected from halogen, N, O, S and P, X15 is an amino acid residue selected from Asp and Glu, X16 is an amino acid residue selected from Ser, Lys, Glu, and Gln, X17 is an amino acid residue selected from Arg, Lys, Glu, Gln, Leu, Aib, Tyr, and Ala, X18 is an amino acid residue selected from Ala, Arg, Aib, Leu, and Tyr, X19 is an amino acid residue selected from Ala, Val, and Aib, X20 is an amino acid residue selected from Pip, (S)MeLys, (R)MeLys, and (S)MeOrn, X21 is an amino acid residue selected from Asp, Glu, and Leu, X28 is an amino acid residue selected from Asn, Ala, Aib, and Ser, X29 is an amino acid residue selected from Gly, Thr, Aib, D-Ala, and Ala, X40 is either absent or is Lys, R.sup.1 is --NH.sub.2, and R.sup.2 is the C-terminal group of the peptidic compound and is selected from --OH and --NH.sub.2, and wherein the reduced relative activity comprises a relative activity of at least 0.04% to at least 0.5% compared to that of natural glucose-dependent insulinotropic polypeptide (GIP) at the GIP receptor, glucagon-like peptide-1(GLP-1) (7-36) at the GLP-1 receptor, or natural glucagon at the glucagon receptor.

22. The compound, salt or solvate of claim 21, wherein the peptidic compound has a relative activity of at least 0.04% compared to that of natural GIP at the GIP receptor.

23. The compound, salt or solvate of claim 22, wherein the peptidic compound has a relative activity of at least 0.2% compared to that of natural GIP at the GIP receptor.

24. The compound, salt or solvate of claim 21, wherein the peptidic compound exhibits a relative activity of at least 0.07% compared to that of GLP-1(7-36) at the GLP-1 receptor.

25. The compound, salt or solvate of claim 24, wherein the peptidic compound exhibits a relative activity of at least 0.4% compared to that of GLP-1(7-36) at the GLP-1 receptor.

26. The compound, salt or solvate of claim 24, wherein the peptidic compound further exhibits a relative activity of at least 0.1% compared to that of natural glucagon at the glucagon receptor.

27. The compound, salt or solvate of claim 26, wherein the peptidic compound exhibits a relative activity of at least 0.5% compared to that of natural glucagon at the glucagon receptor.

28. The pharmaceutical composition according to claim 17, wherein the additional therapeutically active agent is a GLP-1 agonist.

29. A peptidic compound consisting of the amino acid sequence of SEQ ID NO: 12, or a salt or solvate thereof.

30. The pharmaceutical composition according to claim 15 further comprising at least one additional therapeutically active agent, wherein said additional therapeutically active agent is selected from the group consisting of: insulin and insulin derivatives selected from the group consisting of: insulin glargine, insulin glusiline, insulin detemir, insulin lispro, insulin degludec, insulin aspart, basal insulin and analogues thereof, pegylated insulin, recombinant human insulin, polysialated insulins, long-acting insulin, NN1045, insulin in combination with pramlintide, PE0139, fast-acting and short-acting insulins, insulin hydrogel, oral insulin, inhalable insulin, transdermal insulin and sublingual insulin, and insulin derivatives which are bonded to albumin or another protein by a bifunctional linker; GLP-1, GLP-1 analogues, and GLP-1 receptor agonists selected from the group consisting of: lixisenatide, exenatide, ITCA 650, AC-2993, liraglutide, semaglutide, taspoglutide, albiglutide, dulaglutide, rExendin-4, CJC-1134-PC, PB-1023, TTP-054, Langlenatide, HM-11260C, CM-3, ORMD-0901, NN-9924, NN-9926, NN-9927, CVX-096, ZYOG-1, ZYD-1, GSK-2374697, DA-3091, MAR-701, MAR709, ZP-2929, ZP-3022, TT-401, BHM-034, MOD-6030, CAM-2036, DA-15864, ARI-2651, ARI-2255, xtenylated exenatide, xtenylated glucagon, and polymer bound derivatives thereof; dual GLP-1/GIP receptor agonists; dual GLP-1/glucagon receptor agonists; protein YY.sub.3-36(PYY3-36); pancreatic polypeptide; glucagon receptor agonists; GIP receptor agonists or antagonists; ghrelin receptor antagonists or inverse agonists; xenin; dipeptidyl peptidase IV (DPP-IV) inhibitors; sodium glucose cotransporter 2 (SGLT2) inhibitors; dual SGLT2/ SGLT1inhibitors; biguanides; thiazolidinediones; dual peroxisome proliferator-activated receptor (PPAR) agonists; sulfonylureas; meglitinides; alpha-glucosidase inhibitors; amylin; pramlintide; G protein-coupled receptor 119 (GPR119) agonists; GPR40 agonists; GPR120 agonists; GPR142agonists; systemic or low-absorbable transmembrane G protein-coupled receptor 5 (TGR5) agonists; bromocriptine mesylate (Cycloset); inhibitors of 11-beta-hydroxysteroid dehydrogenase (HSD); activators of glucokinase; inhibitors of diacylglycerol acyltransferase (DGAT); inhibitors of protein tyrosinephosphatase 1; inhibitors of glucose-6-phosphatase; inhibitors of fructose-1,6-bisphosphatase; inhibitors of glycogen phosphorylase; inhibitors of phosphoenol pyruvate carboxykinase; inhibitors of glycogen synthase kinase; inhibitors of pyruvate dehydrogenase kinase; alpha2-antagonists; C--C motif receptor (CCR-2) antagonists; modulators of glucose transporter-4; somatostatin receptor 3 agonists; 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA)-reductase inhibitors; fibrates; nicotinic acid and derivatives thereof; nicotinic acid receptor 1 agonists; PPAR-alpha, gamma, or alpha/gamma agonists or modulators; PPAR-delta agonists; acyl-CoA cholesterol acyltransferase (ACAT) inhibitors; cholesterol absorption inhibitors; bile acid-binding substances; ileal bile acid transporter (IBAT) inhibitors; microsomal triglyceride transfer protein (MTP) inhibitors; modulators of proprotein convertase subtilisin/kinexin type 9 (PCSK9); low-density lipoprotein (LDL) receptor up-regulators by liver selective thyroid hormone receptor .beta.agonists; high-density lipoprotein (HDL)-raising compounds; lipid metabolism modulators; phospholipase A2 (PLA2) inhibitors; apolipoprotein A1 (ApoA-1) enhancers; thyroid hormone receptor agonists; cholesterol synthesis inhibitors; and omega-3 fatty acids and derivatives thereof; substances for the treatment of obesity selected from the group consisting of: sibutramine, tesofensine, tetrahydrolipstatin, cannabinoid-1 (CB-1) receptor antagonists, melanin-concentrating hormone-1 (MCH-1) antagonists, melanocortin 4 (MC4) receptor agonists or partial agonists, neuropeptide Y 5(NPY5) or NPY2 antagonists, NPY4 agonists, beta-3-agonists, leptin or leptin mimetics, agonists of the 5HT2c receptor, combinations of bupropione/naltrexone, combinations of bupropione/zonisamide, combinations of bupropione/phentermine, combinations of pramlintide/metreleptin, and combinations of phentermine/topiramate; lipase inhibitors; angiogenesis inhibitors; H3 antagonists; Agouti-related protein (AgRP) inhibitors; triple monoamine uptake inhibitors; methionine aminopeptidase type 2 (MetAP2) inhibitors; nasal formulation of the calcium channel blocker diltiazem; antisense molecules against production of fibroblast growth factor receptor 4; and prohibitin targeting peptide-1; and drugs for influencing high blood pressure, chronic heart failure, or atherosclerosis selected from the groups consisting of: angiotensin II receptor antagonists, angiotensin-converting-enzyme (ACE) inhibitors, endothelin-converting-enzyme (ECE) inhibitors, diuretics, beta-blockers, calcium antagonists, centrally acting hypertensives, antagonists of the alpha-2-adrenergic receptor, inhibitors of neutral endopeptidase, and thrombocyte aggregation inhibitors.

31. A method of treating type 2 diabetes or type 1 diabetes, the method comprising administering to a patient in need thereof, a therapeutically effective amount of a peptidic compound, salt or solvate of claim 1.

32. The method of claim 31 for the treatment of type 2 diabetes.

33. A method for delaying disease progression in type 2 diabetes, delaying the progression from impaired glucose tolerance (IGT) to type 2 diabetes, or delaying the progression from type 2 diabetes to insulin-requiring diabetes, the method comprising administering to a patient in need thereof a therapeutically effective amount of a peptidic compound, salt or solvate of claim 1.

34. A method of treating type 2 diabetes or type 1 diabetes, the method comprising administering to a patient in need thereof, a therapeutically effective amount of the pharmaceutical composition of claim 15.

35. The method of claim 34 for the treatment of type 2 diabetes.

36. A method for delaying disease progression in type 2 diabetes, delaying the progression from impaired glucose tolerance (IGT) to type 2 diabetes, or delaying the progression from type 2 diabetes to insulin-requiring diabetes, the method comprising administering to a patient in need thereof a therapeutically effective amount of the pharmaceutical composition of claim 15.

Details for Patent 9,745,360

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Eli Lilly And Company HUMULIN R U-100 insulin human Injection 018780 10/28/1982 ⤷  Try a Trial 2032-12-21
Eli Lilly And Company HUMULIN R U-500 insulin human Injection 018780 12/29/2015 ⤷  Try a Trial 2032-12-21
Eli Lilly And Company HUMULIN R U-100 insulin human Injection 018780 08/06/1998 ⤷  Try a Trial 2032-12-21
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