WO1997040832A1 - Verwendung von dipeptidyl peptidase iv effektoren zur senkung des blutglukosespiegels in säugern - Google Patents

Verwendung von dipeptidyl peptidase iv effektoren zur senkung des blutglukosespiegels in säugern Download PDF

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Publication number
WO1997040832A1
WO1997040832A1 PCT/DE1997/000820 DE9700820W WO9740832A1 WO 1997040832 A1 WO1997040832 A1 WO 1997040832A1 DE 9700820 W DE9700820 W DE 9700820W WO 9740832 A1 WO9740832 A1 WO 9740832A1
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WIPO (PCT)
Prior art keywords
effectors
blood
glucose
enzyme activity
dipeptidyl peptidase
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/DE1997/000820
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German (de)
English (en)
French (fr)
Inventor
Hans-Ulrich Demuth
Fred Rosche
Jörn Schmidt
Robert P. Pauly
Christopher H. S. Mcintosh
Ray A. Pederson
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Leibniz Institut fuer Naturstoff Forschung und Infektionsbiol eVi
Vivoryon Therapeutics AG
Original Assignee
Probiodrug AG
Leibniz Institut fuer Naturstoff Forschung und Infektionsbiol eVi
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Priority to DE122007000083C priority Critical patent/DE122007000083I1/de
Priority to DK97924866T priority patent/DK0896538T3/da
Priority to CA002252576A priority patent/CA2252576C/en
Priority to EP97924866A priority patent/EP0896538B1/de
Priority to HK99104351.7A priority patent/HK1019204B/xx
Priority to JP53845397A priority patent/JP2001510442A/ja
Priority to DE200712000038 priority patent/DE122007000038I1/de
Priority to NZ332707A priority patent/NZ332707A/xx
Priority to US09/155,833 priority patent/US6303661B1/en
Priority to DE59703959T priority patent/DE59703959D1/de
Priority to AU30233/97A priority patent/AU721477C/en
Application filed by Probiodrug AG, Leibniz Institut fuer Naturstoff Forschung und Infektionsbiol eVi filed Critical Probiodrug AG
Priority to AT97924866T priority patent/ATE202705T1/de
Priority to KR1020117031497A priority patent/KR20120014064A/ko
Priority to KR1019980707018A priority patent/KR100617676B1/ko
Publication of WO1997040832A1 publication Critical patent/WO1997040832A1/de
Anticipated expiration legal-status Critical
Priority to GR20010401649T priority patent/GR3036788T3/el
Priority to LU91334C priority patent/LU91334I2/fr
Priority to NL300280C priority patent/NL300280I2/nl
Priority to NL300308C priority patent/NL300308I2/nl
Priority to LU91382C priority patent/LU91382I2/fr
Priority to US13/458,484 priority patent/US20130116290A1/en
Priority to US15/042,892 priority patent/US20170007582A1/en
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin

Definitions

  • the invention relates to a simple method for lowering the blood sugar concentration with the aid of activity-reducing effectors (substrates, pseudo-substrates, inhibitors, binding proteins, antibodies, etc.) for enzymes with comparable or identical activity to the enzymatic activity of the enzyme dipeptidyl peptidase IV.
  • proteases that are involved in unspecific proteolysis, which ultimately causes the degradation of proteins to amino acids
  • regulatory proteases are known that are involved in the functionalization (activation, deactivation, modulation) of endogenous peptide active ingredients [KIRSCHKE, H., LANGNER , J., RIEMANN, S., WIEDERANDERS, B., AN ⁇ SORGE, S. and BOHLEY, P., Lysosomal cysteine proteases. Excerpta Medica (Ciba Foundation Symposium 75), 15 (1980); KR ⁇ USSLICH, H.-G. and WIMMER, E., Viral Proteinases. Ann. Rev. Biochem. 57: 701 (1987)].
  • convertases signal peptidases or enkephalinases
  • enkephalinases have been discovered in particular in connection with immunological research and neuropeptide research [GOMEZ, S., GLUSCHANKOF, P., LEPAGE, A., MARRAKCHI, N. and COHEN, P. , Proc. Natl. Acad. Be. USA 85, 5468 (1988); ANSORGE, S. and SCH ⁇ N, E., Histochem. 82, 41 (1987)].
  • proline determines both the conformation and the stability of these peptides due to its special structure, by protecting against degradation by unspecific proteases [KESSLER, H., Conformation and biological action of cyclic peptides. Appl. Chem. 94, 509 (1982)].
  • Enzymes on the other hand, which have a highly specific structure-changing effect on sequences containing proline (HIV protease, cyclophylin, etc.) are attractive targets of current drug research.
  • PEP prolin endopeptidase
  • DP IV Dipeptidyl peptidase IV
  • alanine-containing peptides Similar to the extraordinary proline specificity of these enzymes, their high selectivity for the amino acid alanine is discussed within typical recognition regions in substrates of these enzymes, according to which alanine-containing peptides can adopt similar conformations as structure-analogous proline-containing peptides.
  • Such properties of alanine-containing peptide chains have recently been demonstrated by point mutation (exchange of proline for alanine) [DODGE, R.W. and SCHERAGA, H.A., Folding and unfolding kinetics of the proline-to-alanine mutants of bovine pancreatic ribonuclease A. Biochemistry 35 (5) 1548 (1996)].
  • DP IV- or DP IV-analogous activity occurs in the bloodstream, where it releases highly specific dipeptides from the N-terminus of biologically active peptides when proline or alanine represent the adjacent residues of the N-terminal amino acid in their sequence. It is therefore assumed that this enzyme is involved in the regulation of polypeptides in vivo [VANHOOF, G., GOOSSENS, F., DE MEESTER, I., HENDRIKS, D. and SCH ⁇ RPE, S., Prolinc motifs and their biological processing , FASEB Journal 9, 736 (1995)].
  • the glucose-dependent insulinotropic polypeptides Gastric Inhibitory Polypeptides 1-42 (GIP, .42 ) and Glucagon-Like Peptide Amide-1 7-36 (GLP-1 7. 36 ), hormones that stimulate the glucose-induced insulin secretion of the pancreas (also incretins) are substrates of the DP IV, since they can split off the dipeptides tyrosinyl-alanine or histidyl-alanine from the N-terminal sequences of these peptides in vitro and in situ [MENTLEIN, R., GALLWITZ, B., and SCHMIDT, WE, Dipeptidyl Peptidase IV hydrolyzes gastric inhibitory polypeptide, glucagon-like peptide-1 (7-36) amide, peptide histidine methionine and is responsible for their degradation in human serum. Eur. J. Biochem. 214, 829 (1993)].
  • GIP Gastric Inhibitory Polypeptide
  • diabetes mellitus type II is based on reduced insulin secretion or disorders in the receptor function, which are due, among other things, to proteolytically caused concentration anomalies of the incretin [BROWN, 3.C., DAHL, M., KWAWK, S. , MCINTOSH, CHS, OTTE, SC and PEDERSON, RA Peptides 2, 241 (1981); SCHMIDT, WE, SIEGEL, EG, GALLWITZ, B. KÜMMEL, H., EBERT, R. and CREUTZFELDT, W., Characterization of the inulinotropic activity of fragments derived from gastric inhibitory polypeptides.
  • proteolytically caused concentration anomalies of the incretin [BROWN, 3.C., DAHL, M., KWAWK, S. , MCINTOSH, CHS, OTTE, SC and PEDERSON, RA Peptides 2, 241 (1981); SCHMIDT, WE, SIEGEL,
  • hyperglycaemia and the associated causes or sequelae are treated in various dosage forms by administering insulin (e.g. material isolated from bovine pancreas or genetically derived material) to diseased organisms.
  • insulin e.g. material isolated from bovine pancreas or genetically derived material
  • All of the previously known, as well as the more modern procedures are characterized by high material costs, high costs and often by decisive impairments of the quality of life of the patients.
  • the classic method (daily IV insulin injection, common since the 1930s) treats the acute symptoms of the disease, but leads to prolonged use and a. on severe vascular changes (arteriosclerosis) and nerve damage [LACY, P., Status of Islet Cell Transplantation. Diabetes Care 16 (3) 76 (1993)].
  • the aim of the invention is a simple and novel method for lowering the blood glucose level, which according to the invention can be achieved in that the endogenous (or additionally exogenously administered) insulinotropic peptides GIP M2 and GLP are administered causally to an mammalian organism -l 7 .
  • Will be degraded is reduced 3f (oa GLP 1 to 7. 37 or its analogues) by DP IV or DP IV-like enzymes, thus reducing the concentration of those Pepdidhormone or its analogues or the siege verzö ⁇ .
  • the invention is based on the surprising finding that a reduction in the DP IV- or DP IV-like enzymatic activity acting in the blood circulation has a causal effect on the blood sugar level. It has been found that 1. the reduction of DP IV or DP IV analog activity leads to a relative increase in stability of the glucose-stimulated or externally supplied incretins (or their analogs), i.e. the incretin breakdown in the blood can be controlled by applying effectors of the DP IV or DP IV analog proteins.
  • the invention thus relates to the use of effectors of dipeptidyl peptidase VI (DP IV) or DP IV-analogous enzyme activity.
  • DP IV dipeptidyl peptidase VI
  • DP IV-analogous enzyme activity To lower the blood sugar level below the glucose concentration in the serum of a mammalian organism, which is characteristic of hyperglycaemia.
  • the invention relates to the use of effectors of DP IV- or DP IV-analogous enzyme activity in mammals to prevent or alleviate pathological metabolic abnormalities of mammalian organisms selected from glucosuria, hyperlipidemia, metabolic acidosis and diabetes mellitus.
  • the invention relates to a method for lowering the blood sugar level below the glucose concentration in the serum of a mammalian organism which is characteristic of hyperglycaemia, which is characterized in that a therapeutically effective amount of an effect of DP is given to a mammalian organism IV or DP IV-analog enzyme activity administered.
  • the invention relates to effectors of DP IV or DP IV analog enzyme activity for use in a method for lowering the blood sugar level below the glucose concentration in the serum of a mammalian organism which is characteristic of hyperglycaemia.
  • effectors of the DP IV- or DP IV-analogous enzymes applied according to the invention can be used in pharmaceutically usable formulation complexes as inhibitors, substrates, pseudo-substrates, inhibitors of DP IV expression, binding proteins or antibodies of these enzyme proteins or combinations of these different substances, the DP Reduce IV or DP IV analog protein concentration in the mammalian organism.
  • Effectors according to the invention are, for example, DP IV inhibitors such as the dipeptide derivatives or dipeptide mimetics alanyl pyrolidide, isoleucyl thiazolidide and the pseudosubstrate N-valyl prolyl, O-benzoyl hydroxylamine.
  • the method according to the invention represents a novel approach for lowering increased blood glucose concentration in the serum of mammals. It is simple, commercially usable and suitable for use in therapy, in particular of diseases which are based on above-average blood glucose values, in human medicine.
  • the effectors are administered in the form of pharmaceutical preparations containing the active ingredient in combination with customary carrier materials known from the prior art.
  • customary carrier materials known from the prior art.
  • they are applied parenterally (e.g. IV, in physiological saline) or enterally (e.g. orally, formulated with common carrier materials such as glucose).
  • the effectors have to be administered one or more times in order to achieve the desired normalization of the blood glucose values.
  • a dose range can be between 1.0 mg and 10.0 mg effector substance per kilogram.
  • Example 1 Inhibition of the DP IV -catalyzed hydrolysis of the incretins GIP ⁇ 2 and GLP-I7.se in situ
  • incubation of 30 ⁇ M GIP, .42 or 30 ⁇ M GLP-1 7 is achieved in situ.
  • Synthetic GIP,. 42 (5 ⁇ M) and synthetic GLP-1 7.
  • 36 (15 ⁇ M) were treated with human serum (20%) in 0.1 mM TRICINE buffer at pH 7.6 and 30 ° C.
  • Example 2 Inhibition of the degradation of GLP-I ⁇ . ⁇ by the DP IV inhibitor isoleucyl-thiazolidide in vivo.
  • Example 3 Modulation of the insulin effect and lowering of the blood glucose level after i. v. Application of the DP IV inhibitor isoleuzyl thiazolidide in vivo.
  • Figure 3 illustrates these relationships in the inhibitor-dependent changes in plasma parameters: A - DP IV activity, B - plasma insulin levels, C - blood glucose levels.
  • the test group also received an infusion of the inhibitor of 0.75 ⁇ M / min over a test period of 30 minutes (*).
  • the control group was infused with an inhibitor-free 0.9% saline solution in the same period.
  • the animals were given a glucose dose of lg / kg 40% dextrose solution (w / v).
  • Blood samples were taken at ten minute intervals from all test animals. Glucose measurements were performed on whole blood (Lifescan One Touch II analyzer) while the DP IV activity and the insulin concentrations in the plasma were determined.
  • the insulin test used here is sensitive between 10 and 160 mU / ml [PEDERSON, R.A., BUCHAN, A.M.J., ZAHEDI-ASH, S., CHEN, C.B. & BROWN, J.C. Reg. Peptides. 3, 53-63 (1982)].
  • the DP IV activity was determined spectrophotometrically [DEMUTH, H.-U. and HEINS, J., On the catalytic Mechanism of Dipeptidyl Peptidase IV. in Dipeptidyl Peptides IV (CD 26) in Metabolism and the Immune Response (B. Fleischer, Ed.) R.G. Landes, Biomedical Publishers. Georgetown, 1-35 (1995)]. All measured values are given as mean values with standard deviation.

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  • Health & Medical Sciences (AREA)
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  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Peptides Or Proteins (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
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PCT/DE1997/000820 1996-04-25 1997-04-24 Verwendung von dipeptidyl peptidase iv effektoren zur senkung des blutglukosespiegels in säugern Ceased WO1997040832A1 (de)

Priority Applications (21)

Application Number Priority Date Filing Date Title
KR1020117031497A KR20120014064A (ko) 1996-04-25 1997-04-24 포유류에서 혈당을 낮추는데 효과가 있는 이가펩티드성 펩티다제의 활성억제제의 용도
AT97924866T ATE202705T1 (de) 1996-04-25 1997-04-24 Verwendung von aktivitätsmindernden effektoren der dipeptidyl peptidase iv zur senkung des blutglukosespiegels in säugern
CA002252576A CA2252576C (en) 1996-04-25 1997-04-24 Use of dipeptidyl peptidase iv inhibitors for lowering the blood glucose level in mammals
EP97924866A EP0896538B1 (de) 1996-04-25 1997-04-24 Verwendung von aktivitätsmindernden effektoren der dipeptidyl peptidase iv zur senkung des blutglukosespiegels in säugern
HK99104351.7A HK1019204B (en) 1996-04-25 1997-04-24 Use of dipeptidyl peptidase iv inhibitors for lowering the blood glucose level in mammals
JP53845397A JP2001510442A (ja) 1996-04-25 1997-04-24 哺乳動物の血糖値低下のためのジペプチジルペプチダーゼ▲ｉｖ▼エフェクターの使用
DE200712000038 DE122007000038I1 (de) 1996-04-25 1997-04-24 Verwendung von Aktivit{tsmindernden Effektoren derDipeptidyl Peptidase IV zur Senkung des Blutglukosespiegels in S{ugern
DK97924866T DK0896538T3 (da) 1996-04-25 1997-04-24 Anvendelse af aktivitetsformindskende effektorer for dipeptidylpeptidase IV til sænkning af blodglucoseniveauet hos pattedyr
US09/155,833 US6303661B1 (en) 1996-04-25 1997-04-24 Use of dipeptidyl peptidase IV effectors for lowering the blood glucose level in mammals
DE59703959T DE59703959D1 (de) 1996-04-25 1997-04-24 Verwendung von aktivitätsmindernden effektoren der dipeptidyl peptidase iv zur senkung des blutglukosespiegels in säugern
AU30233/97A AU721477C (en) 1996-04-25 1997-04-24 The use of dipeptidyl peptidase IV effectors for lowering blood glucose levels in mammals
DE122007000083C DE122007000083I1 (de) 1996-04-25 1997-04-24 Verwendung von aktivitätsmindernden effektoren der dipeptidyl peptidase iv zur senkung des blutglukosespiegels in säuger
KR1019980707018A KR100617676B1 (ko) 1996-04-25 1997-04-24 포유류에서 혈당을 낮추는 데 효과가 있는 이가펩티드성 펩티다아제의 활성 억제제의 용도
NZ332707A NZ332707A (en) 1996-04-25 1997-04-24 Use of dipeptidyl peptidase iv inhibitors (dpiv) for lowering the blood glucose level in mammals
GR20010401649T GR3036788T3 (en) 1996-04-25 2001-10-03 Use of dipeptidyl peptidase iv inhibitors for lowering the blood glucose level in mammals
LU91334C LU91334I2 (fr) 1996-04-25 2007-04-18 Sitagliptin, ou un sel de celui-ci pharmaceutiquement acceptable, en particulier le sel phosphate (JANUVIA)
NL300280C NL300280I2 (nl) 1996-04-25 2007-04-25 Toepassing van activiteitsverminderende dipeptidylpeptidase IV-effectoren voor het verlagen van glucosespiegel van het bloed by zoogdieren.
NL300308C NL300308I2 (nl) 1996-04-25 2007-12-03 Toepassing van activiteits verminderende dipeptidylpeptidase
LU91382C LU91382I2 (fr) 1996-04-25 2007-12-05 Vildagliptine ou un de ses sels pharmaceutiquementacceptables - GALVUS
US13/458,484 US20130116290A1 (en) 1996-04-25 2012-04-27 Use of Dipeptidyl Peptidase IV Effectors for Normalizing the Blood Glucose Level in Mammals
US15/042,892 US20170007582A1 (en) 1996-04-25 2016-02-12 Use of Dipeptidyl Peptidase IV Effectors for Normalizing the Blood Glucose Level in Mammals

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19616486.9A DE19616486C5 (de) 1996-04-25 1996-04-25 Verfahren zur Senkung des Blutglukosespiegels in Säugern
DE19616486.9 1996-04-25

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US09/155,833 A-371-Of-International US6303661B1 (en) 1996-04-25 1997-04-24 Use of dipeptidyl peptidase IV effectors for lowering the blood glucose level in mammals
US09/932,546 Continuation-In-Part US20020006899A1 (en) 1996-04-25 2001-08-17 Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals

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WO1997040832A1 true WO1997040832A1 (de) 1997-11-06

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PCT/DE1997/000820 Ceased WO1997040832A1 (de) 1996-04-25 1997-04-24 Verwendung von dipeptidyl peptidase iv effektoren zur senkung des blutglukosespiegels in säugern

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US (1) US6303661B1 (enExample)
EP (3) EP1084705B1 (enExample)
JP (3) JP2001510442A (enExample)
KR (5) KR100617676B1 (enExample)
CN (2) CN1132578C (enExample)
AT (1) ATE202705T1 (enExample)
AU (1) AU721477C (enExample)
CA (1) CA2252576C (enExample)
DE (5) DE19616486C5 (enExample)
DK (2) DK1084705T3 (enExample)
ES (2) ES2158562T3 (enExample)
FR (1) FR14C0089I1 (enExample)
GR (1) GR3036788T3 (enExample)
LT (3) LTPA2014045I1 (enExample)
LU (7) LU91334I2 (enExample)
NL (2) NL300280I2 (enExample)
NZ (1) NZ332707A (enExample)
PT (2) PT1084705E (enExample)
RU (1) RU2189233C2 (enExample)
SI (1) SI1084705T1 (enExample)
WO (1) WO1997040832A1 (enExample)

Cited By (123)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999025719A1 (en) * 1997-11-18 1999-05-27 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Novel physiologically active substance sulphostin, process for producing the same, and use thereof
WO1999061431A1 (de) * 1998-05-28 1999-12-02 Probiodrug Gesellschaft für Arzneimittelforschung mbH Neue effektoren von dipeptidylpeptidase iv
WO1999038501A3 (en) * 1998-02-02 2000-01-13 Tufts College Method of regulating glucose metabolism, and reagents related thereto
EP0995440A1 (de) * 1998-07-31 2000-04-26 Probiodrug Gesellschaft für Arzneimittelforschung mbH Verfahren zur Stiegerung des Blutglukosespiegels in Säugern
US6303661B1 (en) 1996-04-25 2001-10-16 Probiodrug Use of dipeptidyl peptidase IV effectors for lowering the blood glucose level in mammals
WO2001040180A3 (en) * 1999-11-30 2001-11-08 Ferring Bv N-substituted 2-cyanopyrrolidines and their use as antidiabetic agents
WO2001062266A3 (en) * 2000-02-25 2002-05-02 Novo Nordisk As Use of dpp-iv inhibitors for the treatment of diabetes
US6395767B2 (en) 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
WO2002083109A1 (en) * 2001-04-11 2002-10-24 Ferring Bv Treatment of type 2 diabetes with inhibitors of dipeptidyl peptidase iv
US6500804B2 (en) 2000-03-31 2002-12-31 Probiodrug Ag Method for the improvement of islet signaling in diabetes mellitus and for its prevention
WO2003004498A1 (en) * 2001-07-06 2003-01-16 Merck & Co., Inc. Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2003015775A1 (en) * 2001-08-17 2003-02-27 Probiodrug Ag New dipeptidyl peptidase iv inhibitors and their uses for lowering blood pressure levels
WO2003033524A2 (en) 2001-10-12 2003-04-24 Probiodrug Ag Peptidyl ketones as inhibitors of dpiv
US6559314B2 (en) 1999-06-10 2003-05-06 Probiodrug Ag Method for the production of thiazolidin
EP1270562A3 (fr) * 2001-06-18 2003-05-07 Les Laboratoires Servier Nouveaux dérivés cycliques d'alpha-amino-gamma-hydroxy-amides, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent
US6710040B1 (en) 2002-06-04 2004-03-23 Pfizer Inc. Fluorinated cyclic amides as dipeptidyl peptidase IV inhibitors
WO2004098591A2 (en) 2003-05-05 2004-11-18 Probiodrug Ag Inhibitors of glutaminyl cyclase and their use in the treatment of neurological diseases
WO2004098625A2 (en) 2003-05-05 2004-11-18 Probiodrug Ag Medical use of inhibitors of glutaminyl and glutamate cyclases
EP1228061A4 (en) * 1999-11-12 2004-12-15 Guilford Pharm Inc DIPEPTIDYL PEPTIDASE IV INHIBITORS; METHODS OF MANUFACTURE AND USE OF SAID INHIBITORS
US6844316B2 (en) 2001-09-06 2005-01-18 Probiodrug Ag Inhibitors of dipeptidyl peptidase I
US6890905B2 (en) 2001-04-02 2005-05-10 Prosidion Limited Methods for improving islet signaling in diabetes mellitus and for its prevention
WO2005075436A2 (en) 2004-02-05 2005-08-18 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
US6946480B2 (en) 2002-02-28 2005-09-20 Hans-Ulrich Demuth Glutaminyl based DPIV inhibitors
US6949515B2 (en) 1999-08-24 2005-09-27 Probiodrug Ag Effectors of dipeptidyl peptidase IV for topical use
EP1598341A1 (en) * 2004-05-21 2005-11-23 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
EP1604980A1 (en) * 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
EP1604989A1 (en) * 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
US6979697B1 (en) 1998-08-21 2005-12-27 Point Therapeutics, Inc. Regulation of substrate activity
US7026316B2 (en) 2001-03-27 2006-04-11 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7053055B2 (en) 1998-06-24 2006-05-30 Prosidion Ltd. Compounds of unstable DP IV-inhibitors
US7074798B2 (en) 2002-02-25 2006-07-11 Eisai Co., Ltd Xanthine derivative and DPPIV inhibitor
US7084120B2 (en) 1998-06-24 2006-08-01 Probiodrug Ag Prodrugs of DP IV-inhibitors
US7098239B2 (en) 2001-06-20 2006-08-29 Merck & Co., Inc Dipeptidyl peptidase inhibitors for the treatment of diabetes
US7101871B2 (en) 2002-10-18 2006-09-05 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7109347B2 (en) 2001-06-27 2006-09-19 Probiodrug Ag Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
US7132104B1 (en) 2000-10-27 2006-11-07 Probiodrug Ag Modulation of central nervous system (CNS) dipeptidyl peptidase IV (DPIV) -like activity for the treatment of neurological and neuropsychological disorders
US7132443B2 (en) 2001-06-27 2006-11-07 Smithklinebeecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
US7157490B2 (en) 2002-11-07 2007-01-02 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7205323B2 (en) 2004-10-12 2007-04-17 Glenmark Pharmaceuticals S.A. Dipeptidyl peptidase IV inhibitors pharmaceutical compositions containing them, and process for their preparation
US7208498B2 (en) 2002-07-15 2007-04-24 Merck & Co., Inc. Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
US7230002B2 (en) 2004-02-03 2007-06-12 Glenmark Pharmaceuticals Ltd. Dipeptidyl peptidase IV inhibitors; processes for their preparation and compositions thereof
WO2007072083A1 (en) 2005-12-23 2007-06-28 Prosidion Limited Treatment of type 2 diabetes with a combination of dpiv inhibitor and metformin or thiazolidinedione
US7253172B2 (en) 2001-06-20 2007-08-07 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
US7259160B2 (en) 2003-07-31 2007-08-21 Merck & Co., Inc. Hexahydrodiazepinones as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
US7262207B2 (en) 2002-09-19 2007-08-28 Abbott Laboratories Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
EP1583534A4 (en) * 2002-12-20 2007-08-29 Merck & Co Inc 3-AMINO-4-PHENYLBUTANIC ACID DERIVATIVES AS DIPEPTIDYL-PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
US7265128B2 (en) 2003-01-17 2007-09-04 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7276371B2 (en) 1997-09-29 2007-10-02 Point Therapeutics, Inc. Stimulation of hematopoietic cells in vitro
US7332520B2 (en) 2003-06-06 2008-02-19 Merck & Co., Inc. Fused indoles as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
EP1891948A1 (en) 2000-10-27 2008-02-27 Probiodrug AG Treatment of neurological and neuropsychological disorders
US7345180B2 (en) 2003-01-31 2008-03-18 Sanwa Kagaku Kenkyusho Co., Ltd. Compound inhibiting dipeptidyl peptidase IV
US7368421B2 (en) 2001-06-27 2008-05-06 Probiodrug Ag Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis
WO2008055945A1 (en) 2006-11-09 2008-05-15 Probiodrug Ag 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
US7381537B2 (en) 2003-05-05 2008-06-03 Probiodrug Ag Use of inhibitors of glutaminyl cyclases for treatment and prevention of disease
WO2008065141A1 (en) 2006-11-30 2008-06-05 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
US7388019B2 (en) 2003-01-31 2008-06-17 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7390809B2 (en) 2002-10-07 2008-06-24 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for diabetes
WO2008120813A1 (ja) 2007-04-03 2008-10-09 Mitsubishi Tanabe Pharma Corporation ジペプチジルペプチダーゼ４阻害化合物と甘味料との併用
US7456204B2 (en) 2003-06-17 2008-11-25 Merck & Co., Inc. Cyclohexylglycine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7470699B2 (en) 2003-07-11 2008-12-30 Arena Pharmaceuticals, Inc. Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
US7470700B2 (en) 2003-08-13 2008-12-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7550590B2 (en) 2003-03-25 2009-06-23 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7560455B2 (en) 2003-05-14 2009-07-14 Merck & Co., Inc. 3-Amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
EP2116235A1 (en) 2005-01-10 2009-11-11 Arena Pharmaceuticals, Inc. Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood GLP-1 level
US7625939B2 (en) 2005-11-14 2009-12-01 Probiodrug Ag Cyclopropyl-fused pyrrolidine derivatives as dipeptidyl peptidase IV inhibitors
US7638638B2 (en) 2003-05-14 2009-12-29 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
US7671073B2 (en) 2004-05-18 2010-03-02 Merck Sharp & Dohme Corp. Cyclohexylalanine derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
US7687492B2 (en) 2004-05-04 2010-03-30 Merck Sharp & Dohme Corp. 1,2,4-Oxadiazole derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
US7728146B2 (en) 2006-04-12 2010-06-01 Probiodrug Ag Enzyme inhibitors
US7727964B2 (en) 2001-11-26 2010-06-01 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
US7820666B2 (en) 2007-05-08 2010-10-26 Concert Pharmaceuticals, Inc. Tetrahydrotriazolopyrazine derivatives and uses thereof
AU2007202745B2 (en) * 1998-02-02 2010-11-18 1149336 Ontario, Inc. Method of regulating glucose metabolism, and reagents related thereto
EP2253311A2 (en) 2006-04-11 2010-11-24 Arena Pharmaceuticals, Inc. Use of GPR119 receptor agonists for increasing bone mass and for treating osteoporosis, as well as combination therapy relating thereto
WO2011005929A1 (en) 2009-07-09 2011-01-13 Arena Pharmaceuticals, Inc. Piperidine derivative and its use for the treatment of diabets and obesity
EP2289498A1 (en) 2003-10-15 2011-03-02 Probiodrug AG Use of inhibitors of glutaminyl clyclase
WO2011028455A1 (en) 2009-09-02 2011-03-10 Merck Sharp & Dohme Corp. Aminotetrahydropyrans as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2011029920A1 (en) 2009-09-11 2011-03-17 Probiodrug Ag Heterocylcic derivatives as inhibitors of glutaminyl cyclase
US7915427B2 (en) 2006-03-08 2011-03-29 Kyorin Pharmaceuticals Co., Ltd. Process for producing aminoacetyl pyrrolidine carbonitrile derivative and intermediate for production thereof
US7960384B2 (en) 2006-03-28 2011-06-14 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
EP2338490A2 (en) 2003-11-03 2011-06-29 Probiodrug AG Combinations Useful for the Treatment of Neuronal Disorders
EP2356997A1 (en) 2005-06-06 2011-08-17 Georgetown University Compositions and methods for lipo modeling
US8003790B2 (en) 2005-02-18 2011-08-23 Mitsubishi Tanabe Pharma Corporation Salt of proline derivative, solvate thereof, and production method thereof
WO2011103256A1 (en) 2010-02-22 2011-08-25 Merck Sharp & Dohme Corp. Substituted aminotetrahydrothiopyrans and derivatives thereof as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
WO2011107530A2 (en) 2010-03-03 2011-09-09 Probiodrug Ag Novel inhibitors
WO2011110613A1 (en) 2010-03-10 2011-09-15 Probiodrug Ag Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
WO2011127051A1 (en) 2010-04-06 2011-10-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
WO2011146358A1 (en) 2010-05-21 2011-11-24 Merck Sharp & Dohme Corp. Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
US8084605B2 (en) 2006-11-29 2011-12-27 Kelly Ron C Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
US8143427B2 (en) 2007-03-22 2012-03-27 Kyorin Pharmaceutical Co., Ltd. Method for producing aminoacetylpyrrolidinecarbonitrile derivative
WO2012040279A1 (en) 2010-09-22 2012-03-29 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012049566A1 (en) 2010-10-14 2012-04-19 Japan Tobacco Inc. Combination therapy for use in treating diabetes
US8222411B2 (en) 2005-09-16 2012-07-17 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2012123563A1 (en) 2011-03-16 2012-09-20 Probiodrug Ag Benz imidazole derivatives as inhibitors of glutaminyl cyclase
WO2012135570A1 (en) 2011-04-01 2012-10-04 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145361A1 (en) 2011-04-19 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145604A1 (en) 2011-04-22 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145603A1 (en) 2011-04-22 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012170702A1 (en) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US8404727B2 (en) 2009-01-07 2013-03-26 Glenmark Pharmaceuticals S.A. Pharmaceutical composition that includes a dipeptidyl peptidase-IV inhibitor
US8410053B2 (en) 2001-11-26 2013-04-02 Trustees Of Tufts College Methods for treating autoimmune disorders, and reagents related thereto
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2013122920A1 (en) 2012-02-17 2013-08-22 Merck Sharp & Dohme Corp. Dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
EP2676961A1 (en) 2008-11-13 2013-12-25 Merck Sharp & Dohme Corporation Combination drugs comprising aminotetrahydropyrans as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes
WO2014018350A1 (en) 2012-07-23 2014-01-30 Merck Sharp & Dohme Corp. Treating diabetes with dipeptidyl peptidase-iv inhibitors
WO2014061031A1 (en) 2012-10-17 2014-04-24 Cadila Healthcare Limited 2-phenyl-5-heterocyclyl-tetrahydro-2h-pyran-3-amine compounds for use in the treatment of diabetes and its associated disorders
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
WO2014113750A1 (en) 2013-01-18 2014-07-24 Dnj Pharma, Inc. Novel ddp-iv inhibitors
US8853385B2 (en) 2008-01-17 2014-10-07 Mitsubishi Tanabe Pharma Corporation Combination therapy comprising SGLT inhibitors and DPP4 inhibitors
US8883714B2 (en) 2008-04-07 2014-11-11 Arena Pharmaceuticals, Inc. Pharmaceutical compositions comprising GPR119 agonists which act as peptide YY (PYY) secretagogues
US8906901B2 (en) 2005-09-14 2014-12-09 Takeda Pharmaceutical Company Limited Administration of dipeptidyl peptidase inhibitors
US8933083B2 (en) 2003-01-14 2015-01-13 Arena Pharmaceuticals, Inc. 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
EP2865670A1 (en) 2007-04-18 2015-04-29 Probiodrug AG Thiourea derivatives as glutaminyl cyclase inhibitors
US9051329B2 (en) 2011-07-05 2015-06-09 Merck Sharp & Dohme Corp. Tricyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors
EP3424927A1 (en) 2017-07-04 2019-01-09 F.I.S.- Fabbrica Italiana Sintetici S.p.A. Efficient process for the preparation of sitagliptin through a very effective preparation of the intermediate 2,4,5-trifluorophenylacetic acid
EP3461819A1 (en) 2017-09-29 2019-04-03 Probiodrug AG Inhibitors of glutaminyl cyclase
EP3524605A1 (en) 2018-02-13 2019-08-14 F.I.S.- Fabbrica Italiana Sintetici S.p.A. New efficient process for the preparation of sitagliptin
US10555929B2 (en) 2015-03-09 2020-02-11 Coherus Biosciences, Inc. Methods for the treatment of nonalcoholic fatty liver disease and/or lipodystrophy
US11007175B2 (en) 2015-01-06 2021-05-18 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
US11253508B2 (en) 2017-04-03 2022-02-22 Coherus Biosciences, Inc. PPARy agonist for treatment of progressive supranuclear palsy
EP4000630A1 (en) 2014-09-03 2022-05-25 Invex Therapeutics Ltd Elevated intracranial pressure treatment
US11884626B2 (en) 2015-06-22 2024-01-30 Arena Pharmaceuticals, Inc. Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(Compound1) for use in S1P1 receptor-associated disorders
US12156866B2 (en) 2018-06-06 2024-12-03 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor

Families Citing this family (177)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6255772B1 (en) 1998-02-27 2001-07-03 Micron Technology, Inc. Large-area FED apparatus and method for making same
US20030176357A1 (en) * 1998-10-06 2003-09-18 Pospisilik Andrew J. Dipeptidyl peptidase IV inhibitors and their uses for lowering blood pressure levels
PT1171465E (pt) 1999-03-29 2004-12-31 Uutech Ltd Analogos de petido inibidor gastrico e sua utilizacao para o tratamento de diabetes
US20050272652A1 (en) * 1999-03-29 2005-12-08 Gault Victor A Peptide analogues of GIP for treatment of diabetes, insulin resistance and obesity
US6890904B1 (en) * 1999-05-25 2005-05-10 Point Therapeutics, Inc. Anti-tumor agents
SK8902002A3 (en) * 1999-12-23 2002-11-06 Novartis Ag Use of hypoglycemic agent for treating impaired glucose metabolism
US6380398B2 (en) 2000-01-04 2002-04-30 Novo Nordisk A/S Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV
ES2487897T3 (es) 2000-01-21 2014-08-25 Novartis Ag Combinaciones que consisten de inhibidores de la dipeptidilpeptidasa-IV y agentes antidiabéticos
AU2001228309A1 (en) * 2000-01-24 2001-08-07 Novo-Nordisk A/S N-substituted 2-cyanopyroles and -pyrrolines which are inhibitors of the enzyme dpp-iv
AR033390A1 (es) 2000-08-22 2003-12-17 Novartis Ag Una composicion farmaceutica que comprende un antagonista del receptor at1 y un potenciador de la secrecion de insulina, el uso de dicha composicion para la fabricacion de un medicamento y un kit de partes
KR20030096227A (ko) * 2000-10-27 2003-12-24 프로비오드룩 아게 신경 및 신경정신 질환의 치료방법
SK288222B6 (sk) * 2000-12-14 2014-09-04 Ortho-Mcneil Pharmaceutical, Inc. Steroidné hormonálne prípravky a spôsoby ich prípravy
US20040180925A1 (en) * 2000-12-27 2004-09-16 Kenji Matsuno Dipeptidylpeptidase-IV inhibitor
DE10100053A1 (de) * 2001-01-02 2002-08-22 Keyneurotek Ag I G Verwendung von Enzyminhibitoren der Dipeptidylpeptidase IV sowie der Aminopeptidase N und pharmazeutischen Zubereitungen daraus zur Prävention und/oder Therapie Ischämie-bedingter akuter und chronischer neurodegenerativer Prozesse und Erkrankungen
SK286975B6 (sk) * 2001-02-24 2009-08-06 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xantínové deriváty, spôsob ich výroby, farmaceutický prostriedok s ich obsahom a ich použitie
US20030060494A1 (en) * 2001-05-18 2003-03-27 Nobuyuki Yasuda Pharmaceutical use of N-carbamoylazole derivatives
CA2419888A1 (en) * 2001-06-27 2003-01-09 Probiodrug Ag Peptide structures useful for competitive modulation of dipeptidyl peptidase iv catalysis
JP2005504766A (ja) * 2001-08-16 2005-02-17 プロバイオドラッグ アーゲー プロリンエンドペプチダーゼ阻害剤の、細胞内シグナルカスケード依存性イノシトール（１，４，５）トリホスフェート濃度調節への使用。
US6861440B2 (en) 2001-10-26 2005-03-01 Hoffmann-La Roche Inc. DPP IV inhibitors
AU2002349513B2 (en) * 2001-11-26 2007-10-18 Asubio Pharma Co., Ltd. Medicinal compositions for nasal absorption
DE60302336T2 (de) 2002-02-13 2006-08-03 F. Hoffmann-La Roche Ag Neue pyridin- und quinolin-derivate
RU2293731C2 (ru) 2002-02-13 2007-02-20 Ф.Хоффманн-Ля Рош Аг Производные пиридина и пиримидина, способы их получения (варианты), фармацевтическая композиция и применение
GB0205693D0 (en) * 2002-03-09 2002-04-24 Astrazeneca Ab Chemical compounds
DE10211555A1 (de) * 2002-03-15 2003-10-02 Imtm Inst Fuer Medizintechnolo Verwendung der Inhibitoren von Enzymen mit Aktivitäten der Aminopeptidase N und/oder der Dipeptidylpeptidase IV und pharmazeutischen Zubereitungen daraus zur Therapie und Prävention dermatologischer Erkrankungen mit sebozytärer Hyperproliferation und veränderten Differenzierungszuständen
ATE373660T1 (de) * 2002-03-25 2007-10-15 Merck & Co Inc Heterocyclische beta-aminoverbindungen als inhibitoren der dipeptidylpeptidase zur behandlung bzw. prävention von diabetes
US20030232761A1 (en) * 2002-03-28 2003-12-18 Hinke Simon A. Novel analogues of glucose-dependent insulinotropic polypeptide
JP2005532338A (ja) * 2002-06-03 2005-10-27 ノバルティス アクチエンゲゼルシャフト 高脂質血症および関連疾患の処置のための置換シアノピロリジンの使用およびそれらを含む組み合わせ製剤
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
US7495005B2 (en) * 2002-08-22 2009-02-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, their preparation and their use in pharmaceutical compositions
US7569574B2 (en) 2002-08-22 2009-08-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Purine derivatives, the preparation thereof and their use as pharmaceutical compositions
US20050176622A1 (en) * 2002-09-18 2005-08-11 Kerstin Kuhn-Wache Secondary binding site of dipeptidyl peptidase IV (DPIV)
US20040058876A1 (en) * 2002-09-18 2004-03-25 Torsten Hoffmann Secondary binding site of dipeptidyl peptidase IV (DP IV)
US20060094722A1 (en) * 2002-09-26 2006-05-04 Eisai Co., Ltd. Combination drug
US7482337B2 (en) * 2002-11-08 2009-01-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
DE10254304A1 (de) * 2002-11-21 2004-06-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
AU2003297564A1 (en) * 2002-12-04 2004-06-23 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7566707B2 (en) 2003-06-18 2009-07-28 Boehringer Ingelheim International Gmbh Imidazopyridazinone and imidazopyridone derivatives, the preparation thereof and their use as pharmaceutical compositions
RU2339636C2 (ru) 2003-06-20 2008-11-27 Ф.Хоффманн-Ля Рош Аг Гексагидропиридоизохинолины в качестве ингибиторов дипептидилпептидазы iv (dpp-iv)
BRPI0411713B8 (pt) 2003-06-20 2021-05-25 Hoffmann La Roche compostos, processo para a sua manufatura, composições farmacêuticas que compreendem os mesmos, método para tratamento e/ou profilaxia de enfermidades que estão associadas com dpp-iv e sua utilização
AU2004261319B2 (en) * 2003-07-25 2010-12-23 Conjuchem Biotechnologies Inc. Long lasting insulin derivatives and methods thereof
US7169926B1 (en) 2003-08-13 2007-01-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7678909B1 (en) 2003-08-13 2010-03-16 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2005026148A1 (en) 2003-09-08 2005-03-24 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
WO2005041926A1 (en) * 2003-10-31 2005-05-12 Alza Corporation Compositions and dosage forms for enhanced absorption of 3-amino-n-butyl-phosphinic acid
US20100099721A1 (en) * 2003-11-03 2010-04-22 Probiodrug Ag Novel compounds for the treatment of neurological disorders
US20050171112A1 (en) * 2003-11-03 2005-08-04 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
JP2007510651A (ja) * 2003-11-04 2007-04-26 メルク　エンド　カムパニー　インコーポレーテッド 糖尿病の治療又は予防のためのジペプチジルペプチダーゼ−ｉｖ阻害剤としての縮合フェニルアラニン誘導体
US7767828B2 (en) 2003-11-12 2010-08-03 Phenomix Corporation Methyl and ethyl substituted pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
US7317109B2 (en) 2003-11-12 2008-01-08 Phenomix Corporation Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
US7576121B2 (en) 2003-11-12 2009-08-18 Phenomix Corporation Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
DK1689757T3 (en) 2003-11-12 2014-12-08 Sino Med Internat Alliance Inc HETEROCYCLIC DRY ACID COMPOUNDS
KR20120008093A (ko) 2003-11-17 2012-01-25 노파르티스 아게 디펩티딜 펩티다제 ⅳ 억제제의 용도
DE10355304A1 (de) * 2003-11-27 2005-06-23 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 8-(Piperazin-1-yl)-und 8-([1,4]Diazepan-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
ES2684325T5 (es) 2004-01-20 2024-06-10 Novartis Ag Formulación y proceso de compresión directa
CN101684089A (zh) * 2004-02-05 2010-03-31 杏林制药株式会社 双环酯类衍生物
US7501426B2 (en) * 2004-02-18 2009-03-10 Boehringer Ingelheim International Gmbh 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
DE102004009039A1 (de) * 2004-02-23 2005-09-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-[3-Amino-piperidin-1-yl]-xanthine, deren Herstellung und Verwendung als Arzneimittel
EP1593671A1 (en) * 2004-03-05 2005-11-09 Graffinity Pharmaceuticals AG DPP-IV inhibitors
US7732446B1 (en) 2004-03-11 2010-06-08 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7393847B2 (en) 2004-03-13 2008-07-01 Boehringer Ingleheim International Gmbh Imidazopyridazinediones, their preparation and their use as pharmaceutical compositions
CN102127057A (zh) 2004-03-15 2011-07-20 武田药品工业株式会社 二肽基肽酶抑制剂
US7179809B2 (en) * 2004-04-10 2007-02-20 Boehringer Ingelheim International Gmbh 2-Amino-imidazo[4,5-d]pyridazin-4-ones, their preparation and their use as pharmaceutical compositions
US7439370B2 (en) * 2004-05-10 2008-10-21 Boehringer Ingelheim International Gmbh Imidazole derivatives, their preparation and their use as intermediates for the preparation of pharmaceutical compositions and pesticides
WO2005118555A1 (en) 2004-06-04 2005-12-15 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
DE102004030502A1 (de) * 2004-06-24 2006-01-12 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Imidazole und Triazole, deren Herstellung und Verwendung als Arzneimittel
WO2006019965A2 (en) 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
AU2005267093B2 (en) * 2004-07-23 2009-10-01 Nuada Llc Peptidase inhibitors
EP1623983A1 (en) * 2004-08-05 2006-02-08 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft Heterocyclic compounds useful as DPP-IV inhibitors
DE102004043944A1 (de) * 2004-09-11 2006-03-30 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 8-(3-Amino-piperidin-1-yl)-7-(but-2-inyl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
DE102004044221A1 (de) * 2004-09-14 2006-03-16 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 3-Methyl-7-butinyl-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
US20060063719A1 (en) * 2004-09-21 2006-03-23 Point Therapeutics, Inc. Methods for treating diabetes
DE102004054054A1 (de) * 2004-11-05 2006-05-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine
WO2006058628A2 (en) * 2004-11-30 2006-06-08 F.Hoffmann-La Roche Ag Substituted benzoquinolizines as dpp-iv inhibitors for the treatment of diabetes
US7411093B2 (en) 2004-12-20 2008-08-12 Hoffman-La Roche Inc. Aminocycloalkanes as DPP-IV inhibitors
BRPI0519585A2 (pt) * 2004-12-20 2009-02-25 Hoffmann La Roche compostos de fàrmula i; processo para a fabricaÇço de compostos de fàrmula i; composiÇÕes farmacÊuticas; mÉtodo para o tratamento e/ou profilaxia de doenÇas que estço associadas com a dpp-iv e usos destes compostos
EP1828192B1 (en) 2004-12-21 2014-12-03 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2006086769A2 (en) 2005-02-11 2006-08-17 Amylin Pharmaceuticals, Inc. Gip analog and hybrid polypeptides with selectable properties
US8263545B2 (en) 2005-02-11 2012-09-11 Amylin Pharmaceuticals, Inc. GIP analog and hybrid polypeptides with selectable properties
KR20080000665A (ko) 2005-04-22 2008-01-02 알란토스 파마슈티컬즈 홀딩, 인코포레이티드 디펩티딜 펩티다아제-ⅳ 억제제
CN101175494B (zh) * 2005-04-26 2011-07-13 田边三菱制药株式会社 用于糖/脂质代谢异常的预防/治疗剂
US7521557B2 (en) * 2005-05-20 2009-04-21 Bristol-Myers Squibb Company Pyrrolopyridine-based inhibitors of dipeptidyl peptidase IV and methods
US7825139B2 (en) 2005-05-25 2010-11-02 Forest Laboratories Holdings Limited (BM) Compounds and methods for selective inhibition of dipeptidyl peptidase-IV
DE102005035891A1 (de) 2005-07-30 2007-02-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
GT200600381A (es) 2005-08-25 2007-03-28 Compuestos organicos
EP1943274A2 (en) * 2005-09-08 2008-07-16 Uutech Limited Treatment of diabetes related obesity
WO2007028632A2 (en) * 2005-09-08 2007-03-15 Uutech Limited Analogs of gastric inhibitory polypeptide as a treatment for age related decreased pancreatic beta cell function
DE102005054994B4 (de) * 2005-11-18 2015-02-12 Bader Gmbh & Co. Kg Verkleidungsanordnung, insbesondere Maschinenverkleidung, mit einer Schiebetür und Führungsanordnung hierfür
DE602007010420D1 (de) 2006-04-11 2010-12-23 Arena Pharm Inc Verfahren zur verwendung des gpr119-rezeptors zur identifizierung von verbindungen zur erhöhung der knochenmasse bei einer person
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
BRPI0711558A2 (pt) 2006-05-04 2011-11-08 Boeringer Ingelheim Internat Gmbh polimorfos
PE20080251A1 (es) 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
WO2008017670A1 (en) * 2006-08-08 2008-02-14 Boehringer Ingelheim International Gmbh Pyrrolo [3, 2 -d] pyrimidines as dpp-iv inhibitors for the treatment of diabetes mellitus
US8497240B2 (en) 2006-08-17 2013-07-30 Amylin Pharmaceuticals, Llc DPP-IV resistant GIP hybrid polypeptides with selectable properties
US8324383B2 (en) 2006-09-13 2012-12-04 Takeda Pharmaceutical Company Limited Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile
RS51965B (sr) * 2006-09-13 2012-02-29 Takeda Pharmaceutical Company Limited Upotreba 2-6-(3-amino-piperidin-1-il)-3-metil-2,4-diokso-3,4-dihidro-2h-pirimidin-1-ilmetil-4-fluoro-benzonitrila za lečenje dijabetesa, kancera, autoimunih poremećaja i hiv infekcije
US8217025B2 (en) * 2006-11-17 2012-07-10 Harbor Therapeutics, Inc. Drug screening and treatment methods
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
US20070172525A1 (en) * 2007-03-15 2007-07-26 Ramesh Sesha Anti-diabetic combinations
US20080064701A1 (en) * 2007-04-24 2008-03-13 Ramesh Sesha Anti-diabetic combinations
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
PE20090938A1 (es) * 2007-08-16 2009-08-08 Boehringer Ingelheim Int Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo
CA2696579C (en) * 2007-08-17 2017-01-24 Boehringer Ingelheim International Gmbh Purine derivatives for use in the treatment of fab-related diseases
US20090076013A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched sitagliptin
US8551524B2 (en) * 2008-03-14 2013-10-08 Iycus, Llc Anti-diabetic combinations
PE20091730A1 (es) 2008-04-03 2009-12-10 Boehringer Ingelheim Int Formulaciones que comprenden un inhibidor de dpp4
PE20100156A1 (es) * 2008-06-03 2010-02-23 Boehringer Ingelheim Int Tratamiento de nafld
EP2318411A2 (en) 2008-07-03 2011-05-11 Ratiopharm GmbH Crystalline salts of sitagliptin
KR20190016601A (ko) 2008-08-06 2019-02-18 베링거 인겔하임 인터내셔날 게엠베하 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
WO2010016584A1 (ja) * 2008-08-07 2010-02-11 杏林製薬株式会社 ビシクロ[２．２．２]オクチルアミン誘導体の製造方法
CA2733778A1 (en) * 2008-08-14 2010-02-18 Hiroshi Uchida Stabilized pharmaceutical composition
NZ604091A (en) * 2008-08-15 2014-08-29 Boehringer Ingelheim Int Purin derivatives for use in the treatment of fab-related diseases
BRPI0919288A2 (pt) 2008-09-10 2015-12-15 Boehring Ingelheim Internat Gmbh teriapia de combinação para tratamento de diabetes e condições relacionadas.
US20200155558A1 (en) 2018-11-20 2020-05-21 Boehringer Ingelheim International Gmbh Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug
CN102316872B (zh) 2008-11-26 2016-12-21 萨蒂奥根制药公司 治疗肥胖症和糖尿病的胆汁酸再循环抑制剂
EP2364161B1 (en) 2008-11-26 2020-03-11 Satiogen Pharmaceuticals, Inc. Compositions containing satiogens and methods of use
AU2009331471B2 (en) 2008-12-23 2015-09-03 Boehringer Ingelheim International Gmbh Salt forms of organic compound
AR074990A1 (es) 2009-01-07 2011-03-02 Boehringer Ingelheim Int Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina
PE20120017A1 (es) 2009-02-13 2012-02-12 Boehringer Ingelheim Int Composicion farmaceutica que comprende un inhibidor de sglt2, un inhibidor de dpp-iv, opcionalmente, un agente antidiabetico adicional, y sus usos
SG175925A1 (en) 2009-05-15 2011-12-29 Novartis Ag Aryl pyridine as aldosterone synthase inhibitors
AU2010247391A1 (en) 2009-05-15 2011-12-01 Novartis Ag Benzoxazolone derivatives as aldosterone synthase inhibitors
EP2435402B1 (en) 2009-05-28 2016-04-13 Novartis AG Substituted aminobutyric derivatives as neprilysin inhibitors
BRPI1011657A2 (pt) 2009-05-28 2019-04-16 Novartis Ag derivados aminopropiônicos substituídos como inibidores de neprilisina
JP5855568B2 (ja) 2009-09-15 2016-02-09 セルリアン・ファーマ・インコーポレイテッド 癌の治療法
WO2011061168A1 (en) 2009-11-17 2011-05-26 Novartis Ag Aryl-pyridine derivatives as aldosterone synthase inhibitors
JO2967B1 (en) 2009-11-20 2016-03-15 نوفارتس ايه جي Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors
EP2503888A4 (en) 2009-11-23 2015-07-29 Cerulean Pharma Inc POLYMERS ON CYCLODEXTRINBASIS FOR THERAPEUTIC ADMINISTRATION
PH12012501037A1 (en) 2009-11-27 2013-01-14 Boehringer Ingelheim Int Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin
US8575160B2 (en) 2009-11-30 2013-11-05 Novartis Ag Imidazole derivatives as aldosterone synthase inhibitors
WO2011090940A1 (en) 2010-01-19 2011-07-28 Cerulean Pharma Inc. Cyclodextrin-based polymers for therapeutic delivery
CA2797310C (en) 2010-05-05 2020-03-31 Boehringer Ingelheim International Gmbh Glp-1 receptor agonist and dpp-4 inhibitor combination therapy
EP3593802A3 (en) 2010-05-26 2020-03-25 Satiogen Pharmaceuticals, Inc. Bile acid recycling inhibitors and satiogens for treatment of diabetes, obesity, and inflammatory gastrointestinal conditions
EP2582709B1 (de) 2010-06-18 2018-01-24 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
KR20230051307A (ko) 2010-06-24 2023-04-17 베링거 인겔하임 인터내셔날 게엠베하 당뇨병 요법
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
US9034883B2 (en) 2010-11-15 2015-05-19 Boehringer Ingelheim International Gmbh Vasoprotective and cardioprotective antidiabetic therapy
US8877815B2 (en) 2010-11-16 2014-11-04 Novartis Ag Substituted carbamoylcycloalkyl acetic acid derivatives as NEP
US8673974B2 (en) 2010-11-16 2014-03-18 Novartis Ag Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors
UY33937A (es) 2011-03-07 2012-09-28 Boehringer Ingelheim Int Composiciones farmacéuticas que contienen inhibidores de dpp-4 y/o sglt-2 y metformina
ES2713566T3 (es) 2011-07-15 2019-05-22 Boehringer Ingelheim Int Derivado de quinazolina dimérico sustituido, su preparación y su uso en composiciones farmacéuticas para el tratamiento de la diabetes de tipo I y II
EP2760862B1 (en) 2011-09-27 2015-10-21 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
EA030839B1 (ru) 2011-10-28 2018-10-31 ЛУМЕНА ФАРМАСЬЮТИКАЛС ЭлЭлСи Ингибиторы рециклинга желчных кислот при лечении холестатических заболеваний печени у детей
WO2013063526A1 (en) 2011-10-28 2013-05-02 Lumena Pharmaceuticals, Inc. Bile acid recycling inhibitors for treatment of hypercholemia and cholestatic liver disease
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
US20130303462A1 (en) 2012-05-14 2013-11-14 Boehringer Ingelheim International Gmbh Use of a dpp-4 inhibitor in podocytes related disorders and/or nephrotic syndrome
EP4151218A1 (en) 2012-05-14 2023-03-22 Boehringer Ingelheim International GmbH Linagliptin, a xanthine derivative as dpp-4 inhibitor, for use in the treatment of sirs and/or sepsis
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
IN2015DN03795A (enExample) 2012-10-24 2015-10-02 Inserm Inst Nat De La Santé Et De La Rech Médicale
UY35144A (es) 2012-11-20 2014-06-30 Novartis Ag Miméticos lineales sintéticos de apelina para el tratamiento de insuficiencia cardiaca
SG11201506018PA (en) 2013-02-14 2015-08-28 Novartis Ag Substituted bisphenyl butanoic phosphonic acid derivatives as nep (neutral endopeptidase) inhibitors
SG11201600211XA (en) 2013-07-25 2016-02-26 Novartis Ag Cyclic polypeptides for the treatment of heart failure
TW201518323A (zh) 2013-07-25 2015-05-16 Novartis Ag 合成ａｐｅｌｉｎ多肽之生物結合物
US9902751B2 (en) 2013-12-30 2018-02-27 Mylan Laboratories Limited Process for the preparation of empagliflozin
EP3110449B1 (en) 2014-02-28 2023-06-28 Boehringer Ingelheim International GmbH Medical use of a dpp-4 inhibitor
DE102014018663A1 (de) 2014-12-13 2015-03-05 Heinz Kiefer Nachweis von vermehrungsfähigen Zellen zur Überprüfung von Arzneimittel-Wirkstoffangaben bei Zulassungsverfahren
AU2016209968B2 (en) 2015-01-23 2018-11-29 Novartis Ag Synthetic apelin fatty acid conjugates with improved half-life
WO2016151018A1 (en) 2015-03-24 2016-09-29 INSERM (Institut National de la Santé et de la Recherche Médicale) Method and pharmaceutical composition for use in the treatment of diabetes
MX2018007681A (es) 2015-12-28 2018-11-14 Wockhardt Ltd Composicion farmaceutica osmotica oral de vildagliptin.
US11013738B2 (en) * 2016-04-29 2021-05-25 Fundació Hospital Universitari Vall D'hebron—Institut De Recerca Dipeptidyl peptidase-4 inhibitors for topical eye treatment of retinal neurodegenerative diseases
WO2017211979A1 (en) 2016-06-10 2017-12-14 Boehringer Ingelheim International Gmbh Combinations of linagliptin and metformin
JOP20190086A1 (ar) 2016-10-21 2019-04-18 Novartis Ag مشتقات نافثيريدينون جديدة واستخدامها في معالجة عدم انتظام ضربات القلب
WO2018162722A1 (en) 2017-03-09 2018-09-13 Deutsches Institut Für Ernährungsforschung Potsdam-Rehbrücke Dpp-4 inhibitors for use in treating bone fractures
EP3474820B1 (en) 2017-08-24 2024-02-07 Novo Nordisk A/S Glp-1 compositions and uses thereof
UY38072A (es) 2018-02-07 2019-10-01 Novartis Ag Compuestos derivados de éster butanoico sustituido con bisfenilo como inhibidores de nep, composiciones y combinaciones de los mismos
WO2020058358A1 (en) 2018-09-18 2020-03-26 Albert-Ludwigs-Universität Freiburg Inhibition of histone methyl transferases to treat cancer
CN113166204B (zh) 2018-11-27 2025-01-28 诺华股份有限公司 作为治疗代谢障碍的蛋白质原转换酶枯草杆菌蛋白酶/kexin 9型（PCSK9）抑制剂的环状肽
UY38485A (es) 2018-11-27 2020-06-30 Novartis Ag Compuestos tetrámeros cíclicos como inhibidores de proproteína convertasa subtilisina/kexina tipo 9 (pcsk9), método de tratamiento, uso y su preparación
EP3887363A1 (en) 2018-11-27 2021-10-06 Novartis AG Cyclic pentamer compounds as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorder
BR112022003183A2 (pt) 2019-09-17 2022-05-17 Novartis Ag Usos do inibidor de dpp-iv e de uma combinação do inibidor de dpp-iv e metformina, composição farmacêutica e combinação para retardar perda do controle glicêmico
PE20230819A1 (es) 2020-02-18 2023-05-19 Novo Nordisk As Composiciones y usos de glp-1
JP2023536346A (ja) 2020-08-05 2023-08-24 エリプシーズ ファーマ リミテッド シクロデキストリン含有ポリマートポイソメラーゼ阻害剤コンジュゲートおよびｐａｒｐ阻害剤を用いた癌の処置
TW202333563A (zh) 2021-11-12 2023-09-01 瑞士商諾華公司 用於治療疾病或障礙之二胺基環戊基吡啶衍生物
AR127698A1 (es) 2021-11-23 2024-02-21 Novartis Ag Derivados de naftiridinona para el tratamiento de una enfermedad o un trastorno
CN114213504B (zh) * 2021-12-24 2023-05-09 西南医科大学 一类具有抗糖尿病活性的化合物及其应用
US20240391941A1 (en) 2023-05-24 2024-11-28 Novartis Ag Naphthyridinone derivatives for the treatment of a disease or disorder

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DD296075A5 (de) * 1989-08-07 1991-11-21 Martin-Luther-Universitaet Halle-Wittenberg,De Verfahren zur herstellung neuer inhibitoren der dipeptidyl peptidase iv
WO1995022326A1 (en) * 1994-02-17 1995-08-24 Zeria Pharmaceutical Co., Ltd. Cholinesterase activator

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE296075C (enExample)
US2961377A (en) 1957-08-05 1960-11-22 Us Vitamin Pharm Corp Oral anti-diabetic compositions and methods
DE2009743A1 (de) 1970-03-03 1971-09-16 Farbenfabriken Bayer Ag, 5090 Leverkusen Substituierte Biguanide mit antihyperglykämischer Wirkung
US3960949A (en) 1971-04-02 1976-06-01 Schering Aktiengesellschaft 1,2-Biguanides
CH602612A5 (enExample) 1974-10-11 1978-07-31 Hoffmann La Roche
US4935493A (en) 1987-10-06 1990-06-19 E. I. Du Pont De Nemours And Company Protease inhibitors
US5433955A (en) 1989-01-23 1995-07-18 Akzo N.V. Site specific in vivo activation of therapeutic drugs
WO1991011457A1 (en) * 1990-01-24 1991-08-08 Buckley Douglas I Glp-1 analogs useful for diabetes treatment
US5462928A (en) * 1990-04-14 1995-10-31 New England Medical Center Hospitals, Inc. Inhibitors of dipeptidyl-aminopeptidase type IV
WO1991017767A1 (en) * 1990-05-21 1991-11-28 New England Medical Center Hospitals, Inc. Method of treating inhibition of dipeptidyl aminopeptidase type iv
FR2674522B1 (fr) * 1991-03-26 1993-07-16 Lipha Nouveaux derives de l'indole, procedes de preparation et medicaments les contenant.
JPH04334357A (ja) 1991-05-02 1992-11-20 Fujirebio Inc 酵素阻害作用を有するアシル誘導体
ES2153831T3 (es) 1991-10-22 2001-03-16 New England Medical Center Inc Inhibidores de dipeptidil-aminopeptidasa de tipo iv.
RU2040926C1 (ru) * 1991-11-25 1995-08-09 Анатолий Григорьевич Гриценко Способ лечения сахарного диабета
IL106998A0 (en) 1992-09-17 1993-12-28 Univ Florida Brain-enhanced delivery of neuroactive peptides by sequential metabolism
FR2696740B1 (fr) 1992-10-13 1994-12-30 Dospharma Sa Dérivés prodrogués de la diméthylbiguanide et applications comme médicaments.
WO1995011689A1 (en) 1993-10-29 1995-05-04 Trustees Of Tufts College Use of inhibitors of dipeptidyl-aminopeptidase to block entry of hiv into cells
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
CA2137206A1 (en) 1993-12-09 1995-06-10 John A. Galloway Glucagon-like insulinotropic peptides, compositions and methods
US5543396A (en) * 1994-04-28 1996-08-06 Georgia Tech Research Corp. Proline phosphonate derivatives
US5512549A (en) * 1994-10-18 1996-04-30 Eli Lilly And Company Glucagon-like insulinotropic peptide analogs, compositions, and methods of use
US5614379A (en) 1995-04-26 1997-03-25 Eli Lilly And Company Process for preparing anti-obesity protein
DE19616486C5 (de) 1996-04-25 2016-06-30 Royalty Pharma Collection Trust Verfahren zur Senkung des Blutglukosespiegels in Säugern
CZ389398A3 (cs) 1996-05-29 1999-07-14 Prototek, Inc. Proléčiva thalidomidu a jejich použití pro modulaci funkce T-buněk
US6006753A (en) 1996-08-30 1999-12-28 Eli Lilly And Company Use of GLP-1 or analogs to abolish catabolic changes after surgery
AR016751A1 (es) 1996-11-22 2001-08-01 Athena Neurosciences Inc Metodo para inhibir la liberacion del peptido beta-amiloide en una celula, composicion farmaceutica y compuestos utiles en dicho metodo
AU3960400A (en) 1999-03-05 2000-09-28 Molteni L. E C. Dei Fratelli Alitti Societa' Di Esercizio S.P.A. Use of metformin in the preparation of pharmaceutical compositions capable of inhibiting the enzyme dipeptidyl peptidase iv

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DD296075A5 (de) * 1989-08-07 1991-11-21 Martin-Luther-Universitaet Halle-Wittenberg,De Verfahren zur herstellung neuer inhibitoren der dipeptidyl peptidase iv
WO1995022326A1 (en) * 1994-02-17 1995-08-24 Zeria Pharmaceutical Co., Ltd. Cholinesterase activator

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
DATABASE WPI Week 9217, Derwent World Patents Index; AN 92-132891, XP002041622 *
H.-U. DEMUTH: "Recent developments in inhibiting cysteine and serine protease.", J. ENZYME INHIB., vol. 3, no. 4, 1990, pages 249 - 278, XP002041620 *
T.J. KIEFFER ET AL.: "degradation of glucose-dependent insulinotropic polypeptide and truncated glucagon-like peptide 1 in vitro and in vivo by dipeptidyl peptidase IV.", ENDOCRINOLOGY, vol. 136, no. 8, 1995, pages 3585 - 3597, XP002041621 *

Cited By (207)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6303661B1 (en) 1996-04-25 2001-10-16 Probiodrug Use of dipeptidyl peptidase IV effectors for lowering the blood glucose level in mammals
US7276371B2 (en) 1997-09-29 2007-10-02 Point Therapeutics, Inc. Stimulation of hematopoietic cells in vitro
US6214340B1 (en) 1997-11-18 2001-04-10 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Physiologically active substance sulphostin, process for producing the same, and use thereof
WO1999025719A1 (en) * 1997-11-18 1999-05-27 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Novel physiologically active substance sulphostin, process for producing the same, and use thereof
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US7459428B2 (en) 1998-02-02 2008-12-02 Trustees Of Tufts College Method of regulating glucose metabolism, and reagents related thereto
JP2002501889A (ja) * 1998-02-02 2002-01-22 トラスティーズ オブ タフツ カレッジ グルコース代謝を調節する方法、およびそれに関連する試薬
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JP2010248253A (ja) * 1998-02-02 2010-11-04 Trustees Of Tufts College グルコース代謝を調節する方法、およびそれに関連する試薬
AU2007202745B2 (en) * 1998-02-02 2010-11-18 1149336 Ontario, Inc. Method of regulating glucose metabolism, and reagents related thereto
US6803357B1 (en) * 1998-02-02 2004-10-12 New England Medical Center Hospitals, Inc. Method of regulating glucose metabolism, and reagents related thereto
EP1520582A3 (en) * 1998-02-02 2009-07-01 Trustees Of Tufts College Use of dipeptidylpetidase inhibitors to regulate glucose metabolism
EP2433623A1 (en) * 1998-02-02 2012-03-28 Trustees Of Tufts College Use of dipeptidylpeptidase inhibitors to regulate glucose metabolism
JP2014144986A (ja) * 1998-02-02 2014-08-14 Trustees Of Tufts College グルコース代謝を調節する方法、およびそれに関連する試薬
JP2014144985A (ja) * 1998-02-02 2014-08-14 Trustees Of Tufts College グルコース代謝を調節する方法、およびそれに関連する試薬
US7157429B1 (en) 1998-02-02 2007-01-02 Trustees Of Tufts College Method of regulating glucose metabolism, and reagents related thereto
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US9044424B2 (en) 1998-02-02 2015-06-02 1149336 Ontario, Inc. Methods of regulating glucose metabolism, and reagents related thereto
JP2017008092A (ja) * 1998-02-02 2017-01-12 トラスティーズ オブ タフツ カレッジ グルコース代謝を調節する方法、およびそれに関連する試薬
JP2018044005A (ja) * 1998-02-02 2018-03-22 トラスティーズ オブ タフツ カレッジ グルコース代謝を調節する方法、およびそれに関連する試薬
US6890898B2 (en) 1998-02-02 2005-05-10 Trustees Of Tufts College Method of regulating glucose metabolism, and reagents related thereto
JP2005041885A (ja) * 1998-02-02 2005-02-17 Trustees Of Tufts College グルコース代謝を調節する方法、およびそれに関連する試薬
US7078381B2 (en) 1998-02-02 2006-07-18 Trustees Of Tufts College Method of regulating glucose metabolism, and reagents related thereto
JP2010248252A (ja) * 1998-02-02 2010-11-04 Trustees Of Tufts College グルコース代謝を調節する方法、およびそれに関連する試薬
EP1428533A3 (de) * 1998-05-28 2004-06-23 Probiodrug AG Verwendung von Thiazolidin- oder Pyrrolidinderivaten von Aminosäuren als antihyperglykämische Mittel
EP1215207A3 (de) * 1998-05-28 2002-07-03 Probiodrug AG Salze von Isoleucyl-Thiazolidin und -Pyrrolidin und ihre Verwendung als Dipeptidylpeptidase-Inhibitoren
EP1398030A3 (de) * 1998-05-28 2004-04-07 Probiodrug AG Effektoren von Dipeptidylpeptidase IV
CN1332954C (zh) * 1998-05-28 2007-08-22 普罗西迪恩有限公司 二肽基肽酶iv的效应物
WO1999061431A1 (de) * 1998-05-28 1999-12-02 Probiodrug Gesellschaft für Arzneimittelforschung mbH Neue effektoren von dipeptidylpeptidase iv
DE19823831A1 (de) * 1998-05-28 1999-12-02 Probiodrug Ges Fuer Arzneim Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen
EP1214936A3 (de) * 1998-05-28 2002-07-03 Probiodrug AG Verwendung von Thiazolidin- oder Pyrrolidinderivaten von Aminosäuren als antihyperglykämische Mittel
EP1304327A3 (de) * 1998-05-28 2003-05-02 Probiodrug AG Glutamin-Thiazolidide und -Pyrrolidide sowie ihre Verwendung als Dipeptidylpeptidase IV Inhibitoren
US6548481B1 (en) 1998-05-28 2003-04-15 Probiodrug Ag Effectors of dipeptidyl peptidase IV
US7053055B2 (en) 1998-06-24 2006-05-30 Prosidion Ltd. Compounds of unstable DP IV-inhibitors
US7166579B2 (en) 1998-06-24 2007-01-23 Prosidion Limited Prodrugs of DP IV-inhibitors
US7084120B2 (en) 1998-06-24 2006-08-01 Probiodrug Ag Prodrugs of DP IV-inhibitors
EP0995440A1 (de) * 1998-07-31 2000-04-26 Probiodrug Gesellschaft für Arzneimittelforschung mbH Verfahren zur Stiegerung des Blutglukosespiegels in Säugern
US6319893B1 (en) 1998-07-31 2001-11-20 Probiodrug Raising blood sugar level in hypoglycemic mammals by administering inhibitors of dipeptidyl peptidase IV
US7265118B2 (en) 1998-08-21 2007-09-04 Point Therapeutics, Inc. Regulation of substrate activity
US6979697B1 (en) 1998-08-21 2005-12-27 Point Therapeutics, Inc. Regulation of substrate activity
US6559314B2 (en) 1999-06-10 2003-05-06 Probiodrug Ag Method for the production of thiazolidin
US6949515B2 (en) 1999-08-24 2005-09-27 Probiodrug Ag Effectors of dipeptidyl peptidase IV for topical use
US7335645B2 (en) 1999-08-24 2008-02-26 Probiodrug Ag Effectors of dipeptidyl peptidase IV for topical use
EP1228061A4 (en) * 1999-11-12 2004-12-15 Guilford Pharm Inc DIPEPTIDYL PEPTIDASE IV INHIBITORS; METHODS OF MANUFACTURE AND USE OF SAID INHIBITORS
WO2001040180A3 (en) * 1999-11-30 2001-11-08 Ferring Bv N-substituted 2-cyanopyrrolidines and their use as antidiabetic agents
US7169806B2 (en) 1999-11-30 2007-01-30 Ferring Bv Antidiabetic agents
RU2265012C2 (ru) * 1999-11-30 2005-11-27 Ферринг Бв Новые антидиабетические агенты
US6911467B2 (en) 1999-11-30 2005-06-28 Ferring Bv Antidiabetic agents
WO2001062266A3 (en) * 2000-02-25 2002-05-02 Novo Nordisk As Use of dpp-iv inhibitors for the treatment of diabetes
US6395767B2 (en) 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
USRE44186E1 (en) 2000-03-10 2013-04-30 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
EP2266665B1 (en) * 2000-03-31 2016-05-11 Royalty Pharma Collection Trust Method for the improvement of islet signaling in diabetes mellitus and for its prevention
EP2266665A1 (en) 2000-03-31 2010-12-29 Prosidion Limited Method for the improvement of islet signaling in diabetes mellitus and for its prevention
JP2003528135A (ja) * 2000-03-31 2003-09-24 プロバイオドラッグ アーゲー 糖尿病のランゲルハンス島シグナリングの改善方法及びその防止方法
EP1283735B2 (en) † 2000-03-31 2012-10-24 Royalty Pharma Collection Trust Method for the improvement of islet signaling in diabetes mellitus and for its prevention
EP2055302A1 (en) 2000-03-31 2009-05-06 Prosidion Limited Method for the improvement of islet signaling in diabetes mellitus and for its prevention
US6500804B2 (en) 2000-03-31 2002-12-31 Probiodrug Ag Method for the improvement of islet signaling in diabetes mellitus and for its prevention
US8168199B2 (en) 2000-10-27 2012-05-01 Stephan von Hoersten Dipeptidyl peptidase IV inhibitors for the treatment of schizophrenia and depression
US7132104B1 (en) 2000-10-27 2006-11-07 Probiodrug Ag Modulation of central nervous system (CNS) dipeptidyl peptidase IV (DPIV) -like activity for the treatment of neurological and neuropsychological disorders
EP1891948A1 (en) 2000-10-27 2008-02-27 Probiodrug AG Treatment of neurological and neuropsychological disorders
US7435420B2 (en) 2000-10-27 2008-10-14 Probiodrug Ag Dipeptidyl peptidase IV inhibitors for the treatment of anxiety
US7026316B2 (en) 2001-03-27 2006-04-11 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US6890905B2 (en) 2001-04-02 2005-05-10 Prosidion Limited Methods for improving islet signaling in diabetes mellitus and for its prevention
WO2002083109A1 (en) * 2001-04-11 2002-10-24 Ferring Bv Treatment of type 2 diabetes with inhibitors of dipeptidyl peptidase iv
EP1270562A3 (fr) * 2001-06-18 2003-05-07 Les Laboratoires Servier Nouveaux dérivés cycliques d'alpha-amino-gamma-hydroxy-amides, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent
US7253172B2 (en) 2001-06-20 2007-08-07 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
US7098239B2 (en) 2001-06-20 2006-08-29 Merck & Co., Inc Dipeptidyl peptidase inhibitors for the treatment of diabetes
US7132443B2 (en) 2001-06-27 2006-11-07 Smithklinebeecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
US7368576B2 (en) 2001-06-27 2008-05-06 Probiodrug Ag Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
US7368421B2 (en) 2001-06-27 2008-05-06 Probiodrug Ag Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis
US7109347B2 (en) 2001-06-27 2006-09-19 Probiodrug Ag Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
US8168637B2 (en) 2001-07-06 2012-05-01 Merck Sharp & Dohme Corp. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment of diabetes
EP2226324A1 (en) 2001-07-06 2010-09-08 Merck Sharp & Dohme Corp. Beta-amino tetrahydroimidazo(1,2-a)pyrazines and tetrahydrotriazolo(4,3-a)pyrazines for use in the treatment of diabetes type ii
WO2003004498A1 (en) * 2001-07-06 2003-01-16 Merck & Co., Inc. Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
EA012701B1 (ru) * 2001-07-06 2009-12-30 Мерк Энд Ко., Инк. Фармацевтическая композиция, содержащая ингибитор фермента дипептидилпептидазы
US7125873B2 (en) 2001-07-06 2006-10-24 Merck & Co., Inc. Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
EP1625847A1 (en) 2001-07-06 2006-02-15 Merck & Co., Inc. Pharmaceutical composition comprising a tetrahydrotriazolo[4,3-a]pyrazine
US6699871B2 (en) 2001-07-06 2004-03-02 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US8440668B2 (en) 2001-07-06 2013-05-14 Merck Sharp & Dohme Corp Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment of type 2 diabetes
HRP20031098B1 (en) * 2001-07-06 2012-03-31 Merck Sharp & Dohme Corp. Beta-amino tetrahydroimidazo (1,2-a) pyrazines and tetrahydrotrioazolo (4,3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
EP2292232A1 (en) 2001-07-06 2011-03-09 Merck Sharp & Dohme Corp. Beta-amino tetrahydroimidazo(1,2-A)pyrazines and tetrahydrotriazolo(4,3-A)pyrazines for use in the treatment of diabetes type II
RU2305553C2 (ru) * 2001-08-17 2007-09-10 Просидайен Лимитед Новые ингибиторы дипептидилпептидазы iv и их применение для понижения кровяного давления
WO2003015775A1 (en) * 2001-08-17 2003-02-27 Probiodrug Ag New dipeptidyl peptidase iv inhibitors and their uses for lowering blood pressure levels
US6844316B2 (en) 2001-09-06 2005-01-18 Probiodrug Ag Inhibitors of dipeptidyl peptidase I
US7144856B2 (en) 2001-09-06 2006-12-05 Probiodrug Ag Inhibitors of dipeptidyl peptidase I
WO2003033524A2 (en) 2001-10-12 2003-04-24 Probiodrug Ag Peptidyl ketones as inhibitors of dpiv
US7608577B2 (en) 2001-10-12 2009-10-27 Osi Pharmaceuticals, Inc. Peptidyl ketones as inhibitors of DPIV
US9757400B2 (en) 2001-11-26 2017-09-12 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
US7727964B2 (en) 2001-11-26 2010-06-01 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
EP2769715A3 (en) * 2001-11-26 2014-09-17 Trustees Of Tufts College Methods for treating autoimmune disorders, and reagents related thereto
US8410053B2 (en) 2001-11-26 2013-04-02 Trustees Of Tufts College Methods for treating autoimmune disorders, and reagents related thereto
US7074798B2 (en) 2002-02-25 2006-07-11 Eisai Co., Ltd Xanthine derivative and DPPIV inhibitor
US6946480B2 (en) 2002-02-28 2005-09-20 Hans-Ulrich Demuth Glutaminyl based DPIV inhibitors
US6710040B1 (en) 2002-06-04 2004-03-23 Pfizer Inc. Fluorinated cyclic amides as dipeptidyl peptidase IV inhibitors
US7208498B2 (en) 2002-07-15 2007-04-24 Merck & Co., Inc. Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
US7262207B2 (en) 2002-09-19 2007-08-28 Abbott Laboratories Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
US8637546B2 (en) 2002-09-19 2014-01-28 Abbvie Inc. Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DDP-IV)
US7390809B2 (en) 2002-10-07 2008-06-24 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for diabetes
US7101871B2 (en) 2002-10-18 2006-09-05 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7157490B2 (en) 2002-11-07 2007-01-02 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
EP1583534A4 (en) * 2002-12-20 2007-08-29 Merck & Co Inc 3-AMINO-4-PHENYLBUTANIC ACID DERIVATIVES AS DIPEPTIDYL-PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
US8933083B2 (en) 2003-01-14 2015-01-13 Arena Pharmaceuticals, Inc. 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
US7265128B2 (en) 2003-01-17 2007-09-04 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7388019B2 (en) 2003-01-31 2008-06-17 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7345180B2 (en) 2003-01-31 2008-03-18 Sanwa Kagaku Kenkyusho Co., Ltd. Compound inhibiting dipeptidyl peptidase IV
US7550590B2 (en) 2003-03-25 2009-06-23 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7381537B2 (en) 2003-05-05 2008-06-03 Probiodrug Ag Use of inhibitors of glutaminyl cyclases for treatment and prevention of disease
US7371871B2 (en) 2003-05-05 2008-05-13 Probiodrug Ag Inhibitors of glutaminyl cyclase
EP2206496A1 (en) 2003-05-05 2010-07-14 Probiodrug AG Medical use of inhibitors of glutaminyl and glutamate cyclases
DE202004021723U1 (de) 2003-05-05 2010-07-15 Probiodrug Ag Medizinische Verwendung von Hemmern von Glutaminyl- und Glutamatcyclasen
WO2004098625A2 (en) 2003-05-05 2004-11-18 Probiodrug Ag Medical use of inhibitors of glutaminyl and glutamate cyclases
WO2004098591A2 (en) 2003-05-05 2004-11-18 Probiodrug Ag Inhibitors of glutaminyl cyclase and their use in the treatment of neurological diseases
US7560455B2 (en) 2003-05-14 2009-07-14 Merck & Co., Inc. 3-Amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7638638B2 (en) 2003-05-14 2009-12-29 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
US7332520B2 (en) 2003-06-06 2008-02-19 Merck & Co., Inc. Fused indoles as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7456204B2 (en) 2003-06-17 2008-11-25 Merck & Co., Inc. Cyclohexylglycine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7470699B2 (en) 2003-07-11 2008-12-30 Arena Pharmaceuticals, Inc. Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
US7259160B2 (en) 2003-07-31 2007-08-21 Merck & Co., Inc. Hexahydrodiazepinones as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
US7470700B2 (en) 2003-08-13 2008-12-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7579357B2 (en) 2003-08-13 2009-08-25 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
EP2289498A1 (en) 2003-10-15 2011-03-02 Probiodrug AG Use of inhibitors of glutaminyl clyclase
EP2338490A2 (en) 2003-11-03 2011-06-29 Probiodrug AG Combinations Useful for the Treatment of Neuronal Disorders
US7230002B2 (en) 2004-02-03 2007-06-12 Glenmark Pharmaceuticals Ltd. Dipeptidyl peptidase IV inhibitors; processes for their preparation and compositions thereof
WO2005075436A2 (en) 2004-02-05 2005-08-18 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
US7687492B2 (en) 2004-05-04 2010-03-30 Merck Sharp & Dohme Corp. 1,2,4-Oxadiazole derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
US7671073B2 (en) 2004-05-18 2010-03-02 Merck Sharp & Dohme Corp. Cyclohexylalanine derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
WO2005113510A1 (en) * 2004-05-21 2005-12-01 Santhera Pharmaceuticals (Schweiz) Ag Dpp-iv inhibitors
EP1598341A1 (en) * 2004-05-21 2005-11-23 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
EP1604980A1 (en) * 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
EP1604989A1 (en) * 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
WO2005121089A1 (en) * 2004-06-08 2005-12-22 Santhera Pharmaceuticals (Schweiz) Ag Dpp-iv inhibitors
WO2005121131A1 (en) * 2004-06-08 2005-12-22 Santhera Pharmaceuticals (Schweiz) Ag Dpp-iv inhibitors
US7205323B2 (en) 2004-10-12 2007-04-17 Glenmark Pharmaceuticals S.A. Dipeptidyl peptidase IV inhibitors pharmaceutical compositions containing them, and process for their preparation
US7538128B2 (en) 2004-10-12 2009-05-26 Glenmark Pharmaceuticals S.A. Dipeptidyl peptidase IV inhibitors, process for their preparation and compositions containing them
US7524844B2 (en) 2004-10-12 2009-04-28 Glenmark Pharmaceuticals S.A. Dipeptidyl peptidase IV inhibitors, process for their preparation and compositions containing them
EP2116235A1 (en) 2005-01-10 2009-11-11 Arena Pharmaceuticals, Inc. Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood GLP-1 level
EP2602259A2 (en) 2005-02-18 2013-06-12 Mitsubishi Tanabe Pharma Corporation Salt of proline derivative, solvate thereof, and production method thereof
US8604198B2 (en) 2005-02-18 2013-12-10 Mitsubishi Tanabe Pharma Corporation Salt of proline derivative, solvate thereof, and production method thereof
US8003790B2 (en) 2005-02-18 2011-08-23 Mitsubishi Tanabe Pharma Corporation Salt of proline derivative, solvate thereof, and production method thereof
EP2356997A1 (en) 2005-06-06 2011-08-17 Georgetown University Compositions and methods for lipo modeling
US8906901B2 (en) 2005-09-14 2014-12-09 Takeda Pharmaceutical Company Limited Administration of dipeptidyl peptidase inhibitors
US8222411B2 (en) 2005-09-16 2012-07-17 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7625939B2 (en) 2005-11-14 2009-12-01 Probiodrug Ag Cyclopropyl-fused pyrrolidine derivatives as dipeptidyl peptidase IV inhibitors
WO2007072083A1 (en) 2005-12-23 2007-06-28 Prosidion Limited Treatment of type 2 diabetes with a combination of dpiv inhibitor and metformin or thiazolidinedione
US7915427B2 (en) 2006-03-08 2011-03-29 Kyorin Pharmaceuticals Co., Ltd. Process for producing aminoacetyl pyrrolidine carbonitrile derivative and intermediate for production thereof
US7960384B2 (en) 2006-03-28 2011-06-14 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
EP2253311A2 (en) 2006-04-11 2010-11-24 Arena Pharmaceuticals, Inc. Use of GPR119 receptor agonists for increasing bone mass and for treating osteoporosis, as well as combination therapy relating thereto
US7728146B2 (en) 2006-04-12 2010-06-01 Probiodrug Ag Enzyme inhibitors
WO2008055945A1 (en) 2006-11-09 2008-05-15 Probiodrug Ag 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
US8084605B2 (en) 2006-11-29 2011-12-27 Kelly Ron C Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
WO2008065141A1 (en) 2006-11-30 2008-06-05 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
US8143427B2 (en) 2007-03-22 2012-03-27 Kyorin Pharmaceutical Co., Ltd. Method for producing aminoacetylpyrrolidinecarbonitrile derivative
WO2008120813A1 (ja) 2007-04-03 2008-10-09 Mitsubishi Tanabe Pharma Corporation ジペプチジルペプチダーゼ４阻害化合物と甘味料との併用
EP2865670A1 (en) 2007-04-18 2015-04-29 Probiodrug AG Thiourea derivatives as glutaminyl cyclase inhibitors
US7820666B2 (en) 2007-05-08 2010-10-26 Concert Pharmaceuticals, Inc. Tetrahydrotriazolopyrazine derivatives and uses thereof
US8853385B2 (en) 2008-01-17 2014-10-07 Mitsubishi Tanabe Pharma Corporation Combination therapy comprising SGLT inhibitors and DPP4 inhibitors
US8883714B2 (en) 2008-04-07 2014-11-11 Arena Pharmaceuticals, Inc. Pharmaceutical compositions comprising GPR119 agonists which act as peptide YY (PYY) secretagogues
EP2676960A1 (en) 2008-11-13 2013-12-25 Merck Sharp & Dohme Corp. Combination drugs comprising aminotetrahydropyrans as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes
EP2676959A1 (en) 2008-11-13 2013-12-25 Merck Sharp & Dohme Corporation Combination drugs comprising aminotetrahydropyrans as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes
EP2676961A1 (en) 2008-11-13 2013-12-25 Merck Sharp & Dohme Corporation Combination drugs comprising aminotetrahydropyrans as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes
US8404727B2 (en) 2009-01-07 2013-03-26 Glenmark Pharmaceuticals S.A. Pharmaceutical composition that includes a dipeptidyl peptidase-IV inhibitor
WO2011005929A1 (en) 2009-07-09 2011-01-13 Arena Pharmaceuticals, Inc. Piperidine derivative and its use for the treatment of diabets and obesity
WO2011028455A1 (en) 2009-09-02 2011-03-10 Merck Sharp & Dohme Corp. Aminotetrahydropyrans as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2011029920A1 (en) 2009-09-11 2011-03-17 Probiodrug Ag Heterocylcic derivatives as inhibitors of glutaminyl cyclase
WO2011103256A1 (en) 2010-02-22 2011-08-25 Merck Sharp & Dohme Corp. Substituted aminotetrahydrothiopyrans and derivatives thereof as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
WO2011107530A2 (en) 2010-03-03 2011-09-09 Probiodrug Ag Novel inhibitors
WO2011110613A1 (en) 2010-03-10 2011-09-15 Probiodrug Ag Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
WO2011127051A1 (en) 2010-04-06 2011-10-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
WO2011146358A1 (en) 2010-05-21 2011-11-24 Merck Sharp & Dohme Corp. Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
US10894787B2 (en) 2010-09-22 2021-01-19 Arena Pharmaceuticals, Inc. Modulators of the GPR119 receptor and the treatment of disorders related thereto
EP3323818A1 (en) 2010-09-22 2018-05-23 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012040279A1 (en) 2010-09-22 2012-03-29 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012049566A1 (en) 2010-10-14 2012-04-19 Japan Tobacco Inc. Combination therapy for use in treating diabetes
WO2012123563A1 (en) 2011-03-16 2012-09-20 Probiodrug Ag Benz imidazole derivatives as inhibitors of glutaminyl cyclase
WO2012135570A1 (en) 2011-04-01 2012-10-04 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145361A1 (en) 2011-04-19 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145603A1 (en) 2011-04-22 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145604A1 (en) 2011-04-22 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012170702A1 (en) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US9051329B2 (en) 2011-07-05 2015-06-09 Merck Sharp & Dohme Corp. Tricyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US9115082B2 (en) 2012-01-18 2015-08-25 Catherine Yang Dipeptidyl-peptidase-IV inhibitors for treatment of type 2 diabetes complex with hypertension
WO2013122920A1 (en) 2012-02-17 2013-08-22 Merck Sharp & Dohme Corp. Dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2014018350A1 (en) 2012-07-23 2014-01-30 Merck Sharp & Dohme Corp. Treating diabetes with dipeptidyl peptidase-iv inhibitors
WO2014061031A1 (en) 2012-10-17 2014-04-24 Cadila Healthcare Limited 2-phenyl-5-heterocyclyl-tetrahydro-2h-pyran-3-amine compounds for use in the treatment of diabetes and its associated disorders
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
WO2014113750A1 (en) 2013-01-18 2014-07-24 Dnj Pharma, Inc. Novel ddp-iv inhibitors
EP4000630A1 (en) 2014-09-03 2022-05-25 Invex Therapeutics Ltd Elevated intracranial pressure treatment
US11007175B2 (en) 2015-01-06 2021-05-18 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
US11400072B2 (en) 2015-03-09 2022-08-02 Coherus Biosciences, Inc. Methods for the treatment of nonalcoholic fatty liver disease and/or lipodystrophy
US10555929B2 (en) 2015-03-09 2020-02-11 Coherus Biosciences, Inc. Methods for the treatment of nonalcoholic fatty liver disease and/or lipodystrophy
US10772865B2 (en) 2015-03-09 2020-09-15 Coherus Biosciences, Inc. Methods for the treatment of nonalcoholic fatty liver disease and/or lipodystrophy
US11884626B2 (en) 2015-06-22 2024-01-30 Arena Pharmaceuticals, Inc. Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(Compound1) for use in S1P1 receptor-associated disorders
US11253508B2 (en) 2017-04-03 2022-02-22 Coherus Biosciences, Inc. PPARy agonist for treatment of progressive supranuclear palsy
US10913747B2 (en) 2017-07-04 2021-02-09 F.I.S.—Fabbrica Italiana Sintetici S.p.A. Efficient process for the preparation of sitagliptin through a very effective preparation of the intermediate 2,4,5-trifluorophenylacetic acid
WO2019007578A1 (en) 2017-07-04 2019-01-10 F.I.S. - Fabbrica Italiana Sintetici S.P.A. EFFICIENT PROCESS FOR THE PREPARATION OF SITAGLIPTIN BY HIGHLY EFFICIENT PREPARATION OF INTERMEDIATE 2,4,5-TRIFLUOROPHENYLACETIC ACID
EP3424927A1 (en) 2017-07-04 2019-01-09 F.I.S.- Fabbrica Italiana Sintetici S.p.A. Efficient process for the preparation of sitagliptin through a very effective preparation of the intermediate 2,4,5-trifluorophenylacetic acid
EP3461819A1 (en) 2017-09-29 2019-04-03 Probiodrug AG Inhibitors of glutaminyl cyclase
WO2019158285A1 (en) 2018-02-13 2019-08-22 F.I.S. - Fabbrica Italiana Sintetici S.P.A. New efficient process for the preparation of sitagliptin.
US11174266B2 (en) 2018-02-13 2021-11-16 F.I.S.—Fabbrica Italiana Sintetici S.p.A. Efficient process for the preparation of sitagliptin
EP3524605A1 (en) 2018-02-13 2019-08-14 F.I.S.- Fabbrica Italiana Sintetici S.p.A. New efficient process for the preparation of sitagliptin
US12156866B2 (en) 2018-06-06 2024-12-03 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor

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US6303661B1 (en) 2001-10-16
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