ZA200307156B - Treatment of type 2 diabetes with inhibitors of dipeptidyl peptidase IV. - Google Patents

Treatment of type 2 diabetes with inhibitors of dipeptidyl peptidase IV. Download PDF

Info

Publication number: ZA200307156B
Authority: ZA; South Africa
Prior art keywords: inhibitor; use according; prodrug; diabetes; dipeptidyl peptidase
Prior art date: 2001-04-11

Application number

ZA200307156A

Other languages

English (en)

Inventor

Pierre Broqua

Beatrice Sudre

Michel L Aubert

Original Assignee

Ferring Bv

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.)

2001-04-11

Filing date

2003-09-12

Publication date

2004-06-04

2003-09-12 Application filed by Ferring Bv filed Critical Ferring Bv

2004-06-04 Publication of ZA200307156B publication Critical patent/ZA200307156B/en

Links

239000003112 inhibitor Substances 0.000 title claims description 33
208000001072 type 2 diabetes mellitus Diseases 0.000 title claims description 20
102000016622 Dipeptidyl Peptidase 4 Human genes 0.000 title claims description 7
101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 title claims description 7
238000011282 treatment Methods 0.000 title description 19
150000001875 compounds Chemical class 0.000 claims description 29
201000010099 disease Diseases 0.000 claims description 10
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
239000000203 mixture Substances 0.000 claims description 10
229940002612 prodrug Drugs 0.000 claims description 10
239000000651 prodrug Substances 0.000 claims description 10
238000009472 formulation Methods 0.000 claims description 8
239000008194 pharmaceutical composition Substances 0.000 claims description 8
150000003839 salts Chemical class 0.000 claims description 6
125000000217 alkyl group Chemical group 0.000 claims description 3
229910052757 nitrogen Inorganic materials 0.000 claims description 3
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
125000003373 pyrazinyl group Chemical group 0.000 claims description 2
125000004076 pyridyl group Chemical group 0.000 claims description 2
125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
102000035195 Peptidases Human genes 0.000 claims 2
108091005804 Peptidases Proteins 0.000 claims 2
235000019833 protease Nutrition 0.000 claims 2
238000000034 method Methods 0.000 description 11
NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 10
241001465754 Metazoa Species 0.000 description 9
238000013293 zucker diabetic fatty rat Methods 0.000 description 7
206010012601 diabetes mellitus Diseases 0.000 description 6
QAEDZJGFFMLHHQ-UHFFFAOYSA-N trifluoroacetic anhydride Chemical compound FC(F)(F)C(=O)OC(=O)C(F)(F)F QAEDZJGFFMLHHQ-UHFFFAOYSA-N 0.000 description 6
102000004877 Insulin Human genes 0.000 description 5
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201000001421 hyperglycemia Diseases 0.000 description 5
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150000002825 nitriles Chemical class 0.000 description 5
DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 description 4
239000013543 active substance Substances 0.000 description 4
230000001684 chronic effect Effects 0.000 description 4
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QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
VLJNHYLEOZPXFW-BYPYZUCNSA-N L-prolinamide Chemical compound NC(=O)[C@@H]1CCCN1 VLJNHYLEOZPXFW-BYPYZUCNSA-N 0.000 description 3
239000002253 acid Substances 0.000 description 3
150000007513 acids Chemical class 0.000 description 3
KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
230000000694 effects Effects 0.000 description 3
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UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 3
RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 description 2
-1 5-cyano-2-pyridyl Chemical group 0.000 description 2
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
102000004190 Enzymes Human genes 0.000 description 2
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VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
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150000003140 primary amides Chemical group 0.000 description 2
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239000003826 tablet Substances 0.000 description 2
125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 2
VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 2
OGYGFUAIIOPWQD-UHFFFAOYSA-N 1,3-thiazolidine Chemical compound C1CSCN1 OGYGFUAIIOPWQD-UHFFFAOYSA-N 0.000 description 1
NIUAJYOMWZYSQR-UHFFFAOYSA-N 6-(2-aminoethylamino)pyridine-3-carbonitrile Chemical compound NCCNC1=CC=C(C#N)C=N1 NIUAJYOMWZYSQR-UHFFFAOYSA-N 0.000 description 1
HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
239000005711 Benzoic acid Substances 0.000 description 1
CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 description 1
208000024172 Cardiovascular disease Diseases 0.000 description 1
208000002249 Diabetes Complications Diseases 0.000 description 1
206010012655 Diabetic complications Diseases 0.000 description 1
102100025101 GATA-type zinc finger protein 1 Human genes 0.000 description 1
101710198884 GATA-type zinc finger protein 1 Proteins 0.000 description 1
DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 description 1
WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
LELOWRISYMNNSU-UHFFFAOYSA-N Hydrocyanic acid Natural products N#C LELOWRISYMNNSU-UHFFFAOYSA-N 0.000 description 1
AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 description 1
AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 1
OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 1
208000017442 Retinal disease Diseases 0.000 description 1
206010038923 Retinopathy Diseases 0.000 description 1
QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 1
239000005864 Sulphur Substances 0.000 description 1
125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 1
230000009471 action Effects 0.000 description 1
239000008186 active pharmaceutical agent Substances 0.000 description 1
230000001154 acute effect Effects 0.000 description 1
125000000266 alpha-aminoacyl group Chemical group 0.000 description 1
229910000147 aluminium phosphate Inorganic materials 0.000 description 1
238000004458 analytical method Methods 0.000 description 1
238000010171 animal model Methods 0.000 description 1
239000003472 antidiabetic agent Substances 0.000 description 1
229940125708 antidiabetic agent Drugs 0.000 description 1
125000004429 atom Chemical group 0.000 description 1
210000003719 b-lymphocyte Anatomy 0.000 description 1
230000004888 barrier function Effects 0.000 description 1
235000010233 benzoic acid Nutrition 0.000 description 1
239000011230 binding agent Substances 0.000 description 1
229920000249 biocompatible polymer Polymers 0.000 description 1
230000000903 blocking effect Effects 0.000 description 1
210000004369 blood Anatomy 0.000 description 1
239000008280 blood Substances 0.000 description 1
239000004067 bulking agent Substances 0.000 description 1
229910052799 carbon Inorganic materials 0.000 description 1
125000004432 carbon atom Chemical group C* 0.000 description 1
239000007795 chemical reaction product Substances 0.000 description 1
239000003795 chemical substances by application Substances 0.000 description 1
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230000003247 decreasing effect Effects 0.000 description 1
238000011161 development Methods 0.000 description 1
238000003745 diagnosis Methods 0.000 description 1
235000014113 dietary fatty acids Nutrition 0.000 description 1
229940079593 drug Drugs 0.000 description 1
125000000031 ethylamino group Chemical group [H]C([H])([H])C([H])([H])N([H])[*] 0.000 description 1
229930195729 fatty acid Natural products 0.000 description 1
239000000194 fatty acid Substances 0.000 description 1
150000004665 fatty acids Chemical class 0.000 description 1
239000000796 flavoring agent Substances 0.000 description 1
235000013355 food flavoring agent Nutrition 0.000 description 1
230000037406 food intake Effects 0.000 description 1
235000012631 food intake Nutrition 0.000 description 1
239000001530 fumaric acid Substances 0.000 description 1
239000008103 glucose Substances 0.000 description 1
235000009200 high fat diet Nutrition 0.000 description 1
229910052739 hydrogen Inorganic materials 0.000 description 1
125000004435 hydrogen atom Chemical group [H]* 0.000 description 1
230000001127 hyperphagic effect Effects 0.000 description 1
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238000010253 intravenous injection Methods 0.000 description 1
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AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 description 1
208000017169 kidney disease Diseases 0.000 description 1
238000011866 long-term treatment Methods 0.000 description 1
VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
239000011976 maleic acid Substances 0.000 description 1
230000007246 mechanism Effects 0.000 description 1
230000002503 metabolic effect Effects 0.000 description 1
125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 description 1
125000002560 nitrile group Chemical group 0.000 description 1
230000003287 optical effect Effects 0.000 description 1
WLJNZVDCPSBLRP-UHFFFAOYSA-N pamoic acid Chemical compound C1=CC=C2C(CC=3C4=CC=CC=C4C=C(C=3O)C(=O)O)=C(O)C(C(O)=O)=CC2=C1 WLJNZVDCPSBLRP-UHFFFAOYSA-N 0.000 description 1
239000000546 pharmaceutical excipient Substances 0.000 description 1
206010036067 polydipsia Diseases 0.000 description 1
230000000291 postprandial effect Effects 0.000 description 1
239000000843 powder Substances 0.000 description 1
239000003755 preservative agent Substances 0.000 description 1
230000000069 prophylactic effect Effects 0.000 description 1
QJRYYOWARFCJQZ-UHFFFAOYSA-N pyrrolidine-1-carbonitrile Chemical compound N#CN1CCCC1 QJRYYOWARFCJQZ-UHFFFAOYSA-N 0.000 description 1
ALSCEGDXFJIYES-UHFFFAOYSA-N pyrrolidine-2-carbonitrile Chemical compound N#CC1CCCN1 ALSCEGDXFJIYES-UHFFFAOYSA-N 0.000 description 1
QROMHLFLMYDBEQ-UHFFFAOYSA-N pyrrolidine-2-carbonitrile;2,2,2-trifluoroacetic acid Chemical compound N#CC1CCCN1.OC(=O)C(F)(F)F QROMHLFLMYDBEQ-UHFFFAOYSA-N 0.000 description 1
QSJTUXCBPTVKQZ-UHFFFAOYSA-N pyrrolidine-2-carbonitrile;hydrochloride Chemical compound Cl.N#CC1CCCN1 QSJTUXCBPTVKQZ-UHFFFAOYSA-N 0.000 description 1
125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
230000035945 sensitivity Effects 0.000 description 1
239000000243 solution Substances 0.000 description 1
239000002904 solvent Substances 0.000 description 1
238000010561 standard procedure Methods 0.000 description 1
239000000758 substrate Substances 0.000 description 1
239000001117 sulphuric acid Substances 0.000 description 1
235000011149 sulphuric acid Nutrition 0.000 description 1
239000000829 suppository Substances 0.000 description 1
230000004083 survival effect Effects 0.000 description 1
239000000725 suspension Substances 0.000 description 1
208000024891 symptom Diseases 0.000 description 1
125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
238000012360 testing method Methods 0.000 description 1
229940124597 therapeutic agent Drugs 0.000 description 1
235000019786 weight gain Nutrition 0.000 description 1

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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
- 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
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
- 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
- A61P3/08—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

Landscapes

Health & Medical Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Animal Behavior & Ethology (AREA)
Medicinal Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
Epidemiology (AREA)
Diabetes (AREA)
Chemical Kinetics & Catalysis (AREA)
Organic Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Obesity (AREA)
Hematology (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Endocrinology (AREA)
Emergency Medicine (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Thiazole And Isothizaole Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Pyrrole Compounds (AREA)
Medicines Containing Plant Substances (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

ZA200307156A 2001-04-11 2003-09-12 Treatment of type 2 diabetes with inhibitors of dipeptidyl peptidase IV. ZA200307156B (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
GBGB0109146.1A GB0109146D0 (en)	2001-04-11	2001-04-11	Treatment of type 2 diabetes

Publications (1)

Publication Number	Publication Date
ZA200307156B true ZA200307156B (en)	2004-06-04

Family

ID=9912727

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
ZA200307156A ZA200307156B (en)	2001-04-11	2003-09-12	Treatment of type 2 diabetes with inhibitors of dipeptidyl peptidase IV.

Country Status (21)

Country	Link
US (1)	US20040209891A1 (de)
EP (1)	EP1377278B1 (de)
JP (1)	JP2004525179A (de)
KR (1)	KR20040025915A (de)
CN (1)	CN1248683C (de)
AT (1)	ATE344029T1 (de)
AU (1)	AU2002244860B2 (de)
CA (1)	CA2443229A1 (de)
CZ (1)	CZ20032927A3 (de)
DE (1)	DE60215787T2 (de)
GB (1)	GB0109146D0 (de)
HU (1)	HUP0303876A3 (de)
IL (1)	IL157821A0 (de)
MX (1)	MXPA03009224A (de)
NO (1)	NO20034549D0 (de)
NZ (1)	NZ528172A (de)
PL (1)	PL366633A1 (de)
RU (1)	RU2328283C2 (de)
UA (1)	UA76452C2 (de)
WO (1)	WO2002083109A1 (de)
ZA (1)	ZA200307156B (de)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
CN1990468A (zh)	2001-06-27	2007-07-04	史密丝克莱恩比彻姆公司	作为二肽酶抑制剂的氟代吡咯烷
GB0125445D0 (en) *	2001-10-23	2001-12-12	Ferring Bv	Protease Inhibitors
AU2002952946A0 (en) *	2002-11-27	2002-12-12	Fujisawa Pharmaceutical Co., Ltd.	Dpp-iv inhibitor
US20040242566A1 (en)	2003-03-25	2004-12-02	Syrrx, Inc.	Dipeptidyl peptidase inhibitors
EP1625122A1 (de)	2003-05-14	2006-02-15	Takeda San Diego, Inc.	Dipeptidylpeptidase-hemmer
US6995183B2 (en)	2003-08-01	2006-02-07	Bristol Myers Squibb Company	Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods
US7169926B1 (en)	2003-08-13	2007-01-30	Takeda Pharmaceutical Company Limited	Dipeptidyl peptidase inhibitors
WO2005016911A1 (en)	2003-08-13	2005-02-24	Takeda Pharmaceutical Company Limited	4-pyrimidone derivatives and their use as peptidyl peptidase inhibitors
US7678909B1 (en)	2003-08-13	2010-03-16	Takeda Pharmaceutical Company Limited	Dipeptidyl peptidase inhibitors
US7790734B2 (en)	2003-09-08	2010-09-07	Takeda Pharmaceutical Company Limited	Dipeptidyl peptidase inhibitors
US20070149451A1 (en) *	2003-11-17	2007-06-28	Holmes David G	Combination of a dpp IV inhibitor and an antiobesity or appetite regulating agent
EP2839832A3 (de)	2003-11-17	2015-06-24	Novartis AG	Verwendung von Dipeptidylpeptidase IV-Inhibitoren
LT3366283T (lt)	2004-01-20	2021-12-10	Novartis Ag	Tiesioginio presavimo formulė ir procesas
US7732446B1 (en)	2004-03-11	2010-06-08	Takeda Pharmaceutical Company Limited	Dipeptidyl peptidase inhibitors
CN102140090A (zh)	2004-03-15	2011-08-03	武田药品工业株式会社	二肽基肽酶抑制剂
JP2008501714A (ja)	2004-06-04	2008-01-24	武田薬品工業株式会社	ジペプチジルペプチダーゼインヒビター
WO2006019965A2 (en)	2004-07-16	2006-02-23	Takeda San Diego, Inc.	Dipeptidyl peptidase inhibitors
WO2006012395A2 (en)	2004-07-23	2006-02-02	Susan Marie Royalty	Peptidase inhibitors
EP2805953B1 (de)	2004-12-21	2016-03-09	Takeda Pharmaceutical Company Limited	Dipeptidyl-Peptidase-Hemmer
DOP2006000008A (es)	2005-01-10	2006-08-31	Arena Pharm Inc	Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1
WO2006116157A2 (en)	2005-04-22	2006-11-02	Alantos Pharmaceuticals Holding, Inc.	Dipeptidyl peptidase-iv inhibitors
EP1917001A2 (de) *	2005-08-11	2008-05-07	F.Hoffmann-La Roche Ag	Pharmazeutische zusammensetzung mit einem dpp-iv-hemmer
JP5027137B2 (ja)	2005-09-14	2012-09-19	武田薬品工業株式会社	ジペプチジルペプチダーゼ阻害剤の投与
WO2007035629A2 (en)	2005-09-16	2007-03-29	Takeda Pharmaceutical Company Limited	Process for the preparation of pyrimidinedione derivatives
GB0526291D0 (en)	2005-12-23	2006-02-01	Prosidion Ltd	Therapeutic method
WO2007112347A1 (en)	2006-03-28	2007-10-04	Takeda Pharmaceutical Company Limited	Dipeptidyl peptidase inhibitors
PE20071221A1 (es)	2006-04-11	2007-12-14	Arena Pharm Inc	Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas
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
TW200838536A (en)	2006-11-29	2008-10-01	Takeda Pharmaceutical	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
US8093236B2 (en)	2007-03-13	2012-01-10	Takeda Pharmaceuticals Company Limited	Weekly administration of dipeptidyl peptidase inhibitors
EP2146210A1 (de)	2008-04-07	2010-01-20	Arena Pharmaceuticals, Inc.	Verfahren zur Verwendung eines AG-Protein-gekoppelten Rezeptors zur Identifikation von Peptid-YY (PPY)-Sekretagogen sowie Verbindungen zur Behandlung durch PYY modulierter Leiden
FR2938999B1 (fr) *	2008-11-24	2011-07-01	Oreal	Procede de preparation d'un parfum au sein d'un systeme comportant une pluralite de terminaux interactifs de formulation de parfums et un serveur agence pour echanger des donnees avec la pluralite de terminaux
AR077642A1 (es)	2009-07-09	2011-09-14	Arena Pharm Inc	Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
MX2012011631A (es)	2010-04-06	2013-01-18	Arena Pharm Inc	Moduladores del receptor gpr119 y el tratamiento de trastornos relacionados con el mismo.
KR101871011B1 (ko)	2010-09-22	2018-06-25	아레나 파마슈티칼스, 인크.	Ｇｐｒ１１９ 수용체의 조절제 및 그와 관련된 장애의 치료
WO2012135570A1 (en)	2011-04-01	2012-10-04	Arena Pharmaceuticals, Inc.	Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20140066369A1 (en)	2011-04-19	2014-03-06	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
WO2013055910A1 (en)	2011-10-12	2013-04-18	Arena Pharmaceuticals, Inc.	Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2014074668A1 (en)	2012-11-08	2014-05-15	Arena Pharmaceuticals, Inc.	Modulators of gpr119 and the treatment of disorders related thereto
GB201415598D0 (en)	2014-09-03	2014-10-15	Univ Birmingham	Elavated Itercranial Pressure Treatment
CN107683135A (zh)	2015-03-09	2018-02-09	因特克林医疗有限公司	用于治疗非酒精性脂肪肝疾病和/或脂肪营养不良的方法
WO2018162722A1 (en)	2017-03-09	2018-09-13	Deutsches Institut Für Ernährungsforschung Potsdam-Rehbrücke	Dpp-4 inhibitors for use in treating bone fractures
CA3058806A1 (en)	2017-04-03	2018-10-11	Coherus Biosciences Inc.	Ppar.gamma. agonist for treatment of progressive supranuclear palsy

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
IL111785A0 (en) *	1993-12-03	1995-01-24	Ferring Bv	Dp-iv inhibitors and pharmaceutical compositions containing them
DE19616486C5 (de) *	1996-04-25	2016-06-30	Royalty Pharma Collection Trust	Verfahren zur Senkung des Blutglukosespiegels in Säugern
TW492957B (en) *	1996-11-07	2002-07-01	Novartis Ag	N-substituted 2-cyanopyrrolidnes
US6011155A (en) *	1996-11-07	2000-01-04	Novartis Ag	N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
DE19823831A1 (de) *	1998-05-28	1999-12-02	Probiodrug Ges Fuer Arzneim	Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen
CO5150173A1 (es) *	1998-12-10	2002-04-29	Novartis Ag	Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv
JP2003518914A (ja) *	1999-02-10	2003-06-17	キュリスインコーポレイテッド	グルコース代謝障害を治療する方法および試薬
GB9906714D0 (en) *	1999-03-23	1999-05-19	Ferring Bv	Compositions for improving fertility
US6110949A (en) *	1999-06-24	2000-08-29	Novartis Ag	N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
US6107317A (en) *	1999-06-24	2000-08-22	Novartis Ag	N-(substituted glycyl)-thiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
JP2003535034A (ja) *	1999-11-12	2003-11-25	ギルフォードファーマシューティカルズインコーポレイテッド	ジペプチジルペプチダーゼｉｖ阻害剤並びにジペプチジルペプチダーゼｉｖ阻害剤の製造及び使用法
GB9928330D0 (en) *	1999-11-30	2000-01-26	Ferring Bv	Novel antidiabetic agents
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
GB0010188D0 (en) *	2000-04-26	2000-06-14	Ferring Bv	Inhibitors of dipeptidyl peptidase IV
GB0014969D0 (en) *	2000-06-19	2000-08-09	Smithkline Beecham Plc	Novel method of treatment

2001
- 2001-04-11 GB GBGB0109146.1A patent/GB0109146D0/en not_active Ceased
2002
- 2002-04-10 WO PCT/GB2002/001674 patent/WO2002083109A1/en active IP Right Grant
- 2002-04-10 JP JP2002580913A patent/JP2004525179A/ja not_active Withdrawn
- 2002-04-10 DE DE60215787T patent/DE60215787T2/de not_active Expired - Fee Related
- 2002-04-10 IL IL15782102A patent/IL157821A0/xx unknown
- 2002-04-10 AT AT02713070T patent/ATE344029T1/de not_active IP Right Cessation
- 2002-04-10 CN CNB028080955A patent/CN1248683C/zh not_active Expired - Fee Related
- 2002-04-10 HU HU0303876A patent/HUP0303876A3/hu unknown
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- 2002-04-10 AU AU2002244860A patent/AU2002244860B2/en not_active Ceased
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- 2002-04-10 RU RU2003132687/14A patent/RU2328283C2/ru not_active IP Right Cessation
- 2002-04-10 US US10/474,676 patent/US20040209891A1/en not_active Abandoned
- 2002-04-10 KR KR10-2003-7013350A patent/KR20040025915A/ko not_active Ceased
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2003
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Also Published As

Publication number	Publication date
UA76452C2 (en)	2006-08-15
EP1377278A1 (de)	2004-01-07
CN1248683C (zh)	2006-04-05
HUP0303876A3 (en)	2005-06-28
WO2002083109A1 (en)	2002-10-24
HUP0303876A2 (hu)	2004-03-01
DE60215787T2 (de)	2007-08-30
CZ20032927A3 (cs)	2004-06-16
RU2003132687A (ru)	2005-04-10
NO20034549L (no)	2003-10-09
KR20040025915A (ko)	2004-03-26
JP2004525179A (ja)	2004-08-19
NZ528172A (en)	2004-09-24
US20040209891A1 (en)	2004-10-21
CN1501796A (zh)	2004-06-02
PL366633A1 (en)	2005-02-07
CA2443229A1 (en)	2002-10-24
AU2002244860B2 (en)	2006-11-16
EP1377278B1 (de)	2006-11-02
IL157821A0 (en)	2004-03-28
GB0109146D0 (en)	2001-05-30
MXPA03009224A (es)	2004-01-29
NO20034549D0 (no)	2003-10-09
HK1059213A1 (en)	2004-06-25
ATE344029T1 (de)	2006-11-15
RU2328283C2 (ru)	2008-07-10
DE60215787D1 (de)	2006-12-14

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