ME01108B - 8-{3-amino-piperidin-1-il}-ksantini, njihovo dobijanje i njihova primjena kao dpp-iv inhibitora - Google Patents
8-{3-amino-piperidin-1-il}-ksantini, njihovo dobijanje i njihova primjena kao dpp-iv inhibitoraInfo
- Publication number
- ME01108B ME01108B MEP-2009-235A MEP23509A ME01108B ME 01108 B ME01108 B ME 01108B ME P23509 A MEP23509 A ME P23509A ME 01108 B ME01108 B ME 01108B
- Authority
- ME
- Montenegro
- Prior art keywords
- methyl
- cyano
- group
- benzyl
- pyridin
- Prior art date
Links
- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 title 1
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 title 1
- 229940065721 systemic for obstructive airway disease xanthines Drugs 0.000 title 1
- -1 benzyl - Chemical class 0.000 claims 114
- 150000001875 compounds Chemical class 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 16
- 150000007522 mineralic acids Chemical class 0.000 claims 10
- 150000007524 organic acids Chemical class 0.000 claims 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
- 239000000969 carrier Substances 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 239000003085 diluting agent Substances 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 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 claims 3
- 208000008589 Obesity Diseases 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- ISVBJQYIQQKSGK-MRXNPFEDSA-N 2-[[8-[(3r)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-2,6-dioxopurin-1-yl]methyl]pyridine-3-carbonitrile Chemical compound O=C1C=2N(CC#CC)C(N3C[C@H](N)CCC3)=NC=2N(C)C(=O)N1CC1=NC=CC=C1C#N ISVBJQYIQQKSGK-MRXNPFEDSA-N 0.000 claims 2
- LRFVTYWOQMYALW-UHFFFAOYSA-N Xanthine Natural products O=C1NC(=O)NC2=C1NC=N2 LRFVTYWOQMYALW-UHFFFAOYSA-N 0.000 claims 2
- 238000001311 chemical methods and process Methods 0.000 claims 2
- 235000005985 organic acids Nutrition 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 229940075420 xanthine Drugs 0.000 claims 2
- PEUGKEHLRUVPAN-RXMQYKEDSA-N (3r)-piperidin-3-amine Chemical compound N[C@@H]1CCCNC1 PEUGKEHLRUVPAN-RXMQYKEDSA-N 0.000 claims 1
- 125000006282 2-chlorobenzyl group Chemical group [H]C1=C([H])C(Cl)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000006494 2-trifluoromethyl benzyl group Chemical group [H]C1=C([H])C([H])=C(C(=C1[H])C([H])([H])*)C(F)(F)F 0.000 claims 1
- 125000003852 3-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(Cl)=C1[H])C([H])([H])* 0.000 claims 1
- 125000006500 3-trifluoromethoxy benzyl group Chemical group [H]C1=C([H])C(=C([H])C(OC(F)(F)F)=C1[H])C([H])([H])* 0.000 claims 1
- 125000006495 3-trifluoromethyl benzyl group Chemical group [H]C1=C([H])C(=C([H])C(=C1[H])C([H])([H])*)C(F)(F)F 0.000 claims 1
- 125000006283 4-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1Cl)C([H])([H])* 0.000 claims 1
- 125000000173 4-trifluoromethoxy benzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1OC(F)(F)F)C([H])([H])* 0.000 claims 1
- 125000001318 4-trifluoromethylbenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C([H])([H])*)C(F)(F)F 0.000 claims 1
- 102000055006 Calcitonin Human genes 0.000 claims 1
- 108060001064 Calcitonin Proteins 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- BBBFJLBPOGFECG-VJVYQDLKSA-N calcitonin Chemical compound N([C@H](C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(N)=O)C(C)C)C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 BBBFJLBPOGFECG-VJVYQDLKSA-N 0.000 claims 1
- 229960004015 calcitonin Drugs 0.000 claims 1
- 229940125904 compound 1 Drugs 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000003564 m-cyanobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(C#N)=C1[H])C([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000006505 p-cyanobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C#N)C([H])([H])* 0.000 claims 1
- PEUGKEHLRUVPAN-UHFFFAOYSA-N piperidin-3-amine Chemical compound NC1CCCNC1 PEUGKEHLRUVPAN-UHFFFAOYSA-N 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 125000000472 sulfonyl group Chemical class *S(*)(=O)=O 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
- C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/16—Masculine contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- 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
- A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/10—Antioedematous agents; Diuretics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Reproductive Health (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Virology (AREA)
- Heart & Thoracic Surgery (AREA)
- Dermatology (AREA)
- Psychiatry (AREA)
- Communicable Diseases (AREA)
- Cardiology (AREA)
- Psychology (AREA)
- Emergency Medicine (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
Claims (16)
1.Jedinjenja opšte formule u kojoj R označava benzil - , 2 - fluorbenzil - , 3 - fluorbenzil - , 4 - fluorbenzil - , 2, 6 - difluor - benzil - , 3, 4 - difluor - benzil - , 2 - hlorbenzil - , 3 - hlorbenzil - ili 4 - hlorbenzil - grupu, 2 - trifluormetil - benzil - , 3 - trifluormetil - benzil - ili 4 - trifluormetil - benzil grupu, 3 - trifluormetoksi - benzil - ili 4 - trifluormetoksi - benzil - grupu, 2 - cijanobenzil - , 3 - cijanobenzil - ili 4 - cijanobenzil - grupu, 2, 6 - dicijanobenzil - , 3, 4 - dicijanobenzil - , 3, 5 - dicijanobenzil - , 2 - trifluormetil - 4 - cijano - benzil - , 3 - nitro - 4 - cijano - benzil - , 2 - cijano - 3 - metoksi - benzil - , 2 - cijano - 4 - metoksi - benzil - , 2 - cijano - 5 - metoksi - benzil - , 2 - cijano - 4 - fluor - benzil - , 2 - cijano - 5 - fluor - benzil - , 2 - cijano - 6 - fluor - benzil - , 3 - cijano - 4 - fluor - benzil - , 4 - cijano - 3 - fluor - benzil - , 2 - fluor - 4 - cijano - benzil - , 2 - cijano - 3 - hlorbenzil - , 2 - hlor - 4 - cijano - benzil - ili 2 - cijano - 4 - brombenzil - grupu, 2 - metoksi - benzil - , 3 - metoksi - benzil - , 4 - metoksi - benzil - , 2 - fluor - 3 - metoksi - benzil - , 2 - fluor - 4 - metoksi - benzil - , 2 - fluor - 5 - metoksi - benzil - , 3 - fluor - 4 - metoksibenzil - , 3, 4 - dimetoksi - benzil - , 3, 5 - dimetoksibenzil - ili 3, 4 - dimetoksi - 6 - fluorbenzil - grupu, (benzo[1, 3]dioksol - 5 - il)metil - grupu, [(4 - cijano - benzo[1, 3]dioksol - 5 - il)metil - grupu, 2 - (3 - ciklopropiloksi - fenil) - 2 - okso - etil - , 2 - (3 - ciklopropilmetoksi - fenil) - 2 - okso - etil - ili 2 - (3 - ciklobutiloksi - fenil) - 2 - okso - etil - grupu, 2 - okso - 2 - [2 - (piridin - 3 - il) - fenil] - etil - ili 2 - okso - 2 - [2 - (piridin - 4 - il) - fenil] - etil - grupu, (3 - cijano - naftalin - 1 - il)metil - , (1, 4 - dicijano - naftalin - 2 - il)metil - ili (2, 4 - dimetoksi naftalin - 1 - il)metil - grupu, (furan - 2 - il)metil - , (furan - 3 - il)metil - , (5 - brom - furan - 2 - il)metil - , (5 - metil - furan - 2 - il)metil - , (5 - cijano - furan - 2 - il)metil - ili (5 - metoksikarbonil - furan - 2 - il)metil - grupu, (piridin - 2 - il)metil - , (6 - fluor - piridin - 2 - il)metil - ili (5 - metoksi - piridin - 2 - il)metil - grupu, (3 - cijanopiridin - 2 - il)metil - , (6 - cijanopiridin - 2 - il)metil - , (5 - cijano - piridin - 2 - il)metil - , (4 - cijano - piridin - 2 - il)metil - , (4 - cijano - piridin - 3 - il)metil - , (3 - cijano - piridin - 4 - il) - metil - , (2 - cijano - piridin - 3 - il)metil - , (2 - cijano - piridin - 4 - il)metil - , (5 - cijano - piridin - 3 - il)metil - , (6 - cijano - piridin - 3 - il)metil - ili (5 - cijano - 6 - metoksi - piridin - 2 - il)metil - grupu, (6 - fenil - piridin - 2 - il)metil - ili ([2, 2ž]bipiridinil - 6 - il)metil - grupu, (pirimidin - 2 - il)metil - , (4 - metil - pirimidin - 2 - il)metil - ili (4, 6 - dimetil - pirimidin - 2 - il)metil - grupu, (2 - fenil - pirimidin - 4 - il)metil - ili (4 - fenil - pirimidin - 2 - il)metil - grupu, [(1 - metil - 1 H - benzotriazol - 5 - il)metil] - grupu, (6 - fluor - hinolin - 2 - il)metil - , (7 - fluor - hinolin - 2 - il)metil - , (2 - metil - hinolin - 4 - il)metil - , (3 - cijano - hinolin - 2 - il)metil - , (3 - cijano - 4 - metil - hinolin - 2 - il)metil - , (4 - cijano - hinolin - 2 - il)metil - , (5 - cijano - hinolin - 2 - il)metil - , (8 - cijano - hinolin - 2 - il)metil - , (6 - amino - hinolin - 2 - il)metil - , (8 - amino - hinolin - 2 - il)metil - , (4 - metoksi - hinolin - 2 - il)metil - , (6 - metoksi - hinolin - 2 - il)metil - , (6, 7 - dimetoksi - hinolin - 2 - il)metil - ili (8 - cijano - hinolin - 7 - il)metil - grupu, (1 - cijano - izohinolin - 3 - il)metil - , (4 - cijano - izohinolin - 1 - il)metil - , (4 - cijanoizohinolin - 3 - il)metil - ili [(4 - (piridin - 2 - il) - izohinolin - 1 - il] metil - grupu, (hinazolin - 6 - il)metil - , (hinazolin - 7 - il)metil - , (2 - metil - hinazolin - 4 - il)metil - , (4, 5 - dimetil - hinazolin - 2 - il)metil - , (4 - etil - hinazolin - 2 - il)metil - , (4 - ciklopropil - hinazolin - 2 - il)metil - , (2 - fenil - hinazolin - 4 - il)metil - , (4 - cijano - hinazolin - 2 - il) - metil - , (4 - fenilamino - hinazolin - 2 - il)metil - ili (4 - benzilamino - hinazolin - 2 - il)metil - grupu, (hinoksalin - 5 - il)metil - , (hinoksalin - 6 - il)metil - ili (2, 3 - dimetil - hinoksalin - 6 - il)metil - grupu, ili ([1, 5]naftiridin - 3 - il)metil - grupu njihovi tautomeri, enantiomeri, dijastereomeri, njihove smeše i njihove soli.
2.Jedinjenja opšte formule u kojoj je R izabrano kao što je definisano u zahtevu 1, kao i njihovi tautomeri i soli.
3.Jedinjenja opšte formule u kojoj je R izabrano kao što je definisano u zahtevu 1, kao i njihovi tautomeri i soli.
4.Fiziološki prihvatljive soli jedinjenja prema jednom od zahteva 1 do 3 sa neorganskim ili organskim kiselinama.
5.Medikament koji sadrži jedinjenje prema jednom od zahteva 1 do 3 ili fiziološki prihvatljivu so prema zahtevu 4 eventualno zajedno sa jednim ili više nosača i/ili razređivača.
6.Primena jedinjenja prema najmanje jednom od zahteva 1 do 4 za dobijanje medikamenta koji je podesan za lečenje dijabetes melitusa tip I i tip II, artritisa, gojaznosti, transplantacije alografta i kalcitoninom izazvane osteoporoze.
7.Postupak za dobijanje medikamenta prema zahtevu 5, naznačen time, što se nehemijskim putem jedinjenje prema najmanje jednom od zahteva 1 do 4 inkorporira u jedan ili više inertnih nosača i/ili razređivača.
8.Postupak za dobijanje jedinjenja opšte formule 1 prema zahtevima 1 do 4, naznačen time što a) jedinjenje opšte formule u kojoj R je izabrano kao što je definisano u zahtevu 1 i Z1 predstavlja odvojivu grupu, kao što je atom halogena, supstituisana hidroksi - , merkapto - , sulfinil - , sulfonil - ili sulfoniloksi - grupa, reaguje sa 3 - aminopiperidinom, njegovim enantiomerima ili njegovim solima, ili b) jedinjenje opšte formule u kojoj je R izabrano kao što je definisano u zahtevu 1, se deprotektuje i/ili eventualno prisutne zaštitne grupe koje se koriste tokom reakcije se odvajaju i/ili ovako dobijena jedinjenja opšte formule 1 se razdvajaju na svoje enantiomere i/ili dijastereomere i/ili dobijena jedinjenja formule 1 se prevode u svoje soli, a naročito za farmaceutsku primenu u svoje fiziološki prihvatljive soli sa neorganskim ili organskim kiselinama.
9.Jedinjenje opšte formule u kojoj R označava (3 - cijanopiridin - 2 -il)metil grupu ili njegova fiziološki prihvatljiva so sa neorganskom ili organskom kiselinom.
10.Jedinjenje opšte formule u kojoj R označava (3 - cijanopiridin - 2 - il)metil grupu ili njegova fiziološki prihvatljiva so sa neorganskom ili organskom kiselinom, eventualno zajedno sa jednim ili više nosača i/ili razređivača.
11.Jedinjenje opšte formule u kojoj R označava (3 - cijanopiridin - 2 - il)metil grupu ili njegovu fiziološki prihvatljivu so sa neorganskom ili organskom kiselinom, za dobijanje farmaceutske kompozicije koja je podesna za lečenje dijabetes melitusa tipa II ili gojaznosti.
12.Postupak za dobijanje farmaceutske kompozicije prema zahtevu 10, naznačen time, što se jedinjenje opšte formule u kojoj R označava (3 - cijanopiridin - 2 - il)metil grupu ili njegova fiziološki prihvatljiva so sa neorganskom ili organskom kiselinom, inkorporira u jedan ili više inertnih nosača i/ili razređivača nehemijskim postupkom.
13.Jedinjenje 1 - [(3 - cijano - piridin - 2 - il)metil] - 3 - metil - 7 - (2 - butin - 1 - il) - 8 - ((R) - 3 - amino - piperidin - 1 - il) - ksantin u obliku fiziološki prihvatljive soli sa neorganskom ili organskom kiselinom.
14.Farmaceutska kompozicija koja sadrži 1 - [(3 - cijano - piridin - 2 - il)metil] - 3 - metil - 7 - (2 - butin - 1 - il) - 8 - ((R) - 3 - amino - piperidin - 1 - il) - ksantin u obliku fiziološki prihvatljive soli sa neorganskom ili organskom kiselinom, eventualno zajedno sa jednim ili više inertnih nosača i/ili razređivača.
15.Primena jedinjenja 1 - [(3 - cijano - piridin - 2 - il)metil] - 3 - metil - 7 - (2 - butin - 1 - il) - 8 - ((R) - 3 - amino - piperidin - 1 - il) - ksantin u obliku fiziološki prihvatljive soli sa neorganskom ili organskom kiselinom za dobijanje farmaceutske kompozicije koja je podesna za lečenje dijabetes melitusa tipa II ili gojaznosti.
16. Postupak za dobijanje farmaceutske kompozicije prema zahtevu 14, naznačen time, što se 1 - [(3 - cijano - piridin - 2 - il)metil] - 3 - metil - 7 - (2 - butin - 1 - il) - 8 - ((R) - 3 - amino - piperidin - 1 - il) - ksantin u obliku fiziološki prihvatljive soli sa neorganskom ili organskom kiselinom inkorporira u jedan ili više inertnih nosača i/ili razređivača nehemijskim postupkom.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102004008112A DE102004008112A1 (de) | 2004-02-18 | 2004-02-18 | 8-[3-Amino-piperidin-1-yl]-xanthine, deren Herstellung und Verwendung als Arzneimittel |
| DE102004012921A DE102004012921A1 (de) | 2004-03-17 | 2004-03-17 | 8-[3-Amino-piperidin-1-yl]-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
| DE102004032263A DE102004032263A1 (de) | 2004-07-03 | 2004-07-03 | 8-[3-Amino-piperidin-1yl]-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
| PCT/EP2005/001427 WO2005085246A1 (de) | 2004-02-18 | 2005-02-12 | 8-[3-amino-piperidin-1-yl]-xanthine, deren herstellung und deren verwendung als dpp-iv hemmer |
| EP05707354A EP1758905B1 (de) | 2004-02-18 | 2005-02-12 | 8-[3-amino-piperidin-1-yl]-xanthine, deren herstellung und deren verwendung als dpp-iv hemmer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME01108B true ME01108B (me) | 2013-03-20 |
Family
ID=34922894
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2009-235A ME01108B (me) | 2004-02-18 | 2005-02-12 | 8-{3-amino-piperidin-1-il}-ksantini, njihovo dobijanje i njihova primjena kao dpp-iv inhibitora |
Country Status (29)
| Country | Link |
|---|---|
| EP (2) | EP2119717B1 (me) |
| JP (2) | JP4733058B2 (me) |
| KR (1) | KR101207224B1 (me) |
| CN (1) | CN102199151A (me) |
| AR (1) | AR047614A1 (me) |
| AT (1) | ATE430150T1 (me) |
| AU (1) | AU2005219508B2 (me) |
| BR (1) | BRPI0507873B8 (me) |
| CA (1) | CA2555050C (me) |
| CY (1) | CY1109284T1 (me) |
| DE (1) | DE502005007196D1 (me) |
| DK (1) | DK1758905T3 (me) |
| EA (2) | EA010854B1 (me) |
| EC (1) | ECSP066775A (me) |
| ES (1) | ES2326666T3 (me) |
| HR (1) | HRP20090346T1 (me) |
| IL (2) | IL176920A (me) |
| ME (1) | ME01108B (me) |
| MY (1) | MY144322A (me) |
| NO (1) | NO20062688L (me) |
| NZ (1) | NZ548901A (me) |
| PE (1) | PE20060210A1 (me) |
| PL (1) | PL1758905T3 (me) |
| PT (1) | PT1758905E (me) |
| RS (1) | RS50982B (me) |
| SI (1) | SI1758905T1 (me) |
| TW (1) | TWI350756B (me) |
| UY (1) | UY28749A1 (me) |
| WO (1) | WO2005085246A1 (me) |
Families Citing this family (93)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| JP4733058B2 (ja) * | 2004-02-18 | 2011-07-27 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ８−［３−アミノ−ピペリジン−１−イル］−キサンチン、その製造及びそのｄｐｐ−ｉｖインヒビターの形態での使用 |
| 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 |
| US7393847B2 (en) | 2004-03-13 | 2008-07-01 | Boehringer Ingleheim International Gmbh | Imidazopyridazinediones, 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 |
| DE102004030502A1 (de) | 2004-06-24 | 2006-01-12 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Imidazole und Triazole, deren Herstellung und Verwendung als Arzneimittel |
| 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 |
| 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 |
| AU2012205240B2 (en) * | 2004-11-05 | 2015-03-26 | Boehringer Ingelheim International Gmbh | Method for producing chiral 8-(3-amino-piperidin-1-yl)-xanthines |
| 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 |
| GB0526291D0 (en) | 2005-12-23 | 2006-02-01 | Prosidion Ltd | Therapeutic method |
| AU2007235876A1 (en) | 2006-04-12 | 2007-10-18 | Probiodrug Ag | Enzyme inhibitors |
| KR101452915B1 (ko) | 2006-05-04 | 2014-10-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 다형태 |
| PE20110235A1 (es) * | 2006-05-04 | 2011-04-14 | Boehringer Ingelheim Int | Combinaciones farmaceuticas que comprenden linagliptina y metmorfina |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| JP2010500326A (ja) * | 2006-08-08 | 2010-01-07 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 糖尿病の治療のためのｄｐｐ−ｉｖ阻害剤としてのピロロ［３，２−ｄ］ピリミジン |
| EP2089383B1 (en) | 2006-11-09 | 2015-09-16 | 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 |
| US9126987B2 (en) | 2006-11-30 | 2015-09-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| JP5667440B2 (ja) | 2007-04-18 | 2015-02-12 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのチオ尿素誘導体 |
| BRPI0701664A2 (pt) * | 2007-05-28 | 2009-01-13 | Fundacao Universidade Fed De Sco Carlos | 4-quinolinonas e quinolinas, processo de preparaÇço, formulaÇÕes farmacÊuticas e uso das mesmas |
| CN101357922B (zh) * | 2007-08-02 | 2011-05-18 | 山东轩竹医药科技有限公司 | 新的dpp-iv抑制剂 |
| PE20090938A1 (es) * | 2007-08-16 | 2009-08-08 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo |
| UY31291A1 (es) * | 2007-08-16 | 2009-03-31 | Composicion farmacéutica que comprende un derivado de pirazol-0-glucosido | |
| BRPI0815405A2 (pt) * | 2007-08-17 | 2015-02-03 | Boehringer Ingelheim Int | Compostos derivados de purina, processo para a preparação de uma composição farmacêutica e uso dos mesmos |
| CN101952252A (zh) | 2008-02-27 | 2011-01-19 | 住友化学株式会社 | 哌啶-3-基氨基甲酸烷基酯的光学拆分方法及其中间体 |
| JP2009256298A (ja) | 2008-03-26 | 2009-11-05 | Sumitomo Chemical Co Ltd | ピペリジン−３−イルカーバメート化合物の光学分割方法およびその中間体 |
| PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| EP2108960A1 (en) | 2008-04-07 | 2009-10-14 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY |
| UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
| KR20190016601A (ko) | 2008-08-06 | 2019-02-18 | 베링거 인겔하임 인터내셔날 게엠베하 | 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료 |
| UA119131C2 (uk) * | 2008-08-15 | 2019-05-10 | Бьорінгер Інгельхайм Інтернаціональ Гмбх | Похідні пурину для застосування при лікуванні пов'язаних із fab захворювань |
| CA2736421A1 (en) | 2008-09-10 | 2010-03-18 | Boehringer Ingelheim International Gmbh | Combination therapy for the treatment of diabetes and related conditions |
| BRPI0920699A2 (pt) * | 2008-10-16 | 2020-09-01 | Boehringer Ingelheim International Gmbh | uso de um inibidor de dpp-4 no tratamento de diabetes em pacientes com controle insuficiente da glicemia apesar de terapia com um fármaco antidiabético oral ou não-oral |
| UY32177A (es) * | 2008-10-16 | 2010-05-31 | Boehringer Ingelheim Int | Tratamiento de diabetes en pacientes con control glucémico insuficiente a pesar de la terapia con fármaco, oral o no, antidiabético |
| 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 |
| JP2012512848A (ja) | 2008-12-23 | 2012-06-07 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 有機化合物の塩の形態 |
| TW201036975A (en) | 2009-01-07 | 2010-10-16 | Boehringer Ingelheim Int | Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy |
| TWI466672B (zh) | 2009-01-29 | 2015-01-01 | Boehringer Ingelheim Int | 小兒科病人糖尿病之治療 |
| BRPI1008560B1 (pt) | 2009-02-13 | 2021-08-31 | Boehringer Ingelheim International Gmbh | Composição farmacêutica compreendendo um inibidor de sglt2, um inibidor de dpp-iv e opcionalmente um outro agente antidiabético e usos dos mesmos |
| AP2011005795A0 (en) | 2009-02-13 | 2011-08-31 | Boehringer Ingelheim Int | SGLT-2 inhibitor for treating type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance or hyperglycemia. |
| EP2395988A2 (en) | 2009-02-13 | 2011-12-21 | Boehringer Ingelheim International GmbH | Antidiabetic medications comprising a dpp-4 inhibitor (linagliptin) optionally in combination with other antidiabetics |
| JP5934645B2 (ja) | 2009-09-11 | 2016-06-15 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体 |
| JP5662453B2 (ja) | 2009-10-02 | 2015-01-28 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 医薬組成物の治療上の使用 |
| KR20240090632A (ko) | 2009-11-27 | 2024-06-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 리나글립틴과 같은 ｄｐｐ－ｉｖ 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료 |
| WO2011107530A2 (en) | 2010-03-03 | 2011-09-09 | Probiodrug Ag | Novel inhibitors |
| JP5688745B2 (ja) | 2010-03-10 | 2015-03-25 | プロビオドルグ エージー | グルタミニルシクラーゼ（ｑｃ、ｅｃ２．３．２．５）の複素環阻害剤 |
| JP2013522279A (ja) | 2010-03-18 | 2013-06-13 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 糖尿病及び関連状態の治療で用いるｇｐｒ１１９作動薬とｄｄｐ−ｉｖ阻害薬リナグリプチンの組合せ |
| EP2368552A1 (en) | 2010-03-25 | 2011-09-28 | Boehringer Ingelheim Vetmedica GmbH | 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[3-(r)-amino-piperidin-1-yl]-xanthine for the treatment of a metabolic disorder of a predominantly carnivorous non-human animal |
| WO2011131748A2 (en) | 2010-04-21 | 2011-10-27 | Probiodrug Ag | Novel inhibitors |
| EA201201509A1 (ru) | 2010-05-05 | 2013-04-30 | Бёрингер Ингельхайм Интернациональ Гмбх | Фармацевтические составы, содержащие пиоглитазон и линаглиптин |
| CA3070513C (en) | 2010-05-05 | 2023-01-03 | Boehringer Ingelheim International Gmbh | A dpp-4 inhibitor for use in treatment of skin-alterations or necrosis |
| KR20130093012A (ko) | 2010-06-24 | 2013-08-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 당뇨병 요법 |
| AR083878A1 (es) | 2010-11-15 | 2013-03-27 | Boehringer Ingelheim Int | Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento |
| IT1403282B1 (it) * | 2010-12-23 | 2013-10-17 | Dipharma Francis Srl | Procedimento per la preparazione di linagliptin |
| CN102617566B (zh) * | 2011-01-30 | 2015-03-04 | 山东轩竹医药科技有限公司 | 吡啶并咪唑烷衍生物 |
| AR085689A1 (es) | 2011-03-07 | 2013-10-23 | Boehringer Ingelheim Int | Composiciones farmaceuticas de metformina, linagliptina y un inhibidor de sglt-2 |
| EP2686313B1 (en) | 2011-03-16 | 2016-02-03 | Probiodrug AG | Benzimidazole derivatives as inhibitors of glutaminyl cyclase |
| WO2012170702A1 (en) | 2011-06-08 | 2012-12-13 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| DK2731947T3 (en) | 2011-07-15 | 2019-04-23 | Boehringer Ingelheim Int | SUBSTITUTED DIMERIC QUINAZOLINE DERIVATIVE, PREPARATION AND USE thereof IN PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF TYPE I AND TYPE II DIABETES |
| AR089645A1 (es) | 2011-08-12 | 2014-09-10 | Boehringer Ingelheim Vetmed | Particula multicapas de sabor enmascarado, metodo, uso, composicion farmaceutica |
| US20130172244A1 (en) | 2011-12-29 | 2013-07-04 | Thomas Klein | Subcutaneous therapeutic use of dpp-4 inhibitor |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| WO2013171167A1 (en) | 2012-05-14 | 2013-11-21 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome |
| WO2013171166A1 (en) | 2012-05-14 | 2013-11-21 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp-4 inhibitor for use in the treatment of sirs and/or sepsis |
| JP6374862B2 (ja) * | 2012-05-24 | 2018-08-15 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 自己免疫性糖尿病、特に、ｌａｄａの治療に使用するためのｄｐｐ−４阻害剤としてのキサンチン誘導体 |
| 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 |
| JP2015518843A (ja) | 2012-05-25 | 2015-07-06 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 創傷、例えば、糖尿病性創傷の処置における、ｄｐｐ−４阻害剤と組み合わせてもよい生物活性物質としてのケラチン生成細胞の使用 |
| WO2014045266A1 (en) | 2012-09-24 | 2014-03-27 | Ulf Eriksson | Treatment of type 2 diabetes and related conditions |
| WO2014152232A2 (en) | 2013-03-15 | 2014-09-25 | Dyax Corp. | Anti-plasma kallikrein antibodies |
| EP2968344A1 (en) | 2013-03-15 | 2016-01-20 | Boehringer Ingelheim International GmbH | Use of linagliptin in cardio- and renoprotective antidiabetic therapy |
| CA2812519A1 (en) | 2013-04-05 | 2014-10-05 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| HRP20190101T1 (hr) | 2013-04-05 | 2019-03-08 | Boehringer Ingelheim International Gmbh | Terapeutske uporabe empagliflozina |
| US11813275B2 (en) | 2013-04-05 | 2023-11-14 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| US20140303097A1 (en) | 2013-04-05 | 2014-10-09 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| FI4000608T3 (fi) | 2013-04-18 | 2026-01-21 | Boehringer Ingelheim Int | Farmaseuttinen koostumus, menetelmä hoitamiseksi ja sen käyttöjä |
| US20160052903A1 (en) * | 2013-04-29 | 2016-02-25 | Archer Daniels Midland Company | 5-(hydroxymethyl) furan-2-carbaldehyde (hmf) sulfonates and process for synthesis thereof |
| EP3110449B1 (en) | 2014-02-28 | 2023-06-28 | Boehringer Ingelheim International GmbH | Medical use of a dpp-4 inhibitor |
| TWI682931B (zh) | 2015-05-29 | 2020-01-21 | 大陸商江蘇天士力帝益藥業有限公司 | 黃嘌呤衍生物、其藥物組成物、其製劑以及其用途 |
| EP4233840A3 (en) | 2016-06-10 | 2023-10-18 | Boehringer Ingelheim International GmbH | Combinations of linagliptin and metformin |
| KR20250097990A (ko) | 2016-11-10 | 2025-06-30 | 베링거 인겔하임 인터내셔날 게엠베하 | 약제학적 조성물, 치료 방법 및 이의 용도 |
| US11285180B2 (en) | 2016-12-06 | 2022-03-29 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Methods of enhancing the potency of incretin-based drugs in subjects in need thereof |
| ES2812698T3 (es) | 2017-09-29 | 2021-03-18 | Probiodrug Ag | Inhibidores de glutaminil ciclasa |
| WO2019191776A1 (en) | 2018-03-31 | 2019-10-03 | Hall John L | Selective anti-cancer agent effective for prevention and treatment |
| WO2024091863A1 (en) | 2022-10-25 | 2024-05-02 | Starrock Pharma Llc | Combinatorial, and rotational combinatorial therapies for obesity and other diseases |
| WO2025227129A2 (en) | 2024-04-25 | 2025-10-30 | Starrock Pharma Llc | Delivery vehicles comprising proglucagon derived polypeptides and anabolic polypeptides and uses thereof |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002002560A2 (en) | 2000-07-04 | 2002-01-10 | Novo Nordisk A/S | Purine-2,6-diones which are inhibitors of the enzyme dipeptidyl peptidase iv (dpp-iv) |
| KR100926247B1 (ko) * | 2001-02-24 | 2009-11-12 | 베링거 잉겔하임 파르마 게엠베하 운트 코 카게 | 크산틴 유도체를 포함하는 약제학적 조성물 및 이의제조방법 |
| WO2003004496A1 (en) * | 2001-07-03 | 2003-01-16 | Novo Nordisk A/S | Dpp-iv-inhibiting purine derivatives for the treatment of diabetes |
| EP1463727A2 (en) | 2001-09-19 | 2004-10-06 | Novo Nordisk A/S | Heterocyclic compounds that are inhibitors of the enzyme dpp-iv |
| DE60304911D1 (de) | 2002-02-25 | 2006-06-08 | Eisai Co Ltd | Xanthin-Derivate als DPP-IV-Inhibitoren |
| JP2004043429A (ja) * | 2002-02-25 | 2004-02-12 | Eisai Co Ltd | 新規キサンチン誘導体およびｄｐｐｉｖ阻害剤 |
| JP2003300977A (ja) | 2002-04-10 | 2003-10-21 | Sumitomo Pharmaceut Co Ltd | キサンチン誘導体 |
| MXPA04012226A (es) * | 2002-06-06 | 2005-04-08 | Eisai Co Ltd | Nuevos derivados de imidazola. |
| EP1532149B9 (de) * | 2002-08-21 | 2011-04-20 | Boehringer Ingelheim Pharma GmbH & Co. KG | 8-[3-amino-piperidin-1-yl] -xanthine, deren herstellung und deren verwendung als arzneimittel |
| AU2003280680A1 (en) | 2002-11-01 | 2004-06-18 | Sumitomo Pharmaceuticals Co., Ltd. | Xanthine compound |
| JP4733058B2 (ja) * | 2004-02-18 | 2011-07-27 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ８−［３−アミノ−ピペリジン−１−イル］−キサンチン、その製造及びそのｄｐｐ−ｉｖインヒビターの形態での使用 |
-
2005
- 2005-02-12 JP JP2006553504A patent/JP4733058B2/ja not_active Expired - Lifetime
- 2005-02-12 EA EA200601496A patent/EA010854B1/ru active IP Right Revival
- 2005-02-12 DE DE502005007196T patent/DE502005007196D1/de not_active Expired - Lifetime
- 2005-02-12 BR BRPI0507873A patent/BRPI0507873B8/pt not_active IP Right Cessation
- 2005-02-12 EP EP09158875.6A patent/EP2119717B1/de not_active Expired - Lifetime
- 2005-02-12 SI SI200530736T patent/SI1758905T1/sl unknown
- 2005-02-12 WO PCT/EP2005/001427 patent/WO2005085246A1/de not_active Ceased
- 2005-02-12 NZ NZ548901A patent/NZ548901A/en not_active IP Right Cessation
- 2005-02-12 RS RSP-2009/0303A patent/RS50982B/sr unknown
- 2005-02-12 PL PL05707354T patent/PL1758905T3/pl unknown
- 2005-02-12 ME MEP-2009-235A patent/ME01108B/me unknown
- 2005-02-12 DK DK05707354T patent/DK1758905T3/da active
- 2005-02-12 ES ES05707354T patent/ES2326666T3/es not_active Expired - Lifetime
- 2005-02-12 EA EA200801601A patent/EA200801601A1/ru unknown
- 2005-02-12 CA CA2555050A patent/CA2555050C/en not_active Expired - Lifetime
- 2005-02-12 AT AT05707354T patent/ATE430150T1/de active
- 2005-02-12 EP EP05707354A patent/EP1758905B1/de not_active Expired - Lifetime
- 2005-02-12 PT PT05707354T patent/PT1758905E/pt unknown
- 2005-02-12 CN CN2011100842167A patent/CN102199151A/zh active Pending
- 2005-02-12 AU AU2005219508A patent/AU2005219508B2/en not_active Expired
- 2005-02-12 HR HR20090346T patent/HRP20090346T1/hr unknown
- 2005-02-15 UY UY28749A patent/UY28749A1/es not_active Application Discontinuation
- 2005-02-16 MY MYPI20050575A patent/MY144322A/en unknown
- 2005-02-16 PE PE2005000183A patent/PE20060210A1/es not_active Application Discontinuation
- 2005-02-17 TW TW094104568A patent/TWI350756B/zh not_active IP Right Cessation
- 2005-02-18 AR ARP050100578A patent/AR047614A1/es active IP Right Grant
-
2006
- 2006-06-09 NO NO20062688A patent/NO20062688L/no not_active Application Discontinuation
- 2006-07-18 IL IL176920A patent/IL176920A/en active IP Right Grant
- 2006-08-18 EC EC2006006775A patent/ECSP066775A/es unknown
- 2006-09-18 KR KR1020067019124A patent/KR101207224B1/ko not_active Expired - Lifetime
-
2009
- 2009-07-23 CY CY20091100791T patent/CY1109284T1/el unknown
-
2010
- 2010-08-09 JP JP2010178510A patent/JP2011006437A/ja active Pending
-
2011
- 2011-12-29 IL IL217268A patent/IL217268A0/en unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ME01108B (me) | 8-{3-amino-piperidin-1-il}-ksantini, njihovo dobijanje i njihova primjena kao dpp-iv inhibitora | |
| JP5650735B2 (ja) | タンパク質キナーゼ調節剤としてのピリジンおよびピラジン誘導体 | |
| DE60311820T2 (de) | Neue verwendung von pyrimidin- oder triazin-2-carbonsäurenitrilen zur behandlung von krankheiten, die mit cysteinproteaseaktivität assoziiert sind, und neue pyridimidin-2-carbonsäurenitrilderivate | |
| EP1532150B1 (de) | Neue purinderivate, deren herstelllung und deren verwendung als arzneimittel | |
| DE60203260T2 (de) | Pharmazeutische kombination, die ein 4-chinazolinamin und paclitaxel, carboplatin oder vinorelbin enthält, zur behandlung von krebs | |
| JP2006508969A5 (me) | ||
| JP2025090577A (ja) | Ｔｙｋ２阻害剤およびその使用 | |
| DE60219887T2 (de) | N-(3,-Dimethylindolin-6-yl)ä2-ä(4-pyridylmethyl)aminoü(3-pyridyl)ücarbonsäureamid und dieses enthaltende pharmazeutische Zubereitungen. | |
| CN100519549C (zh) | 嘧啶化合物以及含有该化合物的药物组合物 | |
| DE602004009089T2 (de) | Pyrrolderivate mit antibakterieller wirkung | |
| US7560450B2 (en) | Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions | |
| EP2287164B1 (de) | Verfahren zur Herstellung chiraler 8-(3-amino-piperidin-1yl)-Xanthine | |
| DE60206756T2 (de) | Purin derivate als a2b adenosin rezeptor antagonisten | |
| US20050004125A1 (en) | Heteroaryl amines as glycogen synthase kinase 3beta inhibitors (gsk3 inhibitors) | |
| DE60211539T2 (de) | Imidazopyridinderivate zur verwendung bei der behandlung von herpes-vireninfektion | |
| CZ305402B6 (cs) | Xanthinové deriváty, jejich výroba a použití v kombinační terapii | |
| WO2004018467A2 (de) | Phenacylxanthinderivate als dpp-iv-hemmer | |
| WO2012101064A1 (en) | N-acyl pyrimidine biaryl compounds as protein kinase inhibitors | |
| EP1644358A2 (en) | Biaryl piperazinyl-pyridine analogues | |
| KR20020015060A (ko) | 축합 이미다졸 화합물 및 당뇨병 치료약 | |
| JP2006512311A (ja) | キサンチン誘導体、その製法及びその医薬組成物としての使用 | |
| BR122022001938B1 (pt) | Composto derivado de amina heterocíclica, composição farmacêutica compreendendo o mesmo e uso do dito composto para prevenir ou tratar doenças autoimunes ou cânceres | |
| DE102004061593A1 (de) | Substituierte N-heterocyclische Verbindungen und ihre therapeutische Verwendung | |
| DE60314105T2 (de) | Alkylammoniumsalze von omeprazol und esomeprazol | |
| CN114502174A (zh) | 2,4,7取代的-7-脱氮-2′-脱氧-2′-氟阿拉伯糖基核苷和核苷酸前药及其用途 |