HRP20090346T1 - 8-[3-amino-piperidin-1-il]-ksantin, njihova priprava i uporaba ka ddp-iv inhibitora - Google Patents
8-[3-amino-piperidin-1-il]-ksantin, njihova priprava i uporaba ka ddp-iv inhibitora Download PDFInfo
- Publication number
- HRP20090346T1 HRP20090346T1 HR20090346T HRP20090346T HRP20090346T1 HR P20090346 T1 HRP20090346 T1 HR P20090346T1 HR 20090346 T HR20090346 T HR 20090346T HR P20090346 T HRP20090346 T HR P20090346T HR P20090346 T1 HRP20090346 T1 HR P20090346T1
- Authority
- HR
- Croatia
- Prior art keywords
- methyl
- cyano
- benzyl
- group
- pyridin
- Prior art date
Links
- 238000004519 manufacturing process Methods 0.000 title claims 2
- WNHHLYZOSOUUQW-UHFFFAOYSA-N 8-(3-aminopiperidin-1-yl)-3,7-dihydropurine-2,6-dione Chemical compound C1C(N)CCCN1C(N1)=NC2=C1C(=O)NC(=O)N2 WNHHLYZOSOUUQW-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- -1 2 , 6-dicyanobenzyl Chemical group 0.000 claims abstract 174
- 150000001875 compounds Chemical class 0.000 claims abstract 18
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract 10
- 125000006508 2,6-difluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C(F)=C1[H])C([H])([H])* 0.000 claims abstract 2
- 125000006282 2-chlorobenzyl group Chemical group [H]C1=C([H])C(Cl)=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract 2
- 125000004847 2-fluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract 2
- 125000002927 2-methoxybenzyl group Chemical group [H]C1=C([H])C([H])=C(C(OC([H])([H])[H])=C1[H])C([H])([H])* 0.000 claims abstract 2
- 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 abstract 2
- 125000006509 3,4-difluorobenzyl group Chemical group [H]C1=C(F)C(F)=C([H])C(=C1[H])C([H])([H])* 0.000 claims abstract 2
- 125000003852 3-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(Cl)=C1[H])C([H])([H])* 0.000 claims abstract 2
- 125000006284 3-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(F)=C1[H])C([H])([H])* 0.000 claims abstract 2
- 125000006497 3-methoxybenzyl group Chemical group [H]C1=C([H])C(=C([H])C(OC([H])([H])[H])=C1[H])C([H])([H])* 0.000 claims abstract 2
- 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 abstract 2
- 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 abstract 2
- 125000006283 4-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1Cl)C([H])([H])* 0.000 claims abstract 2
- 125000004176 4-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1F)C([H])([H])* 0.000 claims abstract 2
- 125000004217 4-methoxybenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1OC([H])([H])[H])C([H])([H])* 0.000 claims abstract 2
- 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 abstract 2
- 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 abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract 2
- 125000003564 m-cyanobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(C#N)=C1[H])C([H])([H])* 0.000 claims abstract 2
- 125000006504 o-cyanobenzyl group Chemical group [H]C1=C([H])C(C#N)=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract 2
- 125000006505 p-cyanobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C#N)C([H])([H])* 0.000 claims abstract 2
- 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
- 239000000825 pharmaceutical preparation Substances 0.000 claims 9
- 239000003085 diluting agent Substances 0.000 claims 6
- 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 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
- 238000001311 chemical methods and process Methods 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- 238000002360 preparation method Methods 0.000 claims 3
- 235000005985 organic acids Nutrition 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 125000002774 3,4-dimethoxybenzyl group Chemical group [H]C1=C([H])C(=C([H])C(OC([H])([H])[H])=C1OC([H])([H])[H])C([H])([H])* 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
- 239000000969 carrier Substances 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- PEUGKEHLRUVPAN-UHFFFAOYSA-N piperidin-3-amine Chemical compound NC1CCCNC1 PEUGKEHLRUVPAN-UHFFFAOYSA-N 0.000 claims 1
- 239000000758 substrate Substances 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 abstract 1
- MMZHUJNATIRHPO-UHFFFAOYSA-N 4-pyridin-2-ylisoquinoline Chemical compound N1=CC=CC=C1C1=CN=CC2=CC=CC=C12 MMZHUJNATIRHPO-UHFFFAOYSA-N 0.000 abstract 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
Abstract
Spojevi, naznačeni time, da su opće formulegdje R je benzil, 2-fluorbenzil, 3-fluorbenzil, 4-fluorbenzil, 2, 6-difluor-benzil, 3, 4-difluor-benzil, 2-klorbenzil, 3-klorbenzil ili 4-klorbenzil skupina, 2-trifluormetil-benzil, 3-trifluormetil-benzil ili 4-trifluormetil-benzil skupina, 3-trifluormetoksi-benzil ili 4-trifluormetoksi-benzil skupina, 2-cijanobenzil, 3-cijanobenzil ili 4-cijanobenzil skupina, 2,6-dicijanobenzil, 3,4-dicijanobenzil, 3,5-dicijanobenzil, 2-trifluormetil-4cijano-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-fluorbenzil, 2-fluor-4-cijano-benzil, 2-cijano-3-klorbenzil, 2-klor-4-cijano-benzil ili 2-cijano-4-brombenzil skupina, 2-metoksi-benzil, 3-metoksi-benzil, 4-metoksi-benzil, 2-fluor-3-metoksi- benzil, 2-fluor-4-metoksi-benzilf, 2-fluor-5-metoksi-benzil, 3-fluor-4-metoksibenzil, 3,4-dimetoksi-benzil, 3,5-dimetoksibenzil ili 3,4-dimetoksi-6-fluorbenzil skupina, (benzo[1,3]dioksol-5-il)metil skupina, (4-cijano-benzo[1,3]dioksol-5-il) metil skupina, 2-(3-ciklopropiloksi-fenil)-2-okso-etil, 2-(3-ciklopropilmetoksi-fenil)-2-okso-etil ili 2-(3-ciklobutiloksi-fenil)-2-okso-etil skupina, 2-okso-2-[2-(piridin-3-il)-fenil]-etil ili 2-okso-2-[2-(piridin-4-il)-fenil]-etil skupina, (3-cijano-naftalen-1-il)metil, (1 4-dicijano-naftalen-2-il)metil ili (2,4-dimetoksi-naftalen-1-il) metil skupina, (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 skupina, (piridin-2-il)metil, (6-fluor-piridin-2-il)metil ili (5-metoksi-piridin-2-il)metil skupina, (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 skupina, (6-fenil-piridin-2-il)metil ili ([2,2']bipiridinil-6-il)metil skupina, (pirimidin-2-il) metil, (4-metil-pirimidin-2-il)metil ili (4,6-dimetil-pirimidin-2-il)metil skupina, (2-fenil-pirimidin-4-il)metil ili (4-fenil-pirimidin-2-il)metil skupina, [(1-metil-1H-benzotriazol-5-il)metil] skupina, (6-fluor-kinolin-2-il)metil, (7-fluor-kinolin-2-il)metil, (2-metil-kinolin-4-il)metil, (3-cijano-kinolin-2-il)metil, (3-cijano-4-metil-kinolin-2-il)metil, (4-cijano-kinolin-2-il)metil, (5-cijano-kinolin-2-il)metil, (8-cijano-kinolin-2- il)metil, (6-amino-kinolin-2-il)metil, (8-amino-kinolin-2-il)metil-, (4-metoksi-kinolin-2-il)metil, (6-metoksi-kinolin-2-il)metil, (6,7-dimetoksi- kinolin-2-il)metil ili (8-cijano-kinolin-7-il)metil skupina, (1-cijano-izokinolin-3-il)metil, (4-cijano-izokinolin-1-il)metil, (4-cijano-izokinolin-3-il) metil ili [(4-(piridin-2-il)-izokinolin-1-il]metil
Claims (16)
1. Spojevi, naznačeni time, da su opće formule
[image]
gdje R je benzil, 2-fluorbenzil, 3-fluorbenzil, 4-fluorbenzil, 2, 6-difluor-benzil, 3, 4-difluor-benzil, 2-klorbenzil, 3-klorbenzil ili 4-klorbenzil skupina,
2-trifluormetil-benzil, 3-trifluormetil-benzil ili 4-trifluormetil-benzil skupina,
3-trifluormetoksi-benzil ili 4-trifluormetoksi-benzil skupina,
2-cijanobenzil, 3-cijanobenzil ili 4-cijanobenzil skupina,
2,6-dicijanobenzil, 3,4-dicijanobenzil, 3,5-dicijanobenzil, 2-trifluormetil-4cijano-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-fluorbenzil, 2-fluor-4-cijano-benzil, 2-cijano-3-klorbenzil, 2-klor-4-cijano-benzil ili 2-cijano-4-brombenzil skupina,
2-metoksi-benzil, 3-metoksi-benzil, 4-metoksi-benzil, 2-fluor-3-metoksi- benzil, 2-fluor-4-metoksi-benzilf, 2-fluor-5-metoksi-benzil, 3-fluor-4-metoksibenzil, 3,4-dimetoksi-benzil, 3,5-dimetoksibenzil ili 3,4-dimetoksi-6-fluorbenzil skupina,
(benzo[1,3]dioksol-5-il)metil skupina,
[(4-cijano-benzo[1,3]dioksol-5-il) metil skupina,
2-(3-ciklopropiloksi-fenil)-2-okso-etil, 2-(3-ciklopropilmetoksi-fenil)-2-okso-etil ili 2-(3-ciklobutiloksi-fenil)-2-okso-etil skupina,
2-okso-2-[2-(piridin-3-il)-fenil]-etil ili 2-okso-2-[2-(piridin-4-il)-fenil]-etil skupina,
(3-cijano-naftalen-1-il)metil, (1 4-dicijano-naftalen-2-il)metil ili (2,4-dimetoksi-naftalen-1-il) metil skupina,
(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 skupina,
(piridin-2-il)metil, (6-fluor-piridin-2-il)metil ili (5-metoksi-piridin-2-il)metil skupina,
(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 skupina,
(6-fenil-piridin-2-il)metil ili ([2,2']bipiridinil-6-il)metil skupina,
(pirimidin-2-il) metil, (4-metil-pirimidin-2-il)metil ili (4,6-dimetil-pirimidin-2-il)metil skupina,
(2-fenil-pirimidin-4-il)metil ili (4-fenil-pirimidin-2-il)metil skupina,
[(1-metil-1H-benzotriazol-5-il)metil] skupina,
(6-fluor-kinolin-2-il)metil, (7-fluor-kinolin-2-il)metil, (2-metil-kinolin-4-il)metil, (3-cijano-kinolin-2-il)metil, (3-cijano-4-metil-kinolin-2-il)metil, (4-cijano-kinolin-2-il)metil, (5-cijano-kinolin-2-il)metil, (8-cijano-kinolin-2- il)metil, (6-amino-kinolin-2-il)metil, (8-amino-kinolin-2-il)metil-, (4-metoksi-kinolin-2-il)metil, (6-metoksi-kinolin-2-il)metil, (6,7-dimetoksi- kinolin-2-il)metil ili (8-cijano-kinolin-7-il)metil skupina,
(1-cijano-izokinolin-3-il)metil, (4-cijano-izokinolin-1-il)metil, (4-cijano-izokinolin-3-il) metil ili [(4-(piridin-2-il)-izokinolin-1-il]metil skupina,
(kinazolin-6-il)metil, (kinazolin-7-il)metil, (2-metil-kinazolin-4-il)metil, (4,5-dimetil-kinazolin-2-il)metil, (4-etil-kinazolin-2-il)metil, (4-ciklopropil-kinazolin-2-il)metil, (2-fenil-kinazolin-4-il)metil, (4-cijano-kinazolin-2-il)metil, (4-fenilamino-kinazolin-2-il)metil ili (4-benzilamino-kinazolin-2-il)metil skupina,
(kinoksalin-5-il)metil, (kinoksalin-6-il)metil ili (2,3-dimetil-kinoksalin-6-il)metil skupina, ili
([1,5]naftiridin-3-il)metil skupina
njihovi tautomeri, enantiomeri, dijastereomeri, njihove smjese i soli.
2. Spoj, naznačen time, da je opće formule
[image]
gdje je R isti kao određen u zahtjevu 1, i njegovi tautomeri i njegove soli.
3. Spoj, naznačen time, da je opće formule
[image]
gdje je R isti kao određen u zahtjevu 1, i njegovi tautomeri i njegove soli.
4. Fiziološki prihvatljive solispojeva prema bilo kojem zahtjevu 1 do 3, naznačene time, da su soli s anorganskim i organskim kiselinama.
5. Farmaceutski pripravci, naznačeni time, da sadrže spoj prema barem jednom zahtjevu 1 do 3 ili fiziološki prihvatljivu sol prema zahtjevu 4 po izboru skupa s jednom ili više inertnih podloga i/ili sredstava za razrijeđivanje.
6. Uporaba spoja prema barem jednom zahtjevu 1 do 4, naznačena time, da se koristi za pripravu farmaceutskog pripravka koji je prikladan za liječenje dijabetesa tipa I i II, artritisa, debljine, odbacivanja tkiva nakon transplatacije i kalcitonin-inducirane osteoporoze.
7. Postupak priprave farmaceutskog pripravka prema zahtjevu 5, naznačen time, da se spoj prema barem jednom zahtjevu 1 do 4 ugrađuje u jednu ili više podloga i/ili sredstava za razrijeđivanje nekemijskim postupkom.
8. Postupak priprave spojeva opće formule I prema zahtjevima 1 do 4, naznačen time, da
a) spoj opće formule
[image]
gdje
R je definiran kao u zahtjevu 1 i
Z' predstavlja otpuštajuću skupinu kao što je atom halogena, supstituirana hidroksi, merkapto, sulfinil, sulfonil ili sulfoniloksi skupina,
reagira s 3-aminopiperidinom, njegovim enantiomerima ili solima, ili
b) spoju opće formule
[image]
gdje
R je definiran kao u zahtjevu 1 se uklanjaju zaštitne skupine,
i/ili
se bilo koja zaštitna skupina korištena za vrijeme reakcije otcjepljuje i/ili
se tako dobiveni spojevi opće formule I odjele u svoje enantiomere i/ili dijastereomere i/ili se tako dobiveni spojevi formule I prevedu u svoje soli, posebno za farmaceutsku uporabu u fiziološki prihvatljive soli s anorganskim ili organskim kiselinama.
9. Spoj, naznačen time, da je opće formule
[image]
gdje R označava (3-cijanopiridin-2-il)metil skupinu
ili njegova fiziološki prihvatljiva sol s anorganskom ili organskom kiselinom.
10. Farmaceutski pripravak, naznačen time, da sadrži spoj opće formule
[image]
gdje R označava (3-cijanopiridin-2-il)metil skupinu
ili njegovu fiziološki prihvatljivu sol s anorganskom ili organskom kiselinom, po izboru skupa s jednom ili više inertnih podloga i/ili sredstava za razrijeđivanje.
11. Uporaba spoja opće formule
[image]
gdje R označava (3-cijanopiridin-2-il)metil skupinu ili njegove fiziološki prihvatljive soli s anorganskom ili organskom kiselinom, naznačena time, da se koristi za pripravu farmaceutskog pripravka prikladnog za liječenje diabetes mellitusa tipa II ili debljine.
12. Postupak priprave farmaceutskog pripravka u skladu sa zahtjevom 10, naznačen time, da se spoj opće formule
[image]
gdje R označava (3-cijanopiridin-2-il)metil skupinu ili njegova fiziološki prihvatljiva sol s anorganskom ili organskom kiselinom ugrađuje u jednu ili više inertnih podloga i/ili sredstava za razrijeđivanje ne-kemijskim postupkom.
13. Spoj, naznačen time, da je 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 s anorganskom ili organskom kiselinom.
14. Farmaceutski pripravak, naznačen time, da 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 s anorganskom ili organskom kiselinom, po izboru skupa s jednom ili više inertnih podloga i/ili sredstava za razrijeđivanje.
15. Uporaba spoja 1-[(3-cijano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)-ksantina u obliku fiziološki prihvatljive soli s anorganskom ili organskom kiselinom, naznačena time, da se koristi za pripravu farmaceutskog pripravka prikladnog za liječenje diabetes mellitusa tipa II ili debljine.
16. Postupak priprave farmaceutskog pripravka u skladu sa zahtjevom 14, naznačen time, da 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 s anorganskom ili organskom kiselinom ugrađuje u jednu ili više inertnih podloga i/ili sredstava za razrijeđivanje ne-kemijskim postupkom.
Applications Claiming Priority (4)
| 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20090346T1 true HRP20090346T1 (hr) | 2009-08-31 |
Family
ID=34922894
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20090346T HRP20090346T1 (hr) | 2004-02-18 | 2009-06-15 | 8-[3-amino-piperidin-1-il]-ksantin, njihova priprava i uporaba ka ddp-iv inhibitora |
Country Status (30)
| Country | Link |
|---|---|
| EP (2) | EP2119717B1 (hr) |
| JP (2) | JP4733058B2 (hr) |
| KR (1) | KR101207224B1 (hr) |
| CN (1) | CN102199151A (hr) |
| AR (1) | AR047614A1 (hr) |
| AT (1) | ATE430150T1 (hr) |
| AU (1) | AU2005219508B2 (hr) |
| BR (1) | BRPI0507873B8 (hr) |
| CA (1) | CA2555050C (hr) |
| CY (1) | CY1109284T1 (hr) |
| DE (1) | DE502005007196D1 (hr) |
| DK (1) | DK1758905T3 (hr) |
| EA (2) | EA010854B1 (hr) |
| EC (1) | ECSP066775A (hr) |
| ES (1) | ES2326666T3 (hr) |
| HK (1) | HK1103402A1 (hr) |
| HR (1) | HRP20090346T1 (hr) |
| IL (2) | IL176920A (hr) |
| ME (1) | ME01108B (hr) |
| MY (1) | MY144322A (hr) |
| NO (1) | NO20062688L (hr) |
| NZ (1) | NZ548901A (hr) |
| PE (1) | PE20060210A1 (hr) |
| PL (1) | PL1758905T3 (hr) |
| PT (1) | PT1758905E (hr) |
| RS (1) | RS50982B (hr) |
| SI (1) | SI1758905T1 (hr) |
| TW (1) | TWI350756B (hr) |
| UY (1) | UY28749A1 (hr) |
| WO (1) | WO2005085246A1 (hr) |
Families Citing this family (86)
| 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 |
| 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 |
| US7495005B2 (en) | 2002-08-22 | 2009-02-24 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Xanthine derivatives, their preparation and their use in 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 |
| EP2119717B1 (de) * | 2004-02-18 | 2018-01-17 | Boehringer Ingelheim International GmbH | 8-[3-amino-piperidin-1-yl]-Xanthine, deren Herstellung und deren Verwendung als DPP IV Hemmer |
| 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 |
| JP2009533393A (ja) | 2006-04-12 | 2009-09-17 | プロビオドルグ エージー | 酵素阻害薬 |
| EP1852108A1 (en) * | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| EP2540725A1 (de) | 2006-05-04 | 2013-01-02 | Boehringer Ingelheim International GmbH | Polymorphe von 1-((4-Methyl-chinazolin-2-yl)methyl)-3-methyl-7-(2-butin-1-yl)-8-(3-(R)-amino-piperidin-1-yl)xanthin |
| US8071583B2 (en) | 2006-08-08 | 2011-12-06 | Boehringer Ingelheim International Gmbh | Pyrrolo[3,2-D] pyrimidines as DPP-IV inhibitors for the treatment of diabetes mellitus |
| JP5379692B2 (ja) | 2006-11-09 | 2013-12-25 | プロビオドルグ エージー | 潰瘍、癌及び他の疾患の治療のためのグルタミニルシクラーゼの阻害薬としての３−ヒドロキシ−１，５−ジヒドロ−ピロール−２−オン誘導体 |
| US9126987B2 (en) | 2006-11-30 | 2015-09-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| DK2142514T3 (da) | 2007-04-18 | 2015-03-23 | Probiodrug Ag | Thioureaderivater som glutaminylcyclase-inhibitorer |
| 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 |
| PE20090597A1 (es) * | 2007-08-16 | 2009-06-06 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un derivado de pirazol-o-glucosido |
| EP3542801A1 (en) * | 2007-08-17 | 2019-09-25 | Boehringer Ingelheim International GmbH | Purin derivatives for use in the treatment of fap-related diseases |
| WO2009107571A1 (ja) | 2008-02-27 | 2009-09-03 | 住友化学株式会社 | アルキルピペリジン－３－イルカーバメートの光学分割方法およびその中間体 |
| 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 |
| PE20140960A1 (es) | 2008-04-03 | 2014-08-15 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| EP2146210A1 (en) | 2008-04-07 | 2010-01-20 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY |
| 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" |
| PE20110297A1 (es) * | 2008-08-15 | 2011-05-26 | Boehringer Ingelheim Int | Inhibidores de dpp-4 para la cicatrizacion de heridas |
| RU2011113823A (ru) | 2008-09-10 | 2012-10-20 | БЕРИНГЕР ИНГЕЛЬХАЙМ ИНТЕРНАЦИОНАЛЬ ГмбХ (DE) | Комбинированная терапия, предназначенная для лечения диабета и связанных с ним состояний |
| 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 |
| 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 |
| 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 |
| CA2752437C (en) | 2009-02-13 | 2017-07-11 | Boehringer Ingelheim International Gmbh | Antidiabetic medications |
| NZ594487A (en) | 2009-02-13 | 2013-11-29 | Boehringer Ingelheim Int | Pharmaceutical composition comprising a sglt2 inhibitor, a dpp-iv inhibitor and optionally a further antidiabetic agent and uses thereof |
| EA022007B1 (ru) | 2009-09-11 | 2015-10-30 | Пробиодруг Аг | Гетероциклические производные в качестве ингибиторов глутаминилциклазы |
| CN102596191B (zh) | 2009-10-02 | 2016-12-21 | 勃林格殷格翰国际有限公司 | 包含bi‑1356和二甲双胍的药物组合物 |
| NZ599298A (en) | 2009-11-27 | 2014-11-28 | Boehringer Ingelheim Int | Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin |
| EP2542549B1 (en) | 2010-03-03 | 2016-05-11 | Probiodrug AG | Inhibitors of glutaminyl cyclase |
| EA022420B1 (ru) | 2010-03-10 | 2015-12-30 | Пробиодруг Аг | Гетероциклические ингибиторы глутаминилциклазы (qc, ec 2.3.2.5) |
| WO2011113947A1 (en) | 2010-03-18 | 2011-09-22 | Boehringer Ingelheim International Gmbh | Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions |
| 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 |
| JP5945532B2 (ja) | 2010-04-21 | 2016-07-05 | プロビオドルグ エージー | グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体 |
| EA201201509A1 (ru) | 2010-05-05 | 2013-04-30 | Бёрингер Ингельхайм Интернациональ Гмбх | Фармацевтические составы, содержащие пиоглитазон и линаглиптин |
| JP6034781B2 (ja) | 2010-05-05 | 2016-11-30 | 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 | 併用療法 |
| EP3725325B1 (en) | 2010-06-24 | 2023-05-31 | Boehringer Ingelheim International GmbH | Diabetes therapy |
| US9034883B2 (en) | 2010-11-15 | 2015-05-19 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
| 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 |
| 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 |
| US8530670B2 (en) | 2011-03-16 | 2013-09-10 | Probiodrug Ag | Inhibitors |
| 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 |
| BR112014003061A2 (pt) | 2011-08-12 | 2017-02-21 | Boehringer Ingelheim Vetmedica Gmbh | composição farmacêutica com sabor mascarado |
| 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 |
| ES2929025T3 (es) * | 2012-05-14 | 2022-11-24 | Boehringer Ingelheim Int | Linagliptina, un derivado de xantina como inhibidor de dpp-4, para su uso en el tratamiento del SRIS y/o de la septicemia |
| EP2849755A1 (en) | 2012-05-14 | 2015-03-25 | Boehringer Ingelheim International GmbH | A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome |
| 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 |
| WO2013174768A1 (en) | 2012-05-24 | 2013-11-28 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in the treatment of autoimmune diabetes, particularly lada |
| EP2854824A1 (en) | 2012-05-25 | 2015-04-08 | Boehringer Ingelheim International GmbH | Use of keratinocytes as a biologically active substance in the treatment of wounds, such as diabetic wounds, optionally in combination with a dpp-4 inhibitor |
| WO2014045266A1 (en) | 2012-09-24 | 2014-03-27 | Ulf Eriksson | Treatment of type 2 diabetes and related conditions |
| US20140303098A1 (en) | 2013-04-05 | 2014-10-09 | 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 |
| US11813275B2 (en) | 2013-04-05 | 2023-11-14 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| ES2906115T3 (es) | 2013-04-18 | 2022-04-13 | Boehringer Ingelheim Int | Composición farmacéutica, métodos de tratamiento y usos de la misma |
| MX2015015103A (es) * | 2013-04-29 | 2016-02-11 | Archer Daniels Midland Co | Sulfonatos de 5- (hidroximetil) furan-2-carbaldehido (hmf) y procesos para su sintesis. |
| JP6615109B2 (ja) | 2014-02-28 | 2019-12-04 | 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 | Ｄｐｐ−４阻害薬の医学的使用 |
| CN106188058B (zh) * | 2015-05-29 | 2020-11-06 | 江苏天士力帝益药业有限公司 | 黄嘌呤衍生物 |
| CA3022202A1 (en) | 2016-06-10 | 2017-12-14 | Boehringer Ingelheim International Gmbh | Combinations of linagliptin and metformin |
| EP3551202B1 (en) | 2016-12-06 | 2024-01-24 | INSERM (Institut National de la Santé et de la Recherche Médicale) | 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 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU6895801A (en) | 2000-07-04 | 2002-01-14 | Novo Nordisk As | Heterocyclic compounds, which are inhibitors of the enzyme dpp-iv |
| DK1953162T3 (da) | 2001-02-24 | 2012-09-10 | Boehringer Ingelheim Pharma | Xanthinderivater, deres fremstilling og deres anvendelse som lægemiddel. |
| JP2005502624A (ja) * | 2001-07-03 | 2005-01-27 | ノボ ノルディスク アクティーゼルスカブ | 糖尿病を治療するための、ｄｐｐ−ｉｖを阻害するプリン誘導体 |
| JP2005509603A (ja) | 2001-09-19 | 2005-04-14 | ノボ ノルディスク アクティーゼルスカブ | Ｄｐｐ−ｉｖ酵素の阻害剤であるヘテロ環化合物 |
| 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 |
| DE60304911D1 (de) | 2002-02-25 | 2006-06-08 | Eisai Co Ltd | Xanthin-Derivate als DPP-IV-Inhibitoren |
| JP2003300977A (ja) | 2002-04-10 | 2003-10-21 | Sumitomo Pharmaceut Co Ltd | キサンチン誘導体 |
| NZ536794A (en) * | 2002-06-06 | 2007-04-27 | Eisai Co Ltd | Condensed imidazole derivatives |
| EP3424926A1 (de) * | 2002-08-21 | 2019-01-09 | 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 |
| EP2119717B1 (de) * | 2004-02-18 | 2018-01-17 | Boehringer Ingelheim International GmbH | 8-[3-amino-piperidin-1-yl]-Xanthine, deren Herstellung und deren Verwendung als DPP IV Hemmer |
-
2005
- 2005-02-12 EP EP09158875.6A patent/EP2119717B1/de active Active
- 2005-02-12 DE DE502005007196T patent/DE502005007196D1/de active Active
- 2005-02-12 AT AT05707354T patent/ATE430150T1/de active
- 2005-02-12 SI SI200530736T patent/SI1758905T1/sl unknown
- 2005-02-12 CA CA2555050A patent/CA2555050C/en active Active
- 2005-02-12 EP EP05707354A patent/EP1758905B1/de active Active
- 2005-02-12 PT PT05707354T patent/PT1758905E/pt unknown
- 2005-02-12 CN CN2011100842167A patent/CN102199151A/zh active Pending
- 2005-02-12 RS RSP-2009/0303A patent/RS50982B/sr unknown
- 2005-02-12 WO PCT/EP2005/001427 patent/WO2005085246A1/de active Application Filing
- 2005-02-12 NZ NZ548901A patent/NZ548901A/en unknown
- 2005-02-12 AU AU2005219508A patent/AU2005219508B2/en active Active
- 2005-02-12 EA EA200601496A patent/EA010854B1/ru active IP Right Revival
- 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 JP JP2006553504A patent/JP4733058B2/ja active Active
- 2005-02-12 EA EA200801601A patent/EA200801601A1/ru unknown
- 2005-02-12 BR BRPI0507873A patent/BRPI0507873B8/pt active IP Right Grant
- 2005-02-12 ES ES05707354T patent/ES2326666T3/es active Active
- 2005-02-15 UY UY28749A patent/UY28749A1/es not_active Application Discontinuation
- 2005-02-16 PE PE2005000183A patent/PE20060210A1/es not_active Application Discontinuation
- 2005-02-16 MY MYPI20050575A patent/MY144322A/en unknown
- 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 active IP Right Grant
-
2007
- 2007-10-31 HK HK07111729.8A patent/HK1103402A1/xx unknown
-
2009
- 2009-06-15 HR HR20090346T patent/HRP20090346T1/hr unknown
- 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 |
|---|---|---|
| HRP20090346T1 (hr) | 8-[3-amino-piperidin-1-il]-ksantin, njihova priprava i uporaba ka ddp-iv inhibitora | |
| JP2006508969A5 (hr) | ||
| EP0526708B1 (de) | Sulfonamide, ihre Herstellung und Verwendung als Heilmittel und Zwischenprodukte | |
| CA1267889A (en) | (4-piperidinylmethyl and -hetero)purines | |
| KR100926247B1 (ko) | 크산틴 유도체를 포함하는 약제학적 조성물 및 이의제조방법 | |
| JP2006503013A5 (hr) | ||
| RU2007109819A (ru) | Стеклообразные матрицы для стабилизации кофейного аромата | |
| US7501426B2 (en) | 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions | |
| JP2006502144A (ja) | 新規なプリン誘導体、その製造方法および医薬組成物としての使用 | |
| DK169271B1 (da) | 8-Phenylxanthinderivater, fremgansmåde til fremstilling heraf, farmaceutisk præparat indeholdende en sådan forbindelse, samt en sådan forbindelse til anvendelse til terapi | |
| ES2314042T3 (es) | Derivados nuevos de adenina. | |
| DE60112609T2 (de) | Pyrazolopyridine | |
| DE60212949T2 (de) | Antivirale pyrazolopyridin verbindungen | |
| DE60311820T2 (de) | Neue verwendung von pyrimidin- oder triazin-2-carbonsäurenitrilen zur behandlung von krankheiten, die mit cysteinproteaseaktivität assoziiert sind, und neue pyridimidin-2-carbonsäurenitrilderivate | |
| US20040082570A1 (en) | Xanthine derivative and DPPIV inhibitor | |
| PL403104A1 (pl) | Sposób otrzymywania kompozycji farmaceutycznej zawierajacej pochodne 8-[3-aminopiperydyn-1-ylo]ksantyny | |
| KR100867484B1 (ko) | 1,3-디히드로이미다졸 축합 고리 화합물 | |
| DE60211539T2 (de) | Imidazopyridinderivate zur verwendung bei der behandlung von herpes-vireninfektion | |
| BR9816067A (pt) | Forma a de omeprazol, omeprazol, processo para a preparação da forma a de omeprazol, formulação farmacêutica, uso de omeprazol, e, método de tratamento de distúrbios gastrointestinais. | |
| DE10254304A1 (de) | Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel | |
| JP2007522251A6 (ja) | 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 | |
| JP2006512311A5 (hr) | ||
| PE20060302A1 (es) | Derivados de benzazepina como antagonistas del receptor h3 | |
| DE69817172T2 (de) | 4-tetrahydropyridylpyrimidin-derivate | |
| EP0297661A1 (en) | [(Bicyclic heterocyclyl)methyl and -hetero] substituted hexahydro-1H-azepines and pyrrolidines |