CZ307821B6 - - Google Patents
Download PDFInfo
- Publication number
- CZ307821B6 CZ307821B6 CZ2015493A CZ2015493A CZ307821B6 CZ 307821 B6 CZ307821 B6 CZ 307821B6 CZ 2015493 A CZ2015493 A CZ 2015493A CZ 2015493 A CZ2015493 A CZ 2015493A CZ 307821 B6 CZ307821 B6 CZ 307821B6
- Authority
- CZ
- Czechia
- Prior art keywords
- formula
- acid
- reacting
- protected
- aminoadamantanecarboxylic
- Prior art date
Links
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 18
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 12
- XKRFYHLGVUSROY-UHFFFAOYSA-N Argon Chemical compound [Ar] XKRFYHLGVUSROY-UHFFFAOYSA-N 0.000 claims description 10
- 150000001875 compounds Chemical class 0.000 claims description 8
- XRSAGGHWUAXBPG-UHFFFAOYSA-N 2-amino-2-hydroxyadamantane-1-carboxylic acid Chemical compound C1C(C2)CC3CC1C(N)(O)C2(C(O)=O)C3 XRSAGGHWUAXBPG-UHFFFAOYSA-N 0.000 claims description 7
- KNDWUKJAYRIVHS-UHFFFAOYSA-N 2-aminoadamantane-1-carboxylic acid Chemical compound C1C(C2)CC3CC1C(N)C2(C(O)=O)C3 KNDWUKJAYRIVHS-UHFFFAOYSA-N 0.000 claims description 7
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 6
- 238000002360 preparation method Methods 0.000 claims description 6
- ONDSBJMLAHVLMI-UHFFFAOYSA-N trimethylsilyldiazomethane Chemical compound C[Si](C)(C)[CH-][N+]#N ONDSBJMLAHVLMI-UHFFFAOYSA-N 0.000 claims description 6
- JIMXXGFJRDUSRO-UHFFFAOYSA-N adamantane-1-carboxylic acid Chemical compound C1C(C2)CC3CC2CC1(C(=O)O)C3 JIMXXGFJRDUSRO-UHFFFAOYSA-N 0.000 claims description 5
- 229910052786 argon Inorganic materials 0.000 claims description 5
- 238000000034 method Methods 0.000 claims description 5
- CTSLXHKWHWQRSH-UHFFFAOYSA-N oxalyl chloride Chemical compound ClC(=O)C(Cl)=O CTSLXHKWHWQRSH-UHFFFAOYSA-N 0.000 claims description 4
- IJXJGQCXFSSHNL-QMMMGPOBSA-N (R)-(-)-2-Phenylglycinol Chemical compound OC[C@H](N)C1=CC=CC=C1 IJXJGQCXFSSHNL-QMMMGPOBSA-N 0.000 claims description 3
- JSMLAOPQAIJVMD-UHFFFAOYSA-N 2-aminoadamantane-1-carboxylic acid hydrochloride Chemical compound Cl.NC1C2(CC3CC(CC1C3)C2)C(=O)O JSMLAOPQAIJVMD-UHFFFAOYSA-N 0.000 claims description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 3
- 239000001257 hydrogen Substances 0.000 claims description 3
- 229910052739 hydrogen Inorganic materials 0.000 claims description 3
- NNFCIKHAZHQZJG-UHFFFAOYSA-N potassium cyanide Chemical compound [K+].N#[C-] NNFCIKHAZHQZJG-UHFFFAOYSA-N 0.000 claims description 3
- 239000012286 potassium permanganate Substances 0.000 claims description 3
- 239000012280 lithium aluminium hydride Substances 0.000 claims description 2
- -1 lithium aluminum hydride Chemical compound 0.000 claims description 2
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 4
- MDVGOOIANLZFCP-UHFFFAOYSA-N 1-adamantylmethanol Chemical compound C1C(C2)CC3CC2CC1(CO)C3 MDVGOOIANLZFCP-UHFFFAOYSA-N 0.000 claims 2
- UIJSJQSZTPTCJI-UHFFFAOYSA-N C12(CC3CC(CC(C1)C3)C2)C(=O)O.NC(C2=CC=CC=C2)C(=O)O Chemical compound C12(CC3CC(CC(C1)C3)C2)C(=O)O.NC(C2=CC=CC=C2)C(=O)O UIJSJQSZTPTCJI-UHFFFAOYSA-N 0.000 claims 2
- DZULQZKFBAHSRX-UHFFFAOYSA-N adamantane-1-carbaldehyde Chemical compound C1C(C2)CC3CC2CC1(C=O)C3 DZULQZKFBAHSRX-UHFFFAOYSA-N 0.000 claims 2
- FQFZASRJFRAEIH-UHFFFAOYSA-N adamantane-1-carbonitrile Chemical class C1C(C2)CC3CC2CC1(C#N)C3 FQFZASRJFRAEIH-UHFFFAOYSA-N 0.000 claims 2
- CLYOOVNORYNXMD-UHFFFAOYSA-N methyl adamantane-1-carboxylate Chemical compound C1C(C2)CC3CC2CC1(C(=O)OC)C3 CLYOOVNORYNXMD-UHFFFAOYSA-N 0.000 claims 2
- DYHSDKLCOJIUFX-UHFFFAOYSA-N tert-butoxycarbonyl anhydride Chemical compound CC(C)(C)OC(=O)OC(=O)OC(C)(C)C DYHSDKLCOJIUFX-UHFFFAOYSA-N 0.000 claims 2
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 27
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 27
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 21
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 15
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 14
- 239000011541 reaction mixture Substances 0.000 description 13
- 239000007787 solid Substances 0.000 description 8
- 239000000243 solution Substances 0.000 description 8
- 239000010410 layer Substances 0.000 description 7
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 6
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 6
- 238000003818 flash chromatography Methods 0.000 description 6
- 239000000203 mixture Substances 0.000 description 6
- 239000000047 product Substances 0.000 description 6
- 239000000741 silica gel Substances 0.000 description 6
- 229910002027 silica gel Inorganic materials 0.000 description 6
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 4
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 4
- 239000000706 filtrate Substances 0.000 description 4
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 description 4
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 3
- 239000008346 aqueous phase Substances 0.000 description 3
- 239000012267 brine Substances 0.000 description 3
- 229920001343 polytetrafluoroethylene Polymers 0.000 description 3
- 229910052938 sodium sulfate Inorganic materials 0.000 description 3
- 235000011152 sodium sulphate Nutrition 0.000 description 3
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- DWAQJAXMDSEUJJ-UHFFFAOYSA-M Sodium bisulfite Chemical compound [Na+].OS([O-])=O DWAQJAXMDSEUJJ-UHFFFAOYSA-M 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 239000003054 catalyst Substances 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 2
- 239000002024 ethyl acetate extract Substances 0.000 description 2
- 150000004702 methyl esters Chemical class 0.000 description 2
- 229910000402 monopotassium phosphate Inorganic materials 0.000 description 2
- 235000019796 monopotassium phosphate Nutrition 0.000 description 2
- 150000002825 nitriles Chemical class 0.000 description 2
- NXJCBFBQEVOTOW-UHFFFAOYSA-L palladium(2+);dihydroxide Chemical compound O[Pd]O NXJCBFBQEVOTOW-UHFFFAOYSA-L 0.000 description 2
- PJNZPQUBCPKICU-UHFFFAOYSA-N phosphoric acid;potassium Chemical compound [K].OP(O)(O)=O PJNZPQUBCPKICU-UHFFFAOYSA-N 0.000 description 2
- 239000004810 polytetrafluoroethylene Substances 0.000 description 2
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 description 2
- 238000010992 reflux Methods 0.000 description 2
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 2
- 238000003828 vacuum filtration Methods 0.000 description 2
- 230000002378 acidificating effect Effects 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 239000012223 aqueous fraction Substances 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- WOBLPDAWNVAVAS-UHFFFAOYSA-N butyl carboxy carbonate Chemical compound CCCCOC(=O)OC(O)=O WOBLPDAWNVAVAS-UHFFFAOYSA-N 0.000 description 1
- 239000006227 byproduct Substances 0.000 description 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 1
- 238000010531 catalytic reduction reaction Methods 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- CETRZFQIITUQQL-UHFFFAOYSA-N dmso dimethylsulfoxide Chemical compound CS(C)=O.CS(C)=O CETRZFQIITUQQL-UHFFFAOYSA-N 0.000 description 1
- 239000000284 extract Substances 0.000 description 1
- 239000006260 foam Substances 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 238000007327 hydrogenolysis reaction Methods 0.000 description 1
- 238000002955 isolation Methods 0.000 description 1
- 238000004949 mass spectrometry Methods 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- XBXCNNQPRYLIDE-UHFFFAOYSA-M n-tert-butylcarbamate Chemical compound CC(C)(C)NC([O-])=O XBXCNNQPRYLIDE-UHFFFAOYSA-M 0.000 description 1
- 239000012044 organic layer Substances 0.000 description 1
- 239000012074 organic phase Substances 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 229910000027 potassium carbonate Inorganic materials 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 239000013557 residual solvent Substances 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000003039 volatile agent Substances 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
-
- 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
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
-
- 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
- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2603/00—Systems containing at least three condensed rings
- C07C2603/56—Ring systems containing bridged rings
- C07C2603/58—Ring systems containing bridged rings containing three rings
- C07C2603/70—Ring systems containing bridged rings containing three rings containing only six-membered rings
- C07C2603/74—Adamantanes
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Endocrinology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Emergency Medicine (AREA)
- Reproductive Health (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Virology (AREA)
- Transplantation (AREA)
- Pregnancy & Childbirth (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Pain & Pain Management (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Neurosurgery (AREA)
- Gynecology & Obstetrics (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US18855500P | 2000-03-10 | 2000-03-10 | |
| CZ2002-2974A CZ304355B6 (cs) | 2000-03-10 | 2001-03-05 | 2-Azabicyklo[3.1.0.]hexan-3-karbonitrilová sloučenina, farmaceutický prostředek a použití |
| CZ2014-33A CZ307784B6 (cs) | 2000-03-10 | 2001-03-05 | Inhibitory dipeptidylpeptidázy IV na bázi cyklopropylu kondenzovaného s pyrrolidinem, způsoby jeho přípravy a jejich použití |
| PCT/US2001/007151 WO2001068603A2 (en) | 2000-03-10 | 2001-03-05 | Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl iv, processes for their preparation, and their use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CZ307821B6 true CZ307821B6 (enEXAMPLES) | 2019-05-29 |
Family
ID=22693638
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CZ2014-33A CZ307784B6 (cs) | 2000-03-10 | 2001-03-05 | Inhibitory dipeptidylpeptidázy IV na bázi cyklopropylu kondenzovaného s pyrrolidinem, způsoby jeho přípravy a jejich použití |
| CZ2015493A CZ307821B6 (enEXAMPLES) | 2000-03-10 | 2001-03-05 | |
| CZ2002-2974A CZ304355B6 (cs) | 2000-03-10 | 2001-03-05 | 2-Azabicyklo[3.1.0.]hexan-3-karbonitrilová sloučenina, farmaceutický prostředek a použití |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CZ2014-33A CZ307784B6 (cs) | 2000-03-10 | 2001-03-05 | Inhibitory dipeptidylpeptidázy IV na bázi cyklopropylu kondenzovaného s pyrrolidinem, způsoby jeho přípravy a jejich použití |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CZ2002-2974A CZ304355B6 (cs) | 2000-03-10 | 2001-03-05 | 2-Azabicyklo[3.1.0.]hexan-3-karbonitrilová sloučenina, farmaceutický prostředek a použití |
Country Status (37)
Families Citing this family (313)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0487425A (ja) * | 1990-07-31 | 1992-03-19 | Fujitsu Ltd | 回線切り替え装置 |
| US6414002B1 (en) * | 1999-09-22 | 2002-07-02 | Bristol-Myers Squibb Company | Substituted acid derivatives useful as antidiabetic and antiobesity agents and method |
| US6395767B2 (en) * | 2000-03-10 | 2002-05-28 | Bristol-Myers Squibb Company | Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method |
| US7622503B2 (en) | 2000-08-24 | 2009-11-24 | University Of Tennessee Research Foundation | Selective androgen receptor modulators and methods of use thereof |
| US6573287B2 (en) * | 2001-04-12 | 2003-06-03 | Bristo-Myers Squibb Company | 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method |
| ES2296979T3 (es) * | 2001-06-27 | 2008-05-01 | Smithkline Beecham Corporation | Fluoropirrolidinas como inhibidores de dipeptidil peptidasa. |
| JP4357293B2 (ja) * | 2001-06-27 | 2009-11-04 | スミスクライン ビーチャム コーポレーション | ジペプチジルペプチダーゼ阻害剤としてのフルオロピロリジン類 |
| JP4300108B2 (ja) * | 2001-06-27 | 2009-07-22 | スミスクライン ビーチャム コーポレーション | ジペプチジルペプチダーゼ阻害剤としてのピロリジン類 |
| US6984645B2 (en) * | 2001-11-16 | 2006-01-10 | Bristol-Myers Squibb Company | Dual inhibitors of adipocyte fatty acid binding protein and keratinocyte fatty acid binding protein |
| US8853266B2 (en) | 2001-12-06 | 2014-10-07 | University Of Tennessee Research Foundation | Selective androgen receptor modulators for treating diabetes |
| US7772433B2 (en) | 2002-02-28 | 2010-08-10 | University Of Tennessee Research Foundation | SARMS and method of use thereof |
| GB0205175D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
| GB0205170D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
| GB0205165D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
| GB0205176D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
| GB0205166D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
| GB0205162D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
| US20040014681A1 (en) * | 2002-05-14 | 2004-01-22 | Ralph Ryback | Method for treating dermatoses and tissue damage |
| US7405234B2 (en) * | 2002-05-17 | 2008-07-29 | Bristol-Myers Squibb Company | Bicyclic modulators of androgen receptor function |
| US7378385B2 (en) * | 2002-08-08 | 2008-05-27 | University Of Cincinnati | Role for GLP-1 to mediate responses to disparate stressors |
| 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 |
| US7262207B2 (en) * | 2002-09-19 | 2007-08-28 | Abbott Laboratories | Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV) |
| US20040121964A1 (en) * | 2002-09-19 | 2004-06-24 | Madar David J. | Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV) |
| US7238724B2 (en) * | 2002-09-19 | 2007-07-03 | Abbott Laboratories | Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV) |
| US7632858B2 (en) * | 2002-11-15 | 2009-12-15 | Bristol-Myers Squibb Company | Open chain prolyl urea-related modulators of androgen receptor function |
| US20080076828A1 (en) | 2006-07-12 | 2008-03-27 | Dalton James T | Substituted acylanilides and methods of use thereof |
| US8309603B2 (en) | 2004-06-07 | 2012-11-13 | University Of Tennessee Research Foundation | SARMs and method of use thereof |
| US7420079B2 (en) * | 2002-12-09 | 2008-09-02 | Bristol-Myers Squibb Company | Methods and compounds for producing dipeptidyl peptidase IV inhibitors and intermediates thereof |
| US20060052382A1 (en) * | 2002-12-20 | 2006-03-09 | Duffy Joseph L | 3-Amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| JP4887139B2 (ja) * | 2003-03-25 | 2012-02-29 | 武田薬品工業株式会社 | ジペプチジルペプチダーゼインヒビター |
| EP2206496B1 (en) | 2003-05-05 | 2014-09-17 | Probiodrug AG | Screening of inhibitors of formation of pyroglutamic acid in amyloid beta peptide |
| EP1620091B1 (en) | 2003-05-05 | 2010-03-31 | Probiodrug AG | Inhibitors of glutaminyl cyclase |
| ATE464889T1 (de) | 2003-05-05 | 2010-05-15 | Probiodrug Ag | Medizinische verwendung von hemmern von glutaminyl und glutamatcyclasen |
| WO2004103993A1 (en) | 2003-05-14 | 2004-12-02 | Syrrx, Inc. | Dipeptidyl peptidase inhibitors |
| US7459474B2 (en) | 2003-06-11 | 2008-12-02 | Bristol-Myers Squibb Company | Modulators of the glucocorticoid receptor and method |
| US6995183B2 (en) | 2003-08-01 | 2006-02-07 | Bristol Myers Squibb Company | Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods |
| US7169926B1 (en) | 2003-08-13 | 2007-01-30 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US7790736B2 (en) * | 2003-08-13 | 2010-09-07 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US7678909B1 (en) | 2003-08-13 | 2010-03-16 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US7205409B2 (en) * | 2003-09-04 | 2007-04-17 | Abbott Laboratories | Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV) |
| EP1699777B1 (en) * | 2003-09-08 | 2012-12-12 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US20050065144A1 (en) * | 2003-09-08 | 2005-03-24 | Syrrx, Inc. | Dipeptidyl peptidase inhibitors |
| US7371759B2 (en) * | 2003-09-25 | 2008-05-13 | Bristol-Myers Squibb Company | HMG-CoA reductase inhibitors and method |
| US7462599B2 (en) | 2003-10-15 | 2008-12-09 | Probiodrug Ag | Use of effectors of glutaminyl and glutamate cyclases |
| WO2005049027A2 (en) | 2003-11-03 | 2005-06-02 | Probiodrug Ag | Combinations useful for the treatment of neuronal disorders |
| US7767828B2 (en) * | 2003-11-12 | 2010-08-03 | Phenomix Corporation | Methyl and ethyl substituted pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV |
| US7576121B2 (en) * | 2003-11-12 | 2009-08-18 | Phenomix Corporation | Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV |
| US7317109B2 (en) * | 2003-11-12 | 2008-01-08 | Phenomix Corporation | Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV |
| DK1689757T3 (en) * | 2003-11-12 | 2014-12-08 | Sino Med Internat Alliance Inc | HETEROCYCLIC DRY ACID COMPOUNDS |
| KR20180050427A (ko) | 2003-11-17 | 2018-05-14 | 노파르티스 아게 | 디펩티딜 펩티다제 ⅳ 억제제의 용도 |
| US20070149451A1 (en) * | 2003-11-17 | 2007-06-28 | Holmes David G | Combination of a dpp IV inhibitor and an antiobesity or appetite regulating agent |
| US7420059B2 (en) * | 2003-11-20 | 2008-09-02 | Bristol-Myers Squibb Company | HMG-CoA reductase inhibitors and method |
| ES2332920T3 (es) | 2004-01-20 | 2010-02-15 | Novartis Ag | Proceso y formulacion de compresion directa. |
| US7470810B2 (en) * | 2004-01-21 | 2008-12-30 | Bristol-Myers Squibb Company | Alkyl and aryl-thiotrifluoroacetates and process |
| WO2005073186A1 (ja) * | 2004-01-29 | 2005-08-11 | Ono Pharmaceutical Co., Ltd. | ピロリジン誘導体 |
| DK1712547T3 (da) * | 2004-02-05 | 2012-03-19 | Kyorin Seiyaku Kk | Bicycloesterderivat |
| WO2005075436A2 (en) | 2004-02-05 | 2005-08-18 | Probiodrug Ag | Novel inhibitors of glutaminyl cyclase |
| WO2005077900A1 (ja) * | 2004-02-18 | 2005-08-25 | Kyorin Pharmaceutical Co., Ltd. | ビシクロアミド誘導体 |
| 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 |
| US7514571B2 (en) * | 2004-02-27 | 2009-04-07 | Kyorin Pharmaceutical Co., Ltd. | Bicyclo derivative |
| US20070238753A1 (en) * | 2004-02-27 | 2007-10-11 | Madar David J | Pharmaceutical Compositions as Inhibitors of Dipeptidyl Peptidase-IV (DPP-IV) |
| US7732446B1 (en) | 2004-03-11 | 2010-06-08 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| CN102134231B (zh) * | 2004-03-15 | 2020-08-04 | 武田药品工业株式会社 | 二肽基肽酶抑制剂 |
| TW200534879A (en) * | 2004-03-25 | 2005-11-01 | Bristol Myers Squibb Co | Coated tablet formulation and method |
| TW200538122A (en) | 2004-03-31 | 2005-12-01 | Bristol Myers Squibb Co | Process for preparing a dipeptidyl peptidase Ⅳ inhibitor and intermediates employed therein |
| US7741082B2 (en) * | 2004-04-14 | 2010-06-22 | Bristol-Myers Squibb Company | Process for preparing dipeptidyl peptidase IV inhibitors and intermediates therefor |
| US7829720B2 (en) * | 2004-05-04 | 2010-11-09 | Bristol-Myers Squibb Company | Process for preparing atazanavir bisulfate and novel forms |
| US20050256314A1 (en) * | 2004-05-04 | 2005-11-17 | Soojin Kim | Process employing controlled crystallization in forming crystals of a pharmaceutical |
| TW200536827A (en) * | 2004-05-04 | 2005-11-16 | Bristol Myers Squibb Co | Enzymatic ammonolysis process for the preparation of intermediates for DPP IV inhibitors |
| US7214702B2 (en) * | 2004-05-25 | 2007-05-08 | Bristol-Myers Squibb Company | Process for producing a dipeptidyl peptidase IV inhibitor |
| TWI415635B (zh) | 2004-05-28 | 2013-11-21 | 必治妥施貴寶公司 | 加衣錠片調製物及製備彼之方法 |
| EP1753730A1 (en) * | 2004-06-04 | 2007-02-21 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US9884038B2 (en) | 2004-06-07 | 2018-02-06 | University Of Tennessee Research Foundation | Selective androgen receptor modulator and methods of use thereof |
| US9889110B2 (en) | 2004-06-07 | 2018-02-13 | University Of Tennessee Research Foundation | Selective androgen receptor modulator for treating hormone-related conditions |
| US7572805B2 (en) | 2004-07-14 | 2009-08-11 | Bristol-Myers Squibb Company | Pyrrolo(oxo)isoquinolines as 5HT ligands |
| WO2006019965A2 (en) | 2004-07-16 | 2006-02-23 | Takeda San Diego, Inc. | Dipeptidyl peptidase inhibitors |
| US7842707B2 (en) * | 2004-07-23 | 2010-11-30 | Nuada, Llc | Peptidase inhibitors |
| TW200608967A (en) | 2004-07-29 | 2006-03-16 | Sankyo Co | Pharmaceutical compositions containing with diabetic agent |
| US20060035954A1 (en) * | 2004-08-11 | 2006-02-16 | Sharma Padam N | Ammonolysis process for the preparation of intermediates for DPP IV inhibitors |
| AR051446A1 (es) * | 2004-09-23 | 2007-01-17 | Bristol Myers Squibb Co | Glucosidos de c-arilo como inhibidores selectivos de transportadores de glucosa (sglt2) |
| 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 |
| EP2805953B1 (en) | 2004-12-21 | 2016-03-09 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US7635699B2 (en) * | 2004-12-29 | 2009-12-22 | Bristol-Myers Squibb Company | Azolopyrimidine-based inhibitors of dipeptidyl peptidase IV and methods |
| US7589088B2 (en) * | 2004-12-29 | 2009-09-15 | Bristol-Myers Squibb Company | Pyrimidine-based inhibitors of dipeptidyl peptidase IV and methods |
| DOP2006000008A (es) * | 2005-01-10 | 2006-08-31 | Arena Pharm Inc | Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1 |
| JP2008024592A (ja) * | 2005-01-28 | 2008-02-07 | Taisho Pharmaceut Co Ltd | シアノピロリジン誘導体含有固形製剤用組成物、それを含有する固形製剤及びその製造方法 |
| US7238702B2 (en) * | 2005-02-10 | 2007-07-03 | Bristol-Myers Squibb Company | Dihydroquinazolinones as 5HT modulators |
| JP2008115080A (ja) * | 2005-04-22 | 2008-05-22 | Taisho Pharmaceutical Co Ltd | 併用医薬 |
| US7521557B2 (en) | 2005-05-20 | 2009-04-21 | Bristol-Myers Squibb Company | Pyrrolopyridine-based inhibitors of dipeptidyl peptidase IV and methods |
| US20060264433A1 (en) * | 2005-05-23 | 2006-11-23 | Backes Bradley J | Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV) |
| US7825139B2 (en) * | 2005-05-25 | 2010-11-02 | Forest Laboratories Holdings Limited (BM) | Compounds and methods for selective inhibition of dipeptidyl peptidase-IV |
| MY152185A (en) | 2005-06-10 | 2014-08-29 | Novartis Ag | Modified release 1-[(3-hydroxy-adamant-1-ylamino)-acetyl]-pyrrolidine-2(s)-carbonitrile formulation |
| MX2008000811A (es) * | 2005-07-28 | 2008-03-18 | Squibb Bristol Myers Co | Tetrahidro-1h-pitido[4,3-b]indoles substituidos como agonistas y antagonistas del receptor de serotonina. |
| 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 |
| TW200738245A (en) * | 2005-08-22 | 2007-10-16 | Sankyo Co | Pharmaceutical composition containing FBPase inhibitor |
| US7795436B2 (en) * | 2005-08-24 | 2010-09-14 | Bristol-Myers Squibb Company | Substituted tricyclic heterocycles as serotonin receptor agonists and antagonists |
| KR101388087B1 (ko) | 2005-08-31 | 2014-04-25 | 유니버시티 오브 테네시 리서치 파운데이션 | 선택적 안드로겐 수용체 조절제를 이용한 신장 질환, 화상,부상 및 척수 손상의 치료 방법 |
| WO2007033265A1 (en) * | 2005-09-14 | 2007-03-22 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors for treating diabetis |
| CN102908350B (zh) * | 2005-09-14 | 2014-07-23 | 武田药品工业株式会社 | 用于治疗糖尿病的二肽基肽酶抑制剂 |
| CN101374523B (zh) * | 2005-09-14 | 2012-04-11 | 武田药品工业株式会社 | 用于治疗糖尿病的二肽基肽酶抑制剂 |
| CA2622642C (en) * | 2005-09-16 | 2013-12-31 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| TW200745079A (en) * | 2005-09-16 | 2007-12-16 | Takeda Pharmaceuticals Co | Polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and methods of use therefor |
| TW200745080A (en) * | 2005-09-16 | 2007-12-16 | Takeda Pharmaceuticals Co | Polymorphs of tartrate salt of 2-[2-(3-(R)-amino-piperidin-1-yl)-5-fluoro-6-oxo-6H-pyrimidin-1-ylmethyl]-benzonitrile and methods of use therefor |
| TW200738266A (en) * | 2005-09-29 | 2007-10-16 | Sankyo Co | Pharmaceutical agent containing insulin resistance improving agent |
| US7488725B2 (en) | 2005-10-31 | 2009-02-10 | Bristol-Myers Squibb Co. | Pyrrolidinyl beta-amino amide-based inhibitors of dipeptidyl peptidase IV and methods |
| EP1971614A1 (en) | 2005-11-14 | 2008-09-24 | Probiodrug AG | Cyclopropyl-fused pyrrolidine derivatives as dipeptidyl peptidase iv inhibitors |
| GB0526291D0 (en) | 2005-12-23 | 2006-02-01 | Prosidion Ltd | Therapeutic method |
| US7915427B2 (en) * | 2006-03-08 | 2011-03-29 | Kyorin Pharmaceuticals Co., Ltd. | Process for producing aminoacetyl pyrrolidine carbonitrile derivative and intermediate for production thereof |
| RU2465264C2 (ru) * | 2006-03-16 | 2012-10-27 | Вертекс Фармасьютикалз Инкорпорейтед | Дейтерированные ингибиторы протеазы гепатита с |
| WO2007112368A1 (en) * | 2006-03-28 | 2007-10-04 | Takeda Pharmaceutical Company Limited | Preparation of (r)-3-aminopiperidine dihydrochloride |
| WO2007112347A1 (en) | 2006-03-28 | 2007-10-04 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US20070238770A1 (en) * | 2006-04-05 | 2007-10-11 | Bristol-Myers Squibb Company | Process for preparing novel crystalline forms of peliglitazar, novel stable forms produced therein and formulations |
| PE20071221A1 (es) | 2006-04-11 | 2007-12-14 | Arena Pharm Inc | Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas |
| PT1971862E (pt) * | 2006-04-11 | 2011-02-14 | Arena Pharm Inc | Métodos de utilização do receptor gpr119 para identificar compostos úteis para aumentar a massa óssea num indivíduo |
| CA2649209A1 (en) | 2006-04-12 | 2007-10-18 | Probiodrug Ag | Enzyme inhibitors |
| EP2014648A4 (en) * | 2006-04-17 | 2010-10-13 | Sumitomo Chemical Co | METHOD FOR PRODUCING A POLYCYCLIC PROLIN DERIVATIVE OR ACID ADDITIONAL SALT THEREOF |
| 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 |
| CN101437823B (zh) | 2006-05-04 | 2014-12-10 | 勃林格殷格翰国际有限公司 | 多晶型 |
| US7919598B2 (en) | 2006-06-28 | 2011-04-05 | Bristol-Myers Squibb Company | Crystal structures of SGLT2 inhibitors and processes for preparing same |
| US9730908B2 (en) | 2006-08-24 | 2017-08-15 | University Of Tennessee Research Foundation | SARMs and method of use thereof |
| US9844528B2 (en) | 2006-08-24 | 2017-12-19 | University Of Tennessee Research Foundation | SARMs and method of use thereof |
| JP2010502670A (ja) | 2006-09-07 | 2010-01-28 | ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング | 真性糖尿病のための組合せ治療 |
| US8324383B2 (en) | 2006-09-13 | 2012-12-04 | Takeda Pharmaceutical Company Limited | Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile |
| KR20170127074A (ko) * | 2006-09-13 | 2017-11-20 | 다케다 야쿠힌 고교 가부시키가이샤 | 2-[6-(3-아미노-피페리딘-1-일)-3-메틸-2,4-디옥소-3,4-디하이드로-2h-피리미딘-1-일메틸]-4-플루오로-벤조니트릴의 용도 |
| TWI430806B (zh) * | 2006-09-13 | 2014-03-21 | Smithkline Beecham Corp | 用於投與長效降血糖藥劑之方法 |
| WO2008036682A2 (en) | 2006-09-18 | 2008-03-27 | Raptor Pharmaceutical Inc. | Treatment of liver disorders by administration of receptor-associated protein (rap)-conjugates |
| US8278345B2 (en) | 2006-11-09 | 2012-10-02 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| US8217025B2 (en) * | 2006-11-17 | 2012-07-10 | Harbor Therapeutics, Inc. | Drug screening and treatment methods |
| TW200838536A (en) * | 2006-11-29 | 2008-10-01 | Takeda Pharmaceutical | Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor |
| US9126987B2 (en) | 2006-11-30 | 2015-09-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| US9604931B2 (en) | 2007-01-22 | 2017-03-28 | Gtx, Inc. | Nuclear receptor binding agents |
| US9623021B2 (en) | 2007-01-22 | 2017-04-18 | Gtx, Inc. | Nuclear receptor binding agents |
| US9078888B2 (en) | 2007-01-22 | 2015-07-14 | Gtx, Inc. | Nuclear receptor binding agents |
| CN101230058A (zh) * | 2007-01-23 | 2008-07-30 | 上海恒瑞医药有限公司 | 双环氮杂烷类衍生物、其制备方法及其在医药上的用途 |
| EA015180B1 (ru) | 2007-02-01 | 2011-06-30 | Такеда Фармасьютикал Компани Лимитед | Твердый препарат, содержащий алоглиптин и пиоглитазон |
| WO2008098256A1 (en) * | 2007-02-09 | 2008-08-14 | Bristol-Myers Squibb Company | Methods for identifying patients with an increased likelihood of responding to dpp-iv inhibitors |
| US8093236B2 (en) | 2007-03-13 | 2012-01-10 | Takeda Pharmaceuticals Company Limited | Weekly administration of dipeptidyl peptidase inhibitors |
| US20080064701A1 (en) * | 2007-04-24 | 2008-03-13 | Ramesh Sesha | Anti-diabetic combinations |
| AR065809A1 (es) | 2007-03-22 | 2009-07-01 | Bristol Myers Squibb Co | Formulaciones farmaceuticas que contienen un inhibidor sglt2 |
| US8143427B2 (en) * | 2007-03-22 | 2012-03-27 | Kyorin Pharmaceutical Co., Ltd. | Method for producing aminoacetylpyrrolidinecarbonitrile derivative |
| CN103330939A (zh) | 2007-04-03 | 2013-10-02 | 田边三菱制药株式会社 | 二肽基肽酶iv抑制化合物和甜味剂的并用 |
| US9656991B2 (en) | 2007-04-18 | 2017-05-23 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| PE20090696A1 (es) * | 2007-04-20 | 2009-06-20 | Bristol Myers Squibb Co | Formas cristalinas de saxagliptina y procesos para preparar las mismas |
| US20080287529A1 (en) * | 2007-05-18 | 2008-11-20 | Bristol-Myers Squibb Company | Crystal structures of sglt2 inhibitors and processes for preparing same |
| ES2465216T3 (es) | 2007-06-04 | 2014-06-05 | Ben Gurion University Of The Negev Research And Development Authority | Compuestos de triarilo y composiciones que comprenden los mismos |
| CN101318925A (zh) * | 2007-06-04 | 2008-12-10 | 上海恒瑞医药有限公司 | 吡咯烷并四元环类衍生物、其制备方法及其在医药上的用途 |
| AU2008268627A1 (en) * | 2007-06-22 | 2008-12-31 | Bristol-Myers Squibb Company | Tableted compositions containing atazanavir |
| DK2178513T3 (da) * | 2007-06-22 | 2011-07-11 | Bristol Myers Squibb Co | Sammensætninger i tabletform indeholdende atazanavir |
| SI2170292T1 (sl) * | 2007-06-22 | 2014-05-30 | Bristol-Myers Squibb Holdings Ireland | Tabletirani sestavki, ki vsebujejo atazanavir |
| AU2008268630A1 (en) * | 2007-06-22 | 2008-12-31 | Bristol-Myers Squibb Company | Tableted compositions containing atazanavir |
| PE20090938A1 (es) | 2007-08-16 | 2009-08-08 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo |
| NZ600126A (en) * | 2007-08-17 | 2013-12-20 | Boehringer Ingelheim Int | Purine derivatives for use in the treatment of fap-related diseases |
| US7968603B2 (en) | 2007-09-11 | 2011-06-28 | University Of Tennessee Research Foundation | Solid forms of selective androgen receptor modulators |
| US20090076118A1 (en) * | 2007-09-13 | 2009-03-19 | Protia, Llc | Deuterium-enriched saxagliptin |
| GB2465132B (en) * | 2007-09-21 | 2012-06-06 | Lupin Ltd | Compounds as dipeptidyl peptidase IV (DPP IV) inhibitors |
| CL2008003653A1 (es) | 2008-01-17 | 2010-03-05 | Mitsubishi Tanabe Pharma Corp | Uso de un inhibidor de sglt derivado de glucopiranosilo y un inhibidor de dppiv seleccionado para tratar la diabetes; y composicion farmaceutica. |
| US8551524B2 (en) * | 2008-03-14 | 2013-10-08 | Iycus, Llc | Anti-diabetic combinations |
| PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| 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 |
| US20110152340A1 (en) * | 2008-05-16 | 2011-06-23 | Bristol-Myers Squibb Company | Methods for Identifying Subjects With an Increased Likelihood of Responding to DPP-IV Inhibitors |
| PE20100156A1 (es) * | 2008-06-03 | 2010-02-23 | Boehringer Ingelheim Int | Tratamiento de nafld |
| US8003689B2 (en) | 2008-06-20 | 2011-08-23 | Gtx, Inc. | Metabolites of selective androgen receptor modulators and methods of use thereof |
| KR20200118243A (ko) | 2008-08-06 | 2020-10-14 | 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" |
| JP5476305B2 (ja) * | 2008-08-07 | 2014-04-23 | 杏林製薬株式会社 | ビシクロ[2.2.2]オクチルアミン誘導体の製造方法 |
| JPWO2010018866A1 (ja) * | 2008-08-14 | 2012-01-26 | 杏林製薬株式会社 | 安定化された医薬組成物 |
| CA2735562C (en) * | 2008-08-15 | 2017-10-17 | Boehringer Ingelheim International Gmbh | Dpp-4 inhibitors for wound healing |
| JP2012502081A (ja) | 2008-09-10 | 2012-01-26 | 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 | 糖尿病及び関連症状の治療のための組み合わせ治療 |
| 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 |
| EP3677275B1 (de) | 2008-10-17 | 2024-06-12 | Sanofi-Aventis Deutschland GmbH | Kombination von einem insulin und einem glp-1-agonisten |
| ES2614427T3 (es) | 2008-11-07 | 2017-05-31 | The General Hospital Corporation | Fragmentos C-terminales de péptido glucagonoide 1 (GLP-1) |
| US20100124541A1 (en) * | 2008-11-19 | 2010-05-20 | Auspex Pharmaceuticals, Inc. | Hydroxyadamantyl inhibitors of dipeptidylpeptidase iv |
| US20100144140A1 (en) * | 2008-12-10 | 2010-06-10 | Novellus Systems, Inc. | Methods for depositing tungsten films having low resistivity for gapfill applications |
| DE102008062136B4 (de) | 2008-12-16 | 2012-05-03 | Kamamed Ug | Pharmazeutische Zusammensetzung auf Basis von Peptid aus Kamelmilch |
| NZ592924A (en) | 2008-12-23 | 2014-05-30 | Boehringer Ingelheim Int | Salt forms of a xanthine derivative |
| TW201036975A (en) | 2009-01-07 | 2010-10-16 | Boehringer Ingelheim Int | Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy |
| US8706650B2 (en) * | 2009-01-14 | 2014-04-22 | Integral Analytics, Inc. | Optimization of microgrid energy use and distribution |
| TWI466672B (zh) | 2009-01-29 | 2015-01-01 | Boehringer Ingelheim Int | 小兒科病人糖尿病之治療 |
| NZ594044A (en) | 2009-02-13 | 2014-08-29 | Boehringer Ingelheim Int | Antidiabetic medications comprising a dpp-4 inhibitor (linagliptin) optionally in combination with other antidiabetics |
| CN102307577A (zh) | 2009-02-13 | 2012-01-04 | 贝林格尔.英格海姆国际有限公司 | 包含sglt2抑制剂、dpp-iv抑制剂和任选的另一种抗糖尿病药的药物组合物及其用途 |
| AU2010229653A1 (en) * | 2009-03-27 | 2011-10-20 | Astrazeneca Ab | Methods for preventing major adverse cardiovascular events with DPP-IV inhibitors |
| RU2011142829A (ru) | 2009-03-27 | 2013-05-10 | Киорин Фармасьютикал Ко., Лтд. | Препарат матричного типа с пролонгированным высвобождением, содержащий базисную добавку |
| CN102459610B (zh) * | 2009-04-08 | 2014-12-17 | 阿斯利康(瑞典)有限公司 | 表达pdh和fdh酶的遗传稳定性质粒 |
| WO2010115974A1 (en) * | 2009-04-09 | 2010-10-14 | Sandoz Ag | Crystal forms of saxagliptin |
| WO2010146597A1 (en) | 2009-06-18 | 2010-12-23 | Lupin Limited | 2-amino-2- [8-(dimethyl carbamoyl)- 8-aza- bicyclo [3.2.1] oct-3-yl]-exo- ethanoyl derivatives as potent dpp-iv inhibitors |
| AR077642A1 (es) | 2009-07-09 | 2011-09-14 | Arena Pharm Inc | Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo |
| PL2475428T3 (pl) | 2009-09-11 | 2015-12-31 | Probiodrug Ag | Pochodne heterocykliczne jako inhibitory cyklazy glutaminowej |
| EP2308847B1 (en) | 2009-10-09 | 2014-04-02 | EMC microcollections GmbH | Substituted pyridines as inhibitors of dipeptidyl peptidase IV and their application for the treatment of diabetes and related diseases |
| EP3831402A1 (de) | 2009-11-13 | 2021-06-09 | Sanofi-Aventis Deutschland GmbH | Pharmazeutische zusammensetzung umfassend einen glp-1-agonisten, ein insulin und methionin |
| CN104825417A (zh) | 2009-11-13 | 2015-08-12 | 阿斯利康(瑞典)有限公司 | 立即释放片剂 |
| CA2780939C (en) | 2009-11-13 | 2018-06-12 | Bristol-Myers Squibb Company | Bilayer tablet formulations |
| UY33025A (es) | 2009-11-13 | 2011-06-30 | Sanofi Aventis Deustschland Gmbh | Composicion farmaceutica que comprende un agonista de glp-1 metionina |
| CA2782179C (en) | 2009-11-27 | 2020-06-23 | Boehringer Ingelheim International Gmbh | Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin |
| TWI562775B (en) | 2010-03-02 | 2016-12-21 | Lexicon Pharmaceuticals Inc | Methods of using inhibitors of sodium-glucose cotransporters 1 and 2 |
| JP6026284B2 (ja) | 2010-03-03 | 2016-11-16 | 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 |
| EA022420B1 (ru) | 2010-03-10 | 2015-12-30 | Пробиодруг Аг | Гетероциклические ингибиторы глутаминилциклазы (qc, ec 2.3.2.5) |
| 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 |
| EP2368874A1 (en) | 2010-03-26 | 2011-09-28 | Sandoz AG | Racemisation of (R)-N-Boc-3-hydroxyadamant-1-yl glycine |
| EP2555617A4 (en) * | 2010-04-05 | 2013-08-14 | Cadila Pharmaceuticals Ltd | NEW COMPOUNDS FOR THE TREATMENT OF HYPOGLYCEMIA |
| US20130023494A1 (en) | 2010-04-06 | 2013-01-24 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| 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 |
| JP5373996B2 (ja) | 2010-05-05 | 2013-12-18 | アッシア・ケミカル・インダストリーズ・リミテッド | サクサグリプチン中間体、サクサグリプチン多形及びそれらの調製方法 |
| KR101927068B1 (ko) | 2010-05-05 | 2018-12-10 | 베링거 인겔하임 인터내셔날 게엠베하 | 체중 감소 치료에 후속하는 dpp-4 억제제에 의한 순차적 병용 요법 |
| KR102018038B1 (ko) | 2010-06-24 | 2019-09-05 | 베링거 인겔하임 인터내셔날 게엠베하 | 당뇨병 요법 |
| WO2012017029A1 (en) | 2010-08-06 | 2012-02-09 | Sandoz Ag | Novel salts of saxagrliptin with organic di-acids |
| EP2601175A1 (en) | 2010-08-06 | 2013-06-12 | Sandoz AG | A novel crystalline compound comprising saxagliptin and phosphoric acid |
| RU2546520C2 (ru) | 2010-08-30 | 2015-04-10 | Санофи-Авентис Дойчланд Гмбх | Применение ave0010 для производства лекарственного средства для лечения сахарного диабета 2 типа |
| WO2012028721A1 (en) | 2010-09-03 | 2012-03-08 | Sandoz Ag | PROCESS FOR THE REDUCTIVE AMINATION OF α-KETO CARBOXYLIC ACIDS |
| MX2013002146A (es) | 2010-09-03 | 2013-04-03 | Astrazeneca Uk Ltd | Formulaciones farmaceuticas que utilizan antioxidantes solubles en agua. |
| US9616097B2 (en) | 2010-09-15 | 2017-04-11 | Synergy Pharmaceuticals, Inc. | Formulations of guanylate cyclase C agonists and methods of use |
| CA2812061A1 (en) | 2010-09-22 | 2012-03-29 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| US20120077778A1 (en) | 2010-09-29 | 2012-03-29 | Andrea Bourdelais | Ladder-Frame Polyether Conjugates |
| WO2012047871A1 (en) | 2010-10-04 | 2012-04-12 | Assia Chemical Industries Ltd | Polymorphs of saxagliptin hydrochloride and processes for preparing them |
| US9040481B2 (en) | 2010-11-02 | 2015-05-26 | The General Hospital Corporation | Methods for treating steatotic disease |
| US9034883B2 (en) | 2010-11-15 | 2015-05-19 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
| TWI631963B (zh) | 2011-01-05 | 2018-08-11 | 雷西肯製藥股份有限公司 | 包含鈉-葡萄糖共同輸送體1與2之抑制劑的組合物與應用方法 |
| DK2670486T3 (en) | 2011-01-31 | 2016-05-17 | Cadila Healthcare Ltd | TREATMENT FOR LIPODYSTROPHY |
| EP2670397B1 (en) | 2011-02-01 | 2020-05-13 | Bristol-Myers Squibb Company | Pharmaceutical formulations including an amine compound |
| WO2012123563A1 (en) | 2011-03-16 | 2012-09-20 | Probiodrug Ag | Benz imidazole derivatives as inhibitors of glutaminyl cyclase |
| US20140018371A1 (en) | 2011-04-01 | 2014-01-16 | Arena Pharmaceuticals, Inc. | Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto |
| WO2012145361A1 (en) | 2011-04-19 | 2012-10-26 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| US20140051714A1 (en) | 2011-04-22 | 2014-02-20 | Arena Pharmaceuticals, Inc. | Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto |
| US20140038889A1 (en) | 2011-04-22 | 2014-02-06 | Arena Pharmaceuticals, Inc. | Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto |
| US9821032B2 (en) | 2011-05-13 | 2017-11-21 | Sanofi-Aventis Deutschland Gmbh | Pharmaceutical combination for improving glycemic control as add-on therapy to basal insulin |
| WO2012170702A1 (en) | 2011-06-08 | 2012-12-13 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| WO2013006692A2 (en) | 2011-07-06 | 2013-01-10 | The General Hospital Corporation | Methods of treatment using a pentapeptide derived from the c-terminus of glucagon-like peptide 1 (glp-1) |
| PL3517539T3 (pl) | 2011-07-15 | 2023-04-24 | Boehringer Ingelheim International Gmbh | Podstawiona dimeryczna pochodna chinazoliny, sposób jej wytwarzania i jej zastosowanie w kompozycjach farmaceutycznych do leczenia cukrzycy typu I i II |
| HUE027989T2 (en) | 2011-08-29 | 2016-11-28 | Sanofi Aventis Deutschland | A pharmaceutical composition for use in glycemic control in patients with type 2 diabetes |
| AR087744A1 (es) | 2011-09-01 | 2014-04-16 | Sanofi Aventis Deutschland | Composicion farmaceutica para uso en el tratamiento de una enfermedad neurodegenerativa |
| EA201490556A1 (ru) | 2011-09-07 | 2014-08-29 | Сановел Илач Санайи Ве Тиджарет Аноним Ширкети | Составы ингибитора дпп-4 |
| ES2487271T3 (es) | 2011-10-06 | 2014-08-20 | Sanovel Ilac Sanayi Ve Ticaret A.S. | Formulaciones de dosificación sólidas inhibidoras de DPP-IV |
| WO2013055910A1 (en) | 2011-10-12 | 2013-04-18 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| WO2013081100A1 (ja) * | 2011-11-30 | 2013-06-06 | 積水メディカル株式会社 | アダマンチルヒダントイン化合物 |
| US9115082B2 (en) | 2012-01-18 | 2015-08-25 | Catherine Yang | Dipeptidyl-peptidase-IV inhibitors for treatment of type 2 diabetes complex with hypertension |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| EP2841419A1 (en) | 2012-04-25 | 2015-03-04 | Enantia, S.L. | Crystalline forms of saxagliptin |
| US20130303554A1 (en) | 2012-05-14 | 2013-11-14 | Boehringer Ingelheim International Gmbh | Use of a dpp-4 inhibitor in sirs and/or sepsis |
| JP6224084B2 (ja) | 2012-05-14 | 2017-11-01 | 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 | 糸球体上皮細胞関連障害及び/又はネフローゼ症候群の治療に用いるdpp−4阻害薬としてのキサンチン誘導体 |
| US8664443B2 (en) | 2012-05-23 | 2014-03-04 | Divi's Laboratories Ltd. | Process for the preparation of (1S, 3S, 5S)-2-[2(S)-2-amino-2-(3-hydroxy-1-adamantan-1-yl) acetyl]-2-azabicyclo [3.1.0] hexane-3-carbonitrile |
| 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 |
| WO2013175297A1 (en) | 2012-05-24 | 2013-11-28 | Apotex Pharmachem India Pvt. Ltd | Salts of saxagliptin with organic acids |
| AU2013285078A1 (en) | 2012-07-02 | 2015-01-29 | Sun Pharmaceutical Industries Limited | Saxagliptin salts |
| CN103539724B (zh) * | 2012-07-12 | 2017-09-26 | 博瑞生物医药(苏州)股份有限公司 | 沙格列汀单一立体异构体的新晶型和纯化方法 |
| US10258596B2 (en) | 2012-07-13 | 2019-04-16 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS) |
| PL2872482T3 (pl) | 2012-07-13 | 2021-03-08 | Oncternal Therapeutics, Inc. | Sposób leczenia raków sutka z użyciem selektywnego modulatora receptora androgenowego (sarm) |
| US9622992B2 (en) | 2012-07-13 | 2017-04-18 | Gtx, Inc. | Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs) |
| US9969683B2 (en) | 2012-07-13 | 2018-05-15 | Gtx, Inc. | Method of treating estrogen receptor (ER)-positive breast cancers with selective androgen receptor modulator (SARMS) |
| US9744149B2 (en) | 2012-07-13 | 2017-08-29 | Gtx, Inc. | Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs) |
| US10314807B2 (en) | 2012-07-13 | 2019-06-11 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS) |
| US10987334B2 (en) | 2012-07-13 | 2021-04-27 | University Of Tennessee Research Foundation | Method of treating ER mutant expressing breast cancers with selective androgen receptor modulators (SARMs) |
| WO2014030051A1 (en) | 2012-08-23 | 2014-02-27 | Aurobindo Pharma Limited | Stable pharmaceutical compositions comprising saxagliptin |
| WO2014057495A1 (en) | 2012-10-11 | 2014-04-17 | Lee Pharma Limited | A process for industrial preparation of [(s)-n-tert butoxycarbonyl-3-hydroxy]adamantylglycine |
| TWI500613B (zh) | 2012-10-17 | 2015-09-21 | Cadila Healthcare Ltd | 新穎之雜環化合物 |
| WO2014074668A1 (en) | 2012-11-08 | 2014-05-15 | Arena Pharmaceuticals, Inc. | Modulators of gpr119 and the treatment of disorders related thereto |
| DK3489226T3 (da) | 2012-11-20 | 2021-04-26 | Lexicon Pharmaceuticals Inc | Hæmmere for natriumglucose-cotransporter 1 |
| US20150250734A1 (en) | 2012-12-21 | 2015-09-10 | Wockhardt Limited | Stable pharmaceutical compositions of saxagliptin or salts thereof |
| WO2014096983A1 (en) | 2012-12-21 | 2014-06-26 | Wockhardt Limited | Stable pharmaceutical compositions of saxagliptin or salts thereof |
| WO2014108830A1 (en) | 2013-01-10 | 2014-07-17 | Wockhardt Limited | A process for preparing pharmaceutically acceptable salt of saxagliptin |
| ITMI20130132A1 (it) * | 2013-01-30 | 2014-07-31 | Laboratorio Chimico Int Spa | Procedimento per la preparazione di intermedi di sintesi di saxagliptina e nuovi composti |
| TWI641381B (zh) | 2013-02-04 | 2018-11-21 | 法商賽諾菲公司 | 胰島素類似物及/或胰島素衍生物之穩定化醫藥調配物 |
| US8652527B1 (en) | 2013-03-13 | 2014-02-18 | Upsher-Smith Laboratories, Inc | Extended-release topiramate capsules |
| US9101545B2 (en) | 2013-03-15 | 2015-08-11 | Upsher-Smith Laboratories, Inc. | Extended-release topiramate capsules |
| CN104059068B (zh) * | 2013-03-20 | 2017-02-08 | 中国科学院上海药物研究所 | β‑氨基羰基类化合物、其制备方法、药物组合物及其用途 |
| CN104098481B (zh) * | 2013-04-10 | 2016-05-11 | 浙江九洲药物科技有限公司 | 一种沙格列汀中间体的制备方法 |
| EA201592020A1 (ru) | 2013-04-22 | 2016-05-31 | Кадила Хелзкэр Лимитед | Новая композиция для неалкогольной жировой болезни печени (нажбп) |
| WO2014193528A1 (en) * | 2013-04-29 | 2014-12-04 | Anovel Pharmaceuticals, Llc | Amorphous dosage forms and methods |
| US20160107989A1 (en) | 2013-05-30 | 2016-04-21 | Cadila Healthcare Limited | A process for preparation of pyrroles having hypolipidemic hypocholesteremic activities |
| SI3004138T1 (sl) | 2013-06-05 | 2024-07-31 | Bausch Health Ireland Limited | Ultra čisti agonisti gvanilat ciklaze C, postopek za njihovo pripravo in uporabo |
| TW201513857A (zh) | 2013-07-05 | 2015-04-16 | Cadila Healthcare Ltd | 協同性組成物 |
| IN2013MU02470A (enEXAMPLES) | 2013-07-25 | 2015-06-26 | Cadila Healthcare Ltd | |
| EP2832723B1 (en) | 2013-07-29 | 2017-02-15 | Zentiva, a.s. | Stabilised amorphous forms of Saxagliptin |
| IN2013MU02813A (enEXAMPLES) * | 2013-08-28 | 2015-07-03 | Amneal Pharmaceuticals Llc | |
| WO2015033357A2 (en) | 2013-09-06 | 2015-03-12 | Cadila Healthcare Limited | An improved process for the preparation of pyrrole derivatives |
| ITMI20131677A1 (it) * | 2013-10-10 | 2015-04-11 | Olon Spa | Procedimento per la preparazione di saxagliptina |
| WO2015068156A1 (en) | 2013-11-05 | 2015-05-14 | Ben-Gurion University Of The Negev Research And Development Authority | Compounds for the treatment of diabetes and disease complications arising from same |
| WO2015067223A1 (en) | 2013-11-06 | 2015-05-14 | Zentiva, K., S. | L-tartrate salt of (1s,3s,5s)-2-[(2s)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl) acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile and process for preparation thereof |
| WO2015071887A1 (en) | 2013-11-18 | 2015-05-21 | Ranbaxy Laboratories Limited | Oral pharmaceutical compositions of saxagliptin |
| WO2015071889A1 (en) | 2013-11-18 | 2015-05-21 | Ranbaxy Laboratories Limited | Oral compositions of saxagliptin |
| WO2015087262A1 (en) | 2013-12-11 | 2015-06-18 | Ranbaxy Laboratories Limited | Process for the preparation of saxagliptin and its intermediates |
| CA2932877A1 (en) | 2014-01-09 | 2015-07-16 | Sanofi | Stabilized pharmaceutical formulations of insulin analogues and/or insulin derivatives |
| JP6735674B2 (ja) | 2014-01-09 | 2020-08-05 | サノフイSanofi | インスリンアスパルトの安定化された医薬製剤 |
| US9895424B2 (en) | 2014-01-09 | 2018-02-20 | Sanofi | Stabilized pharmaceutical formulations of insulin analogues and/or insulin derivatives |
| WO2015128453A1 (en) | 2014-02-28 | 2015-09-03 | Boehringer Ingelheim International Gmbh | Medical use of a dpp-4 inhibitor |
| CZ2014177A3 (cs) * | 2014-03-24 | 2015-10-07 | Zentiva, K.S. | Způsob výroby saxagliptinu |
| JP6649902B2 (ja) | 2014-05-30 | 2020-02-19 | ファイザー・インク | 選択的アンドロゲン受容体モジュレーターとしてのカルボニトリル誘導体 |
| WO2016016770A1 (en) | 2014-07-26 | 2016-02-04 | Wockhardt Limited | A novel modified release pharmaceutical composition of sitagliptin or pharmaceutically acceptable salt thereof |
| GB201415598D0 (en) | 2014-09-03 | 2014-10-15 | Univ Birmingham | Elavated Itercranial Pressure Treatment |
| CN104557667A (zh) * | 2014-12-12 | 2015-04-29 | 山东省药学科学院 | 2-氰基吡咯烷类化合物、制备方法及其应用 |
| PE20171622A1 (es) | 2014-12-12 | 2017-11-02 | Sanofi Aventis Deutschland | Formulacion de relacion fija de insulina glargina/lixisenatida |
| AU2016229982B2 (en) | 2015-03-09 | 2020-06-18 | Intekrin Therapeutics, Inc. | Methods for the treatment of nonalcoholic fatty liver disease and/or lipodystrophy |
| TWI748945B (zh) | 2015-03-13 | 2021-12-11 | 德商賽諾菲阿凡提斯德意志有限公司 | 第2型糖尿病病患治療 |
| TW201705975A (zh) | 2015-03-18 | 2017-02-16 | 賽諾菲阿凡提斯德意志有限公司 | 第2型糖尿病病患之治療 |
| CN105037245B (zh) * | 2015-08-03 | 2017-04-12 | 沧州那瑞化学科技有限公司 | 一种沙格列汀中间体的制备方法 |
| WO2017064635A2 (en) | 2015-10-14 | 2017-04-20 | Cadila Healthcare Limited | Pyrrole compound, compositions and process for preparation thereof |
| KR101715682B1 (ko) | 2015-10-29 | 2017-03-13 | 경동제약 주식회사 | 삭사글립틴의 제조를 위한 신규 중간체, 이의 제조방법 및 이를 이용한 삭사글립틴의 제조방법 |
| NZ747331A (en) | 2016-06-10 | 2025-06-27 | Boehringer Ingelheim Int | Combinations of linagliptin and metformin |
| US11583516B2 (en) | 2016-09-07 | 2023-02-21 | Trustees Of Tufts College | Dash inhibitors, and uses related thereto |
| MX382765B (es) | 2016-12-09 | 2025-03-13 | Zydus Lifesciences Ltd | Tratamiento para la colangitis biliar primaria. |
| WO2018162722A1 (en) | 2017-03-09 | 2018-09-13 | Deutsches Institut Für Ernährungsforschung Potsdam-Rehbrücke | Dpp-4 inhibitors for use in treating bone fractures |
| EP3606527A1 (en) | 2017-04-03 | 2020-02-12 | Coherus Biosciences, Inc. | Ppar-gamma agonist for treatment of progressive supranuclear palsy |
| EP3461819B1 (en) | 2017-09-29 | 2020-05-27 | Probiodrug AG | Inhibitors of glutaminyl cyclase |
| CN109970620B (zh) * | 2017-12-27 | 2022-07-12 | 江苏威凯尔医药科技有限公司 | 一种制备沙格列汀中间体的方法 |
| CN112567468A (zh) * | 2018-06-14 | 2021-03-26 | 阿斯利康(英国)有限公司 | 用二肽基肽酶-4抑制剂药物组合物降低血糖的方法 |
| KR20210034039A (ko) | 2018-07-19 | 2021-03-29 | 아스트라제네카 아베 | 다파글리플로진을 사용하는 HFpEF의 치료 방법 및 이를 포함하는 조성물 |
| WO2020068661A1 (en) | 2018-09-26 | 2020-04-02 | Lexicon Pharmaceuticals, Inc. | Crystalline forms of n-(1 -((2-(dimethylamino)ethyl)amino)-2-m ethyl-1 -oopropan-2-yl)-4-(4-(2-methyl-5- (2s,3r,4r,5s,6r)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2h-pyran-2-yl)benzyl) phenl)butanamide and methods of their synthesis |
| RU2712097C1 (ru) * | 2018-09-28 | 2020-01-24 | Общество с ограниченной ответственностью "Необиотек" | Ингибитор дипептидилпептидазы-4 для лечения сахарного диабета 2-го типа, соединения (варианты) |
| RU2727898C1 (ru) * | 2020-02-25 | 2020-07-24 | Общество с ограниченной ответственностью «Необиотек» | Фармацевтическая композиция на основе действующего вещества, ингибитора дипептидилпептидазы-4, для предупреждения развития и лечения сахарного диабета 2 типа |
| TW202220672A (zh) | 2020-07-27 | 2022-06-01 | 瑞典商阿斯特捷利康公司 | 用達格列淨治療慢性腎臟病之方法 |
| WO2023275715A1 (en) | 2021-06-30 | 2023-01-05 | Pfizer Inc. | Metabolites of selective androgen receptor modulators |
| CN113666846B (zh) * | 2021-08-31 | 2023-06-27 | 济南立德医药技术有限公司 | 沙格列汀中间体的合成方法 |
| CN118510504A (zh) | 2022-01-26 | 2024-08-16 | 阿斯利康(瑞典)有限公司 | 用于在治疗糖尿病前期或降低发展2型糖尿病的风险中使用的达格列净 |
| WO2025090919A1 (en) * | 2023-10-25 | 2025-05-01 | Piton Therapeutics, Inc. | Compositions and methods for treating inflammatory bowel disease |
Family Cites Families (90)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3325478A (en) * | 1964-11-17 | 1967-06-13 | Du Pont | alpha-amino-1-adamantylmethyl penicillins |
| US3674836A (en) | 1968-05-21 | 1972-07-04 | Parke Davis & Co | 2,2-dimethyl-{11 -aryloxy-alkanoic acids and salts and esters thereof |
| US4027009A (en) | 1973-06-11 | 1977-05-31 | Merck & Co., Inc. | Compositions and methods for depressing blood serum cholesterol |
| JPS5246949B2 (enEXAMPLES) * | 1973-10-19 | 1977-11-29 | ||
| YU36151B (en) * | 1974-05-16 | 1982-02-25 | Pliva Zagreb | Process for preparing alpha-amino-2-adamantyl acetic acid |
| JPS5612114B2 (enEXAMPLES) | 1974-06-07 | 1981-03-18 | ||
| US4183857A (en) | 1978-07-06 | 1980-01-15 | Shell Oil Company | 3-Benzyl-3-azabicyclo(3.1.0)hexane-2,4-dione |
| NO154918C (no) | 1977-08-27 | 1987-01-14 | Bayer Ag | Analogifremgangsmaate til fremstilling av terapeutisk aktive derivater av 3,4,5-trihydroksypiperidin. |
| CA1117127A (en) | 1978-06-27 | 1982-01-26 | Janet A. Day | Derivatives of 3-azabicyclo(3.1.0)hexane and a process for their preparation |
| US4231938A (en) | 1979-06-15 | 1980-11-04 | Merck & Co., Inc. | Hypocholesteremic fermentation products and process of preparation |
| DE2951135A1 (de) | 1979-12-19 | 1981-06-25 | Hoechst Ag, 6230 Frankfurt | Sulfonylharnstoffe, verfahren zu ihrer herstellung, pharmazeutische praeparate auf basis dieser verbindungen und ihre verwendung |
| MX7065E (es) | 1980-06-06 | 1987-04-10 | Sankyo Co | Un procedimiento microbiologico para preparar derivados de ml-236b |
| US4450171A (en) | 1980-08-05 | 1984-05-22 | Merck & Co., Inc. | Antihypercholesterolemic compounds |
| US4448784A (en) | 1982-04-12 | 1984-05-15 | Hoechst-Roussel Pharmaceuticals, Inc. | 1-(Aminoalkylphenyl and aminoalkylbenzyl)-indoles and indolines and analgesic method of use thereof |
| US5354772A (en) | 1982-11-22 | 1994-10-11 | Sandoz Pharm. Corp. | Indole analogs of mevalonolactone and derivatives thereof |
| DE3324263A1 (de) | 1983-07-06 | 1985-01-17 | Hoechst Ag, 6230 Frankfurt | Derivate der 2-azabicyclo(3.1.0)hexan-3-carbonsaeure, verfahren zu ihrer herstellung, diese enthaltende mittel und deren verwendung sowie 2-azabicyclo(3.1.0)hexan-derivate als zwischenprodukte und verfahren zu deren herstellung |
| JPS6051189A (ja) | 1983-08-30 | 1985-03-22 | Sankyo Co Ltd | チアゾリジン誘導体およびその製造法 |
| DE3536687A1 (de) | 1985-10-15 | 1987-04-16 | Hoechst Ag | Verfahren zur behandlung von atherosklerose, thrombose und der peripheren gefaesskrankheit |
| DE3543999A1 (de) | 1985-12-13 | 1987-06-19 | Bayer Ag | Hochreine acarbose |
| US5614492A (en) | 1986-05-05 | 1997-03-25 | The General Hospital Corporation | Insulinotropic hormone GLP-1 (7-36) and uses thereof |
| US4681893A (en) | 1986-05-30 | 1987-07-21 | Warner-Lambert Company | Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis |
| US4759923A (en) | 1987-06-25 | 1988-07-26 | Hercules Incorporated | Process for lowering serum cholesterol using poly(diallylmethylamine) derivatives |
| JP2569746B2 (ja) | 1987-08-20 | 1997-01-08 | 日産化学工業株式会社 | キノリン系メバロノラクトン類 |
| US4924024A (en) | 1988-01-11 | 1990-05-08 | E. R. Squibb & Sons, Inc. | Phosphorus-containing squalene synthetase inhibitors, new intermediates and method |
| US4871721A (en) | 1988-01-11 | 1989-10-03 | E. R. Squibb & Sons, Inc. | Phosphorus-containing squalene synthetase inhibitors |
| NO177005C (no) | 1988-01-20 | 1995-07-05 | Bayer Ag | Analogifremgangsmåte for fremstilling av substituerte pyridiner, samt mellomprodukter til bruk ved fremstillingen |
| FI94339C (fi) | 1989-07-21 | 1995-08-25 | Warner Lambert Co | Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi |
| DE3926606A1 (de) | 1989-08-11 | 1991-02-14 | Hoechst Ag | Verfahren zur behandlung der cardialen sowie der vasculaeren hypertrophie und hyperplasie |
| US5462928A (en) | 1990-04-14 | 1995-10-31 | New England Medical Center Hospitals, Inc. | Inhibitors of dipeptidyl-aminopeptidase type IV |
| US5177080A (en) | 1990-12-14 | 1993-01-05 | Bayer Aktiengesellschaft | Substituted pyridyl-dihydroxy-heptenoic acid and its salts |
| JP2648897B2 (ja) | 1991-07-01 | 1997-09-03 | 塩野義製薬株式会社 | ピリミジン誘導体 |
| DK0610317T3 (da) | 1991-10-22 | 2001-02-19 | New England Medical Center Inc | Inhibitorer af dipeptidyl-aminopeptidase type IV |
| US5595872A (en) | 1992-03-06 | 1997-01-21 | Bristol-Myers Squibb Company | Nucleic acids encoding microsomal trigyceride transfer protein |
| DK36392D0 (da) | 1992-03-19 | 1992-03-19 | Novo Nordisk As | Anvendelse af kemisk forbindelse |
| GB9209628D0 (en) | 1992-05-05 | 1992-06-17 | Smithkline Beecham Plc | Compounds |
| US5470845A (en) | 1992-10-28 | 1995-11-28 | Bristol-Myers Squibb Company | Methods of using α-phosphonosulfonate squalene synthetase inhibitors including the treatment of atherosclerosis and hypercholesterolemia |
| US5594016A (en) | 1992-12-28 | 1997-01-14 | Mitsubishi Chemical Corporation | Naphthalene derivatives |
| WO1994016693A1 (en) | 1993-01-19 | 1994-08-04 | Warner-Lambert Company | Stable oral ci-981 formulation and process of preparing same |
| US5346701A (en) | 1993-02-22 | 1994-09-13 | Theratech, Inc. | Transmucosal delivery of macromolecular drugs |
| US5739135A (en) | 1993-09-03 | 1998-04-14 | Bristol-Myers Squibb Company | Inhibitors of microsomal triglyceride transfer protein and method |
| US5484944A (en) * | 1993-10-27 | 1996-01-16 | Neurogen Corporation | Certain fused pyrrolecarboxanilides and their use as GABA brain receptor ligands |
| IL111785A0 (en) | 1993-12-03 | 1995-01-24 | Ferring Bv | Dp-iv inhibitors and pharmaceutical compositions containing them |
| US5776983A (en) | 1993-12-21 | 1998-07-07 | Bristol-Myers Squibb Company | Catecholamine surrogates useful as β3 agonists |
| US5488064A (en) | 1994-05-02 | 1996-01-30 | Bristol-Myers Squibb Company | Benzo 1,3 dioxole derivatives |
| US5385929A (en) | 1994-05-04 | 1995-01-31 | Warner-Lambert Company | [(Hydroxyphenylamino) carbonyl] pyrroles |
| US5561146A (en) | 1994-06-10 | 1996-10-01 | Bristol-Myers Squibb Company | Modified guanidino and amidino thrombin inhibitors |
| US5491134A (en) | 1994-09-16 | 1996-02-13 | Bristol-Myers Squibb Company | Sulfonic, phosphonic or phosphiniic acid β3 agonist derivatives |
| US5541204A (en) | 1994-12-02 | 1996-07-30 | Bristol-Myers Squibb Company | Aryloxypropanolamine β 3 adrenergic agonists |
| US5620997A (en) | 1995-05-31 | 1997-04-15 | Warner-Lambert Company | Isothiazolones |
| JP3068200B2 (ja) | 1995-06-06 | 2000-07-24 | ファイザー・インコーポレーテッド | グリコーゲンホスホリラーゼ阻害剤としての置換n−(インドール−2−カルボニル−)アミドおよび誘導体 |
| MX9709875A (es) | 1995-06-06 | 1998-03-31 | Pfizer | N-(indol-2-carbonil)-glicinamidas substituidas y derivados como inhibidores de glicogeno fosforilasa, composiciones que las contienen y uso de las mismas. |
| AU6966696A (en) | 1995-10-05 | 1997-04-28 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
| DE69625825T2 (de) | 1995-10-25 | 2003-09-04 | Degussa Ag | Herbizide sulfonamide |
| EP0873361B1 (en) | 1995-12-13 | 2006-11-02 | The Regents Of The University Of California | Crystals of the ligand-binding domain of the thyroid hormone receptor complexed to a ligand |
| US5770615A (en) | 1996-04-04 | 1998-06-23 | Bristol-Myers Squibb Company | Catecholamine surrogates useful as β3 agonists |
| DE122010000020I1 (de) | 1996-04-25 | 2010-07-08 | Prosidion Ltd | Verfahren zur Senkung des Blutglukosespiegels in Säugern |
| US5962440A (en) | 1996-05-09 | 1999-10-05 | Bristol-Myers Squibb Company | Cyclic phosphonate ester inhibitors of microsomal triglyceride transfer protein and method |
| US5827875A (en) | 1996-05-10 | 1998-10-27 | Bristol-Myers Squibb Company | Inhibitors of microsomal triglyceride transfer protein and method |
| US5885983A (en) | 1996-05-10 | 1999-03-23 | Bristol-Myers Squibb Company | Inhibitors of microsomal triglyceride transfer protein and method |
| HRP970330B1 (en) | 1996-07-08 | 2004-06-30 | Bayer Ag | Cycloalkano pyridines |
| TW492957B (en) * | 1996-11-07 | 2002-07-01 | Novartis Ag | N-substituted 2-cyanopyrrolidnes |
| US6011155A (en) | 1996-11-07 | 2000-01-04 | Novartis Ag | N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV |
| US5952322A (en) | 1996-12-05 | 1999-09-14 | Pfizer Inc. | Method of reducing tissue damage associated with non-cardiac ischemia using glycogen phosphorylase inhibitors |
| US5760246A (en) | 1996-12-17 | 1998-06-02 | Biller; Scott A. | Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method |
| GB9713739D0 (en) | 1997-06-27 | 1997-09-03 | Karobio Ab | Thyroid receptor ligands |
| DE19742601A1 (de) * | 1997-09-26 | 1999-04-29 | Siemens Ag | Verfahren und Vorrichtung zur Erzeugung von Rahmen um Videobilder |
| UA57811C2 (uk) | 1997-11-21 | 2003-07-15 | Пфайзер Продактс Інк. | Фармацевтична композиція, що містить інгібітор альдозоредуктази та інгібітор глікогенфосфорилази (варіанти), комплект, який її включає, та способи лікування ссавців зі станом інсулінорезистентності |
| US6803357B1 (en) | 1998-02-02 | 2004-10-12 | New England Medical Center Hospitals, Inc. | Method of regulating glucose metabolism, and reagents related thereto |
| US5998463A (en) | 1998-02-27 | 1999-12-07 | Pfizer Inc | Glycogen phosphorylase inhibitors |
| IL136588A0 (en) | 1998-02-27 | 2001-06-14 | Pfizer Prod Inc | N-[(substituted five-membered di-or triaza diunsaturated ring) carbonyl] guanidine derivatives for the treatment of ischemia |
| WO1999047545A2 (en) * | 1998-03-19 | 1999-09-23 | Vertex Pharmaceuticals Incorporated | Inhibitors of caspases |
| DE19828114A1 (de) | 1998-06-24 | 2000-01-27 | Probiodrug Ges Fuer Arzneim | Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV |
| EP0978279A1 (en) | 1998-08-07 | 2000-02-09 | Pfizer Products Inc. | Inhibitors of human glycogen phosphorylase |
| KR20010079669A (ko) | 1998-08-21 | 2001-08-22 | 바바라 피. 월너 | 기질 활성의 조절 |
| CO5150173A1 (es) | 1998-12-10 | 2002-04-29 | Novartis Ag | Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv |
| US6462091B1 (en) | 1998-12-23 | 2002-10-08 | G.D. Searle & Co. | Combinations of cholesteryl ester transfer protein inhibitors and HMG coA reductase inhibitors for cardiovascular indications |
| AU760174B2 (en) | 1999-02-09 | 2003-05-08 | Bristol-Myers Squibb Company | Lactam inhibitors of FXa and method |
| AU2535700A (en) | 1999-02-12 | 2000-08-29 | Novo Nordisk A/S | Use of pyrrolidine derivatives for the manufacture of a pharmaceutical composition for the treatment or prophylaxis of obesity or appetite regulation |
| WO2000053171A1 (en) | 1999-03-05 | 2000-09-14 | Molteni L. E C. Dei Fratelli Alitti Societa' Di Esercizio S.P.A. | Use of metformin in the preparation of pharmaceutical compositions capable of inhibiting the enzyme dipeptidyl peptidase iv |
| GB9906715D0 (en) | 1999-03-23 | 1999-05-19 | Ferring Bv | Compositions for promoting growth |
| GB9906714D0 (en) | 1999-03-23 | 1999-05-19 | Ferring Bv | Compositions for improving fertility |
| PT1041068E (pt) | 1999-04-01 | 2004-07-30 | Pfizer Prod Inc | Compostos para o tratamento e prevencao de complicacoes diabeticas |
| JP4121215B2 (ja) | 1999-05-17 | 2008-07-23 | 財団法人微生物化学研究会 | スルフォスチン類縁体、並びにスルフォスチン及びその類縁体の製造方法 |
| US6110949A (en) | 1999-06-24 | 2000-08-29 | Novartis Ag | N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV |
| US6395767B2 (en) * | 2000-03-10 | 2002-05-28 | Bristol-Myers Squibb Company | Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method |
| JP2004518688A (ja) | 2001-01-30 | 2004-06-24 | ブリストル−マイヤーズ スクイブ カンパニー | ファクターXa阻害剤のスルホンアミドラクタムおよびその方法 |
| DE10132375A1 (de) | 2001-07-07 | 2003-01-16 | Trench Germany Gmbh | Verfahren und Vorrichtung zur Herstellung eines elektrischen Kunststoffisolators |
| CN101023052A (zh) | 2004-09-17 | 2007-08-22 | 雅宝公司 | 2-(3-羟基-1-金刚烷基)-2-乙醛酸的合成方法 |
| US7205432B2 (en) | 2005-05-31 | 2007-04-17 | Kemfine Oy | Process for the preparation of adamantane derivatives |
| KR101386282B1 (ko) | 2005-06-17 | 2014-04-17 | 아포지 바이오테크놀로지 코포레이션 | 스핑고신 키나제 저해제 |
-
2001
- 2001-02-16 US US09/788,173 patent/US6395767B2/en not_active Ceased
- 2001-02-28 EG EG2001020212A patent/EG25854A/xx active
- 2001-03-05 EP EP15186007.9A patent/EP2995615B1/en not_active Expired - Lifetime
- 2001-03-05 CZ CZ2014-33A patent/CZ307784B6/cs not_active IP Right Cessation
- 2001-03-05 PL PL365520A patent/PL207041B1/pl unknown
- 2001-03-05 DE DE122010000008C patent/DE122010000008I1/de active Pending
- 2001-03-05 AU AU2001245466A patent/AU2001245466B2/en active Active
- 2001-03-05 CN CNA2005100785188A patent/CN1698601A/zh active Pending
- 2001-03-05 IL IL15137201A patent/IL151372A0/xx unknown
- 2001-03-05 EP EP01918383A patent/EP1261586B1/en not_active Expired - Lifetime
- 2001-03-05 JP JP2001567699A patent/JP4460205B2/ja not_active Expired - Lifetime
- 2001-03-05 EP EP05005368.5A patent/EP1559710B1/en not_active Expired - Lifetime
- 2001-03-05 EP EP10178907.1A patent/EP2272825B1/en not_active Expired - Lifetime
- 2001-03-05 CA CA2402894A patent/CA2402894C/en not_active Expired - Lifetime
- 2001-03-05 MX MXPA02008837A patent/MXPA02008837A/es active IP Right Grant
- 2001-03-05 HU HU1200545A patent/HU230347B1/hu unknown
- 2001-03-05 ES ES10178907.1T patent/ES2553573T3/es not_active Expired - Lifetime
- 2001-03-05 DE DE60134122T patent/DE60134122D1/de not_active Expired - Lifetime
- 2001-03-05 TW TW095105942A patent/TW200624420A/zh unknown
- 2001-03-05 HU HU0302792A patent/HU228110B1/hu active Protection Beyond IP Right Term
- 2001-03-05 CN CNB018063152A patent/CN1213028C/zh not_active Expired - Lifetime
- 2001-03-05 AT AT01918383T patent/ATE396176T1/de active
- 2001-03-05 ES ES05005368.5T patent/ES2456667T3/es not_active Expired - Lifetime
- 2001-03-05 ES ES15186007T patent/ES2768961T3/es not_active Expired - Lifetime
- 2001-03-05 CZ CZ2015493A patent/CZ307821B6/cs not_active IP Right Cessation
- 2001-03-05 PT PT01918383T patent/PT1261586E/pt unknown
- 2001-03-05 RU RU2002125491/04A patent/RU2286986C2/ru active Protection Beyond IP Right Term
- 2001-03-05 KR KR1020027011806A patent/KR100754089B1/ko not_active Expired - Lifetime
- 2001-03-05 DK DK01918383T patent/DK1261586T3/da active
- 2001-03-05 BR BRPI0109115A patent/BRPI0109115B8/pt not_active IP Right Cessation
- 2001-03-05 HK HK03101079.9A patent/HK1049330B/en unknown
- 2001-03-05 AU AU4546601A patent/AU4546601A/xx active Pending
- 2001-03-05 TW TW090104965A patent/TWI258468B/zh not_active IP Right Cessation
- 2001-03-05 KR KR1020067004515A patent/KR100758407B1/ko not_active Expired - Lifetime
- 2001-03-05 ES ES01918383T patent/ES2305062T3/es not_active Expired - Lifetime
- 2001-03-05 SG SG200405783-2A patent/SG152030A1/en unknown
- 2001-03-05 HU HU1200546A patent/HU230380B1/hu unknown
- 2001-03-05 CZ CZ2002-2974A patent/CZ304355B6/cs unknown
- 2001-03-05 NZ NZ520821A patent/NZ520821A/en not_active IP Right Cessation
- 2001-03-05 WO PCT/US2001/007151 patent/WO2001068603A2/en active Application Filing
- 2001-03-08 CO CO01018857A patent/CO5280198A1/es active IP Right Grant
- 2001-03-09 MY MYPI20011103A patent/MY124512A/en unknown
- 2001-03-09 AR ARP010101122A patent/AR027634A1/es active IP Right Grant
- 2001-03-12 UY UY26613A patent/UY26613A1/es not_active IP Right Cessation
- 2001-06-12 PE PE2001000554A patent/PE20020771A1/es not_active Application Discontinuation
-
2002
- 2002-08-21 IL IL151372A patent/IL151372A/en active Protection Beyond IP Right Term
- 2002-08-26 ZA ZA200206816A patent/ZA200206816B/en unknown
- 2002-09-09 NO NO20024295A patent/NO324227B1/no not_active IP Right Cessation
-
2006
- 2006-07-23 IL IL177018A patent/IL177018A0/en active IP Right Grant
- 2006-07-23 IL IL177019A patent/IL177019A/en active IP Right Grant
-
2008
- 2008-08-20 CY CY20081100885T patent/CY1108273T1/el unknown
-
2010
- 2010-01-14 JP JP2010006181A patent/JP5427047B2/ja not_active Expired - Lifetime
- 2010-02-11 BE BE2010C008C patent/BE2010C008I2/fr unknown
- 2010-02-17 LU LU91650C patent/LU91650I2/fr unknown
- 2010-02-17 NL NL300436C patent/NL300436I1/nl unknown
- 2010-02-22 FR FR10C0010C patent/FR10C0010I2/fr active Active
- 2010-03-16 NO NO2010006C patent/NO2010006I2/no unknown
- 2010-03-30 CY CY2010005C patent/CY2010005I1/el unknown
-
2011
- 2011-12-01 US US13/308,658 patent/USRE44186E1/en not_active Expired - Lifetime
-
2012
- 2012-04-18 BE BE2012C016C patent/BE2012C016I2/fr unknown
- 2012-04-23 FR FR12C0028C patent/FR12C0028I2/fr active Active
- 2012-04-23 DE DE201212000023 patent/DE122012000023I1/de active Pending
- 2012-04-24 CY CY2012009C patent/CY2012009I2/el unknown
- 2012-04-25 LU LU91985C patent/LU91985I2/fr unknown
- 2012-05-21 NO NO2012009C patent/NO2012009I2/no unknown
- 2012-11-30 JP JP2012263345A patent/JP2013040219A/ja active Pending
- 2012-12-14 HU HUS1200031C patent/HUS1200031I1/hu unknown
- 2012-12-14 HU HUS1200030C patent/HUS1200030I1/hu unknown
-
2013
- 2013-03-20 UY UY0001034691A patent/UY34691A/es unknown
- 2013-12-02 JP JP2013249334A patent/JP5953292B2/ja not_active Expired - Lifetime
-
2015
- 2015-04-28 JP JP2015092196A patent/JP5951843B2/ja not_active Expired - Lifetime
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CZ307821B6 (enEXAMPLES) | ||
| JP2018523633A5 (enEXAMPLES) | ||
| US6605744B2 (en) | Production of 2-amin-2-[2-(2-(40-C2-20-alkyl-phenyl)ethyl]propane-1,3-diols | |
| CZ384697A3 (cs) | Způsob přípravy kyseliny (S)-3-(aminomethyl)-5-methylhexanové | |
| EP0742209A2 (en) | A process for producing an optically active quinolinemevalonolactone and a process for producing an optically active quinolinemevalonic acid salt | |
| JP4281248B2 (ja) | キノリン誘導体の製造法及び中間体 | |
| JP2004518737A (ja) | 2−(4−クロロベンゾイルアミノ)−3−[2(1h)−キノールリノン−4−イル]プロピオン酸の製造方法 | |
| SU843749A3 (ru) | Способ получени 4а,9в-транс- гЕКСАгидРО- -КАРбОлиНА | |
| CN106748966B (zh) | 一种雷米普利关键中间体的合成方法 | |
| RU2225859C2 (ru) | Синтез 3-амино-3-арилпропаноатов | |
| JP2005047803A (ja) | (3r,5s)−7−置換−3,5−ジヒドロキシヘプト−6−エン酸の製法 | |
| SK286717B6 (sk) | Spôsob prípravy substituovanej imidazopyridínovej zlúčeniny | |
| JP4790901B2 (ja) | 4−アミノ−5−シアノイミダゾール誘導体及びその中間体の製造方法 | |
| WO2015137408A1 (ja) | ヘテロアリールカルボン酸エステル誘導体の製造方法及びその製造中間体 | |
| KR100850558B1 (ko) | 아토르바스타틴의 효율적인 제조방법 | |
| JP3596262B2 (ja) | 2,3,4−トリフルオロ−5−トリフルオロメチル安息香酸、そのエステル類及びその製造法 | |
| KR100856133B1 (ko) | 아토르바스타틴의 개선된 제조방법 | |
| KR20090027276A (ko) | 이미다프릴의 제조 방법 및 신규한 중간체 | |
| FR2785903A1 (fr) | Derives de 1-aminoethylquinoleine, leur preparation et leur application en therapeutique | |
| JP2604589B2 (ja) | イミダゾリジン誘導体の製造法 | |
| JP3719269B2 (ja) | 2−アルキル−4−オキソ−5、6、7、8−テトラヒドロ−シクロヘプトイミダゾールの製造方法 | |
| JPH07149729A (ja) | 1,2,3,4−テトラヒドロキノリン−8−スルホン酸およびそのクロリド体、それらの製法、並びに合成中間体としてのそれらの用途 | |
| SK568590A3 (en) | Glutaric acid derivatives and method for the preparation thereof, and intermediate product of said method | |
| JPH09169748A (ja) | 2−アミノチアゾール−5−カルボニトリル誘導体の製造方法 | |
| SU904295A1 (ru) | Способ получени 3-[имидазо(1,2- @ )бензимидазолил-3]акриловых кислот |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MK4A | Patent expired |
Effective date: 20210305 |