CZ20011785A3 - Pouľití benzoylguanidinů pro oąetřování diabetes mellitus nezávislého na inzulínu - Google Patents

Pouľití benzoylguanidinů pro oąetřování diabetes mellitus nezávislého na inzulínu Download PDF

Info

Publication number: CZ20011785A3
Authority: CZ; Czechia
Prior art keywords: group; methyl; het; insulin; diaminomethylene
Prior art date: 1998-11-26

Application number

CZ20011785A

Other languages

Czech (cs)

English (en)

Inventor

Rolf Gericke

Manfred Baumgarth

Klaus Minck

Didier Mesangeau

Liliane Doare

Micheline Kergoat

Original Assignee

Merck Patent Gmbh

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

1998-11-26

Filing date

1999-11-16

Publication date

2001-10-17

1999-11-16 Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh

2001-10-17 Publication of CZ20011785A3 publication Critical patent/CZ20011785A3/cs

Links

AJDQRQQNNLZLPM-UHFFFAOYSA-N n-(diaminomethylidene)benzamide Chemical class NC(N)=NC(=O)C1=CC=CC=C1 AJDQRQQNNLZLPM-UHFFFAOYSA-N 0.000 title claims abstract description 10
206010012601 diabetes mellitus Diseases 0.000 title claims description 9
NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 title claims description 8
102000004877 Insulin Human genes 0.000 title claims description 4
108090001061 Insulin Proteins 0.000 title claims description 4
229940125396 insulin Drugs 0.000 title claims description 4
125000004432 carbon atom Chemical group C* 0.000 claims abstract description 23
150000003839 salts Chemical class 0.000 claims abstract description 18
125000000217 alkyl group Chemical group 0.000 claims abstract description 14
208000001072 type 2 diabetes mellitus Diseases 0.000 claims abstract description 14
238000004519 manufacturing process Methods 0.000 claims abstract description 11
239000012453 solvate Substances 0.000 claims abstract description 9
125000000753 cycloalkyl group Chemical group 0.000 claims abstract description 8
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract description 5
150000001875 compounds Chemical class 0.000 claims description 36
239000004480 active ingredient Substances 0.000 claims description 8
239000008194 pharmaceutical composition Substances 0.000 claims description 7
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 6
239000000203 mixture Substances 0.000 claims description 5
229910052801 chlorine Inorganic materials 0.000 claims description 4
UADMBZFZZOBWBB-UHFFFAOYSA-N n-(diaminomethylidene)-2-methyl-5-methylsulfonyl-4-pyrrol-1-ylbenzamide Chemical compound C1=C(C(=O)N=C(N)N)C(C)=CC(N2C=CC=C2)=C1S(C)(=O)=O UADMBZFZZOBWBB-UHFFFAOYSA-N 0.000 claims description 4
229910052760 oxygen Inorganic materials 0.000 claims description 4
229910005965 SO 2 Inorganic materials 0.000 claims description 3
125000006615 aromatic heterocyclic group Chemical group 0.000 claims description 3
QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 3
125000002619 bicyclic group Chemical group 0.000 claims description 3
125000002950 monocyclic group Chemical group 0.000 claims description 3
XYEIQWWYUKARGX-UHFFFAOYSA-N n-(diaminomethylidene)-2-methyl-5-methylsulfonyl-4-(trifluoromethyl)benzamide Chemical compound CC1=CC(C(F)(F)F)=C(S(C)(=O)=O)C=C1C(=O)N=C(N)N XYEIQWWYUKARGX-UHFFFAOYSA-N 0.000 claims description 3
HNFKKQSEFIJHEP-UHFFFAOYSA-N n-(diaminomethylidene)-2-methyl-5-methylsulfonyl-4-propan-2-ylbenzamide Chemical compound CC(C)C1=CC(C)=C(C(=O)N=C(N)N)C=C1S(C)(=O)=O HNFKKQSEFIJHEP-UHFFFAOYSA-N 0.000 claims description 3
229910052757 nitrogen Inorganic materials 0.000 claims description 3
239000001301 oxygen Substances 0.000 claims description 3
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 3
229920006395 saturated elastomer Polymers 0.000 claims description 3
229910052794 bromium Inorganic materials 0.000 claims description 2
NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
239000003795 chemical substances by application Substances 0.000 claims 1
229910052717 sulfur Inorganic materials 0.000 claims 1
239000011593 sulfur Substances 0.000 claims 1
208000035408 type 1 diabetes mellitus 1 Diseases 0.000 claims 1
239000003814 drug Substances 0.000 abstract description 10
-1 3,3-dimethylbutyl Chemical group 0.000 description 53
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 15
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 13
125000001462 1-pyrrolyl group Chemical group [*]N1C([H])=C([H])C([H])=C1[H] 0.000 description 11
239000002253 acid Substances 0.000 description 8
239000000243 solution Substances 0.000 description 8
125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 description 7
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125000004076 pyridyl group Chemical group 0.000 description 7
125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 7
125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 description 5
125000005479 oxodihydropyridyl group Chemical group 0.000 description 5
125000004483 piperidin-3-yl group Chemical group N1CC(CCC1)* 0.000 description 5
239000003826 tablet Substances 0.000 description 5
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HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 description 4
125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 4
QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 3
KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 3
239000002585 base Substances 0.000 description 3
239000000460 chlorine Substances 0.000 description 3
239000012154 double-distilled water Substances 0.000 description 3
239000007924 injection Substances 0.000 description 3
238000002347 injection Methods 0.000 description 3
125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 3
230000000144 pharmacologic effect Effects 0.000 description 3
239000000829 suppository Substances 0.000 description 3
239000000454 talc Substances 0.000 description 3
235000012222 talc Nutrition 0.000 description 3
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XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 description 2
125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 description 2
VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical compound C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 description 2
NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
102000052126 Sodium-Hydrogen Exchangers Human genes 0.000 description 2
108091006672 Sodium–hydrogen antiporter Proteins 0.000 description 2
239000013543 active substance Substances 0.000 description 2
230000001154 acute effect Effects 0.000 description 2
239000003708 ampul Substances 0.000 description 2
230000003178 anti-diabetic effect Effects 0.000 description 2
125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
230000001413 cellular effect Effects 0.000 description 2
125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 2
125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 2
XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 2
BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 description 2
239000008298 dragée Substances 0.000 description 2
229910052731 fluorine Inorganic materials 0.000 description 2
229920000159 gelatin Polymers 0.000 description 2
235000019322 gelatine Nutrition 0.000 description 2
239000008103 glucose Substances 0.000 description 2
125000000623 heterocyclic group Chemical group 0.000 description 2
239000003112 inhibitor Substances 0.000 description 2
239000008101 lactose Substances 0.000 description 2
239000007788 liquid Substances 0.000 description 2
235000019359 magnesium stearate Nutrition 0.000 description 2
BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 description 2
239000002674 ointment Substances 0.000 description 2
125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 description 2
235000019271 petrolatum Nutrition 0.000 description 2
235000011007 phosphoric acid Nutrition 0.000 description 2
WLJVNTCWHIRURA-UHFFFAOYSA-N pimelic acid Chemical compound OC(=O)CCCCCC(O)=O WLJVNTCWHIRURA-UHFFFAOYSA-N 0.000 description 2
229920001592 potato starch Polymers 0.000 description 2
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125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 2
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239000000126 substance Substances 0.000 description 2
125000004434 sulfur atom Chemical group 0.000 description 2
125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 2
VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 2
125000004178 (C1-C4) alkyl group Chemical group 0.000 description 1
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OOSZCNKVJAVHJI-UHFFFAOYSA-N 1-[(4-fluorophenyl)methyl]piperazine Chemical compound C1=CC(F)=CC=C1CN1CCNCC1 OOSZCNKVJAVHJI-UHFFFAOYSA-N 0.000 description 1
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OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 description 1
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125000004539 5-benzimidazolyl group Chemical group N1=CNC2=C1C=CC(=C2)* 0.000 description 1
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125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
201000001421 hyperglycemia Diseases 0.000 description 1
239000007943 implant Substances 0.000 description 1
239000012442 inert solvent Substances 0.000 description 1
230000003914 insulin secretion Effects 0.000 description 1
125000004491 isohexyl group Chemical group C(CCC(C)C)* 0.000 description 1
238000002955 isolation Methods 0.000 description 1
125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 description 1
VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
239000011976 maleic acid Substances 0.000 description 1
229910052751 metal Inorganic materials 0.000 description 1
239000002184 metal Substances 0.000 description 1
XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 description 1
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125000006217 methyl sulfide group Chemical group [H]C([H])([H])S* 0.000 description 1
150000007522 mineralic acids Chemical class 0.000 description 1
125000004312 morpholin-2-yl group Chemical group [H]N1C([H])([H])C([H])([H])OC([H])(*)C1([H])[H] 0.000 description 1
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LNOPIUAQISRISI-UHFFFAOYSA-N n'-hydroxy-2-propan-2-ylsulfonylethanimidamide Chemical compound CC(C)S(=O)(=O)CC(N)=NO LNOPIUAQISRISI-UHFFFAOYSA-N 0.000 description 1
WNBSDCKJFDZMHT-UHFFFAOYSA-N n-(diaminomethylidene)pyrazine-2-carboxamide Chemical class NC(N)=NC(=O)C1=CN=CC=N1 WNBSDCKJFDZMHT-UHFFFAOYSA-N 0.000 description 1
YZMHQCWXYHARLS-UHFFFAOYSA-N naphthalene-1,2-disulfonic acid Chemical compound C1=CC=CC2=C(S(O)(=O)=O)C(S(=O)(=O)O)=CC=C21 YZMHQCWXYHARLS-UHFFFAOYSA-N 0.000 description 1
125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
230000003204 osmotic effect Effects 0.000 description 1
125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 description 1
238000007911 parenteral administration Methods 0.000 description 1
125000003538 pentan-3-yl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])[H] 0.000 description 1
125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 1
229940066842 petrolatum Drugs 0.000 description 1
239000000546 pharmaceutical excipient Substances 0.000 description 1
150000003016 phosphoric acids Chemical class 0.000 description 1
OXNIZHLAWKMVMX-UHFFFAOYSA-N picric acid Chemical class OC1=C([N+]([O-])=O)C=C([N+]([O-])=O)C=C1[N+]([O-])=O OXNIZHLAWKMVMX-UHFFFAOYSA-N 0.000 description 1
239000006187 pill Substances 0.000 description 1
125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 description 1
IUGYQRQAERSCNH-UHFFFAOYSA-N pivalic acid Chemical compound CC(C)(C)C(O)=O IUGYQRQAERSCNH-UHFFFAOYSA-N 0.000 description 1
229920001223 polyethylene glycol Polymers 0.000 description 1
230000003389 potentiating effect Effects 0.000 description 1
238000002360 preparation method Methods 0.000 description 1
239000003755 preservative agent Substances 0.000 description 1
235000019260 propionic acid Nutrition 0.000 description 1
238000000746 purification Methods 0.000 description 1
125000003373 pyrazinyl group Chemical group 0.000 description 1
125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 description 1
125000004940 pyridazin-4-yl group Chemical group N1=NC=C(C=C1)* 0.000 description 1
125000004943 pyrimidin-6-yl group Chemical group N1=CN=CC=C1* 0.000 description 1
IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
125000003548 sec-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
239000011734 sodium Substances 0.000 description 1
229940074545 sodium dihydrogen phosphate dihydrate Drugs 0.000 description 1
239000007787 solid Substances 0.000 description 1
239000002904 solvent Substances 0.000 description 1
239000008347 soybean phospholipid Substances 0.000 description 1
239000003381 stabilizer Substances 0.000 description 1
235000019698 starch Nutrition 0.000 description 1
ZSJLQEPLLKMAKR-GKHCUFPYSA-N streptozocin Chemical compound O=NN(C)C(=O)N[C@H]1[C@@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O ZSJLQEPLLKMAKR-GKHCUFPYSA-N 0.000 description 1
229960001052 streptozocin Drugs 0.000 description 1
239000005720 sucrose Substances 0.000 description 1
150000003460 sulfonic acids Chemical class 0.000 description 1
QAOWNCQODCNURD-UHFFFAOYSA-N sulfuric acid group Chemical class S(O)(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 1
239000000725 suspension Substances 0.000 description 1
239000006188 syrup Substances 0.000 description 1
235000020357 syrup Nutrition 0.000 description 1
238000011200 topical administration Methods 0.000 description 1
230000000699 topical effect Effects 0.000 description 1
235000010487 tragacanth Nutrition 0.000 description 1
239000000196 tragacanth Substances 0.000 description 1
229940116362 tragacanth Drugs 0.000 description 1
URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 description 1
229960002622 triacetin Drugs 0.000 description 1
150000003626 triacylglycerols Chemical class 0.000 description 1
125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 1
235000015112 vegetable and seed oil Nutrition 0.000 description 1
239000008158 vegetable oil Substances 0.000 description 1
239000011782 vitamin Substances 0.000 description 1
229940088594 vitamin Drugs 0.000 description 1
229930003231 vitamin Natural products 0.000 description 1
235000013343 vitamin Nutrition 0.000 description 1
238000005303 weighing Methods 0.000 description 1
239000000080 wetting agent Substances 0.000 description 1

Classifications

- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- 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
- A61K31/402—1-aryl substituted, e.g. piretanide
- 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
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones

Landscapes

Health & Medical Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
Chemical & Material Sciences (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Animal Behavior & Ethology (AREA)
Life Sciences & Earth Sciences (AREA)
Diabetes (AREA)
Epidemiology (AREA)
Chemical Kinetics & Catalysis (AREA)
Organic Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Endocrinology (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Hematology (AREA)
Obesity (AREA)
Emergency Medicine (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Pyrrole Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

CZ20011785A 1998-11-26 1999-11-16 Pouľití benzoylguanidinů pro oąetřování diabetes mellitus nezávislého na inzulínu CZ20011785A3 (cs)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
EP98122419		1998-11-26

Publications (1)

Publication Number	Publication Date
CZ20011785A3 true CZ20011785A3 (cs)	2001-10-17

Family

ID=8233036

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
CZ20011785A CZ20011785A3 (cs)	1998-11-26	1999-11-16	Pouľití benzoylguanidinů pro oąetřování diabetes mellitus nezávislého na inzulínu

Country Status (14)

Country	Link
EP (1)	EP1131064A2 (pt)
JP (1)	JP2002530325A (pt)
KR (1)	KR20010080597A (pt)
CN (1)	CN1328452A (pt)
AR (1)	AR023064A1 (pt)
AU (1)	AU1553500A (pt)
BR (1)	BR9915667A (pt)
CA (1)	CA2352154A1 (pt)
CZ (1)	CZ20011785A3 (pt)
HU (1)	HUP0104418A2 (pt)
ID (1)	ID29523A (pt)
NO (1)	NO20012563L (pt)
PL (1)	PL348152A1 (pt)
WO (1)	WO2000030624A2 (pt)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
CN101103977A (zh) *	2002-06-05	2008-01-16	株式会社医药分子设计研究所	糖尿病治疗药
US7381841B2 (en)	2003-08-22	2008-06-03	Sanofi-Aventis Deutschland Gmbh	Pentafluorosulfanylphenyl-substituted benzoylguanidines, processes for their preparation, their use as medicament or diagnostic aid, and medicament comprising them
DE102004054847A1 (de) *	2004-11-13	2006-05-24	Sanofi-Aventis Deutschland Gmbh	Substituierte Benzoylguanidine, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament oder Diagnostikum sowie sie enthaltendes Medikament

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
DE4430916A1 (de) *	1994-08-31	1996-03-07	Merck Patent Gmbh	Alkyl-benzoylguanidin-Derivate
DE4430861A1 (de) *	1994-08-31	1996-03-07	Merck Patent Gmbh	Heterocyclyl-benzoylguanidine
DE4437874A1 (de) *	1994-10-22	1996-04-25	Merck Patent Gmbh	Alkyl-5-methylsulfonyl-benzoylguanidin-Derivate
DE19502644A1 (de) *	1995-01-28	1996-08-01	Merck Patent Gmbh	4-Amino-benzoylguanidin-Derivate
DE19502895A1 (de) *	1995-01-31	1996-08-01	Merck Patent Gmbh	4-Mercapto-benzoylguanidin-Derivate
DE19517848A1 (de) *	1995-05-16	1996-11-21	Merck Patent Gmbh	Fluorhaltige Benzoylguanidine
DE19531138A1 (de) *	1995-08-24	1997-02-27	Merck Patent Gmbh	Alkenyl-benzoylguanidin-Derivate

1999
- 1999-11-16 BR BR9915667-9A patent/BR9915667A/pt not_active Application Discontinuation
- 1999-11-16 KR KR1020017006615A patent/KR20010080597A/ko not_active Withdrawn
- 1999-11-16 CZ CZ20011785A patent/CZ20011785A3/cs unknown
- 1999-11-16 WO PCT/EP1999/008795 patent/WO2000030624A2/en not_active Ceased
- 1999-11-16 HU HU0104418A patent/HUP0104418A2/hu unknown
- 1999-11-16 EP EP99958047A patent/EP1131064A2/en not_active Ceased
- 1999-11-16 JP JP2000583507A patent/JP2002530325A/ja active Pending
- 1999-11-16 ID IDW00200101318A patent/ID29523A/id unknown
- 1999-11-16 CA CA002352154A patent/CA2352154A1/en not_active Abandoned
- 1999-11-16 AU AU15535/00A patent/AU1553500A/en not_active Abandoned
- 1999-11-16 CN CN99813826A patent/CN1328452A/zh active Pending
- 1999-11-16 PL PL99348152A patent/PL348152A1/xx unknown
- 1999-11-26 AR ARP990106043A patent/AR023064A1/es unknown
2001
- 2001-05-25 NO NO20012563A patent/NO20012563L/no not_active Application Discontinuation

Also Published As

Publication number	Publication date
NO20012563D0 (no)	2001-05-25
CN1328452A (zh)	2001-12-26
ID29523A (id)	2001-09-06
PL348152A1 (en)	2002-05-06
HUP0104418A2 (hu)	2002-04-29
EP1131064A2 (en)	2001-09-12
JP2002530325A (ja)	2002-09-17
AU1553500A (en)	2000-06-13
CA2352154A1 (en)	2000-06-02
BR9915667A (pt)	2001-08-14
KR20010080597A (ko)	2001-08-22
WO2000030624A3 (en)	2000-10-05
NO20012563L (no)	2001-05-25
AR023064A1 (es)	2002-09-04
WO2000030624A2 (en)	2000-06-02

Publication	Publication Date	Title
EP0699666B1 (de)	1999-01-07	Heterocyclyl-benzoylguanidine
DE10161767A1 (de)	2003-06-26	2-Guanidino-4-heterocyclyl-chinazoline
US6399658B1 (en)	2002-06-04	Composition containing ascorbic acid
EP1370525B1 (en)	2009-11-18	Biguanide derivatives
EP0699663B1 (de)	1998-11-04	Alkyl-benzoylguanidin-Derivate
CZ20011785A3 (cs)	2001-10-17	Pouľití benzoylguanidinů pro oąetřování diabetes mellitus nezávislého na inzulínu
CZ140896A3 (en)	1997-02-12	Derivative of fluorine containing benzoylguanidine, process of its preparation and pharmaceutical composition containing thereof
DE19706675A1 (de)	1998-08-27	Sulfonamid-substituierte Chromane, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament oder Diagnostikum sowie sie enthaltendes Medikament
EP0723963B1 (de)	2001-06-13	4-Amino-benzoylguanidin-Derivate
WO2003039543A1 (de)	2003-05-15	Derivate des phenoxy-n-'4-(isothiazolidin-1,1-dioxid-2yl)pheny!-valerian-säureamids und andere verbindungen als inhibitoren des koagulationsfaktors xa zur behandlung von thromboembolischen erkrankungen und tumoren
RU2160732C2 (ru)	2000-12-20	Гетероциклилокси-бензоилгуанидины, способы их получения, их фармацевтическая композиция и способ ее получения
EP1385818A2 (de)	2004-02-04	Biurethanderivate
EP0725062B1 (de)	2001-06-13	4-Mercapto-benzoylguanidin-Derivate
JPH0317083A (ja)	1991-01-25	置換チエノピリミジン誘導体
EP1499591A1 (de)	2005-01-26	Carbonsäureamide als inhibitoren des koagulationsfaktors xa
MXPA01005295A (en)	2002-06-05	Use of benzoylguanidines for the treatment of non-insulin-dependent diabetes mellitus
DE19705133A1 (de)	1998-08-13	Sulfonamid-substituierte Verbindungen, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament oder Diagnostikum sowie sie enthaltendes Medikament
DE10129508A1 (de)	2003-01-09	Verwendung von Inhibitoren des Na+/H+-Antiporters zur Krebsbekämpfung