MXPA06002049A - Una composicion farmaceutica para el tratamiento de la obesidad o para facilitar o promover la perdida de peso. - Google Patents
Una composicion farmaceutica para el tratamiento de la obesidad o para facilitar o promover la perdida de peso.Info
- Publication number
- MXPA06002049A MXPA06002049A MXPA06002049A MXPA06002049A MXPA06002049A MX PA06002049 A MXPA06002049 A MX PA06002049A MX PA06002049 A MXPA06002049 A MX PA06002049A MX PA06002049 A MXPA06002049 A MX PA06002049A MX PA06002049 A MXPA06002049 A MX PA06002049A
- Authority
- MX
- Mexico
- Prior art keywords
- methyl
- acid
- triene
- hexahydro
- methano
- Prior art date
Links
- 208000008589 Obesity Diseases 0.000 title claims abstract description 37
- 235000020824 obesity Nutrition 0.000 title claims abstract description 37
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 22
- 230000004580 weight loss Effects 0.000 title claims description 18
- 239000003446 ligand Substances 0.000 claims abstract description 30
- 238000000034 method Methods 0.000 claims abstract description 25
- 206010033307 Overweight Diseases 0.000 claims abstract description 11
- 239000003937 drug carrier Substances 0.000 claims abstract description 10
- -1 3-amino-8- (2,3-difluoro-phenyl) -5-methylene-octanoic acid Chemical compound 0.000 claims description 51
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 48
- 239000002253 acid Substances 0.000 claims description 39
- 150000003839 salts Chemical class 0.000 claims description 37
- 229940123925 Nicotinic receptor agonist Drugs 0.000 claims description 26
- 239000000181 nicotinic agonist Substances 0.000 claims description 26
- HIOSTWNYLIZTIU-UHFFFAOYSA-N (3z,7z)-1h-1,5-diazocin-2-one Chemical compound O=C1NC=CC=NC=C1 HIOSTWNYLIZTIU-UHFFFAOYSA-N 0.000 claims description 21
- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 claims description 17
- 239000000203 mixture Substances 0.000 claims description 17
- 241000124008 Mammalia Species 0.000 claims description 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 15
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 15
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 15
- 229960002715 nicotine Drugs 0.000 claims description 11
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims description 9
- FGAQZLNPJNNZOY-UHFFFAOYSA-N (2z,4z,6z)-1h-diazocin-8-one Chemical compound O=C1NN=CC=CC=C1 FGAQZLNPJNNZOY-UHFFFAOYSA-N 0.000 claims description 9
- BIGWXAGEQONZGD-UHFFFAOYSA-N 2h-oxadiazol-5-one Chemical compound O=C1C=NNO1 BIGWXAGEQONZGD-UHFFFAOYSA-N 0.000 claims description 9
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 9
- 206010020772 Hypertension Diseases 0.000 claims description 9
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 claims description 9
- XFXPMWWXUTWYJX-UHFFFAOYSA-N Cyanide Chemical compound N#[C-] XFXPMWWXUTWYJX-UHFFFAOYSA-N 0.000 claims description 8
- 230000001965 increasing effect Effects 0.000 claims description 8
- 230000003287 optical effect Effects 0.000 claims description 8
- 239000013543 active substance Substances 0.000 claims description 7
- 125000003396 thiol group Chemical group [H]S* 0.000 claims description 7
- 208000032928 Dyslipidaemia Diseases 0.000 claims description 6
- 208000010235 Food Addiction Diseases 0.000 claims description 6
- 208000017170 Lipid metabolism disease Diseases 0.000 claims description 6
- LOWSIVQZHWWKGQ-UHFFFAOYSA-N C1C2CNCC1CN1C2=CC=C(C(=O)OC)C1=O Chemical compound C1C2CNCC1CN1C2=CC=C(C(=O)OC)C1=O LOWSIVQZHWWKGQ-UHFFFAOYSA-N 0.000 claims description 5
- BGGGFMGAUXAEKO-UHFFFAOYSA-N FC1=CC=CC(F)=C1C(C1=O)=CC=C2N1CC1CNCC2C1 Chemical compound FC1=CC=CC(F)=C1C(C1=O)=CC=C2N1CC1CNCC2C1 BGGGFMGAUXAEKO-UHFFFAOYSA-N 0.000 claims description 5
- 239000004480 active ingredient Substances 0.000 claims description 5
- 239000000556 agonist Substances 0.000 claims description 5
- 229960002870 gabapentin Drugs 0.000 claims description 5
- AYXYPKUFHZROOJ-ZETCQYMHSA-N pregabalin Chemical compound CC(C)C[C@H](CN)CC(O)=O AYXYPKUFHZROOJ-ZETCQYMHSA-N 0.000 claims description 5
- IGRXMNYYQGKFCK-UHFFFAOYSA-N trideca-2,4,6-triene Chemical compound CCCCCCC=CC=CC=CC IGRXMNYYQGKFCK-UHFFFAOYSA-N 0.000 claims description 5
- 125000004215 2,4-difluorophenyl group Chemical group [H]C1=C([H])C(*)=C(F)C([H])=C1F 0.000 claims description 4
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims description 4
- DWDCLEHDNICBMI-UHFFFAOYSA-N 3-bromocytisine Chemical compound C1C2CNCC1CN1C2=CC=C(Br)C1=O DWDCLEHDNICBMI-UHFFFAOYSA-N 0.000 claims description 4
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims description 4
- NBGMTBMAENFSAW-UHFFFAOYSA-N chembl64496 Chemical compound C1C2CNCC1CN1C2=CC=C(Cl)C1=O NBGMTBMAENFSAW-UHFFFAOYSA-N 0.000 claims description 4
- 201000000083 maturity-onset diabetes of the young type 1 Diseases 0.000 claims description 4
- 229940035339 tri-chlor Drugs 0.000 claims description 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 4
- IVYDEZGCXPEAHO-HTQZYQBOSA-N (2r,4r)-2-(aminomethyl)-4-methylheptanoic acid Chemical compound CCC[C@@H](C)C[C@H](CN)C(O)=O IVYDEZGCXPEAHO-HTQZYQBOSA-N 0.000 claims description 3
- IVYDEZGCXPEAHO-JGVFFNPUSA-N (2r,4s)-2-(aminomethyl)-4-methylheptanoic acid Chemical compound CCC[C@H](C)C[C@H](CN)C(O)=O IVYDEZGCXPEAHO-JGVFFNPUSA-N 0.000 claims description 3
- GUEQOLSQPOTTME-RQJHMYQMSA-N (3s,5r)-3-amino-5-methylheptanoic acid Chemical compound CC[C@@H](C)C[C@H](N)CC(O)=O GUEQOLSQPOTTME-RQJHMYQMSA-N 0.000 claims description 3
- XKWDZEJCUWTBOM-BDAKNGLRSA-N (3s,5r)-3-amino-5-methylnonanoic acid Chemical compound CCCC[C@@H](C)C[C@H](N)CC(O)=O XKWDZEJCUWTBOM-BDAKNGLRSA-N 0.000 claims description 3
- HDLUMIBBUPOCSA-PWSUYJOCSA-N (3s,5r)-3-amino-7-cyclopentyl-5-methylheptanoic acid Chemical compound OC(=O)C[C@@H](N)C[C@H](C)CCC1CCCC1 HDLUMIBBUPOCSA-PWSUYJOCSA-N 0.000 claims description 3
- YEJJKVAYXOGIIA-UHFFFAOYSA-N 2,3-dihydro-1h-isoindole-4-carboxylic acid Chemical compound OC(=O)C1=CC=CC2=C1CNC2 YEJJKVAYXOGIIA-UHFFFAOYSA-N 0.000 claims description 3
- KYZTUNCFUQURFU-UHFFFAOYSA-N 2-(1-aminoethyl)benzoic acid Chemical compound CC(N)C1=CC=CC=C1C(O)=O KYZTUNCFUQURFU-UHFFFAOYSA-N 0.000 claims description 3
- ITHHAXKQXGKQMU-UHFFFAOYSA-N 2-(4-phenylbutylamino)acetic acid Chemical compound OC(=O)CNCCCCC1=CC=CC=C1 ITHHAXKQXGKQMU-UHFFFAOYSA-N 0.000 claims description 3
- ZTOJKCGCPJHZPN-UHFFFAOYSA-N 2-(aminomethyl)-3-[1-(4-methylpentyl)cyclopropyl]propanoic acid Chemical compound CC(C)CCCC1(CC(CN)C(O)=O)CC1 ZTOJKCGCPJHZPN-UHFFFAOYSA-N 0.000 claims description 3
- POJKDIZXVVJRGB-UHFFFAOYSA-N 2-(aminomethyl)-3-bromobenzoic acid Chemical compound NCC1=C(Br)C=CC=C1C(O)=O POJKDIZXVVJRGB-UHFFFAOYSA-N 0.000 claims description 3
- VCOJPHSIBVJVDU-UHFFFAOYSA-N 2-(aminomethyl)-4,4,8-trimethylnonanoic acid Chemical compound CC(C)CCCC(C)(C)CC(CN)C(O)=O VCOJPHSIBVJVDU-UHFFFAOYSA-N 0.000 claims description 3
- QRNWJQJJPFXIDQ-UHFFFAOYSA-N 2-(aminomethyl)-4,6-dimethylheptanoic acid Chemical compound CC(C)CC(C)CC(CN)C(O)=O QRNWJQJJPFXIDQ-UHFFFAOYSA-N 0.000 claims description 3
- NETRIHFONCPRQM-UHFFFAOYSA-N 2-(aminomethyl)-4-cyclohexyl-3-methylbutanoic acid Chemical compound NCC(C(O)=O)C(C)CC1CCCCC1 NETRIHFONCPRQM-UHFFFAOYSA-N 0.000 claims description 3
- IVYDEZGCXPEAHO-UHFFFAOYSA-N 2-(aminomethyl)-4-methylheptanoic acid Chemical compound CCCC(C)CC(CN)C(O)=O IVYDEZGCXPEAHO-UHFFFAOYSA-N 0.000 claims description 3
- UOPIILYKLVDKTK-UHFFFAOYSA-N 2-[1-(aminomethyl)-3-methylcyclohexyl]acetic acid Chemical compound CC1CCCC(CN)(CC(O)=O)C1 UOPIILYKLVDKTK-UHFFFAOYSA-N 0.000 claims description 3
- HYVKVSAZCPKHDV-UHFFFAOYSA-N 2-[1-(aminomethyl)-3-methylcyclopentyl]acetic acid Chemical compound CC1CCC(CN)(CC(O)=O)C1 HYVKVSAZCPKHDV-UHFFFAOYSA-N 0.000 claims description 3
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims description 3
- 125000004211 3,5-difluorophenyl group Chemical group [H]C1=C(F)C([H])=C(*)C([H])=C1F 0.000 claims description 3
- BWBQMUPZKXFEIP-UHFFFAOYSA-N 3-(1-aminoethyl)-5-methylheptanoic acid Chemical compound CCC(C)CC(C(C)N)CC(O)=O BWBQMUPZKXFEIP-UHFFFAOYSA-N 0.000 claims description 3
- PVOZHPMILBKJAX-UHFFFAOYSA-N 3-amino-5-methyl-7-phenylheptanoic acid Chemical compound OC(=O)CC(N)CC(C)CCC1=CC=CC=C1 PVOZHPMILBKJAX-UHFFFAOYSA-N 0.000 claims description 3
- XKWDZEJCUWTBOM-UHFFFAOYSA-N 3-amino-5-methylnonanoic acid Chemical compound CCCCC(C)CC(N)CC(O)=O XKWDZEJCUWTBOM-UHFFFAOYSA-N 0.000 claims description 3
- JXEHXYFSIOYTAH-UHFFFAOYSA-N 3-amino-5-methyloctanoic acid Chemical compound CCCC(C)CC(N)CC(O)=O JXEHXYFSIOYTAH-UHFFFAOYSA-N 0.000 claims description 3
- HDLUMIBBUPOCSA-UHFFFAOYSA-N 3-amino-7-cyclopentyl-5-methylheptanoic acid Chemical compound OC(=O)CC(N)CC(C)CCC1CCCC1 HDLUMIBBUPOCSA-UHFFFAOYSA-N 0.000 claims description 3
- WXJZPMQTLWNDGI-UHFFFAOYSA-N 3-amino-8-(2,4-difluorophenyl)-5-methyloctanoic acid Chemical compound OC(=O)CC(N)CC(C)CCCC1=CC=C(F)C=C1F WXJZPMQTLWNDGI-UHFFFAOYSA-N 0.000 claims description 3
- IUVMAUQEZFTTFB-YUMQZZPRSA-N Atagabalin Chemical compound C[C@H]1CC(CN)(CC(O)=O)C[C@@H]1C IUVMAUQEZFTTFB-YUMQZZPRSA-N 0.000 claims description 3
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- MYEABNSFVNHLCV-UHFFFAOYSA-N C1C2CNCC1CN1C2=CC=C(C)C1=O Chemical compound C1C2CNCC1CN1C2=CC=C(C)C1=O MYEABNSFVNHLCV-UHFFFAOYSA-N 0.000 claims description 3
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- MEWSNTOMQFCKKK-UHFFFAOYSA-N C1NCC2CN3C(=O)C(C#N)=CC=C3C1C2 Chemical compound C1NCC2CN3C(=O)C(C#N)=CC=C3C1C2 MEWSNTOMQFCKKK-UHFFFAOYSA-N 0.000 claims description 3
- ZOHVETOLVNHRNP-UHFFFAOYSA-N FC1=CC=CC=C1C(C1=O)=CC=C2N1CC1CNCC2C1 Chemical compound FC1=CC=CC=C1C(C1=O)=CC=C2N1CC1CNCC2C1 ZOHVETOLVNHRNP-UHFFFAOYSA-N 0.000 claims description 3
- JXEHXYFSIOYTAH-SFYZADRCSA-N imagabalin Chemical compound CCC[C@@H](C)C[C@H](N)CC(O)=O JXEHXYFSIOYTAH-SFYZADRCSA-N 0.000 claims description 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 3
- 150000004702 methyl esters Chemical class 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
- BJANXPDEYWSHLC-UHFFFAOYSA-N tert-butyl 2-[2-(4-methylsulfanylphenyl)sulfanylethylamino]acetate Chemical compound CSC1=CC=C(SCCNCC(=O)OC(C)(C)C)C=C1 BJANXPDEYWSHLC-UHFFFAOYSA-N 0.000 claims description 3
- LLAPDLPYIYKTGQ-UHFFFAOYSA-N 1-aminoethyl Chemical group C[CH]N LLAPDLPYIYKTGQ-UHFFFAOYSA-N 0.000 claims description 2
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- KFUYJCLUBOFHHM-UHFFFAOYSA-N 2-(aminomethyl)-3-(1-methylcyclopropyl)propanoic acid Chemical compound NCC(C(O)=O)CC1(C)CC1 KFUYJCLUBOFHHM-UHFFFAOYSA-N 0.000 claims description 2
- PGWUHTMNEHONRF-UHFFFAOYSA-N 2-(aminomethyl)-4,5-dichlorobenzoic acid Chemical compound NCC1=CC(Cl)=C(Cl)C=C1C(O)=O PGWUHTMNEHONRF-UHFFFAOYSA-N 0.000 claims description 2
- ATYKFZPYPABAPV-UHFFFAOYSA-N 2-(aminomethyl)-5-chlorobenzoic acid Chemical compound NCC1=CC=C(Cl)C=C1C(O)=O ATYKFZPYPABAPV-UHFFFAOYSA-N 0.000 claims description 2
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- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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Landscapes
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- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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| US49735303P | 2003-08-22 | 2003-08-22 | |
| PCT/IB2004/002604 WO2005018622A1 (en) | 2003-08-22 | 2004-08-09 | A pharmaceutical composition for the treatment of obesity or to facilitate or promote weight loss |
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| MXPA06002049A true MXPA06002049A (es) | 2006-05-19 |
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| MXPA06002049A MXPA06002049A (es) | 2003-08-22 | 2004-08-09 | Una composicion farmaceutica para el tratamiento de la obesidad o para facilitar o promover la perdida de peso. |
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| EP (1) | EP1658059A1 (enExample) |
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| CA (1) | CA2534271A1 (enExample) |
| MX (1) | MXPA06002049A (enExample) |
| WO (1) | WO2005018622A1 (enExample) |
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| WO2005000806A2 (en) * | 2003-06-10 | 2005-01-06 | Georgetown University | Ligands for nicotinic acetylcholine receptors, and methods of making and using them |
| EP1670452A2 (en) * | 2003-09-25 | 2006-06-21 | Warner-Lambert Company LLC | Method of use of aminoacids having affinity for the a2d protein |
| KR100768974B1 (ko) * | 2003-09-25 | 2007-10-22 | 워너-램버트 캄파니 엘엘씨 | 알파2델타-단백질에 대한 친화성을 갖는 아미노산 |
| WO2007115092A2 (en) * | 2006-03-29 | 2007-10-11 | Georgetown University | 10-substituted cytisine derivatives and methods of use thereof |
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| TR200001840T2 (tr) * | 1997-12-31 | 2000-12-21 | Pfizer Products Inc. | Arile bağlı azopolisiklik bileşikler |
| AU3735000A (en) * | 1999-05-05 | 2000-11-21 | Warner-Lambert Company | Modulation of substance p by gaba analogs and methods relating thereto |
| US20010036943A1 (en) * | 2000-04-07 | 2001-11-01 | Coe Jotham W. | Pharmaceutical composition for treatment of acute, chronic pain and/or neuropathic pain and migraines |
| US20020010192A1 (en) * | 2000-06-02 | 2002-01-24 | Coe Jotham Wadsworth | Pharmaceutical composition for the treatment of obesity or to facilitate or promote weight loss |
| CA2451267A1 (en) * | 2002-12-13 | 2004-06-13 | Warner-Lambert Company Llc | Pharmaceutical uses for alpha2delta ligands |
-
2004
- 2004-06-17 US US10/870,208 patent/US20050043406A1/en not_active Abandoned
- 2004-08-09 MX MXPA06002049A patent/MXPA06002049A/es unknown
- 2004-08-09 BR BRPI0413670-5A patent/BRPI0413670A/pt not_active IP Right Cessation
- 2004-08-09 WO PCT/IB2004/002604 patent/WO2005018622A1/en not_active Ceased
- 2004-08-09 JP JP2006523699A patent/JP2007503384A/ja not_active Abandoned
- 2004-08-09 CA CA002534271A patent/CA2534271A1/en not_active Abandoned
- 2004-08-09 EP EP04744239A patent/EP1658059A1/en not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| BRPI0413670A (pt) | 2006-10-24 |
| JP2007503384A (ja) | 2007-02-22 |
| US20050043406A1 (en) | 2005-02-24 |
| WO2005018622A1 (en) | 2005-03-03 |
| EP1658059A1 (en) | 2006-05-24 |
| CA2534271A1 (en) | 2005-03-03 |
| WO2005018622A8 (en) | 2005-04-28 |
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