ZA200303638B - Piperidine MCH antagonists and their use in the treatment of obesity. - Google Patents
Piperidine MCH antagonists and their use in the treatment of obesity. Download PDFInfo
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- ZA200303638B ZA200303638B ZA200303638A ZA200303638A ZA200303638B ZA 200303638 B ZA200303638 B ZA 200303638B ZA 200303638 A ZA200303638 A ZA 200303638A ZA 200303638 A ZA200303638 A ZA 200303638A ZA 200303638 B ZA200303638 B ZA 200303638B
- Authority
- ZA
- South Africa
- Prior art keywords
- alkyl
- compound
- group
- aryl
- composition
- Prior art date
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- 125000002346 iodo group Chemical group I* 0.000 description 1
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- 239000010410 layer Substances 0.000 description 1
- 238000004895 liquid chromatography mass spectrometry Methods 0.000 description 1
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- 229940063718 lodine Drugs 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 230000002934 lysing effect Effects 0.000 description 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
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- CZNGTXVOZOWWKM-UHFFFAOYSA-N methyl 4-bromobenzoate Chemical compound COC(=O)C1=CC=C(Br)C=C1 CZNGTXVOZOWWKM-UHFFFAOYSA-N 0.000 description 1
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- 125000002757 morpholinyl group Chemical group 0.000 description 1
- 239000003149 muscarinic antagonist Substances 0.000 description 1
- CMWYAOXYQATXSI-UHFFFAOYSA-N n,n-dimethylformamide;piperidine Chemical compound CN(C)C=O.C1CCNCC1 CMWYAOXYQATXSI-UHFFFAOYSA-N 0.000 description 1
- RCHKEJKUUXXBSM-UHFFFAOYSA-N n-benzyl-2-(3-formylindol-1-yl)acetamide Chemical compound C12=CC=CC=C2C(C=O)=CN1CC(=O)NCC1=CC=CC=C1 RCHKEJKUUXXBSM-UHFFFAOYSA-N 0.000 description 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 1
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- HGIYUCGNFWTGMD-UHFFFAOYSA-N quinazoline-6-carbaldehyde Chemical compound N1=CN=CC2=CC(C=O)=CC=C21 HGIYUCGNFWTGMD-UHFFFAOYSA-N 0.000 description 1
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- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 1
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- 241001223854 teleost fish Species 0.000 description 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
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Classifications
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- 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
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4525—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/453—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
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- A—HUMAN NECESSITIES
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- 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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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/34—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Applications Claiming Priority (1)
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US25787300P | 2000-12-22 | 2000-12-22 |
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EP (1) | EP1343761B1 (es) |
JP (2) | JP4025200B2 (es) |
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CN (1) | CN1273451C (es) |
AR (1) | AR031930A1 (es) |
AT (1) | ATE302185T1 (es) |
AU (1) | AU2002231097B2 (es) |
CA (1) | CA2431953A1 (es) |
DE (1) | DE60112791T2 (es) |
ES (1) | ES2243588T3 (es) |
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PE (1) | PE20020658A1 (es) |
WO (1) | WO2002051809A1 (es) |
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EP1366030A2 (en) | 2000-07-06 | 2003-12-03 | Neurogen Corporation | Melanin concentrating hormone receptor ligands |
US6809104B2 (en) | 2001-05-04 | 2004-10-26 | Tularik Inc. | Fused heterocyclic compounds |
EP1392298B1 (en) | 2001-05-04 | 2009-02-18 | Amgen Inc. | Fused heterocyclic compounds |
MXPA03010612A (es) * | 2001-05-22 | 2004-04-02 | Neurogen Corp | Ligandos receptores de la hormona concentradora de melanina: analogos de 1-bencil-4-aril piperazina substiruidos. |
WO2003045313A2 (en) | 2001-11-27 | 2003-06-05 | Merck & Co. Inc. | 2-aminoquinoline compounds |
JP2005526709A (ja) | 2002-01-10 | 2005-09-08 | ニューロジェン・コーポレーション | メラニン凝集ホルモン受容体リガンド:置換ベンゾイミダゾールアナログ |
CA2473236A1 (en) | 2002-01-10 | 2003-07-24 | Neurogen Corporation | Melanin concentrating hormone receptor ligands: substituted 2-(4-benzyl-piperazin-1-ylmethyl)- and 2-(4-benzyl-diazepan-1-ylmethyl)-1h-benzoimidazole analogues |
US7105526B2 (en) | 2002-06-28 | 2006-09-12 | Banyu Pharmaceuticals Co., Ltd. | Benzimidazole derivatives |
DE10238865A1 (de) * | 2002-08-24 | 2004-03-11 | Boehringer Ingelheim International Gmbh | Neue Carbonsäureamid-Verbindungen mit MCH-antagonistischer Wirkung, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung |
US7351719B2 (en) | 2002-10-31 | 2008-04-01 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Amide compounds having MCH-antagonistic activity and medicaments comprising these compounds |
PL376659A1 (pl) * | 2002-11-06 | 2006-01-09 | Tularik Inc. | Skondensowane związki heterocykliczne |
US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
WO2004069798A1 (ja) * | 2003-02-10 | 2004-08-19 | Banyu Pharmaceutical Co.,Ltd. | ピペリジン誘導体を有効成分とするメラニン凝集ホルモン受容体拮抗剤 |
WO2004072018A1 (ja) * | 2003-02-12 | 2004-08-26 | Takeda Pharmaceutical Company Limited | アミン誘導体 |
US20050256161A1 (en) * | 2003-08-13 | 2005-11-17 | Tempest Paul A | Melanin concentrating hormone receptor antagonists |
MXPA06001636A (es) * | 2003-08-13 | 2006-04-28 | Amgen Inc | Antagonista del receptor de la hormona concentradora de melanina. |
WO2005028438A1 (ja) | 2003-09-22 | 2005-03-31 | Banyu Pharmaceutical Co., Ltd. | 新規ピペリジン誘導体 |
US20060247239A1 (en) * | 2003-10-01 | 2006-11-02 | Hu Xiufeng E | Melanin concentrating hormone antagonists |
EP1667958A2 (en) * | 2003-10-01 | 2006-06-14 | The Procter & Gamble Company | Melanin concentrating hormone antagonists |
US7592373B2 (en) | 2003-12-23 | 2009-09-22 | Boehringer Ingelheim International Gmbh | Amide compounds with MCH antagonistic activity and medicaments comprising these compounds |
EP2305352A1 (en) | 2004-04-02 | 2011-04-06 | Merck Sharp & Dohme Corp. | 5-alpha-reductase inhibitors for use in the treatment of men with metabolic and anthropometric disorders |
US20050239791A1 (en) * | 2004-04-07 | 2005-10-27 | Hutchison Alan J | Substituted 1-heteroaryl-4-substituted piperazine and piperidine analogues |
WO2005110982A2 (en) * | 2004-04-07 | 2005-11-24 | Neurogen Corporation | Substituted 1-benzyl-4-substituted piperazine analogues |
DE102004017934A1 (de) | 2004-04-14 | 2005-11-03 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel |
US7524862B2 (en) | 2004-04-14 | 2009-04-28 | Boehringer Ingelheim International Gmbh | Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds |
TW200609219A (en) * | 2004-06-17 | 2006-03-16 | Neurogen Corp | Aryl-substituted piperazine derivatives |
US7063034B2 (en) * | 2004-08-10 | 2006-06-20 | Watermark Paddlesports, Inc. | Spray skirt for watercraft |
CA2577060A1 (en) | 2004-08-13 | 2006-02-23 | Amgen Inc. | Substituted benzofused heterocycles |
US8394765B2 (en) | 2004-11-01 | 2013-03-12 | Amylin Pharmaceuticals Llc | Methods of treating obesity with two different anti-obesity agents |
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2001
- 2001-12-17 DE DE60112791T patent/DE60112791T2/de not_active Expired - Lifetime
- 2001-12-17 HU HU0302582A patent/HUP0302582A2/hu unknown
- 2001-12-17 AR ARP010105839A patent/AR031930A1/es unknown
- 2001-12-17 AT AT01991369T patent/ATE302185T1/de not_active IP Right Cessation
- 2001-12-17 KR KR10-2003-7008345A patent/KR20040011447A/ko not_active Application Discontinuation
- 2001-12-17 JP JP2002552906A patent/JP4025200B2/ja not_active Expired - Fee Related
- 2001-12-17 MX MXPA03005744A patent/MXPA03005744A/es active IP Right Grant
- 2001-12-17 EP EP01991369A patent/EP1343761B1/en not_active Expired - Lifetime
- 2001-12-17 ES ES01991369T patent/ES2243588T3/es not_active Expired - Lifetime
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- 2001-12-17 CN CNB018210066A patent/CN1273451C/zh not_active Expired - Fee Related
- 2001-12-17 AU AU2002231097A patent/AU2002231097B2/en not_active Ceased
- 2001-12-17 CA CA002431953A patent/CA2431953A1/en not_active Abandoned
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- 2001-12-17 WO PCT/US2001/049301 patent/WO2002051809A1/en active IP Right Grant
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- 2003-09-18 HK HK03106690.7A patent/HK1054390B/zh unknown
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MY134017A (en) | 2007-11-30 |
DE60112791T2 (de) | 2006-06-08 |
JP2004516314A (ja) | 2004-06-03 |
US6472394B1 (en) | 2002-10-29 |
HUP0302582A2 (hu) | 2003-12-29 |
EP1343761A1 (en) | 2003-09-17 |
ES2243588T3 (es) | 2005-12-01 |
CN1481361A (zh) | 2004-03-10 |
AU2002231097B2 (en) | 2004-12-09 |
WO2002051809A1 (en) | 2002-07-04 |
HK1054390A1 (en) | 2003-11-28 |
NZ525723A (en) | 2004-11-26 |
AR031930A1 (es) | 2003-10-08 |
KR20040011447A (ko) | 2004-02-05 |
IL155772A0 (en) | 2003-12-23 |
JP4025200B2 (ja) | 2007-12-19 |
MXPA03005744A (es) | 2003-09-05 |
EP1343761B1 (en) | 2005-08-17 |
ATE302185T1 (de) | 2005-09-15 |
PE20020658A1 (es) | 2002-07-23 |
CA2431953A1 (en) | 2002-07-04 |
CN1273451C (zh) | 2006-09-06 |
JP2007284451A (ja) | 2007-11-01 |
HK1054390B (zh) | 2006-01-06 |
DE60112791D1 (de) | 2005-09-22 |
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