HUP0402346A2 - Humán 11CBy receptor antagonista hatású laktámszármazékok, eljárás ezek előállítására és alkalmazásuk gyógyszerkészítmény előállítására - Google Patents
Humán 11CBy receptor antagonista hatású laktámszármazékok, eljárás ezek előállítására és alkalmazásuk gyógyszerkészítmény előállításáraInfo
- Publication number
- HUP0402346A2 HUP0402346A2 HU0402346A HUP0402346A HUP0402346A2 HU P0402346 A2 HUP0402346 A2 HU P0402346A2 HU 0402346 A HU0402346 A HU 0402346A HU P0402346 A HUP0402346 A HU P0402346A HU P0402346 A2 HUP0402346 A2 HU P0402346A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- heterocyclic ring
- ring
- membered
- substituted
- Prior art date
Links
- 150000003951 lactams Chemical class 0.000 title abstract 3
- 239000005557 antagonist Substances 0.000 title 1
- -1 methoxymethoxy Chemical group 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000004432 carbon atom Chemical group C* 0.000 abstract 4
- 229910052760 oxygen Inorganic materials 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 2
- 125000005330 8 membered heterocyclic group Chemical group 0.000 abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 abstract 1
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 239000011593 sulfur Substances 0.000 abstract 1
- 125000005034 trifluormethylthio group Chemical group FC(S*)(F)F 0.000 abstract 1
Classifications
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- 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
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
- C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
- C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
- C07D239/96—Two oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
- C07D257/10—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
- C07D257/12—Six-membered rings having four nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Psychiatry (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Anesthesiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Hydrogenated Pyridines (AREA)
- Peptides Or Proteins (AREA)
- Pyrrole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Steroid Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Indole Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Abstract
A találmány tárgyát képezik laktámszármazékok, amelyek a humán 11CByreceptort antagonizálják, valamint eljárás ezek eléállítására, ésezeket tartalmazó gyógyszerkészítmény és végül ezek gyógyászatbantörténő alkalmazása. A találmány tárgyát képező laktámszármazékok (I)általános képletű vegyületek, és ezek sói vagy szolvátjai, ahol aképletben M jelentése O, S, C=O, NH vagy CH2-csoport; L jelentése 2-vagy 3-tagú alkilénlánc; ahol az M-L együtt adott esetbenszubsztituálva lehet legalább egy metil-, etil-, hidroxi- és C1-3alkoxicsoporttal; (i) R1 és R2 jelentése egymástól függetlenülhidrogénatom, 1-6 szénatomos egyenes vagy elágazó szénláncúalkilcsoport, amely adott esetben szubsztituálva lehet fenilcsoporttalés 3-6 szénatomos cikloalkilcsoport, amely adott esetbenszubsztituálva lehet egy vagy több 1-6 szénatomos alkilcsoporttal;vagy (ii) R1 és R2 azzal a nitrogénatommal együtt, amelyhezkapcsolódnak, egy 4-8 tagú heterociklusos gyűrűt vagy egy 7-10 tagúbiciklusos heterociklusos gyűrűt alkot, amely 1, 2, 3 vagy 4heteroatomot tartalmaz a nitrogénatom, kénatom és oxigénatom közül, ésahol a 4-8 tagú heterociklusos gyűrű és a 7-10 tagú biciklusosheterociklusos gyűrű adott esetben szubsztituálva van fenilcsoporttalvagy egy-négy 1-3 szénatomos alkilcsoporttal; minden egyes R6jelentése egymástól függetlenül hidroxi, 1-2 szénatomos alkil-, 1-3szénatomos alkoxi-, halogénatom, 2-3 szénatomos alkenil-, benzil- vagy-C(Ra)NORb általános képletű csoport, ahol Ra és Rb jelentéseegymástól függetlenül hidrogénatom, metilcsoport, metoximetil-,metoximetoxi- és metoxietoxicsoport és n értéke 1, 2, 3 vagy 4; QYjelentése biciklusos kondenzált heterociklusos gyűrű, ahol Q és Y egybiciklusos kondenzált heterociklusos csoport, ahol az Y gyűrű 1-3nitrogénatomot tartalmaz és a fenilgyűrűhöz az (I) általános képletűnitrogénatomon keresztül kapcsolódik, és az említett Q gyűrű egy 5vagy 6 tagú aril- vagy heterociklusos gyűrű, amely ZR3 csoporttalrendelkezik, és Z a Q gyűrűhöz kapcsolódik; Z jelentése közvetlenkötés, NH, NCH3, O, S vagy CH2-csoport; és R3 jelentése aril-, alk-2-én-l-il-, cikloalkil- vagy cikloalk-2-én- -l-il-csoport, ahol azemlített aril-, alk-2-én-l-il-, cikloalkil- és cikloalk-2-én-l-il-csoport adott esetben szubsztituálva van 1-3 szubsztituenssel azalábbi csoportból kiválasztva: C1-3 alkil-, halogénatom, amino-,alkilamino-, dialkilamino-, hidroxi-, C1-3 alkoxi-, ciano-,trifluormetil- és metiltiocsoport. Ó
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB0124627.1A GB0124627D0 (en) | 2001-10-15 | 2001-10-15 | Novel compounds |
PCT/US2002/032740 WO2003033480A1 (en) | 2001-10-15 | 2002-10-15 | Lactam derivatives as antagonists for human 11cby receptors |
Publications (1)
Publication Number | Publication Date |
---|---|
HUP0402346A2 true HUP0402346A2 (hu) | 2005-02-28 |
Family
ID=9923785
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0402335A HUP0402335A3 (en) | 2001-10-15 | 2002-10-15 | Pyrimidinones condensated by a carbo- or heterocycle, process for their preparation and their use |
HU0402346A HUP0402346A2 (hu) | 2001-10-15 | 2002-10-15 | Humán 11CBy receptor antagonista hatású laktámszármazékok, eljárás ezek előállítására és alkalmazásuk gyógyszerkészítmény előállítására |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0402335A HUP0402335A3 (en) | 2001-10-15 | 2002-10-15 | Pyrimidinones condensated by a carbo- or heterocycle, process for their preparation and their use |
Country Status (21)
Country | Link |
---|---|
EP (2) | EP1442025B1 (hu) |
JP (2) | JP2005508966A (hu) |
KR (2) | KR20040045833A (hu) |
CN (2) | CN1571774A (hu) |
AT (2) | ATE356119T1 (hu) |
BR (2) | BR0213242A (hu) |
CA (2) | CA2463508A1 (hu) |
CO (2) | CO5580779A2 (hu) |
CZ (2) | CZ2004499A3 (hu) |
DE (2) | DE60217147T2 (hu) |
ES (2) | ES2279009T3 (hu) |
GB (1) | GB0124627D0 (hu) |
HU (2) | HUP0402335A3 (hu) |
IL (2) | IL161074A0 (hu) |
MX (2) | MXPA04003532A (hu) |
NO (2) | NO20041504L (hu) |
NZ (1) | NZ531911A (hu) |
PL (2) | PL370587A1 (hu) |
RU (1) | RU2004110053A (hu) |
WO (2) | WO2003033480A1 (hu) |
ZA (2) | ZA200402672B (hu) |
Families Citing this family (90)
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CN1592739A (zh) | 2001-11-26 | 2005-03-09 | 先灵公司 | 用于治疗肥胖和cns疾病的基于哌啶的mch拮抗剂 |
JP2005519876A (ja) | 2001-11-27 | 2005-07-07 | メルク エンド カムパニー インコーポレーテッド | 2−アミノキノリン化合物 |
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 |
US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
MXPA05010859A (es) * | 2003-04-11 | 2005-12-14 | Smithkline Beecham Corp | Antagonistas mchr1 heterociclicos. |
AU2004265189B2 (en) * | 2003-08-15 | 2010-03-04 | Banyu Pharmaceutical Co., Ltd. | Imidazopyridine derivatives |
KR100747042B1 (ko) * | 2003-08-19 | 2007-08-07 | 솔젠트 (주) | 신물질6-메틸-3-펜에틸-3,4-디히드로-1h-큐나졸린-2-티온,이의 제조방법 및 이를 유효성분으로 포함하는 미백 효능조성물 |
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US7592373B2 (en) | 2003-12-23 | 2009-09-22 | Boehringer Ingelheim International Gmbh | Amide compounds with MCH antagonistic activity and medicaments comprising these compounds |
UA83416C2 (en) * | 2004-02-13 | 2008-07-10 | Баниу Фармасьютикал Ко., Лтд. | Fused ring 4-oxopyrimidine derivative |
DE102004010893A1 (de) * | 2004-03-06 | 2005-09-22 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue ß-Ketoamid-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel |
US7605176B2 (en) | 2004-03-06 | 2009-10-20 | Boehringer Ingelheim International Gmbh | β-ketoamide compounds with MCH antagonistic activity |
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 |
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JP4211867B2 (ja) * | 2005-02-14 | 2009-01-21 | 萬有製薬株式会社 | 4(3h)−キナゾリノン誘導体の結晶 |
US7989445B2 (en) | 2005-04-28 | 2011-08-02 | Takeda Pharmaceutical Company Limited | Thienopyrimidone compound |
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UA91560C2 (ru) * | 2005-08-31 | 2010-08-10 | Селджин Корпорэйшн | Соединения ряда изоиндолимидов, их композиция и применение |
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US8618115B2 (en) | 2005-10-26 | 2013-12-31 | Bristol-Myers Squibb Company | Substituted thieno[3,2-d]pyrimidinones as MCHR1 antagonists and methods for using them |
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MY149854A (en) | 2006-02-15 | 2013-10-31 | Sanofi Aventis | Novel aminoalcohol-substituted aryldihydroisoquinolinones, process for their preparation and their use as medicaments |
WO2007142217A1 (ja) * | 2006-06-07 | 2007-12-13 | Banyu Pharmaceutical Co., Ltd. | 1-フェニルピリドン誘導体 |
US8263772B2 (en) | 2006-06-08 | 2012-09-11 | Eli Lilly And Company | MCH receptor antagonists |
EP2029610A2 (en) | 2006-06-08 | 2009-03-04 | Eli Lilly & Company | Novel mch receptor antagonists |
KR20090047458A (ko) | 2006-08-08 | 2009-05-12 | 사노피-아벤티스 | 아릴아미노아릴-알킬-치환된 이미다졸리딘-2,4-디온, 이의 제조방법, 이들 화합물을 포함하는 약제 및 이의 용도 |
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PL137227B2 (en) * | 1984-03-28 | 1986-05-31 | Univ Lodzki | Process for preparing novel n-/dialkylaminoalkoxyphenyl/-imides of tetrahydrophtalic acids |
DK0958296T3 (da) * | 1996-12-31 | 2003-08-18 | Reddys Lab Ltd Dr | Heterocykliske forbindelser, fremgangsmåde til deres fremstilling og farmaceutiske præparater, der indeholder dem, og deres anvendelse i behandlingen af diabetes og beslægtede sygdomme |
US7115750B1 (en) * | 1999-09-20 | 2006-10-03 | Takeda Pharmaceutical Company Limited | Melanin concentrating hormone antagonist |
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