NO20071193L - Fluorsubstituerte sykloalkanoindoler og deres anvendelse som prostaglandin D2-reseptorantagonister - Google Patents
Fluorsubstituerte sykloalkanoindoler og deres anvendelse som prostaglandin D2-reseptorantagonisterInfo
- Publication number
- NO20071193L NO20071193L NO20071193A NO20071193A NO20071193L NO 20071193 L NO20071193 L NO 20071193L NO 20071193 A NO20071193 A NO 20071193A NO 20071193 A NO20071193 A NO 20071193A NO 20071193 L NO20071193 L NO 20071193L
- Authority
- NO
- Norway
- Prior art keywords
- prostaglandin
- fluoro
- alkyl
- receptor antagonists
- tetrahydrocyclopenta
- Prior art date
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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
- C07D209/56—Ring systems containing three or more rings
- C07D209/80—[b, c]- or [b, d]-condensed
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- 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
- A61K31/404—Indoles, e.g. pindolol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P11/02—Nasal agents, e.g. decongestants
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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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- A61P11/06—Antiasthmatics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P13/08—Drugs for disorders of the urinary system of the prostate
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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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- 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
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
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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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- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P27/16—Otologicals
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- A—HUMAN NECESSITIES
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- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
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- A—HUMAN NECESSITIES
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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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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- 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
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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
- C07D209/56—Ring systems containing three or more rings
- C07D209/80—[b, c]- or [b, d]-condensed
- C07D209/82—Carbazoles; Hydrogenated carbazoles
- C07D209/88—Carbazoles; Hydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Neurosurgery (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Gynecology & Obstetrics (AREA)
- Transplantation (AREA)
- Anesthesiology (AREA)
- Vascular Medicine (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (AREA)
Abstract
Forbindelser av formel I: og farmasøytisk akseptable salter derav, hvor n er 0 eller 1; m er 1, 2 eller 3; R1 er H, C1-C3-alkyl, halogenert C1-C3-alkyl eller syklo-propyl; R2 er 4-klorfenyl eller 2,4,6-triklorfenyl, bortsett fra isomeren (-) -[4-(4-klorbenzyl)-7-fluor-5-(metansulfonyl)-1,2,3,4-tetrahydrosyklopenta[b]indol-3-yl]eddiksyre, er terapeutisk aktive og kan anvendes ved fremstilling av et medikament for behandling av en prostaglandin D2-mediert sykdom, fortrinnsvis nasal kongestion, rhinitt eller astma. Forbindelser av formel I: og farmasøytisk akseptable salter derav, hvor n er 0 eller 1; m er 1, 2 eller 3; R1 er H, C1-C3-alkyl, halogenert C1-C3-alkyl eller syklo-propyl; R2 er 4-klorfenyl eller 2,4,6-triklorfenyl, bortsett fra isomeren (-) -[4-(4-klorbenzyl)-7-fluor-5-(metansulfonyl)-1,2,3,4-tetrahydrosyklopenta[b]indol-3-yl]eddiksyre, er terapeutisk aktive og kan anvendes ved fremstilling av et medikament for behandling av en prostaglandin D2-mediert sykdom, fortrinnsvis nasal kongestion, rhinitt eller astma.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US35138402P | 2002-01-24 | 2002-01-24 | |
PCT/CA2003/000084 WO2003062200A2 (en) | 2002-01-24 | 2003-01-22 | Fluoro substituted cycloalkanoindoles and their use as prostaglandin d2 receptor antagonists |
Publications (1)
Publication Number | Publication Date |
---|---|
NO20071193L true NO20071193L (no) | 2004-08-24 |
Family
ID=27613492
Family Applications (3)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
NO20043536A NO327322B1 (no) | 2002-01-24 | 2004-08-24 | Fluorsubstituert forbindelse og farmasoytisk preparat |
NO20071193A NO20071193L (no) | 2002-01-24 | 2007-03-02 | Fluorsubstituerte sykloalkanoindoler og deres anvendelse som prostaglandin D2-reseptorantagonister |
NO2009013C NO2009013I2 (no) | 2002-01-24 | 2009-06-19 | Laropiprant eller et farmasøytisk akseptabelt saltderav |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
NO20043536A NO327322B1 (no) | 2002-01-24 | 2004-08-24 | Fluorsubstituert forbindelse og farmasoytisk preparat |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
NO2009013C NO2009013I2 (no) | 2002-01-24 | 2009-06-19 | Laropiprant eller et farmasøytisk akseptabelt saltderav |
Country Status (39)
Country | Link |
---|---|
US (6) | US20030158246A1 (no) |
EP (3) | EP2295409B1 (no) |
JP (2) | JP4008885B2 (no) |
KR (2) | KR100859230B1 (no) |
CN (3) | CN101851191A (no) |
AR (1) | AR038136A1 (no) |
AT (1) | ATE414690T1 (no) |
AU (1) | AU2003202343B2 (no) |
BR (1) | BR0307050A (no) |
CA (1) | CA2471952C (no) |
CY (3) | CY1108841T1 (no) |
DE (2) | DE60324767D1 (no) |
DK (2) | DK1470107T3 (no) |
DO (1) | DOP2003000566A (no) |
EA (1) | EA006134B1 (no) |
EC (1) | ECSP045203A (no) |
EG (1) | EG24978A (no) |
ES (2) | ES2391747T3 (no) |
FR (1) | FR09C0010I2 (no) |
GE (1) | GEP20074078B (no) |
HR (1) | HRP20040665B1 (no) |
IL (3) | IL162825A0 (no) |
IS (2) | IS2633B (no) |
JO (1) | JO2481B1 (no) |
LU (1) | LU91534I2 (no) |
MX (1) | MXPA04007167A (no) |
MY (1) | MY137040A (no) |
NL (1) | NL300377I2 (no) |
NO (3) | NO327322B1 (no) |
NZ (1) | NZ533786A (no) |
PE (1) | PE20030982A1 (no) |
PL (1) | PL208527B1 (no) |
PT (2) | PT2045241E (no) |
RS (2) | RS20100338A (no) |
SI (2) | SI1470107T1 (no) |
TW (1) | TWI259080B (no) |
UA (1) | UA75520C2 (no) |
WO (1) | WO2003062200A2 (no) |
ZA (1) | ZA200404999B (no) |
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US7273883B2 (en) * | 2000-09-14 | 2007-09-25 | Allergan, Inc. | Prostaglandin EP4 antagonist |
AR038136A1 (es) * | 2002-01-24 | 2004-12-29 | Merck Frosst Canada Inc | Cicloalcanindoles con sustitucion con fluor composiciones que contienen estos compuestos y metodos de tratamiento |
AR041089A1 (es) * | 2003-05-15 | 2005-05-04 | Merck & Co Inc | Procedimiento y composiciones farmaceutiicas para tratar aterosclerosis, dislipidemias y afecciones relacionadas |
WO2004104205A2 (en) * | 2003-05-16 | 2004-12-02 | Merck & Co., Inc. | Enzymatic preparation of chiral indole esters |
CN1791577A (zh) * | 2003-05-20 | 2006-06-21 | 麦克弗罗斯特加拿大有限公司 | 氟-甲基磺酰取代的环烷并吲哚和它们作为前列腺素d2拮抗剂的用途 |
WO2005013985A1 (en) * | 2003-08-07 | 2005-02-17 | Merck Sharp & Dohme Limited | Treatment for alzheimer's disease and related conditions |
TWI258478B (en) | 2003-10-31 | 2006-07-21 | Arena Pharm Inc | Tetrazole derivatives and methods of treatment of metabolic-related disorders thereof |
US7019022B2 (en) * | 2003-12-15 | 2006-03-28 | Merck Frosst Canada & Co. | Substituted tetrahydrocarbazole and cyclopentanoindole derivatives |
BRPI0508540B8 (pt) | 2004-03-11 | 2021-05-25 | Actelion Pharmaceuticals Ltd | composto, composição farmacêutica, e, uso de um composto |
ATE384046T1 (de) * | 2004-04-02 | 2008-02-15 | Merck & Co Inc | Verfahren zur asymmetrischen hydrierung, das sich für die herstellung von cycloalkanindolderivaten eignet |
GT200500284A (es) | 2004-10-15 | 2006-03-27 | Aventis Pharma Inc | Pirimidinas como antagonistas del receptor de prostaglandina d2 |
US20070299122A1 (en) * | 2004-11-08 | 2007-12-27 | Tobert Jonathan A | Method of Treating Pathological Blushing |
PE20060949A1 (es) | 2004-12-23 | 2006-10-11 | Arena Pharm Inc | Derivados fusionados de pirazol como agonistas del receptor de niacina |
JPWO2006068162A1 (ja) * | 2004-12-24 | 2008-06-12 | 塩野義製薬株式会社 | 慢性閉塞性肺疾患の治療剤 |
PL1833791T3 (pl) | 2004-12-27 | 2011-12-30 | Actelion Pharmaceuticals Ltd | Pochodne 2,3,4,9-tetrahydro-1H-karbazolu jako antagonisty receptora CRTH2 |
US20080139604A1 (en) * | 2005-02-17 | 2008-06-12 | Shaun Fitzpatrick | Method of Treating Atherosclerosis, Dyslipidemias and Related Conditions |
CA2603757A1 (en) * | 2005-04-13 | 2006-10-26 | Merck & Co., Inc. | Niacin receptor agonists, compositions containing such compounds and methods of treatment |
EP1911759A4 (en) | 2005-07-22 | 2010-07-21 | Shionogi & Co | AZAINDOL DERIVATIVE ANTAGONISTIC EFFECT ON PGD2 RECEPTOR |
EP2397476A3 (en) | 2005-07-22 | 2011-12-28 | Shionogi & Co., Ltd. | Indole derivative having PGD2 receptor antagonist activity |
JP5147401B2 (ja) | 2005-09-06 | 2013-02-20 | 塩野義製薬株式会社 | Pgd2受容体アンタゴニスト活性を有するインドールカルボン酸誘導体 |
PL2037967T3 (pl) | 2006-06-16 | 2017-07-31 | The Trustees Of The University Of Pennsylvania | Antagoniści receptora prostaglandyny D2 w leczeniu łysienia androgenowego |
JP5220013B2 (ja) | 2006-08-07 | 2013-06-26 | アクテリオン ファーマシューティカルズ リミテッド | (3−アミノ−1,2,3,4−テトラヒドロ−9h−カルバゾール−9−イル)−酢酸誘導体 |
US20100260841A1 (en) * | 2007-02-08 | 2010-10-14 | Paolini John F | Method of Treating Atherosclerosis, Dyslipidemias and Related Conditions |
US20090076117A1 (en) * | 2007-09-17 | 2009-03-19 | Protia, Llc | Deuterium-enriched laropiprant |
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US8507473B2 (en) | 2008-09-11 | 2013-08-13 | Arena Pharmaceuticals, Inc. | 3H-imidazo[4,5-b]pyridin-5-ol derivatives useful in the treatment of GPR81 receptor disorders |
CN102224154A (zh) * | 2008-09-25 | 2011-10-19 | 默克弗罗斯特加拿大有限公司 | 作为EP4受体拮抗剂的β-咔啉磺酰脲衍生物 |
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US9180114B2 (en) * | 2008-11-26 | 2015-11-10 | President And Fellows Of Harvard College | Neurodegenerative diseases and methods of modeling |
US8882678B2 (en) * | 2009-03-13 | 2014-11-11 | Atrium Medical Corporation | Pleural drainage system and method of use |
MA34094B1 (fr) | 2010-03-22 | 2013-03-05 | Actelion Pharmaceuticals Ltd | Dérivés de 3-(hétéroarylamino)-1,2,3,4-tétrahydro-9h-carbazole et leur utilisation comme modulateurs du récepteur de la prostaglandine d2 |
MX338516B (es) | 2011-04-14 | 2016-04-20 | Actelion Pharmaceuticals Ltd | Derivados de acido 7- (heteroaril-amino) -6, 7, 8, 9- tetrahidropirido[1,2-a] indol acetico y sus usos como modulador del receptor de prostaglandina. |
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