FI114099B - Pyrrolitsin- och pyrrolo[2,1-b] tiazolderivat och deras användning i farmacin - Google Patents

Pyrrolitsin- och pyrrolo[2,1-b] tiazolderivat och deras användning i farmacin Download PDF

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Publication number
FI114099B
FI114099B FI964773A FI964773A FI114099B FI 114099 B FI114099 B FI 114099B FI 964773 A FI964773 A FI 964773A FI 964773 A FI964773 A FI 964773A FI 114099 B FI114099 B FI 114099B
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Prior art keywords
phenyl
formula
compounds
alkyl
compound
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FI964773A
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English (en)
Finnish (fi)
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FI964773A0 (sv
FI964773A (sv
Inventor
Stefan Laufer
Hans Guenther Striegel
Gerd Dannhardt
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Merckle Gmbh
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Publication of FI964773A0 publication Critical patent/FI964773A0/sv
Publication of FI964773A publication Critical patent/FI964773A/sv
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/08Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (7)

1. Pyrrolitsin- och pyrrolo[2,1-b] tiazolderivat kännetecknade av att de har formeln I: Rl 1X1 J R7R^IfR2 1 R5 13 där tvä av resterna R1, R2 och R3, vilka kan vara lika eller olika, stir för en fenyl- eller tienylrest, vilken eventuellt uppvisar en substituent genom halogen eller CF3/ och , .·. den tredje av resterna R1, R2 och R3 star för Cx-C.j-alkylen-» · CONR8R9, • · · • I t ,:. R8 är en väteatom eller Ci-C8-alkyl, . R9 är S02-Ci-C8-alkyl, vilken eventuellt uppvisar en substituent genom halogen eller S02-fenyl, vilken eventuellt uppvisar en substituent genom Ci-C8-alkyl R4, R5, R6 och R7, vilka kan vara lika eller olika, stär för ] . H eller Ci-C8-alkyl, och » 1 I · ’·’ X är CH2 eller S, » 114099 de optiska isomerema, f armaceutiskt acceptabla salterna och fysiologiskt lätt hydrolyserade ester av dessa.
2. Föreningar enligt patentkrav 1, kännetecknade av att de har formeln I, där R1 stär för fenyl, R2 star för fenyl eller en genom halogen eller CF3 substituerad fenyl, tienyl eller en genom halogen substituerad tienyl.
3. Föreningar enligt nägot av patentkraven 1 eller 2, kännetecknade av att R8 stär för H.
4. Föreningar enligt patentkrav 3, kännetecknade av att R9 star för S02CF3, S02CH3, S02-fenyl, eller S02-tolyl.
5. Förening enligt patentkrav 1, kännetecknad av att den ar [6-(4-trifluormetylfenyl)-2,2-dimetyl-7-fenyl-2,3- dihydro-lH-pyrrolitsin-5-yl]-ättiksyrametansulfonimid.
6. Farmaceutiskt medel, innehällande minst en förening ·': enligt nägot av patentkraven 1-5, eventuellt i kombination ·,, med farmaceutiskt fördragbara bärar- eller tillsatsmaterial. > I
» : .7. Användning av minst en förening enlit nägot av : i : patentkraven 1-6, kännetecknad av att den används för framställning av ett farmaceutiskt medel för prevention av iti'|* allergiskt inducerade sjukdomar eller för behandling av • * i sjukdomar inom det reumatiska omrädet. * * « I » i » * t * * < I r » i » *
FI964773A 1994-06-01 1996-11-29 Pyrrolitsin- och pyrrolo[2,1-b] tiazolderivat och deras användning i farmacin FI114099B (sv)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DE4419247 1994-06-01
DE4419247A DE4419247A1 (de) 1994-06-01 1994-06-01 Sulfonylierte Pyrrolizincarbonsäureamide und deren Anwendung in der Pharmazie
PCT/EP1995/002079 WO1995032972A1 (de) 1994-06-01 1995-05-31 [a]-ANNELIERTE PYRROLDERIVATE UND DEREN ANWENDUNG IN DER PHARMAZIE
EP9502079 1995-05-31

Publications (3)

Publication Number Publication Date
FI964773A0 FI964773A0 (sv) 1996-11-29
FI964773A FI964773A (sv) 1997-01-27
FI114099B true FI114099B (sv) 2004-08-13

Family

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Family Applications (1)

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FI964773A FI114099B (sv) 1994-06-01 1996-11-29 Pyrrolitsin- och pyrrolo[2,1-b] tiazolderivat och deras användning i farmacin

Country Status (13)

Country Link
US (1) US5942535A (sv)
EP (1) EP0763037B1 (sv)
JP (1) JP3671303B2 (sv)
KR (1) KR100378884B1 (sv)
AT (1) ATE208777T1 (sv)
AU (1) AU2673095A (sv)
DE (2) DE4419247A1 (sv)
DK (1) DK0763037T3 (sv)
ES (1) ES2166823T3 (sv)
FI (1) FI114099B (sv)
NO (1) NO310076B1 (sv)
PT (1) PT763037E (sv)
WO (1) WO1995032972A1 (sv)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU741754B2 (en) * 1997-09-12 2001-12-06 Merck Frosst Canada Ltd. 2-aminopyridines as inhibitors of cyclooxygenase-2
US6004950A (en) * 1997-09-12 1999-12-21 Merck Frosst Canada, Inc. 2-aminopyridines as inhibitors of cyclooxygenase-2
JP2003505390A (ja) 1999-11-23 2003-02-12 メルクル・ゲーエムベーハー 抗炎症薬用のピロリジンのオキソ及びヒドロキシ誘導体、並びにその使用方法
DE10001166A1 (de) * 2000-01-13 2001-07-19 Merckle Gmbh Anellierte Pyrrolverbindungen, diese enthaltende pharmazeutische Mittel und deren Verwendung
JP5143326B2 (ja) * 2000-01-28 2013-02-13 メルクル・ゲーエムベーハー 6−(4−クロロフェニル)−2,2−ジメチル−7−フェニル−2,3−ジヒドロ−1h−ピロリジン−5−イル酢酸の製造法
DE10004157A1 (de) * 2000-02-01 2001-08-02 Merckle Gmbh Chem Pharm Fabrik 4-Pyridyl-und 2,4-Pyrimidinyl-substituierte Pyrrolderivate und ihre Anwendung in der Pharmazie
KR20010108722A (ko) * 2000-05-31 2001-12-08 우진석 피롤리진 유도체가 부착된 신규의 올리고뉴클레오타이드화합물, 이의 제조방법, 이를 포함하는 조성물, 및 이를유전자 관련 질병의 치료, 진단 및 분석에 사용하는 방법
DE10141285A1 (de) 2001-08-23 2003-03-27 Merckle Gmbh Verfahren zur Herstellung von 6-(4-Chlorphenyl)-2,2-dimethyl-7-phnyl-2,3-dihydro-1H-pyrrolizin-5-yl-essigsäure
BR0212244A (pt) 2001-08-30 2004-10-05 Merckle Gmbh Uso de um ou mais do que um composto e seus isÈmeros ópticos, derivados e sais fisiologicamente aceitáveis, composição farmacêutica, e, método de tratamento ou de prevenção da degeneração ou da destruição de cartilagem articular e/ou de osso subcondral em uma ou mais articulações de um mamìfero
US6953787B2 (en) * 2002-04-12 2005-10-11 Arena Pharmaceuticals, Inc. 5HT2C receptor modulators
CN1805938B (zh) * 2003-06-17 2010-06-16 艾尼纳制药公司 用于治疗5ht2c受体相关疾病的苯并氮杂卓衍生物
ES2571220T3 (es) 2003-06-17 2016-05-24 Arena Pharm Inc Clorhidrato de 8-cloro-1-metil-2,3,4,5-tetrahidro-1H-3-benzazepina
US20070275949A1 (en) * 2003-10-22 2007-11-29 Arena Pharmaceuticals, Inc. Benzazepine Derivatives and Methods of Prophylaxis or Treatment of 5Ht2C Receptor Associated Diseases
WO2005042491A1 (en) * 2003-10-22 2005-05-12 Arena Pharmaceuticals, Inc. Benzazepine derivatives and methods of prophylaxis or treatment of 5ht2c receptor associated diseases
ATE442359T1 (de) 2004-12-21 2009-09-15 Arena Pharm Inc Kristalline formen von (r)-8-chlor-1-methyl-2,3,4,5-tetrahydro-1h-3-be zazepinhydrochlorid
DK1833473T3 (da) * 2004-12-23 2010-01-11 Arena Pharm Inc 5HT2C-Receptormodulator-sammensætninger og metoder for anvendelse
DE102005012971A1 (de) * 2005-03-21 2006-09-28 Merckle Gmbh Polymorphe Form von 6-(4-Chlorphenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl-essigsäure
CN101228171A (zh) * 2005-07-26 2008-07-23 默克勒有限公司 作为5-脂氧化酶和环加氧酶抑制剂的吡咯里嗪和中氮茚化合物的大环内酯偶联物
CN101466684B (zh) 2006-04-03 2012-06-20 艾尼纳制药公司 8-氯-1-甲基-2,3,4,5-四氢-1h-3-苯并氮杂卓的制备工艺和其相关中间体
SG177128A1 (en) * 2006-12-05 2012-01-30 Arena Pharm Inc Processes for preparing (r)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine and intermediates thereof
EP2288585A1 (en) * 2008-03-04 2011-03-02 Arena Pharmaceuticals, Inc. Processes for the preparation of intermediates related to the 5-ht2c agonist (r)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine
US8952197B2 (en) 2009-06-18 2015-02-10 Arena Pharmaceuticals, Inc. Processes for the preparation of 5-HT2C receptor agonists
WO2011153206A1 (en) 2010-06-02 2011-12-08 Arena Pharmaceuticals, Inc. Processes for the preparation of 5-ht2c receptor agonists
CN103189359A (zh) 2010-09-01 2013-07-03 艾尼纳制药公司 5-ht2c激动剂的光学活性酸盐
EP2611449A1 (en) 2010-09-01 2013-07-10 Arena Pharmaceuticals, Inc. Administration of lorcaserin to individuals with renal impairment
EP2611433A2 (en) 2010-09-01 2013-07-10 Arena Pharmaceuticals, Inc. Non-hygroscopic salts of 5-ht2c agonists
KR20180118801A (ko) 2010-09-01 2018-10-31 에자이 알앤드디 매니지먼트 가부시키가이샤 체중 관리에 유용한 5-ht2c 작동제의 변형-방출 투여 형태
MX2015004532A (es) 2012-10-09 2016-01-20 Arena Pharm Inc Metodo de control del peso.
WO2015077905A1 (en) * 2013-11-29 2015-06-04 Merck Sharp & Dohme Corp. Bicycloamine-substituted-n-benzenesulfonamide compounds with selective activity in voltage-gated sodium channels
US10206904B2 (en) * 2015-07-17 2019-02-19 The Board Of Regents Of The University Of Oklahoma Licofelone derivatives and methods of use
KR101695566B1 (ko) 2015-09-24 2017-01-11 주식회사 지오엔씨 라미네이터용 히팅롤의 간극조절장치

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1461592A (en) * 1973-04-25 1977-01-13 Agfa Gevaert Specially sensitized direct positive silver halide emulsions
US3920672A (en) * 1974-08-22 1975-11-18 Syntex Inc Thiacycl (2.2.2.)azine carboxylic acids
US4536512A (en) * 1982-10-08 1985-08-20 Merck & Co., Inc. 5-(2,3-Dihydro-1H-pyrrolizin-5-oyl)-2,3-dihydro-1H-pyrrolizine-1-alkanoic or carboxylic acids and use thereof as anti-inflammatory and analgesic agents
AU562833B2 (en) * 1983-01-13 1987-06-18 Rhone-Poulenc Sante Ortho-fused pyrrole derivatives
FR2539417A1 (fr) * 1983-01-13 1984-07-20 Rhone Poulenc Sante Nouveaux pyrrolo-1, 2 heterocycles, leur preparation et les medicaments qui les contiennent
FR2557111B1 (fr) * 1983-12-21 1986-04-11 Rhone Poulenc Sante Nouveaux derives ortho-condenses du pyrrole, leur preparation et les medicaments qui les contiennent
US5260451A (en) * 1989-05-11 1993-11-09 Merckle Gmbh Substituted pyrrole compounds and use thereof in pharmaceutical compositions
DE3915450A1 (de) * 1989-05-11 1990-11-15 Gerd Prof Dr Dannhardt Substituierte pyrrolverbindungen und deren anwendung in der pharmazie
JPH05289267A (ja) * 1992-04-07 1993-11-05 Fuji Photo Film Co Ltd ハロゲン化銀カラー写真感光材料
US5552422A (en) * 1995-01-11 1996-09-03 Merck Frosst Canada, Inc. Aryl substituted 5,5 fused aromatic nitrogen compounds as anti-inflammatory agents

Also Published As

Publication number Publication date
PT763037E (pt) 2002-05-31
NO965095L (no) 1996-11-29
DE4419247A1 (de) 1995-12-07
ES2166823T3 (es) 2002-05-01
EP0763037B1 (de) 2001-11-14
FI964773A0 (sv) 1996-11-29
NO965095D0 (no) 1996-11-29
ATE208777T1 (de) 2001-11-15
FI964773A (sv) 1997-01-27
JPH10506370A (ja) 1998-06-23
EP0763037A1 (de) 1997-03-19
KR100378884B1 (ko) 2003-08-06
JP3671303B2 (ja) 2005-07-13
WO1995032972A1 (de) 1995-12-07
NO310076B1 (no) 2001-05-14
DK0763037T3 (da) 2002-03-04
US5942535A (en) 1999-08-24
DE59509846D1 (de) 2001-12-20
AU2673095A (en) 1995-12-21
KR970703346A (ko) 1997-07-03

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