JP5777030B2 - １１β−ヒドロキシステロイドデヒドロゲナーゼ１の阻害剤 - Google Patents

１１β−ヒドロキシステロイドデヒドロゲナーゼ１の阻害剤 Download PDF

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JP5777030B2
JP5777030B2 JP2011519178A JP2011519178A JP5777030B2 JP 5777030 B2 JP5777030 B2 JP 5777030B2 JP 2011519178 A JP2011519178 A JP 2011519178A JP 2011519178 A JP2011519178 A JP 2011519178A JP 5777030 B2 JP5777030 B2 JP 5777030B2
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alkyl
cycloalkyl
alkoxy
halo
hydroxy
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JP2011529029A (ja
JP2011529029A5 (enExample
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ヒンメルスバッハ，フランク
エクハルト，マティアス
ハミルトン，ブラッドフォード・エス
シューラー−メッツ，アネッテ
ツァン，リンハン
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ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
ヴァイティー ファーマシューティカルズ，インコーポレイテッド
ヴァイティー ファーマシューティカルズ，インコーポレイテッド
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    • 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
    • C07D413/10—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 aromatic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/08—Antibacterial agents for leprosy
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Reproductive Health (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
JP2011519178A 2008-07-25 2009-07-23 １１β−ヒドロキシステロイドデヒドロゲナーゼ１の阻害剤 Active JP5777030B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US13593308P 2008-07-25 2008-07-25
US61/135,933 2008-07-25
US20676709P 2009-02-04 2009-02-04
US61/206,767 2009-02-04
PCT/EP2009/059509 WO2010010157A2 (en) 2008-07-25 2009-07-23 INHIBITORS OF 11beta-HYDROXYSTEROID DEHYDROGENASE 1

Publications (3)

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JP2011529029A JP2011529029A (ja) 2011-12-01
JP2011529029A5 JP2011529029A5 (enExample) 2012-09-13
JP5777030B2 true JP5777030B2 (ja) 2015-09-09

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Country Status (7)

Country Link
US (1) US8846668B2 (enExample)
EP (1) EP2324017B1 (enExample)
JP (1) JP5777030B2 (enExample)
AR (1) AR072753A1 (enExample)
CA (1) CA2729998A1 (enExample)
TW (1) TW201016691A (enExample)
WO (1) WO2010010157A2 (enExample)

Families Citing this family (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2125750B1 (en) 2007-02-26 2014-05-21 Vitae Pharmaceuticals, Inc. Cyclic urea and carbamate inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US8329897B2 (en) 2007-07-26 2012-12-11 Vitae Pharmaceuticals, Inc. Synthesis of inhibitors of 11β-hydroxysteroid dehydrogenase type 1
AR069207A1 (es) 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
EP2220048B1 (en) 2007-11-16 2017-01-25 Boehringer Ingelheim International GmbH Aryl- and heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use
JP5490014B2 (ja) 2007-12-11 2014-05-14 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１型の環状尿素阻害剤
TW200934490A (en) 2008-01-07 2009-08-16 Vitae Pharmaceuticals Inc Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1
EP2252601B1 (en) * 2008-01-24 2012-12-19 Vitae Pharmaceuticals, Inc. Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2254872A2 (en) 2008-02-15 2010-12-01 Vitae Pharmaceuticals, Inc. Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
JP5538365B2 (ja) 2008-05-01 2014-07-02 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状阻害剤
CL2009001058A1 (es) 2008-05-01 2010-09-10 Vitae Pharmaceuticals Inc Compuestos derivados de oxazinas sustituidas, inhibidores de la 11b-hidroxiesteroide deshidrogenasa de tipo-1; composicion farmaceutica; y uso del compuesto para inhibir la actividad de 11b-hsd1, como en el tratamiento de la diabetes, dislipidemia, hipertension, obesidad, cancer, glaucoma, entre otras.
CA2722427A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
WO2009138386A2 (en) 2008-05-13 2009-11-19 Boehringer Ingelheim International Gmbh Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use
RU2539979C2 (ru) 2008-07-25 2015-01-27 Вайтаи Фармасьютиклз, Инк. Циклические ингибиторы 11бета-гидроксистероид-дегидрогеназы 1
JP5777030B2 (ja) 2008-07-25 2015-09-09 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １１β−ヒドロキシステロイドデヒドロゲナーゼ１の阻害剤
WO2010010150A1 (en) 2008-07-25 2010-01-28 Boehringer Ingelheim International Gmbh Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
EP2350068B1 (en) 2008-10-23 2017-08-30 Boehringer Ingelheim International GmbH Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use
WO2010089303A1 (en) * 2009-02-04 2010-08-12 Boehringer Ingelheim International Gmbh CYCLIC INHIBITORS OF 11 β-HYDROXYSTEROID DEHYDROGENASE 1
MA33216B1 (fr) 2009-04-30 2012-04-02 Boehringer Ingelheim Int Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1
AR076492A1 (es) * 2009-04-30 2011-06-15 Boehringer Ingelheim Int Inhibidores ciclicos de 11 beta -hidroxiesteroide deshidrogenasa 1
US20100331320A1 (en) * 2009-04-30 2010-12-30 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5670440B2 (ja) 2009-06-02 2015-02-18 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状阻害剤
EP2440537A1 (en) 2009-06-11 2012-04-18 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure
WO2011002910A1 (en) 2009-07-01 2011-01-06 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5750449B2 (ja) 2009-11-05 2015-07-22 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規キラルリンリガンド
TWI531571B (zh) 2009-11-06 2016-05-01 維它藥物公司 六氫茚并吡啶及八氫苯并喹啉之芳基－及雜芳基羰基衍生物
EP2576570A1 (en) 2010-05-26 2013-04-10 Boehringer Ingelheim International GmbH 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives
EP2582698B1 (en) 2010-06-16 2016-09-14 Vitae Pharmaceuticals, Inc. Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
JP5813106B2 (ja) 2010-06-25 2015-11-17 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 代謝障害の処置のための１１−β−ＨＳＤ１のインヒビターとしてのアザスピロヘキサノン
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
BR112013010021A2 (pt) 2010-11-02 2019-09-24 Boehringer Ingelheim Int combinações farmacêuticas para o tratamento de distúrbios metabólicos.
TWI537258B (zh) 2010-11-05 2016-06-11 百靈佳殷格翰國際股份有限公司 六氫茚并吡啶及八氫苯并喹啉之芳基－及雜環芳基羰基衍生物
EP2704573A4 (en) * 2011-05-03 2014-10-15 Merck Sharp & Dohme AMINOMETHYL biaryl BENZOTRIAZOL DERIVATIVES
JP2014524438A (ja) 2011-08-17 2014-09-22 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング インデノピリジン誘導体
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
CN103342700B (zh) * 2012-01-19 2016-04-20 通化济达医药有限公司 11β-羟基类固醇脱氢酶1型抑制剂
CN104788384A (zh) * 2015-03-31 2015-07-22 山东友帮生化科技有限公司 一种3-羟基-6-氯哒嗪的合成方法
EP3235813A1 (en) 2016-04-19 2017-10-25 Cidqo 2012, S.L. Aza-tetra-cyclo derivatives

Family Cites Families (229)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3378587A (en) 1963-03-14 1968-04-16 Du Pont 3, 3'-diaminomethyl-1, 1'-biadamantane
NL127995C (enExample) 1963-12-20 Geigy Ag J R
US3341538A (en) 1965-06-18 1967-09-12 Geigy Chem Corp Certain 2, 6-methano-3-benzazocines
DE2108954A1 (en) 1971-02-25 1972-09-07 Boehringer Sohn Ingelheim 2-(furylmethyl)-6,7-benzomorphans - useful as cns active agents
DE1801556A1 (de) 1968-10-05 1970-05-21 Huels Chemische Werke Ag Verfahren zur Herstellung von substituierten Hexahydropyrimidinonen-(2)
GB1304175A (enExample) 1969-03-31 1973-01-24
DE2105743C3 (de) 1971-02-08 1979-11-29 Boehringer Sohn Ingelheim 2-(Furylmethyl)- a -5,9-dialkyl -6,7benzomorphane, Verfahren zu ihrer Herstellung und deren Verwendung
US3681349A (en) 1970-03-05 1972-08-01 Morton Norwich Products Inc 1-(substituted benzyl) tetrahydro-2-(1h) pyrimidones
US4043927A (en) 1972-03-07 1977-08-23 Sun Ventures, Inc. Friction or tractive drive containing ethers of adamantanes
DE2229695A1 (de) 1972-06-19 1974-01-31 Boehringer Sohn Ingelheim 2-(heteroaryl-methyl)-5,9 beta-dialkyl6,7-benzomorphane, deren saeureadditionssalze sowie verfahren zu deren herstellung
DE2338369A1 (de) 1973-07-26 1975-02-13 Schering Ag Mikrobiologische hydroxylierung von 2,6-methano-3-benzazocinen
SU510999A3 (ru) 1973-10-27 1976-04-15 К.Х.Берингер Зон, (Фирма) Способ получени (метоксиметил-фурилметил)6,7-бензоморфанов илиморфинанов
US4009171A (en) 1974-02-21 1977-02-22 Sterling Drug Inc. N-acylated-11-oxygenated-2,6-methano-3-benzazocine intermediates
DE2411382C3 (de) 1974-03-09 1979-09-06 C.H. Boehringer Sohn, 6507 Ingelheim 2-Tetrahydrofurfuryl-6,7-benzomorphane, Verfahren zur Herstellung und deren Verwendung
US4136145A (en) 1974-07-05 1979-01-23 Schering Aktiengesellschaft Medicament carriers in the form of film having active substance incorporated therein
US4136162A (en) 1974-07-05 1979-01-23 Schering Aktiengesellschaft Medicament carriers in the form of film having active substance incorporated therein
DE2437610A1 (de) 1974-08-05 1976-02-26 Boehringer Sohn Ingelheim Neue 5,9-beta-disubstituierte 2-tetrahydrofurfuryl-6,7-benzomorphane, deren saeureadditionssalze, ihre verwendung als arzneimittel und verfahren zu deren herstellung
GB1513961A (en) 1975-02-25 1978-06-14 Acf Chemiefarma Nv 6,7-benzomorphans method for their preparation and intermediates
US4108857A (en) 1975-08-18 1978-08-22 Sterling Drug Inc. Imidazolylmethyl methanobenzazocines
DE2828039A1 (de) 1978-06-26 1980-01-10 Boehringer Sohn Ingelheim 2-(2-alkoxyethyl)-2'-hydroxy-6,7-benzomorphane deren saeureadditionssalze diese enthaltende arzneimittel und verfahren zu deren herstellung
CA2023492A1 (en) 1989-08-31 1991-03-01 Barry Clifford Lange Herbicidal glutarimides
US5393735A (en) 1990-08-09 1995-02-28 Rohm And Haas Company Herbicidal glutarimides
US5098916A (en) 1990-03-29 1992-03-24 G. D. Searle & Co. Propanobicyclic amine derivatives for cns disorders
EP0454444A1 (en) 1990-04-24 1991-10-30 Nissan Chemical Industries Ltd. Glutarimide derivatives and herbicides
US5215992A (en) 1990-04-30 1993-06-01 G. D. Searle & Co. Ethanobicyclic amine derivatives for CNS disorders
US5089506A (en) 1990-04-30 1992-02-18 G. D. Searle & Co. Ethanobicyclic amine derivatives for cns disorders
DK204291D0 (da) 1991-12-20 1991-12-20 Novo Nordisk As Heterocykliske forbindelser deres fremstilling og anvendelse
CA2049244A1 (en) 1990-08-16 1992-02-17 Steven H. Christiansen Process for absorption of sulfur compounds from fluids using heterocyclic compounds having at least one ring nitrogen atom
PH31566A (en) 1990-10-10 1998-11-03 Schering Corp Pyridine and pyridine n-oxide derivatives for diaryl methyl piperidines or piperazines and compositions and methods of use thereof.
GB9023583D0 (en) 1990-10-30 1990-12-12 Beecham Group Plc Novel compounds
HU221816B1 (hu) 1991-10-11 2003-01-28 Bristol-Myers Squibb Pharma Company Gyűrűs karbonil vegyületek, és ezeket tartalmazó gyógyászati készítmények
US5610294A (en) 1991-10-11 1997-03-11 The Du Pont Merck Pharmaceutical Company Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors
HU220601B1 (hu) 1992-04-30 2002-03-28 Taiho Pharmaceutical Co. Ltd. Fenoxi-alkil-oxazolidin-származékok, eljárás előállításukra és ezeket tartalmazó gyógyszerkészítmények
JPH0753721B2 (ja) 1992-09-11 1995-06-07 工業技術院長 環状ウレタン化合物の製造法
GB9225377D0 (en) 1992-12-04 1993-01-27 Ici Plc Herbicides
AU668818B2 (en) 1993-04-07 1996-05-16 Taiho Pharmaceutical Co., Ltd. Thiazolidine derivative and pharmaceutical composition containing the same
TW280812B (enExample) 1993-07-02 1996-07-11 Bayer Ag
EP0640594A1 (en) 1993-08-23 1995-03-01 Fujirebio Inc. Hydantoin derivative as metalloprotease inhibitor
JPH07157681A (ja) 1993-12-08 1995-06-20 Konica Corp 有機顔料の製造方法及び有機顔料を含有する電子写真感光体
DE19500118A1 (de) 1994-05-18 1995-11-23 Bayer Ag Substituierte Diazacyclohexandi(thi)one
WO1996014297A1 (en) 1994-11-04 1996-05-17 Sumitomo Pharmaceuticals Company, Limited Novel lactam derivatives
FR2729954B1 (fr) 1995-01-30 1997-08-01 Sanofi Sa Composes heterocycliques substitues, procede pour leur preparation et compositions pharmaceutiques les contenant
US5780466A (en) 1995-01-30 1998-07-14 Sanofi Substituted heterocyclic compounds method of preparing them and pharmaceutical compositions in which they are present
GB9510459D0 (en) 1995-05-24 1995-07-19 Zeneca Ltd Bicyclic amines
US5776959A (en) 1995-06-05 1998-07-07 Washington University Anticonvulsant and anxiolytic lactam and thiolactam derivatives
GB9517622D0 (en) 1995-08-29 1995-11-01 Univ Edinburgh Regulation of intracellular glucocorticoid concentrations
JPH09151179A (ja) 1995-11-30 1997-06-10 Canon Inc 光学活性化合物、これを含む液晶組成物、それを有する液晶素子、それらを用いた液晶装置及び表示方法
JP2000508631A (ja) 1996-04-03 2000-07-11 メルク エンド カンパニー インコーポレーテッド ファルネシルタンパク質トランスフェラーゼの阻害剤
WO1998004534A1 (en) 1996-07-31 1998-02-05 Nikken Chemicals Co., Ltd. 6-phenyltetrahydro-1,3-oxazin-2-one derivatives and medicinal compositions containing the same
US6794390B2 (en) 1996-08-02 2004-09-21 Cv Therapeutics, Inc. Purine inhibitors of cyclin dependent kinase 2 & ikappabalpha
US5866702A (en) 1996-08-02 1999-02-02 Cv Therapeutics, Incorporation Purine inhibitors of cyclin dependent kinase 2
GB9623944D0 (en) 1996-11-15 1997-01-08 Zeneca Ltd Bicyclic amine derivatives
JP2002505683A (ja) 1997-06-18 2002-02-19 シナプティック・ファーマスーティカル・コーポレーション 複素環置換されたピペリジン類及びその使用
US6159990A (en) 1997-06-18 2000-12-12 Synaptic Pharmaceutical Corporation Oxazolidinones as α1A receptor antagonists
DE19731784A1 (de) 1997-07-24 1999-02-04 Bayer Ag Substituierte N-Aryl-N-thioxocarbonyl-sulfonamide
GB9715892D0 (en) 1997-07-29 1997-10-01 Zeneca Ltd Heterocyclic compounds
US5912114A (en) 1997-09-12 1999-06-15 Johnson & Johnson Medical, Inc. Wound diagnosis by quantitating cortisol in wound fluids
US5936124A (en) 1998-06-22 1999-08-10 Sepacor Inc. Fluoxetine process from benzoylpropionic acid
US7410995B1 (en) 1998-08-14 2008-08-12 Gpi Nil Holdings Inc. N-linked sulfonamide of heterocyclic thioesters for vision and memory disorders
DE19918725A1 (de) 1999-04-24 2000-10-26 Bayer Ag Substituierte N-Cyano-sulfonsäureanilide
DE19929348A1 (de) 1999-06-26 2000-12-28 Bayer Ag Verfahren zur Herstellung von 2-Heterocyclylmethyl-benzoesäurederivaten
US7256005B2 (en) 1999-08-10 2007-08-14 The Chancellor, Masters And Scholars Of The University Of Oxford Methods for identifying iminosugar derivatives that inhibit HCV p7 ion channel activity
EP1206262A4 (en) 1999-08-26 2003-01-02 Bristol Myers Squibb Co Y NEUROPEPTID ANTAGONISTS: SPIROISOQUINOLINONE DERIVATIVES
CN1434805A (zh) 1999-12-17 2003-08-06 先灵公司 选择性神经激肽拮抗剂
US6436928B1 (en) 1999-12-17 2002-08-20 Schering Corporation Selective neurokinin antagonists
WO2001055063A1 (en) 2000-01-25 2001-08-02 Idemitsu Petrochemical Co., Ltd. Novel bisadamantane compounds, process for preparing the same, and novel biadamantane derivatives
GB0003397D0 (en) 2000-02-14 2000-04-05 Merck Sharp & Dohme Therapeutic agents
DE10034623A1 (de) * 2000-07-17 2002-01-31 Bayer Ag Heterocyclisch substituierte Pyridine als Cytokin-Inhibitoren
DE10034803A1 (de) 2000-07-18 2002-01-31 Bayer Ag Substituierte Sulfonsäureanilide
DE10034800A1 (de) 2000-07-18 2002-01-31 Bayer Ag Substituierte Benzostickstoffheterocyclen
DE10035928A1 (de) 2000-07-21 2002-03-07 Asta Medica Ag Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel
DE10035908A1 (de) 2000-07-21 2002-03-07 Asta Medica Ag Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel
DE10035927A1 (de) 2000-07-21 2002-03-07 Asta Medica Ag Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel
WO2002014269A2 (en) 2000-08-16 2002-02-21 Neurogen Corporation 2,4-substituted pyridine derivatives
AU2001290873B2 (en) 2000-09-11 2006-07-27 Sepracor Inc. Ligands for monoamine receptors and transporters, and methods of use thereof (neurotransmission)
US7294637B2 (en) 2000-09-11 2007-11-13 Sepracor, Inc. Method of treating addiction or dependence using a ligand for a monamine receptor or transporter
JP2002179572A (ja) 2000-10-06 2002-06-26 Nikken Chem Co Ltd アレルギー性眼疾患治療剤
US6841671B2 (en) 2000-10-26 2005-01-11 Pfizer Inc. Spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors
US20030143668A1 (en) 2001-06-18 2003-07-31 National Institute Of Advanced Industrial Guanosine triphosphate-binding protein coupled receptors
JP3873115B2 (ja) 2001-09-25 2007-01-24 独立行政法人産業技術総合研究所 環状ウレタン製造方法
AR037243A1 (es) 2001-10-15 2004-11-03 Schering Corp Antagonistas del receptor de adenosina a2a,a5-amino-imidazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]pirimidina, composiciones farmaceuticas y el uso de dichos compuestos para la preparacion de un medicamento
RU2004118719A (ru) 2001-11-22 2005-03-27 Оно Фармасьютикал Ко., Лтд. (Jp) Производные пиперидин-2-она и фармацевтические композиции, содержащие такие соединения в качестве активного ингредиента
WO2003057673A1 (en) 2001-12-28 2003-07-17 Bayer Pharmaceuticals Corporation 1h-pyrazolyl derivative compounds, for use in diseases associated with the 5-ht2c receptor
JP2003300884A (ja) 2002-04-08 2003-10-21 Nikken Chem Co Ltd ＴＮＦ−α産生阻害剤
JP2005527598A (ja) 2002-04-26 2005-09-15 ファイザー・プロダクツ・インク トリアリール−オキシ−アリール−スピロ−ピリミジン−２，４，６−トリオンメタロプロテイナーゼ阻害剤
MXPA04010545A (es) 2002-04-26 2005-01-25 Pfizer Prod Inc Inhibidores de metaloproteinasa de heteroariloxi-aril-espiero-pirimidina-2,4,6-triona n-sustituida.
US7196085B2 (en) 2002-04-30 2007-03-27 Kudos Pharmaceuticals Limited Phthalazinone derivatives
AU2003234621A1 (en) 2002-05-17 2003-12-02 Jenken Biosciences, Inc. Opioid and opioid-like compounds and uses thereof
MXPA05000196A (es) 2002-07-03 2005-06-06 Schering Corp Derivados de 1-amido-4-fenil-4-benciloximetil-piperidina y compuestos relacionados como antagonistas de neurocinina-1(nk-1)para el tratamiento de vomito, depresion, ansiedad y tos.
WO2004009559A2 (en) 2002-07-18 2004-01-29 Queen's University At Kingston Dihydrouracil compounds as anti-ictogenic or anti-epileptogenic agents
GB0218630D0 (en) 2002-08-10 2002-09-18 Tanabe Seiyaku Co Novel compounds
TWI347946B (en) 2002-10-11 2011-09-01 Otsuka Pharma Co Ltd 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound
WO2004046137A1 (en) 2002-11-21 2004-06-03 Vicore Pharma Ab New tricyclic angiotensin ii agonists
GB0228410D0 (en) 2002-12-05 2003-01-08 Glaxo Group Ltd Novel Compounds
EP1581520A4 (en) 2002-12-13 2006-08-23 Smithkline Beecham Corp COMPOUNDS, COMPOSITIONS AND METHODS
WO2004056744A1 (en) 2002-12-23 2004-07-08 Janssen Pharmaceutica N.V. Adamantyl acetamides as hydroxysteroid dehydrogenase inhibitors
CN1764458A (zh) 2003-03-26 2006-04-26 麦克公司 作为黑皮质素－4受体激动剂的双环哌啶衍生物
ATE482747T1 (de) 2003-04-11 2010-10-15 High Point Pharmaceuticals Llc Neue amide derivate und deren pharmazeutische verwendungen
US7700583B2 (en) 2003-04-11 2010-04-20 High Point Pharmaceuticals, Llc 11β-hydroxysteroid dehydrogenase type 1 active compounds
JP2006523710A (ja) 2003-04-16 2006-10-19 メモリー・ファーマシューティカルズ・コーポレイション ホスホジエステラーゼ４インヒビター
ITMI20031292A1 (it) 2003-06-25 2004-12-26 Nikem Research Srl Derivati biciclici nk-2 antagonisti selettivi.
DE10358004A1 (de) 2003-12-11 2005-07-14 Abbott Gmbh & Co. Kg Ketolactam-Verbindungen und ihre Verwendung
US7186844B2 (en) 2004-01-13 2007-03-06 Mitsubishi Gas Chemical Co., Inc. Method for producing cyclic carbamate ester
JP4324669B2 (ja) 2004-01-21 2009-09-02 独立行政法人産業技術総合研究所 環状ウレタンの製造方法
JP2005239670A (ja) 2004-02-27 2005-09-08 Ono Pharmaceut Co Ltd 含窒素複素環化合物およびその医薬用途
JP2007528396A (ja) 2004-03-09 2007-10-11 メルク　エンド　カムパニー　インコーポレーテッド Ｈｉｖインテグラーゼ阻害薬
US8519158B2 (en) 2004-03-12 2013-08-27 Ligand Pharmaceuticals Incorporated Androgen receptor modulator compounds and methods
JP2005272321A (ja) 2004-03-23 2005-10-06 Ono Pharmaceut Co Ltd 含窒素複素環化合物およびその医薬用途
CN101001836B (zh) 2004-05-07 2010-12-22 詹森药业有限公司 作为11-β羟基类固醇脱氢酶抑制剂的吡咯烷-2-酮和哌啶-2-酮衍生物
NZ551076A (en) 2004-05-07 2009-05-31 Janssen Pharmaceutica Nv Adamantyl pyrrolidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors
GB0411404D0 (en) 2004-05-21 2004-06-23 Glaxo Group Ltd Novel compounds
CN1964956B (zh) 2004-05-24 2013-03-27 安美基公司 11-β-羟基类固醇脱氢酶1型的抑制剂
WO2006002349A1 (en) 2004-06-24 2006-01-05 Incyte Corporation Amido compounds and their use as pharmaceuticals
GB0414438D0 (en) 2004-06-28 2004-07-28 Syngenta Participations Ag Chemical compounds
DOP2005000123A (es) 2004-07-02 2011-07-15 Merck Sharp & Dohme Inhibidores de cetp
EP1621539A1 (en) 2004-07-27 2006-02-01 Aventis Pharma S.A. Heterocycle -substituted cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
EP1621535A1 (en) 2004-07-27 2006-02-01 Aventis Pharma S.A. Substituted cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
EP1621536A1 (en) 2004-07-27 2006-02-01 Aventis Pharma S.A. Amino cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
US7465726B2 (en) 2004-08-02 2008-12-16 Osi Pharmaceuticals, Inc. Substituted pyrrolo[2.3-B]pyridines
AU2005290081B2 (en) 2004-08-23 2010-12-02 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
BRPI0515121A (pt) 2004-08-30 2008-07-08 Janssen Pharmaceutica Nv derivados da n-2 adamantil-2-fenóxi acetamida como inibidores da 11-beta hidroxiesteróide desidrogenase
KR101197672B1 (ko) 2004-08-30 2012-11-07 얀센 파마슈티카 엔.브이. 11-베타 하이드록시스테로이드 데하이드로게나제저해제로서 트리사이클릭 락탐 유도체
AU2005285035B2 (en) 2004-09-10 2012-03-22 Janssen Pharmaceutica N.V. Novel imidazolidin-2-one derivatives as selective androgen receptor modulators (SARMS)
US8138342B2 (en) 2004-10-12 2012-03-20 High Point Pharmacueticals, LLC 11β-hydroxysteroid dehydrogenase type 1 active spiro compounds
CA2581745A1 (en) 2004-10-13 2006-04-27 Neurogen Corporation Aryl substituted 8-azabicyclo[3.2.1]octane compounds as ligands of the melanin concentrating hormone receptor
ES2318577T3 (es) 2004-10-29 2009-05-01 Eli Lilly And Company Derivados de cicloalquil lactama como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa 1'.
KR101368228B1 (ko) 2004-11-10 2014-02-27 인사이트 코포레이션 락탐 화합물 및 약제로서의 이의 용도
US20060167044A1 (en) 2004-12-20 2006-07-27 Arnaiz Damian O Piperidine derivatives and their use as anti-inflammatory agents
WO2006066924A2 (en) 2004-12-23 2006-06-29 Chiesi Farmaceutici S.P.A. Azole derivatives with antimuscarinic activity
US7994172B2 (en) 2004-12-28 2011-08-09 Exelixis, Inc. [1H-pyrazolo[3, 4-D]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (P70s6k, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases
CA2595205A1 (en) 2005-01-19 2006-07-27 Neurogen Corporation Heteroaryl substituted piperazinyl-pyridine analogues
CN101146793A (zh) 2005-02-16 2008-03-19 先灵公司 具有cxcr3拮抗剂活性的新的杂环取代了的吡啶或苯基化合物
MX2007010068A (es) 2005-02-16 2007-10-10 Schering Corp Piperazino-piperidinas con actividad antagonista de cxcr3.
CN101163692B (zh) 2005-02-16 2012-01-18 先灵公司 具有cxcr3拮抗活性的杂环取代的哌嗪
EP1856098B1 (en) 2005-02-16 2012-08-01 Schering Corporation Pyrazinyl substituted piperazine-piperidines with cxcr3 antagonist activity
CA2598460C (en) 2005-02-16 2013-05-07 Schering Corporation Amine-linked pyridyl and phenyl substituted piperazine-piperidines with cxcr3 antagonist activity
MX2007009946A (es) 2005-02-16 2007-09-26 Schering Corp Piperazin-piperidinas sustituidas con piridilo y fenilo con actividad antagonista de cxcr3.
KR100890886B1 (ko) 2005-02-24 2009-03-31 니혼노야쿠가부시키가이샤 신규 할로알킬설폰아닐리드 유도체, 제초제 및 이의 이용방법
US20090264650A1 (en) 2005-03-31 2009-10-22 Nobuo Cho Prophylactic/Therapeutic Agent for Diabetes
KR101284573B1 (ko) 2005-04-12 2013-07-11 바이코어 파마 아베 신규한 트리시클릭 안지오텐신 ⅱ 아고니스트
WO2007008529A2 (en) 2005-07-08 2007-01-18 Kalypsys, Inc Celullar cholesterol absorption modifiers
EP1924265A4 (en) 2005-08-16 2010-06-02 Genzyme Corp COMPOUNDS BINDING TO CHEMOKINE RECEPTORS
US7781437B2 (en) 2005-10-11 2010-08-24 Schering Corporation Substituted heterocyclic compounds with CXCR3 antagonist activity
AU2006308167A1 (en) 2005-10-27 2007-05-03 Ucb Pharma, S.A. Compounds comprising a lactam or a lactam derivative moiety, processes for making them, and their uses
KR20080076916A (ko) 2005-11-01 2008-08-20 트랜스테크 파르마, 인크. 치환된 아미드의 약학적 사용
JP2007140188A (ja) 2005-11-18 2007-06-07 Fujifilm Corp ポジ型感光性組成物及びそれを用いたパターン形成方法
EP1951696A2 (en) 2005-11-22 2008-08-06 Amgen Inc. Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
AU2006322060A1 (en) 2005-12-05 2007-06-14 Incyte Corporation Lactam compounds and methods of using the same
EP1801098A1 (en) 2005-12-16 2007-06-27 Merck Sante 2-Adamantylurea derivatives as selective 11B-HSD1 inhibitors
WO2007076055A2 (en) 2005-12-22 2007-07-05 Entremed, Inc. Compositions and methods comprising proteinase activated receptor antagonists
DE102005062990A1 (de) 2005-12-28 2007-07-05 Grünenthal GmbH Substituierte Thiazole und ihre Verwendung zur Herstellung von Arzneimitteln
EP1973546B1 (en) * 2005-12-30 2012-06-13 Merck Sharp & Dohme Corp. Cholesteryl ester transfer protein inhibitors
WO2007079186A2 (en) 2005-12-30 2007-07-12 Merck & Co., Inc. 1, 3-oxazolidin-2-one derivatives useful as cetp inhibitors
US7910592B2 (en) 2005-12-30 2011-03-22 Merck Sharp & Dohme Corp. CETP inhibitors
CA2635010A1 (en) 2005-12-30 2007-07-19 Amjad Ali Oxazolidinone derivatives as cetp inhibitors
WO2007084314A2 (en) 2006-01-12 2007-07-26 Incyte Corporation MODULATORS OF 11-ß HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME
ES2791724T3 (es) 2006-02-27 2020-11-05 Ascensia Diabetes Care Holdings Ag Medida de analito ajustada en temperatura para sistemas de biosensor
US20070213311A1 (en) 2006-03-02 2007-09-13 Yun-Long Li Modulators of 11-beta hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same
WO2007103719A2 (en) 2006-03-03 2007-09-13 Incyte Corporation MODULATORS OF 11-β HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME
WO2007109456A2 (en) 2006-03-16 2007-09-27 Pharmacopeia, Inc. Substituted biphenyl isoxazole sulfonamides as dual angiotensin endothelin receptor antagonists
JP2007254409A (ja) 2006-03-24 2007-10-04 Taisho Pharmaceut Co Ltd イミダゾリジノン誘導体
US7435833B2 (en) 2006-04-07 2008-10-14 Abbott Laboratories Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme
MX2008013305A (es) 2006-04-20 2008-10-27 Du Pont Agentes heterociclicos de cinco miembros para el control de plagas de invertebrados.
AU2007240450B2 (en) 2006-04-21 2011-12-22 Eli Lilly And Company Cyclohexylimidazole lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
CN101541747B (zh) 2006-04-21 2012-11-14 伊莱利利公司 作为11-β-羟基甾族化合物脱氢酶1的抑制剂的联苯基酰胺内酰胺衍生物
CA2647677C (en) 2006-04-21 2014-03-18 Eli Lilly And Company Cyclohexylpyrazole-lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
AU2007244960B2 (en) * 2006-04-24 2012-03-01 Eli Lilly And Company Substituted pyrrolidinones as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
ATE471311T1 (de) 2006-04-25 2010-07-15 Lilly Co Eli Inhibitoren von11-beta- hydroxysteroiddehydrogenase 1
US8178005B2 (en) 2006-06-20 2012-05-15 Chemtura Corporation Liquid phosphite compositions having different alkyl groups
PE20080344A1 (es) 2006-06-27 2008-06-09 Sanofi Aventis Compuestos 8-azabiciclo[3.2.1]oct-8-il-1,2,3,4-tetrahidroquinolina sustituidos como inhibidores 11b-hsd1
WO2008012622A2 (en) 2006-07-25 2008-01-31 Pfizer Products Inc. Azabenzimidazolyl compounds as potentiators of mglur2 subtype of glutamate receptor
WO2008012623A1 (en) 2006-07-25 2008-01-31 Pfizer Products Inc. Benzimidazolyl compounds as potentiators of mglur2 subtype of glutamate receptor
WO2008021337A1 (en) 2006-08-15 2008-02-21 Wyeth Oxazinan-2-one derivatives useful as pr modulators
US7649007B2 (en) 2006-08-15 2010-01-19 Wyeth Llc Oxazolidine derivatives as PR modulators
US7618989B2 (en) 2006-08-15 2009-11-17 Wyeth Tricyclic oxazolidone derivatives useful as PR modulators
EP2064187A2 (en) 2006-08-25 2009-06-03 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
EP2061780A4 (en) 2006-09-14 2010-12-22 Zalicus Pharmaceuticals Ltd DIARYLE PIPERIDINE COMPOUNDS AS CALCIUM CHANNEL BLOCKERS
CN101516877B (zh) 2006-09-22 2013-09-11 诺瓦提斯公司 杂环有机化合物
DE102007005799B4 (de) 2006-10-18 2018-01-25 Heinz-Jürgen Mühlen Verfahren zur Erzeugung eines wasserstoffreichen Produktgases
RU2439062C2 (ru) 2006-10-19 2012-01-10 Ф.Хоффманн-Ля Рош Аг Производные имидазолона и имидазолидинона как 11в-hsd1 ингибиторы при диабете
TW200829171A (en) 2006-11-17 2008-07-16 Nihon Nohyaku Co Ltd Haloalkyl sulfonanilide derivatives or salts thereof, herbicide using it as effective constituent and use-method thereof
EP1935420A1 (en) 2006-12-21 2008-06-25 Merck Sante 2-Adamantyl-butyramide derivatives as selective 11beta-HSD1 inhibitors
EP2125750B1 (en) 2007-02-26 2014-05-21 Vitae Pharmaceuticals, Inc. Cyclic urea and carbamate inhibitors of 11beta-hydroxysteroid dehydrogenase 1
MX2009010207A (es) 2007-03-23 2009-10-19 Schering Corp Peptidos de hidrazido como inhibidores de proteasa ns3 de virus de hepatitis c.
WO2008119663A1 (en) 2007-03-29 2008-10-09 F. Hoffmann-La Roche Ag Heterocyclic antiviral compounds
US8329897B2 (en) 2007-07-26 2012-12-11 Vitae Pharmaceuticals, Inc. Synthesis of inhibitors of 11β-hydroxysteroid dehydrogenase type 1
WO2009020140A1 (ja) 2007-08-06 2009-02-12 Dainippon Sumitomo Pharma Co., Ltd. アダマンチルウレア誘導体
JP2009110842A (ja) 2007-10-31 2009-05-21 Sumitomo Chemical Co Ltd ボタンスイッチ被覆用積層樹脂体
AR069207A1 (es) 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
EP2220048B1 (en) 2007-11-16 2017-01-25 Boehringer Ingelheim International GmbH Aryl- and heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use
JP5490014B2 (ja) 2007-12-11 2014-05-14 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１型の環状尿素阻害剤
KR101460359B1 (ko) 2007-12-13 2014-11-10 삼성전자주식회사 이동통신 시스템에서의 핸드오버 방법 및 장치
TW200934490A (en) 2008-01-07 2009-08-16 Vitae Pharmaceuticals Inc Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1
EP2252601B1 (en) 2008-01-24 2012-12-19 Vitae Pharmaceuticals, Inc. Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CA2714532A1 (en) 2008-02-11 2009-08-20 Vitae Pharmaceuticals, Inc. 1,3-oxazepan-2-one and 1,3-diazepan-2-one inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
ATE531696T1 (de) 2008-02-12 2011-11-15 Boehringer Ingelheim Int Harnstoff-derivate von benzomorphanen, entsprechende gerüste, medikamente mit solchen verbindungen und ihre verwendung
EP2254872A2 (en) 2008-02-15 2010-12-01 Vitae Pharmaceuticals, Inc. Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
JP5108557B2 (ja) 2008-02-27 2012-12-26 東京エレクトロン株式会社 ロードロック装置および基板冷却方法
WO2009108332A1 (en) 2008-02-27 2009-09-03 Vitae Pharmaceuticals, Inc. INHIBITORS OF 11β -HYDROXYSTEROID DEHYDROGENASE TYPE 1
EP2274287B1 (en) 2008-03-18 2016-03-09 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
TW200944526A (en) 2008-04-22 2009-11-01 Vitae Pharmaceuticals Inc Carbamate and urea inhibitors of 11β-hydroxysteroid dehydrogenase 1
EP2291373B1 (en) 2008-05-01 2013-09-11 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CL2009001058A1 (es) 2008-05-01 2010-09-10 Vitae Pharmaceuticals Inc Compuestos derivados de oxazinas sustituidas, inhibidores de la 11b-hidroxiesteroide deshidrogenasa de tipo-1; composicion farmaceutica; y uso del compuesto para inhibir la actividad de 11b-hsd1, como en el tratamiento de la diabetes, dislipidemia, hipertension, obesidad, cancer, glaucoma, entre otras.
JP5538365B2 (ja) 2008-05-01 2014-07-02 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状阻害剤
CA2722427A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
WO2009138386A2 (en) 2008-05-13 2009-11-19 Boehringer Ingelheim International Gmbh Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use
US20110224242A1 (en) 2008-07-23 2011-09-15 Bioalliance Pharma Styrlyquinolines, their process of preparation and their therapeutic uses
WO2010010149A1 (en) 2008-07-23 2010-01-28 Bioalliance Pharma Styrylquinolines, their process of preparation and their therapeutic uses
JP5777030B2 (ja) 2008-07-25 2015-09-09 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １１β−ヒドロキシステロイドデヒドロゲナーゼ１の阻害剤
RU2539979C2 (ru) 2008-07-25 2015-01-27 Вайтаи Фармасьютиклз, Инк. Циклические ингибиторы 11бета-гидроксистероид-дегидрогеназы 1
US8309597B2 (en) 2008-07-25 2012-11-13 Boehringer Ingelheim International Gmbh 1,1′-diadamantyl carboxylic acids, medicaments containing such compounds and their use
WO2010010150A1 (en) 2008-07-25 2010-01-28 Boehringer Ingelheim International Gmbh Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
US8609690B2 (en) 2008-08-25 2013-12-17 Boehringer Ingelheim International Gmbh Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use
EP2350068B1 (en) 2008-10-23 2017-08-30 Boehringer Ingelheim International GmbH Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use
EP2393813B1 (en) 2009-02-04 2013-07-31 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11 ß-hydroxysteroid dehydrogenase 1 useful for the treatment of diseases related to elevated level of cortisol
WO2010089303A1 (en) 2009-02-04 2010-08-12 Boehringer Ingelheim International Gmbh CYCLIC INHIBITORS OF 11 β-HYDROXYSTEROID DEHYDROGENASE 1
WO2010104830A1 (en) 2009-03-09 2010-09-16 Bristol-Myers Squibb Company Pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists
MA33216B1 (fr) 2009-04-30 2012-04-02 Boehringer Ingelheim Int Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1
US20100331320A1 (en) 2009-04-30 2010-12-30 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5670440B2 (ja) 2009-06-02 2015-02-18 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状阻害剤
AR076936A1 (es) 2009-06-02 2011-07-20 Vitae Pharmaceuticals Inc Inhibidores de carbamato y urea de la 11 beta hidroxiesteroide deshidrogenasa 1
EP2440537A1 (en) 2009-06-11 2012-04-18 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure
WO2011002910A1 (en) 2009-07-01 2011-01-06 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
KR20120104521A (ko) 2009-09-11 2012-09-21 사일린 파마슈티칼스, 인크 약제학적으로 유용한 헤테로사이클－치환된 락탐
JP5750449B2 (ja) 2009-11-05 2015-07-22 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規キラルリンリガンド
TWI531571B (zh) 2009-11-06 2016-05-01 維它藥物公司 六氫茚并吡啶及八氫苯并喹啉之芳基－及雜芳基羰基衍生物
EP2582698B1 (en) 2010-06-16 2016-09-14 Vitae Pharmaceuticals, Inc. Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use
JP5813106B2 (ja) 2010-06-25 2015-11-17 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 代謝障害の処置のための１１−β−ＨＳＤ１のインヒビターとしてのアザスピロヘキサノン
BR112013010021A2 (pt) 2010-11-02 2019-09-24 Boehringer Ingelheim Int combinações farmacêuticas para o tratamento de distúrbios metabólicos.

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