JP2002527504A - システインプロテアーゼのICE/ced−3系の置換アシルジペプチジル抑制剤 - Google Patents
システインプロテアーゼのICE/ced−3系の置換アシルジペプチジル抑制剤Info
- Publication number
- JP2002527504A JP2002527504A JP2000577149A JP2000577149A JP2002527504A JP 2002527504 A JP2002527504 A JP 2002527504A JP 2000577149 A JP2000577149 A JP 2000577149A JP 2000577149 A JP2000577149 A JP 2000577149A JP 2002527504 A JP2002527504 A JP 2002527504A
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- naphthyl
- substituted
- cycloalkyl
- mmol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
- C07D215/20—Oxygen atoms
- C07D215/22—Oxygen atoms attached in position 2 or 4
- C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P25/00—Drugs for disorders of the nervous system
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- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P9/00—Drugs for disorders of the cardiovascular system
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- C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
- C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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- C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
- C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C311/09—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton the carbon skeleton being further substituted by at least two halogen atoms
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- 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
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
- C07D215/20—Oxygen atoms
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- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
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- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/06—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
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- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
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- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
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- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
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- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
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- C07D239/32—One oxygen, sulfur or nitrogen atom
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- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
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- C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
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- C07D309/30—Oxygen atoms, e.g. delta-lactones
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
- C07F9/32—Esters thereof
- C07F9/3258—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
- C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/14—The ring being saturated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2602/00—Systems containing two condensed rings
- C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
- C07C2602/04—One of the condensed rings being a six-membered aromatic ring
- C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2603/00—Systems containing at least three condensed rings
- C07C2603/56—Ring systems containing bridged rings
- C07C2603/58—Ring systems containing bridged rings containing three rings
- C07C2603/70—Ring systems containing bridged rings containing three rings containing only six-membered rings
- C07C2603/74—Adamantanes
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Crystallography & Structural Chemistry (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Quinoline Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Furan Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US09/177,546 | 1998-10-22 | ||
| US09/177,546 US6242422B1 (en) | 1998-10-22 | 1998-10-22 | (Substituted)Acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases |
| PCT/US1999/024756 WO2000023421A1 (en) | 1998-10-22 | 1999-10-22 | (SUBSTITUTED)ACYL DIPEPTIDYL INHIBITORS OF THE ICE/ced-3 FAMILY OF CYSTEINE PROTEASES |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2002527504A true JP2002527504A (ja) | 2002-08-27 |
| JP2002527504A5 JP2002527504A5 (https=) | 2006-12-07 |
Family
ID=22649018
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000577149A Pending JP2002527504A (ja) | 1998-10-22 | 1999-10-22 | システインプロテアーゼのICE/ced−3系の置換アシルジペプチジル抑制剤 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US6242422B1 (https=) |
| EP (1) | EP1123272A1 (https=) |
| JP (1) | JP2002527504A (https=) |
| KR (1) | KR20010093779A (https=) |
| AU (1) | AU1221500A (https=) |
| CA (1) | CA2347792A1 (https=) |
| HK (1) | HK1039317A1 (https=) |
| IL (1) | IL142665A0 (https=) |
| NO (1) | NO20011968L (https=) |
| WO (1) | WO2000023421A1 (https=) |
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| JP2007506803A (ja) * | 2003-05-27 | 2007-03-22 | バーテックス ファーマシューティカルズ インコーポレイテッド | カスパーゼ阻害剤およびそれらの用途 |
| JP2008538205A (ja) * | 2005-03-07 | 2008-10-16 | ガンガ, ラジュ ゴカラジュ, | ボスウェル酸及び選択的に濃縮したボスウェル酸の新規な塩、ならびにそのための方法 |
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| JP2013545763A (ja) * | 2010-11-30 | 2013-12-26 | バイエル・インテレクチユアル・プロパテイー・ゲー・エム・ベー・ハー | ピリミジン誘導体 |
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- 1998-10-22 US US09/177,546 patent/US6242422B1/en not_active Expired - Fee Related
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1999
- 1999-10-22 AU AU12215/00A patent/AU1221500A/en not_active Abandoned
- 1999-10-22 JP JP2000577149A patent/JP2002527504A/ja active Pending
- 1999-10-22 WO PCT/US1999/024756 patent/WO2000023421A1/en not_active Ceased
- 1999-10-22 EP EP99970657A patent/EP1123272A1/en not_active Withdrawn
- 1999-10-22 KR KR1020017004971A patent/KR20010093779A/ko not_active Withdrawn
- 1999-10-22 HK HK02100909.8A patent/HK1039317A1/zh unknown
- 1999-10-22 CA CA002347792A patent/CA2347792A1/en not_active Abandoned
- 1999-10-22 IL IL14266599A patent/IL142665A0/xx unknown
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2001
- 2001-04-16 US US09/836,442 patent/US20020091089A1/en not_active Abandoned
- 2001-04-20 NO NO20011968A patent/NO20011968L/no not_active Application Discontinuation
Cited By (27)
| Publication number | Priority date | Publication date | Assignee | Title |
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| JP2003506389A (ja) * | 1999-08-06 | 2003-02-18 | バーテックス ファーマシューティカルズ インコーポレイテッド | カスパーゼ阻害剤およびその使用 |
| JP2007506803A (ja) * | 2003-05-27 | 2007-03-22 | バーテックス ファーマシューティカルズ インコーポレイテッド | カスパーゼ阻害剤およびそれらの用途 |
| JP4791365B2 (ja) * | 2003-05-27 | 2011-10-12 | バーテックス ファーマシューティカルズ インコーポレイテッド | カスパーゼ阻害剤およびそれらの用途 |
| JP2012036206A (ja) * | 2003-05-27 | 2012-02-23 | Vertex Pharmaceuticals Inc | カスパーゼ阻害剤およびそれらの用途 |
| JP2009108067A (ja) * | 2004-11-24 | 2009-05-21 | Vertex Pharmaceut Inc | 3−[2−(3−アシルアミノ−2−オキソ−2h−ピリジン−1−イル)−アセチルアミノ]−4−オキソ−ペンタン酸誘導体、およびカスパーゼ阻害剤としてのそれらの使用 |
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| JP2008538205A (ja) * | 2005-03-07 | 2008-10-16 | ガンガ, ラジュ ゴカラジュ, | ボスウェル酸及び選択的に濃縮したボスウェル酸の新規な塩、ならびにそのための方法 |
| EP2253311A2 (en) | 2006-04-11 | 2010-11-24 | Arena Pharmaceuticals, Inc. | Use of GPR119 receptor agonists for increasing bone mass and for treating osteoporosis, as well as combination therapy relating thereto |
| WO2011005929A1 (en) | 2009-07-09 | 2011-01-13 | Arena Pharmaceuticals, Inc. | Piperidine derivative and its use for the treatment of diabets and obesity |
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Also Published As
| Publication number | Publication date |
|---|---|
| KR20010093779A (ko) | 2001-10-29 |
| US20020091089A1 (en) | 2002-07-11 |
| NO20011968D0 (no) | 2001-04-20 |
| AU1221500A (en) | 2000-05-08 |
| HK1039317A1 (zh) | 2002-04-19 |
| WO2000023421A1 (en) | 2000-04-27 |
| EP1123272A1 (en) | 2001-08-16 |
| IL142665A0 (en) | 2002-03-10 |
| NO20011968L (no) | 2001-06-19 |
| CA2347792A1 (en) | 2000-04-27 |
| US6242422B1 (en) | 2001-06-05 |
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