JPH11509535A - 環状gmp特異性ホスフォジエステラーゼインヒビター - Google Patents
環状gmp特異性ホスフォジエステラーゼインヒビターInfo
- Publication number
- JPH11509535A JPH11509535A JP9506249A JP50624997A JPH11509535A JP H11509535 A JPH11509535 A JP H11509535A JP 9506249 A JP9506249 A JP 9506249A JP 50624997 A JP50624997 A JP 50624997A JP H11509535 A JPH11509535 A JP H11509535A
- Authority
- JP
- Japan
- Prior art keywords
- compound
- compound according
- formula
- benzofuranyl
- indole
- 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.)
- Granted
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
-
- 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
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.下記化学式(I)の化合物及びその溶媒和物。 式中、 R0は、水素原子、ハロゲン又は炭素数1から6のアルキルを表し、 R1は、水素原子又は炭素数1から6のアルキルを表し、 R2は、ハロゲン及び炭素数1から3のアルキルから選ばれる1又はそれ以上 のグループにより置換されても良い2環(下記化学式に示される)であり、 そして、 R3は、水素原子又は炭素数1から3のアルキルを表す。 2.R0が、水素原子を表す請求の範囲第1項に記載の化合物。 3.R1が、水素原子、メチル及びイソプロピルから選択される請求の範囲第1 項又は第2項に記載の化合物。 4.R3が、水素原子又はメチルを表す請求の範囲第1項から第3項のいずれか に記載の化合物。 5.(6R,12aR)-2,3,6,7,12,12a-ヘキサヒドロ-6-(5-ベンゾフラニル)-2-メチル- ピラジノ[2',1':6,1]ピリド[3,4-b]インドール-1,4-ジオン; (6R,12aR)-2,3,6,7,12,12a-ヘキサヒドロ-6-(5-ベンゾフラニル)-ピラジノ[2' ,1',:6,1]ピリド[3,4-b]インドール-1,4-ジオン; (3S,6R,12aR)-2,3,6,7,12,12a-ヘキサヒドロ-6-(5-ベンゾフラニル)-3-メチル -ピラジノ[2',1':6,1]ピリド[3,4-b]インドール-1,4-ジオン; (3S,6R,12aR)-2,3,6,7,12,12a-ヘキサヒドロ-6-(5-ベンゾフラニル)-2,3-ジメ チル-ピラジノ[2',1':6,1]ピリド[3,4-b]インドール-1,4-ジオン; (6R,12aR)-2,3,6,7,12,12a-ヘキサヒドロ-6-(5-ベンゾフラニル)-2-イソプロ ピル-ピラジノ[2',1':6,1]ピリド[3,4-b]インドール-1,4-ジオン; 及びこれらの生理学上許容できる溶媒和物。 6.(6R,12aR)-2,3,6,7,12,12a-ヘキサヒドロ-6-(5-ベンゾフラニル)-2-メチル- ピラジノ[2',1':6,1]ピリド[3,4-b]インドール-1,4-ジオン; 及びこの生理学上許容できる溶媒和物。 7.治療における用途のための、請求の範囲第1項から第6項のいずれかに記載 の化合物。 8.cGMP特異性PDEの阻害が治療上有益である状態の処置における用途の ための、請求の範囲第1項から第6項のいずれかに記載の化合物。 9.cGMP特異性PDEの阻害が治療上有益である状態の処置のための医薬の 製造のための、請求の範囲第1項から第6項のいずれかに記載の化合物の用途。 10.請求の範囲第1項から第6項のいずれかに記載の化合物の治療上有効な量 を体内に投与することを含む、ヒト又はヒト以外の動物の体内においてcGMP 特異性PDEの阻害が治療上有益である状態の処置方法。 11.請求の範囲第1項から第6項のいずれかに記載の化合物を、医薬上許容さ れるその希釈剤又は担体とともに含む医薬組成物。 12.請求の範囲第1項から第6項のいずれかに記載の化合物を医薬上許容され るその希釈剤又は担体と混合することを含む、その化合物を含む医薬組成物の調 製方法。 13.下記化学式(II)の化合物を第一級アミンR1NH2とともに処理すること を含む、請求の範囲第1項に記載の化合物を調製するための方法(A); 若しくは 加熱温度で、アルコールのような適切な溶媒中で、触媒の存在下、化学式(II I)の化合物を水素化することを含む方法(B): 又は 方法(A)又は(B)を含み、さらに i)相互転換ステップ 及び/若しくは ii)溶媒和物形成 が行われる方法(C)。 (化学式(II)において、Alkは炭素数1から6のアルキルを表し、Halはハロゲ ン原子を表す) (化学式(III)において、Alkは上記の通りであり、Cbzはカルボベンジルオキ シグループを表す)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB9514465.5 | 1995-07-14 | ||
GBGB9514465.5A GB9514465D0 (en) | 1995-07-14 | 1995-07-14 | Chemical compounds |
PCT/EP1996/003025 WO1997003985A1 (en) | 1995-07-14 | 1996-07-11 | Cyclic gmp-specific phosphodiesterase inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH11509535A true JPH11509535A (ja) | 1999-08-24 |
JP4150818B2 JP4150818B2 (ja) | 2008-09-17 |
Family
ID=10777696
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP50624997A Expired - Fee Related JP4150818B2 (ja) | 1995-07-14 | 1996-07-11 | 環状gmp特異性ホスフォジエステラーゼインヒビター |
Country Status (24)
Country | Link |
---|---|
US (1) | US5981527A (ja) |
EP (1) | EP0846118B1 (ja) |
JP (1) | JP4150818B2 (ja) |
CN (1) | CN1069318C (ja) |
AR (1) | AR003455A1 (ja) |
AT (1) | ATE216997T1 (ja) |
AU (1) | AU702324B2 (ja) |
BR (1) | BR9609780A (ja) |
CA (1) | CA2226761A1 (ja) |
CO (1) | CO4700455A1 (ja) |
CZ (1) | CZ3298A3 (ja) |
DE (1) | DE69621026T2 (ja) |
ES (1) | ES2176471T3 (ja) |
GB (1) | GB9514465D0 (ja) |
HR (1) | HRP960321B1 (ja) |
HU (1) | HUP9900006A3 (ja) |
IL (1) | IL122923A0 (ja) |
MX (1) | MX9800411A (ja) |
NO (1) | NO980154L (ja) |
PL (1) | PL324527A1 (ja) |
SK (1) | SK3898A3 (ja) |
WO (1) | WO1997003985A1 (ja) |
YU (1) | YU42296A (ja) |
ZA (1) | ZA965934B (ja) |
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US3644384A (en) * | 1969-06-09 | 1972-02-22 | Sterling Drug Inc | Certain 2-(alpha-haloacetyl) - 1 2 3 4-tetrahydro - 9h - pyrido(3 4-b)indole-3-carboxylates and derivatives |
US3717638A (en) * | 1971-03-11 | 1973-02-20 | Sterling Drug Inc | 1,2,3,4,6,7,12,12A-OCTAHYDRO-2-PHENYLPYRAZINO[2',1':6,1]PYRIDO[3,4-b]INDOLES AND INTERMEDIATES THEREFOR |
US3917599A (en) * | 1973-03-30 | 1975-11-04 | Council Scient Ind Res | 2-Substituted-1,2,3,4,6,7,12,12A-octahydropyrazino(2{40 ,1{40 :6,1)pyrido(3,4-B)indoles |
GB1454171A (en) * | 1973-10-19 | 1976-10-27 | Council Scient Ind Res | Tetracyclic compounds |
US4188390A (en) * | 1977-11-05 | 1980-02-12 | Pfizer Inc. | Antihypertensive 4-amino-2-[4-(1,4-benzodioxan-2-carbonyl) piperazin-1-yl or homopiperazin-1-yl]quinazolines |
US4656174A (en) * | 1982-07-24 | 1987-04-07 | Pfizer Inc. | Quinoline therapeutic agents |
IT1217190B (it) * | 1988-04-22 | 1990-03-14 | Recordati Chem Pharm | Composti utili per il trattamento e diagnosi di disfunzioni frettili |
EP0357122A3 (en) * | 1988-08-29 | 1991-10-23 | Duphar International Research B.V | Use of beta-carbolines, their bio-isosteric benzofuran and benzothiophene analogues for the manufacture of a medicament having cytostatic properties |
DE3830096A1 (de) * | 1988-09-03 | 1990-03-15 | Hoechst Ag | Piperazindione mit psychotroper wirkung |
FR2649613B1 (fr) * | 1989-07-11 | 1991-09-27 | Virag Ronald | Medicament vaso-actif |
JPH0344324A (ja) * | 1989-07-13 | 1991-02-26 | Kazuoki Tsuchiya | 性機能賦活剤 |
EP0459666B1 (en) * | 1990-05-31 | 1994-11-09 | Pfizer Inc. | Medicaments against impotence |
US5270323A (en) * | 1990-05-31 | 1993-12-14 | Pfizer Inc. | Method of treating impotence |
GB9013750D0 (en) * | 1990-06-20 | 1990-08-08 | Pfizer Ltd | Therapeutic agents |
GB9114760D0 (en) * | 1991-07-09 | 1991-08-28 | Pfizer Ltd | Therapeutic agents |
GB9218322D0 (en) * | 1992-08-28 | 1992-10-14 | Pfizer Ltd | Therapeutic agents |
GB9301192D0 (en) * | 1993-06-09 | 1993-06-09 | Trott Francis W | Flower shaped mechanised table |
GB9401090D0 (en) * | 1994-01-21 | 1994-03-16 | Glaxo Lab Sa | Chemical compounds |
-
1995
- 1995-07-14 GB GBGB9514465.5A patent/GB9514465D0/en active Pending
-
1996
- 1996-07-05 HR HR960321A patent/HRP960321B1/xx not_active IP Right Cessation
- 1996-07-11 ES ES96923986T patent/ES2176471T3/es not_active Expired - Lifetime
- 1996-07-11 JP JP50624997A patent/JP4150818B2/ja not_active Expired - Fee Related
- 1996-07-11 CN CN96196751A patent/CN1069318C/zh not_active Expired - Fee Related
- 1996-07-11 IL IL12292396A patent/IL122923A0/xx unknown
- 1996-07-11 PL PL96324527A patent/PL324527A1/xx unknown
- 1996-07-11 US US09/000,192 patent/US5981527A/en not_active Expired - Lifetime
- 1996-07-11 HU HU9900006A patent/HUP9900006A3/hu unknown
- 1996-07-11 MX MX9800411A patent/MX9800411A/es not_active Application Discontinuation
- 1996-07-11 BR BR9609780A patent/BR9609780A/pt not_active Application Discontinuation
- 1996-07-11 EP EP96923986A patent/EP0846118B1/en not_active Expired - Lifetime
- 1996-07-11 CA CA002226761A patent/CA2226761A1/en not_active Abandoned
- 1996-07-11 DE DE69621026T patent/DE69621026T2/de not_active Expired - Fee Related
- 1996-07-11 AT AT96923986T patent/ATE216997T1/de active
- 1996-07-11 AU AU64192/96A patent/AU702324B2/en not_active Ceased
- 1996-07-11 CZ CZ9832A patent/CZ3298A3/cs unknown
- 1996-07-11 WO PCT/EP1996/003025 patent/WO1997003985A1/en active IP Right Grant
- 1996-07-11 SK SK38-98A patent/SK3898A3/sk unknown
- 1996-07-12 ZA ZA9605934A patent/ZA965934B/xx unknown
- 1996-07-12 AR ARP960103558A patent/AR003455A1/es unknown
- 1996-07-12 YU YU42296A patent/YU42296A/sh unknown
- 1996-07-12 CO CO96036775A patent/CO4700455A1/es unknown
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1998
- 1998-01-13 NO NO980154A patent/NO980154L/no not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
HUP9900006A2 (hu) | 1999-04-28 |
ZA965934B (en) | 1997-02-03 |
AU6419296A (en) | 1997-02-18 |
BR9609780A (pt) | 1999-03-09 |
NO980154L (no) | 1998-03-10 |
ES2176471T3 (es) | 2002-12-01 |
SK3898A3 (en) | 1998-11-04 |
AU702324B2 (en) | 1999-02-18 |
IL122923A0 (en) | 1998-08-16 |
NO980154D0 (no) | 1998-01-13 |
CZ3298A3 (cs) | 1998-06-17 |
DE69621026T2 (de) | 2002-08-22 |
EP0846118B1 (en) | 2002-05-02 |
MX9800411A (es) | 1998-04-30 |
JP4150818B2 (ja) | 2008-09-17 |
YU42296A (sh) | 1998-12-23 |
HRP960321B1 (en) | 2003-06-30 |
PL324527A1 (en) | 1998-06-08 |
EP0846118A1 (en) | 1998-06-10 |
DE69621026D1 (de) | 2002-06-06 |
AR003455A1 (es) | 1998-08-05 |
GB9514465D0 (en) | 1995-09-13 |
CA2226761A1 (en) | 1997-02-06 |
US5981527A (en) | 1999-11-09 |
WO1997003985A1 (en) | 1997-02-06 |
HRP960321A2 (en) | 1998-08-31 |
CN1069318C (zh) | 2001-08-08 |
ATE216997T1 (de) | 2002-05-15 |
CO4700455A1 (es) | 1998-12-29 |
CN1195349A (zh) | 1998-10-07 |
HUP9900006A3 (en) | 1999-11-29 |
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