BG99729A - Заместени 6-азаандростенони - Google Patents

Заместени 6-азаандростенони

Info

Publication number
BG99729A
BG99729A BG99729A BG9972995A BG99729A BG 99729 A BG99729 A BG 99729A BG 99729 A BG99729 A BG 99729A BG 9972995 A BG9972995 A BG 9972995A BG 99729 A BG99729 A BG 99729A
Authority
BG
Bulgaria
Prior art keywords
substituted
hydrogen
lower alkyl
bond
double
Prior art date
Application number
BG99729A
Other languages
English (en)
Inventor
Robert Andrews
Cynthia Cribbs
Stephen Frye
Curt Haffner
Patrick Maloney
Original Assignee
Glaxo Wellcome Inc.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Glaxo Wellcome Inc. filed Critical Glaxo Wellcome Inc.
Publication of BG99729A publication Critical patent/BG99729A/bg

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/50—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
    • C07D317/58—Radicals substituted by nitrogen atoms
    • 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
    • A61P37/08—Antiallergic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/33—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C211/39—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of an unsaturated carbon skeleton
    • C07C211/41—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of an unsaturated carbon skeleton containing condensed ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/43—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C211/44—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to only one six-membered aromatic ring
    • C07C211/45—Monoamines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no 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
    • C07D309/14—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D335/00—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
    • C07D335/02—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
    • C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • 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
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/18—Systems containing only non-condensed rings with a ring being at least seven-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/36—Systems containing two condensed rings the rings having more than two atoms in common
    • C07C2602/46—Systems containing two condensed rings the rings having more than two atoms in common the bicyclo ring system containing nine carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pulmonology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (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)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Изобретението се отнася до заместени 17 -субституирани-6-азаандрост-4-ен-3-они с формула в която R1 и R2 означават независимо един от друг водород или нисш алкил и връзката между въглеродите, носещи R1 и R2, е единична или двойна или R1 и R2 заедно са -СН2-група, образуваща циклопропанов пръстен, и връзката между въглеродите, носещи R1 и R2, е единична, R3 за предпочитане означава водород, халоген или нисш алкил, R4 за предпочитане е водород или нисш алкил, Х за предпочитане е СН2, Y за предпочитане означава водород и Z за предпочитане означава CONR14R15 и R14 и R15 представляват различни органични групи. Изобретението се отнася и до техни фармацевтично приемливи соли, до методи за получаването им, до приложението им в медицината и дофармацевтични препаративни форми.
BG99729A 1992-12-18 1995-06-19 Заместени 6-азаандростенони BG99729A (bg)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US99393092A 1992-12-18 1992-12-18
US8066593A 1993-06-18 1993-06-18
PCT/US1993/012419 WO1994014833A2 (en) 1992-12-18 1993-12-17 Substituted 6-azaandrostenones

Publications (1)

Publication Number Publication Date
BG99729A true BG99729A (bg) 1996-01-31

Family

ID=26763785

Family Applications (1)

Application Number Title Priority Date Filing Date
BG99729A BG99729A (bg) 1992-12-18 1995-06-19 Заместени 6-азаандростенони

Country Status (24)

Country Link
EP (1) EP0674651B1 (bg)
JP (1) JPH08504825A (bg)
CN (1) CN1095383A (bg)
AP (1) AP459A (bg)
AT (1) ATE172738T1 (bg)
AU (1) AU673899B2 (bg)
BG (1) BG99729A (bg)
CA (1) CA2152053A1 (bg)
CZ (1) CZ157695A3 (bg)
DE (1) DE69321849D1 (bg)
FI (1) FI953009A7 (bg)
HU (1) HUT72083A (bg)
IL (1) IL108073A0 (bg)
IS (1) IS4106A (bg)
LV (1) LV10958B (bg)
MX (1) MX9308015A (bg)
NO (1) NO952402L (bg)
NZ (1) NZ261415A (bg)
OA (1) OA10167A (bg)
PL (1) PL314532A1 (bg)
SI (1) SI9300665A (bg)
SK (1) SK79495A3 (bg)
TW (1) TW293824B (bg)
WO (1) WO1994014833A2 (bg)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
US5516779A (en) * 1994-06-08 1996-05-14 Merck & Co., Inc. 17β-substituted-6-azasteroid derivatives useful as 5α-reductase inhibitors
US5817818A (en) * 1994-09-16 1998-10-06 Glaxo Wellcome Inc. Androstenones
US5541322A (en) * 1994-10-14 1996-07-30 Glaxo Wellcome Inc. Synthesis of 6-azaandrostenones
US5543417A (en) * 1994-10-21 1996-08-06 Merck & Co., Inc. Combination method of treating acne using 4-AZA-5α-cholestan-ones and 4-AZA-5α-androstan-ones as selective 5α-reductase inhibitors with anti-bacterial, keratolytic, or anti-inflammatory agents
US5595996A (en) * 1994-10-25 1997-01-21 Merck & Co., Inc. 7-substituted 4-aza cholanic acid derivatives and their use
GB9506678D0 (en) * 1995-03-31 1995-05-24 Glaxo Inc Substituted 6-azacholesten-3-ones
WO1997014418A1 (en) * 1995-10-19 1997-04-24 Merck & Co., Inc. 16-substituted-6-aza-steroid 5-alpha-reductase inhibitors
US5935968A (en) * 1997-03-17 1999-08-10 Merck & Co., Inc. Methods for treating polycystic ovary syndrome
CN1805915A (zh) 2003-04-15 2006-07-19 茵弗莱采姆药物有限公司 作为药物活性剂的茚衍生物
US7790770B2 (en) * 2005-11-23 2010-09-07 Bristol-Myers Squibb Company Heterocyclic CETP inhibitors
US10100056B2 (en) 2013-03-14 2018-10-16 Aquinox Pharmaceuticals (Canada) Inc. SHIP1 modulators and methods related thereto
EP2970122B1 (en) 2013-03-14 2019-05-08 Aquinox Pharmaceuticals (Canada) Inc. Ship1 modulators
EP3313811A1 (en) 2015-06-26 2018-05-02 Aquinox Pharmaceuticals (Canada) Inc. Crystalline solid forms of the acetate salt of (1s,3s,4r)-4-((3as,4r,5s,7as)-4-(aminomethyl)-7a-methyl-1-methyleneoctahydro-1h-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexanol
WO2017127753A1 (en) 2016-01-20 2017-07-27 Aquinox Pharmaceuticals (Canada) Inc. Synthesis of a substituted indene derivative
BR112018072255B1 (pt) * 2016-04-29 2024-02-06 The Research Foundation For The State University Of New York Azasteroides para tratamento de tuberculose
EP4284804A1 (en) 2021-01-26 2023-12-06 Schrödinger, Inc. Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07502511A (ja) * 1991-12-20 1995-03-16 グラクソ、インコーポレーテッド ５‐α‐テストステロンレダクターゼ阻害剤
US5438061A (en) * 1993-07-16 1995-08-01 Merck & Co., Inc. 7-substituted-δ4-6-azasteroid derivatives as 5α-reductase inhibitors

Also Published As

Publication number Publication date
FI953009A0 (fi) 1995-06-16
AU673899B2 (en) 1996-11-28
LV10958A (lv) 1995-12-20
JPH08504825A (ja) 1996-05-28
EP0674651B1 (en) 1998-10-28
CA2152053A1 (en) 1994-07-07
AP459A (en) 1996-02-14
NZ261415A (en) 1997-03-24
AU6015094A (en) 1994-07-19
PL314532A1 (en) 1996-09-16
SK79495A3 (en) 1995-11-08
NO952402L (no) 1995-08-16
AP9300599A0 (en) 1994-01-31
WO1994014833A2 (en) 1994-07-07
HUT72083A (en) 1996-03-28
FI953009L (fi) 1995-08-15
CZ157695A3 (en) 1995-12-13
LV10958B (en) 1996-10-20
ATE172738T1 (de) 1998-11-15
NO952402D0 (no) 1995-06-16
OA10167A (en) 1996-12-18
DE69321849D1 (de) 1998-12-03
FI953009A7 (fi) 1995-08-15
WO1994014833A3 (en) 1994-09-29
IL108073A0 (en) 1994-04-12
HU9501775D0 (en) 1995-08-28
MX9308015A (es) 1994-08-31
IS4106A (is) 1994-06-19
TW293824B (bg) 1996-12-21
CN1095383A (zh) 1994-11-23
SI9300665A (en) 1994-06-30
EP0674651A1 (en) 1995-10-04

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