WO1994020062A3 - Balanoids as protein kinase c inhibitors - Google Patents

Balanoids as protein kinase c inhibitors Download PDF

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Publication number
WO1994020062A3
WO1994020062A3 PCT/US1994/002283 US9402283W WO9420062A3 WO 1994020062 A3 WO1994020062 A3 WO 1994020062A3 US 9402283 W US9402283 W US 9402283W WO 9420062 A3 WO9420062 A3 WO 9420062A3
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WO
WIPO (PCT)
Prior art keywords
balanoids
protein kinase
inhibitors
treatment
denominated
Prior art date
Application number
PCT/US1994/002283
Other languages
French (fr)
Other versions
WO1994020062A2 (en
Inventor
Steven Edward Hall
Lawrence M Ballas
Palaniappan Kulanthaivel
Christie Boros
Jack B Jiang
Gunnar Erik Jagdmann Jr
Yen-Shi Lai
Christopher K Biggers
Hong Hu
Yali Hallock
Philip F Hughes
Jean Marie Defauw
Michael Patrick Lynch
John William Crossley Lampe
David Steven Menaldino
Julia Marie Heerding
William P Janzen
Sean Patrick Hollinshead
Jeffrey Bailey Nichols
Original Assignee
Nichols Gina M & Lf
Sphinx Pharma Corp
Steven Edward Hall
Lawrence M Ballas
Palaniappan Kulanthaivel
Christie Boros
Jack B Jiang
Gunnar Erik Jagdmann Jr
Lai Yen Shi
Christopher K Biggers
Hong Hu
Yali Hallock
Philip F Hughes
Jean Marie Defauw
Michael Patrick Lynch
John William Crossley Lampe
David Steven Menaldino
Julia Marie Heerding
William P Janzen
Sean Patrick Hollinshead
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 Nichols Gina M & Lf, Sphinx Pharma Corp, Steven Edward Hall, Lawrence M Ballas, Palaniappan Kulanthaivel, Christie Boros, Jack B Jiang, Gunnar Erik Jagdmann Jr, Lai Yen Shi, Christopher K Biggers, Hong Hu, Yali Hallock, Philip F Hughes, Jean Marie Defauw, Michael Patrick Lynch, John William Crossley Lampe, David Steven Menaldino, Julia Marie Heerding, William P Janzen, Sean Patrick Hollinshead filed Critical Nichols Gina M & Lf
Priority to EP94909847A priority Critical patent/EP0687249A1/en
Priority to AU62527/94A priority patent/AU6252794A/en
Priority to JP6520148A priority patent/JPH09503994A/en
Publication of WO1994020062A2 publication Critical patent/WO1994020062A2/en
Publication of WO1994020062A3 publication Critical patent/WO1994020062A3/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/54—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/52—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of six-membered aromatic rings being part of condensed ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D207/14—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
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    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
    • C07D207/48—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
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    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings 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
    • C07D223/12—Nitrogen atoms not forming part of a nitro radical
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    • C07—ORGANIC CHEMISTRY
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    • C07D313/00—Heterocyclic compounds containing rings of more than six members having one oxygen atom as the only ring hetero atom
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D337/00—Heterocyclic compounds containing rings of more than six members having one sulfur atom as the only ring hetero atom
    • C07D337/02—Seven-membered rings
    • C07D337/04—Seven-membered rings not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572—Five-membered rings
    • 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
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    • C07C2601/18—Systems containing only non-condensed rings with a ring being at least seven-membered

Abstract

A novel class of therapeutic compounds, denominated Balanoids, is disclosed. Balanoids have protein kinase C inhibitory activity and selectivity among the isoforms of protein kinase C. Balanoids are useful for treatment of diseases related to protein kinase C in animals, especially humans and is especially indicated for treatment of inflammatory diseases.
PCT/US1994/002283 1993-03-03 1994-03-02 Balanoids as protein kinase c inhibitors WO1994020062A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP94909847A EP0687249A1 (en) 1993-03-03 1994-03-02 Balanoids
AU62527/94A AU6252794A (en) 1993-03-03 1994-03-02 Balanoids
JP6520148A JPH09503994A (en) 1993-03-03 1994-03-02 Balanoid

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US2584693A 1993-03-03 1993-03-03
US08/025,846 1993-03-03

Publications (2)

Publication Number Publication Date
WO1994020062A2 WO1994020062A2 (en) 1994-09-15
WO1994020062A3 true WO1994020062A3 (en) 1996-08-15

Family

ID=21828367

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1994/002283 WO1994020062A2 (en) 1993-03-03 1994-03-02 Balanoids as protein kinase c inhibitors

Country Status (7)

Country Link
EP (1) EP0687249A1 (en)
JP (1) JPH09503994A (en)
AU (1) AU6252794A (en)
CA (1) CA2157412A1 (en)
IL (1) IL108849A0 (en)
WO (1) WO1994020062A2 (en)
ZA (1) ZA941478B (en)

Families Citing this family (25)

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Publication number Priority date Publication date Assignee Title
AU686691B2 (en) * 1994-01-12 1998-02-12 F. Hoffmann-La Roche Ag Novel azepanes and homologs thereof
US5583221A (en) * 1994-05-04 1996-12-10 Eli Lilly And Company Substituted fused and bridged bicyclic compounds as therapeutic agents
TW339325B (en) * 1995-07-05 1998-09-01 Hoffmann La Roche Novel azepane derivatives, process for the preparation thereof and pharmaceutical composition containing the same
US6914140B1 (en) 1996-04-17 2005-07-05 Hoffmann-La Roche Inc. Asymmetric synthesis process
EP0802190A1 (en) * 1996-04-17 1997-10-22 F. Hoffmann-La Roche Ag Process and intermediates for preparing azepines
US5902882A (en) * 1996-04-17 1999-05-11 Hoffmann-La Roche Inc. Assymetric synthesis of azepines
WO2000012074A2 (en) 1998-08-28 2000-03-09 Scios Inc. Use of piperidines and/or piperazines as inhibitors of p38-alpha kinase
DZ3083A1 (en) * 1999-02-19 2004-06-02 Smithkline Beecham Corp New protease inhibitor compounds, process for their preparation and pharmaceutical compositions containing them
AR018698A1 (en) 1999-06-01 2001-11-28 Procter & Gamble METHOD FOR THE TREATMENT OF LOSS OF HAIR WHICH IS INCLUDED TO MANAGE A COMPOSITION THAT INCLUDES A COMPOUND WHICH DOES NOT AFFECT THE HEART
MXPA01012494A (en) 1999-06-01 2002-07-02 Univ Texas Southwestern Med Ct Method of treating hair loss using sulfonyl thyromimetic compounds.
US6680344B1 (en) 1999-06-01 2004-01-20 The University Of Texas Southwestern Medical Center Method of treating hair loss using diphenylmethane derivatives
US6541477B2 (en) 1999-08-27 2003-04-01 Scios, Inc. Inhibitors of p38-a kinase
CA2384240A1 (en) 1999-10-15 2001-04-26 Dean A. Wacker Benzylcycloalkyl amines as modulators of chemokine receptor activity
TWI290136B (en) 2000-04-05 2007-11-21 Daiichi Seiyaku Co Ethylenediamine derivatives
US6706712B2 (en) 2000-12-20 2004-03-16 Bristol-Myers Squibb Pharma Company Cyclic derivatives as modulators of chemokine receptor activity
GEP20063741B (en) 2001-02-23 2006-02-10 Merck & Co Inc Nonaryl-Heterocyclic NMDA/NR2B Antagonists
WO2002080928A1 (en) 2001-04-03 2002-10-17 Merck & Co., Inc. N-substituted nonaryl-heterocyclo amidyl nmda/nr2b antagonists
WO2003000657A1 (en) 2001-06-20 2003-01-03 Daiichi Pharmaceutical Co., Ltd. Diamine derivatives
JP4128138B2 (en) * 2001-06-20 2008-07-30 第一三共株式会社 Diamine derivatives
MXPA04001272A (en) * 2001-08-09 2004-05-27 Daiichi Seiyaku Co Diamine derivatives.
CA2459364A1 (en) 2001-09-13 2003-03-20 F. Hoffmann-La Roche Ag Ccr-3 receptor antagonists v
EP1483241A4 (en) 2002-03-08 2006-12-13 Bristol Myers Squibb Co Cyclic derivatives as modulators of chemokine receptor activity
US6887864B2 (en) * 2002-03-12 2005-05-03 Hoffmann-La Roche Inc. Azepane derivatives
US20170144965A1 (en) * 2014-06-05 2017-05-25 The University Of Kansas Marmelin analogs and methods of use in cancer treatment
CN111801322B (en) 2017-10-31 2024-03-15 迈阿密大学 Kinase inhibitors for the treatment of central and peripheral nervous system disorders

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993003730A1 (en) * 1991-08-22 1993-03-04 Sphinx Pharmaceuticals Corporation Protein kinase c inhibition and novel compound balanol

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993003730A1 (en) * 1991-08-22 1993-03-04 Sphinx Pharmaceuticals Corporation Protein kinase c inhibition and novel compound balanol

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
CHEMICAL ABSTRACTS, vol. 119, no. 17, 25 October 1993, Columbus, Ohio, US; abstract no. 177243h, page 423; column L; *
KULANTHAIVEL, PALANAPPAN ET. AL., JOURNAL OF AMERICAN CHEMICAL SOCIETY, vol. 115, no. 14, 1993, WASHINGTON, pages 6452 - 6453 *

Also Published As

Publication number Publication date
ZA941478B (en) 1995-09-05
IL108849A0 (en) 1994-06-24
JPH09503994A (en) 1997-04-22
EP0687249A1 (en) 1995-12-20
WO1994020062A2 (en) 1994-09-15
AU6252794A (en) 1994-09-26
CA2157412A1 (en) 1994-09-15

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