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MX9202466A - NOVELTY IMMUNOSUPPRESSIVE COMPOUNDS. - Google Patents

NOVELTY IMMUNOSUPPRESSIVE COMPOUNDS.

Info

Publication number
MX9202466A
MX9202466A MX9202466A MX9202466A MX9202466A MX 9202466 A MX9202466 A MX 9202466A MX 9202466 A MX9202466 A MX 9202466A MX 9202466 A MX9202466 A MX 9202466A MX 9202466 A MX9202466 A MX 9202466A
Authority
MX
Mexico
Prior art keywords
compounds
immunosuppressive
immunosuppressive compounds
rotamase
novelty
Prior art date
Application number
MX9202466A
Other languages
Spanish (es)
Inventor
John P Duffy
Original Assignee
Vertex Pharma
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 Vertex Pharma filed Critical Vertex Pharma
Publication of MX9202466A publication Critical patent/MX9202466A/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/96—Sulfur atom
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D207/46—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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Transplantation (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)

Abstract

La presente invención se refiere a una clase novedosa de compuestos inmunosupresores que tiene una afinidad para la proteína de aglutinación FK-506 (PAKF). Una vez enlazados con esta proteína, los compuestos inmunosupresores inhiben la actividad de la isomerasa cistrans del prolilpeptidilo (rotamasa) de la PAFK, e inhiben la activación de la célula T. Como tales, los compuestos de la presente invención se pueden utilizar como fármacos inmunosupresores para prevenir o reducir significativamente el rechazo de injerto en los trasplantes de médula ósea y de órganos, y para utilizarse en el tratamiento de una amplia variedad de enfermedades autoinmunes en seres humanos y en otros mamíferos.The present invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 agglutination protein (PAKF). Once bound with this protein, the immunosuppressive compounds inhibit the activity of the prolylpeptidyl (rotamase) cistrans isomerase (rotamase) of PAFK, and inhibit T-cell activation. As such, the compounds of the present invention can be used as immunosuppressive drugs. to prevent or significantly reduce graft rejection in bone marrow and organ transplants, and to be used in the treatment of a wide variety of autoimmune diseases in humans and other mammals.

MX9202466A 1991-05-24 1992-05-25 NOVELTY IMMUNOSUPPRESSIVE COMPOUNDS. MX9202466A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US70537191A 1991-05-24 1991-05-24

Publications (1)

Publication Number Publication Date
MX9202466A true MX9202466A (en) 1994-06-30

Family

ID=24833176

Family Applications (1)

Application Number Title Priority Date Filing Date
MX9202466A MX9202466A (en) 1991-05-24 1992-05-25 NOVELTY IMMUNOSUPPRESSIVE COMPOUNDS.

Country Status (6)

Country Link
EP (1) EP0587756A1 (en)
JP (1) JP3163104B2 (en)
AU (1) AU2185092A (en)
CA (1) CA2102178A1 (en)
MX (1) MX9202466A (en)
WO (1) WO1992021313A2 (en)

Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5798355A (en) * 1995-06-07 1998-08-25 Gpi Nil Holdings, Inc. Inhibitors of rotamase enzyme activity
US5846981A (en) * 1993-05-28 1998-12-08 Gpi Nil Holdings Inc. Inhibitors of rotamase enzyme activity
US5859031A (en) 1995-06-07 1999-01-12 Gpi Nil Holdings, Inc. Small molecule inhibitors of rotamase enzyme activity
US5696135A (en) * 1995-06-07 1997-12-09 Gpi Nil Holdings, Inc. Inhibitors of rotamase enzyme activity effective at stimulating neuronal growth
GB2324527B (en) * 1995-06-07 1999-12-22 Guilford Pharm Inc Small molecule inhibitors of rotamase enzyme activity
US5707985A (en) * 1995-06-07 1998-01-13 Tanabe Seiyaku Co. Ltd. Naphthyl-, quinolyl- and isoquinolyl- sulfonamide derivatives as cell adhesion modulators
US5801197A (en) * 1995-10-31 1998-09-01 Gpi Nil Holdings, Inc. Rotamase enzyme activity inhibitors
FR2750087B1 (en) * 1996-06-19 1998-09-04 Faure Bertrand Equipements Sa VEHICLE SEAT ELEMENT HAVING A TENSIONED HEADPHONES ON A METAL FRAME
US6218424B1 (en) 1996-09-25 2001-04-17 Gpi Nil Holdings, Inc. Heterocyclic ketone and thioester compounds and uses
US5786378A (en) * 1996-09-25 1998-07-28 Gpi Nil Holdings, Inc. Heterocyclic thioesters
US5801187A (en) 1996-09-25 1998-09-01 Gpi-Nil Holdings, Inc. Heterocyclic esters and amides
US5935989A (en) * 1996-12-31 1999-08-10 Gpi Nil Holdings Inc. N-linked ureas and carbamates of heterocyclic thioesters
SK57899A3 (en) 1996-12-31 2000-05-16 Guilford Pharm Inc N-linked ureas and carbamates of heterocyclic thioesters
US5721256A (en) * 1997-02-12 1998-02-24 Gpi Nil Holdings, Inc. Method of using neurotrophic sulfonamide compounds
US5846979A (en) 1997-02-28 1998-12-08 Gpi Nil Holdings, Inc. N-oxides of heterocyclic esters, amides, thioesters, and ketones
US6271244B1 (en) 1998-06-03 2001-08-07 Gpi Nil Holdings, Inc. N-linked urea or carbamate of heterocyclic thioester hair growth compositions and uses
US6274602B1 (en) 1998-06-03 2001-08-14 Gpi Nil Holdings, Inc. Heterocyclic thioester and ketone hair growth compositions and uses
US6187784B1 (en) 1998-06-03 2001-02-13 Gpi Nil Holdings, Inc. Pipecolic acid derivative hair growth compositions and uses
US5945441A (en) * 1997-06-04 1999-08-31 Gpi Nil Holdings, Inc. Pyrrolidine carboxylate hair revitalizing agents
US6187796B1 (en) 1998-06-03 2001-02-13 Gpi Nil Holdings, Inc. Sulfone hair growth compositions and uses
US6852496B1 (en) 1997-08-12 2005-02-08 Oregon Health And Science University Methods of screening for agents that promote nerve cell growth
US6268384B1 (en) * 1997-08-29 2001-07-31 Vertex Pharmaceuticals Incorporated Compounds possessing neuronal activity
BR9811923A (en) * 1997-08-29 2000-08-15 Vertex Pharma Compounds having neuronal activity
DE19742263A1 (en) * 1997-09-25 1999-04-01 Asta Medica Ag New specific immunophilin ligands as anti-asthmatic, anti-allergic, anti-rheumatic, immunosuppressive, anti-psoriatic, neuroprotective
US5968921A (en) 1997-10-24 1999-10-19 Orgegon Health Sciences University Compositions and methods for promoting nerve regeneration
GB9804426D0 (en) * 1998-03-02 1998-04-29 Pfizer Ltd Heterocycles
JP2002516857A (en) * 1998-06-02 2002-06-11 ブリストルーマイヤーズ スクイブ カンパニー Neurotrophic difluoroamide
US6172087B1 (en) 1998-06-03 2001-01-09 Gpi Nil Holding, Inc. N-oxide of heterocyclic ester, amide, thioester, or ketone hair growth compositions and uses
JP2002516904A (en) 1998-06-03 2002-06-11 ジーピーアイ ニル ホールディングス インコーポレイテッド N-linked sulfonamides of N-heterocyclic carboxylic acids or carboxylic acid isosteres
JP2002516843A (en) 1998-06-03 2002-06-11 ジー・ピー・アイ ニイル ホールディングス インコーポレィティッド Heterocyclic ester and amide hair growth compositions and uses thereof
GB9815880D0 (en) 1998-07-21 1998-09-16 Pfizer Ltd Heterocycles
US6376517B1 (en) * 1998-08-14 2002-04-23 Gpi Nil Holdings, Inc. Pipecolic acid derivatives for vision and memory disorders
US6399648B1 (en) 1998-08-14 2002-06-04 Gpi Nil Holdings, Inc. N-oxides of heterocyclic ester, amide, thioester, or ketone for vision and memory disorders
US7265150B1 (en) * 1998-08-14 2007-09-04 Gpi Nil Holdings Inc. Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds for vision and memory disorders
US6333340B1 (en) * 1998-08-14 2001-12-25 Gpi Nil Holdings, Inc. Small molecule sulfonamides for vision and memory disorders
US6218423B1 (en) 1998-08-14 2001-04-17 Gpi Nil Holdings, Inc. Pyrrolidine derivatives for vision and memory disorders
US6395758B1 (en) 1998-08-14 2002-05-28 Gpi Nil Holdings, Inc. Small molecule carbamates or ureas for vision and memory disorders
US6337340B1 (en) 1998-08-14 2002-01-08 Gpi Nil Holdings, Inc. Carboxylic acids and isosteres of heterocyclic ring compounds having multiple heteroatoms for vision and memory disorders
US6384056B1 (en) 1998-08-14 2002-05-07 Gpi Nil Holdings, Inc. Heterocyclic thioesters or ketones for vision and memory disorders
US6335348B1 (en) 1998-08-14 2002-01-01 Gpi Nil Holdings, Inc. Nitrogen-containing linear and azepinyl/ compositions and uses for vision and memory disorders
US7338976B1 (en) * 1998-08-14 2008-03-04 Gpi Nil Holdings, Inc. Heterocyclic esters or amides for vision and memory disorders
US6506788B1 (en) 1998-08-14 2003-01-14 Gpi Nil Holdings, Inc. N-linked urea or carbamate of heterocyclic thioesters for vision and memory disorders
US6339101B1 (en) 1998-08-14 2002-01-15 Gpi Nil Holdings, Inc. N-linked sulfonamides of N-heterocyclic carboxylic acids or isosteres for vision and memory disorders
US6462072B1 (en) 1998-09-21 2002-10-08 Gpi Nil Holdings, Inc. Cyclic ester or amide derivatives
US6300341B1 (en) 1998-09-30 2001-10-09 The Procter & Gamble Co. 2-substituted heterocyclic sulfonamides
US6307049B1 (en) 1998-09-30 2001-10-23 The Procter & Gamble Co. Heterocyclic 2-substituted ketoamides
US6228872B1 (en) 1998-11-12 2001-05-08 Bristol-Myers Squibb Company Neurotrophic diamide and carbamate agents
US6734211B1 (en) 1999-07-09 2004-05-11 Oregon Health & Sciences University Compositions and methods for promoting nerve regeneration
AU6388500A (en) * 1999-08-05 2001-03-05 Procter & Gamble Company, The Multivalent sulfonamides
WO2001010838A1 (en) * 1999-08-05 2001-02-15 The Procter & Gamble Company Multivalent compounds
US6417189B1 (en) 1999-11-12 2002-07-09 Gpi Nil Holdings, Inc. AZA compounds, pharmaceutical compositions and methods of use
US7253169B2 (en) 1999-11-12 2007-08-07 Gliamed, Inc. Aza compounds, pharmaceutical compositions and methods of use
JP2003518122A (en) 1999-12-21 2003-06-03 ジーピーアイ エヌアイエル ホールディングズ インコーポレーテッド Hydantoin derivative compounds, pharmaceutical synthetic products and methods of using them
US20110104186A1 (en) 2004-06-24 2011-05-05 Nicholas Valiante Small molecule immunopotentiators and assays for their detection
CN110054665B (en) * 2019-04-29 2022-08-26 湖南新汇制药股份有限公司 Application of cyclic pentapeptide compound in preparation of immunosuppressant drug

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2431734A1 (en) * 1974-07-02 1976-01-29 Basf Ag Beta-keto propane sultones and sultams - useful as immunosuppressants, esp. for inhibiting transplant rejection
JPS6137764A (en) * 1984-07-31 1986-02-22 Suntory Ltd Novel physiologically active compound having anti-prolyl-endopeptidase activity
JP2691442B2 (en) * 1989-02-20 1997-12-17 株式会社ヤクルト本社 Novel proline derivative
US5192773A (en) * 1990-07-02 1993-03-09 Vertex Pharmaceuticals, Inc. Immunosuppressive compounds

Also Published As

Publication number Publication date
JP3163104B2 (en) 2001-05-08
WO1992021313A3 (en) 1993-01-07
WO1992021313A2 (en) 1992-12-10
JPH06508141A (en) 1994-09-14
CA2102178A1 (en) 1992-11-25
EP0587756A1 (en) 1994-03-23
AU2185092A (en) 1993-01-08

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