EA199800329A1 - Ингибиторы ротамазной ферментативной активности - Google Patents

Ингибиторы ротамазной ферментативной активности

Info

Publication number
EA199800329A1
EA199800329A1 EA199800329A EA199800329A EA199800329A1 EA 199800329 A1 EA199800329 A1 EA 199800329A1 EA 199800329 A EA199800329 A EA 199800329A EA 199800329 A EA199800329 A EA 199800329A EA 199800329 A1 EA199800329 A1 EA 199800329A1
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibitors
activity
rotamic
enzymative
rotamase
Prior art date
Application number
EA199800329A
Other languages
English (en)
Other versions
EA001481B1 (ru
Inventor
Джозеф П. Стайнер
Грегори С. Хэмилтон
Original Assignee
Гилфорд Фармасьютикалз Инк.
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
Priority claimed from US08/551,026 external-priority patent/US20020013344A1/en
Application filed by Гилфорд Фармасьютикалз Инк. filed Critical Гилфорд Фармасьютикалз Инк.
Publication of EA199800329A1 publication Critical patent/EA199800329A1/ru
Publication of EA001481B1 publication Critical patent/EA001481B1/ru

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Abstract

Изобретение относится к способу использования специально полученных нейротрофических соединений, производных пипеколиновой кислоты, обладающих сродством к иммунофилинам FKBP-типа, в качестве ингибиторов ферментативной активности, ассоциированной с иммунофилиновыми белками, и в частности ингибиторов пептидилпролилизомеразной или ротамазной ферментативной активности, чтобы стимулировать или активировать нейронный рост или регенерацию.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA199800329A 1995-10-31 1996-08-26 Ингибиторы ротамазной ферментативной активности EA001481B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US08/551,026 US20020013344A1 (en) 1995-10-31 1995-10-31 Rotamas enzyme activity inhibitors
US08/645,149 US5801197A (en) 1995-10-31 1996-05-13 Rotamase enzyme activity inhibitors
PCT/US1996/013624 WO1997016190A1 (en) 1995-10-31 1996-08-26 Rotamase enzyme activity inhibitors

Publications (2)

Publication Number Publication Date
EA199800329A1 true EA199800329A1 (ru) 1998-12-24
EA001481B1 EA001481B1 (ru) 2001-04-23

Family

ID=27069634

Family Applications (1)

Application Number Title Priority Date Filing Date
EA199800329A EA001481B1 (ru) 1995-10-31 1996-08-26 Ингибиторы ротамазной ферментативной активности

Country Status (17)

Country Link
US (1) US5801197A (ru)
EP (1) EP0859614A4 (ru)
JP (1) JPH11514643A (ru)
KR (1) KR19990067257A (ru)
BG (1) BG62596B1 (ru)
BR (1) BRPI9611271A2 (ru)
CA (1) CA2236328A1 (ru)
CZ (1) CZ125198A3 (ru)
EA (1) EA001481B1 (ru)
EE (1) EE9800125A (ru)
HU (1) HUP9901752A3 (ru)
LV (1) LV12102B (ru)
NO (1) NO981903L (ru)
NZ (1) NZ316361A (ru)
PL (1) PL326420A1 (ru)
SK (1) SK55998A3 (ru)
WO (1) WO1997016190A1 (ru)

Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5898029A (en) * 1994-04-12 1999-04-27 The John Hopkins University Direct influences on nerve growth of agents that interact with immunophilins in combination with neurotrophic factors
US5859031A (en) 1995-06-07 1999-01-12 Gpi Nil Holdings, Inc. Small molecule inhibitors of rotamase enzyme activity
AT500192B1 (de) * 1995-06-07 2008-05-15 Guilford Pharm Inc Neurotrophe verbindung, diese enthaltende pharmazeutische masse, verwendung der verbindung und verfahren zu ihrer herstellung
US6291510B1 (en) 1995-06-07 2001-09-18 Gpi Nil Holdings, Inc. Small molecule inhibitors of rotamase enzyme activity
US7056935B2 (en) * 1995-06-07 2006-06-06 Gpi Nil Holdings, Inc. Rotamase enzyme activity inhibitors
US6509477B1 (en) 1998-11-12 2003-01-21 Guilford Pharmaceuticals Inc. Small molecule inhibitors of rotamase enzyme activity
AT500193B1 (de) * 1995-06-07 2007-11-15 Guilford Pharm Inc Neurotrophe verbindung und verfahren zu ihrer herstellung
US6037370A (en) 1995-06-08 2000-03-14 Vertex Pharmaceuticals Incorporated Methods and compositions for stimulating neurite growth
US5801187A (en) 1996-09-25 1998-09-01 Gpi-Nil Holdings, Inc. Heterocyclic esters and amides
US5786378A (en) * 1996-09-25 1998-07-28 Gpi Nil Holdings, Inc. Heterocyclic thioesters
US5780484A (en) * 1996-11-13 1998-07-14 Vertex Pharmaceuticals Incorporated Methods for stimulating neurite growth with piperidine compounds
US5811434A (en) * 1996-11-13 1998-09-22 Vertex Pharmacueticals Incorporated Methods and compositions for stimulating neurite growth
US5840736A (en) * 1996-11-13 1998-11-24 Vertex Pharmaceuticals Incorporated Methods and compositions for stimulating neurite growth
US5958949A (en) * 1996-12-31 1999-09-28 Gpi Nil Holdings Inc. N-linked ureas and carbamates of piperidyl thioesters
US5935989A (en) 1996-12-31 1999-08-10 Gpi Nil Holdings 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
US20010049381A1 (en) * 1997-06-04 2001-12-06 Gpl Nil Holdings, Inc., Pyrrolidine derivative hair growth compositions and uses
US5945441A (en) * 1997-06-04 1999-08-31 Gpi Nil Holdings, Inc. Pyrrolidine carboxylate hair revitalizing agents
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
US6121280A (en) * 1998-03-24 2000-09-19 Pfizer Inc. Azabicyclic rotomase inhibitors
EP1087763A4 (en) 1998-06-02 2002-10-31 Bristol Myers Squibb Co NEUROTROPHIC DIFLUOROAMID
BR9815882A (pt) 1998-06-03 2002-09-17 Gpi Nil Holding Inc Sulfonamidas ligadas por n de ácido carboxìlicos n-heterocìclicos ouou de isósteros de ácidos carboxìlicos
AU770459B2 (en) * 1998-06-03 2004-02-19 Gpi Nil Holdings, Inc. Heterocyclic ester and amide hair growth compositions and uses
US6331537B1 (en) 1998-06-03 2001-12-18 Gpi Nil Holdings, Inc. Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds
PL345598A1 (en) 1998-07-17 2001-12-17 Agouron Pharma Compounds, compositions, and methods for stimulating neuronal growth and elongation
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
US7338976B1 (en) * 1998-08-14 2008-03-04 Gpi Nil Holdings, Inc. Heterocyclic esters or amides 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
JP4503180B2 (ja) * 1998-08-14 2010-07-14 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 視覚および記憶障害のための組成物および使用法
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
US6462072B1 (en) 1998-09-21 2002-10-08 Gpi Nil Holdings, Inc. Cyclic ester or amide derivatives
US6307049B1 (en) 1998-09-30 2001-10-23 The Procter & Gamble Co. Heterocyclic 2-substituted ketoamides
US6300341B1 (en) 1998-09-30 2001-10-09 The Procter & Gamble Co. 2-substituted heterocyclic sulfonamides
US6228872B1 (en) 1998-11-12 2001-05-08 Bristol-Myers Squibb Company Neurotrophic diamide and carbamate agents
US6284779B1 (en) 1999-02-03 2001-09-04 Schering Aktiiengesellschaft Heteroaromatic compounds
WO2000046181A1 (en) * 1999-02-03 2000-08-10 Schering Aktiengesellschaft Carboxylic acid derivatives, process for their preparation and their use as rotamase enzyme activity inhibitors
EP1196400A1 (en) * 1999-07-06 2002-04-17 Vertex Pharmaceuticals Incorporated Amino-alkyl derivatives
JP2003503482A (ja) * 1999-07-06 2003-01-28 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 環化アミノ酸誘導体
JP2003503479A (ja) 1999-07-06 2003-01-28 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 N置換化グリシン誘導体
WO2001004091A1 (en) 1999-07-09 2001-01-18 Ortho-Mcneil Pharmaceutical, Inc. Neurotrophic 2-azetidinecarboxylic acid derivatives, and related compositions and methods
HUP0202249A3 (en) 1999-07-09 2003-01-28 Ortho Mcneil Pharm Inc Neurotrophic pyrrolidines and piperidines, compositions containing them and use of the compounds
WO2001004090A2 (en) 1999-07-09 2001-01-18 Ortho-Mcneil Pharmaceutical, Inc. Neurotrophic tetrahydroisoquinolines and tetrahydrothienopyridines, and related compositions and methods
EP1214293A1 (en) 1999-09-08 2002-06-19 Guilford Pharmaceuticals Inc. Non-peptidic cyclophilin binding compounds and their use
US7253169B2 (en) 1999-11-12 2007-08-07 Gliamed, Inc. Aza compounds, pharmaceutical compositions and methods of use
US6417189B1 (en) 1999-11-12 2002-07-09 Gpi Nil Holdings, Inc. AZA compounds, pharmaceutical compositions and methods of use
GT200000203A (es) * 1999-12-01 2002-05-24 Compuestos, composiciones y metodos para estimular el crecimiento y elongacion de neuronas.
US6818643B1 (en) 1999-12-08 2004-11-16 Bristol-Myers Squibb Company Neurotrophic bicyclic diamides
AU1464101A (en) 1999-12-21 2001-07-03 Gpi Nil Holdings, Inc. Hydantoin derivative compounds, pharmaceutical compositions, and methods of using same
EP1356108A2 (en) * 2000-11-28 2003-10-29 Wyeth Expression analysis of fkbp nucleic acids and polypeptides useful in the diagnosis and treatment of prostate cancer
JP2004532187A (ja) 2001-01-25 2004-10-21 ギルフォード ファーマシュウティカルズ インコーポレイテッド 三置換カルボサイクリックサイクロフィリン結合化合物とその用途
US6593362B2 (en) 2001-05-21 2003-07-15 Guilford Pharmaceuticals Inc. Non-peptidic cyclophilin binding compounds and their use
ATE361072T1 (de) * 2002-10-15 2007-05-15 Astellas Pharma Inc N-acetyl-l-pipecolic säure als promoter der produktion des neurotrophischen faktors
PT1778637E (pt) * 2004-06-29 2012-05-25 Aventis Pharma Inc Composição de ligação a fkbp e sua utilização farmacêutica
US20060189551A1 (en) * 2004-10-04 2006-08-24 Duke University Combination therapies for fungal pathogens
DE102008060549A1 (de) 2008-12-04 2010-06-10 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Wirkstoff-Peptid-Konstrukt zur extrazellulären Anreicherung
US20100317711A1 (en) * 2008-12-17 2010-12-16 Gliamed, Inc. Stem-like cells and method for reprogramming adult mammalian somatic cells
EP2705856A1 (en) 2012-09-07 2014-03-12 Deutsches Zentrum für Neurodegenerative Erkrankungen e.V. Compounds for the treatment of neurodegenerative disorders

Family Cites Families (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL58849A (en) * 1978-12-11 1983-03-31 Merck & Co Inc Carboxyalkyl dipeptides and derivatives thereof,their preparation and pharmaceutical compositions containing them
US4390695A (en) * 1980-06-23 1983-06-28 E. R. Squibb & Sons, Inc. Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids
US4310461A (en) * 1980-06-23 1982-01-12 E. R. Squibb & Sons, Inc. Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids
US4578474A (en) * 1980-06-23 1986-03-25 E. R. Squibb & Sons, Inc. Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids
US4950649A (en) * 1980-09-12 1990-08-21 University Of Illinois Didemnins and nordidemnins
EP0048159A3 (en) * 1980-09-17 1982-05-12 University Of Miami Novel carboxyalkyl peptides and thioethers and ethers of peptides as antihypertensive agents
DE3174844D1 (en) * 1980-10-23 1986-07-24 Schering Corp Carboxyalkyl dipeptides, processes for their production and pharmaceutical compositions containing them
ZA817261B (en) * 1980-10-23 1982-09-29 Schering Corp Carboxyalkyl dipeptides,processes for their production and pharmaceutical compositions containing them
ZA826022B (en) * 1981-08-21 1983-08-31 Univ Miami Novel complex amido and imido derivatives of carboxyalkyl peptides and thioethers and ethers of peptides
US4535167A (en) * 1981-12-14 1985-08-13 Merck & Co. Inc. Chiral, N-protected, N-substituted α-amino acids
EP0088350B1 (en) * 1982-03-08 1985-02-20 Schering Corporation Carboxyalkyl dipeptides, processes for their production and pharmaceutical compositions containing them
US4531964A (en) * 1982-09-13 1985-07-30 Nippon Kayaku Kabushiki Kaisha Heterocyclic compound and a herbicidal composition containing said compound
US4574079A (en) * 1983-05-27 1986-03-04 Gavras Haralambos P Radiolabeled angiotensin converting enzyme inhibitors for radiolabeling mammalian organ sites
US4593102A (en) * 1984-04-10 1986-06-03 A. H. Robins Company, Inc. N-[(amino)alkyl]-1-pyrrolidine, 1-piperidine and 1-homopiperidinecarboxamides (and thiocarboxamides) with sulfur linked substitution in the 2, 3 or 4-position
DE3508251A1 (de) * 1985-03-08 1986-09-11 Merck Patent Gmbh, 6100 Darmstadt Dipeptide
CN86101850A (zh) * 1985-03-22 1987-02-04 森得克斯(美国)有限公司 N,n′-二烷基胍基二肽的制造方法与用途
ES2037723T3 (es) * 1986-09-10 1993-07-01 Syntex (U.S.A.) Inc. Amidinacion selectiva de diaminas.
IT1206078B (it) * 1987-06-03 1989-04-14 Polifarma Spa Procedimento per la produzione di acido 3-indolpiruvico e suoi derivati loro uso farmaceutico
US5187156A (en) * 1988-03-16 1993-02-16 Fujisawa Pharmaceutical Co., Ltd. Peptide compounds, processes for preparation thereof and pharmaceutical composition comprising the same
US5156797A (en) * 1988-06-30 1992-10-20 Idemitsu Kosan Co., Ltd. Nonwoven fabrics
IL90872A0 (en) * 1988-07-08 1990-02-09 Smithkline Beckman Corp Retroviral protease binding peptides
DE3931051A1 (de) * 1988-09-22 1990-03-29 Hoechst Ag Salze von herbizid-saeuren mit langkettigen stickstoffbasen
EP0378318A1 (en) * 1989-01-11 1990-07-18 Merck & Co. Inc. Process for synthesis of FK-506 and tricarbonyl intermediates
WO1990012805A1 (en) * 1989-04-15 1990-11-01 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Postostatin and related compound thereof, or their salts
US5359138A (en) * 1989-04-15 1994-10-25 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Poststatin and related compounds or salts thereof
US5164525A (en) * 1989-06-30 1992-11-17 Merck & Co., Inc. Synthetic process for fk-506 type macrolide intermediates
NZ234883A (en) * 1989-08-22 1995-01-27 Merck Frosst Canada Inc Quinolin-2-ylmethoxy indole derivatives, preparation and pharmaceutical compositions thereof
GB8922026D0 (en) * 1989-09-29 1989-11-15 Pharma Mar Sa Novel anti-viral and cytotoxic agent
US5115098A (en) * 1990-02-28 1992-05-19 President And Fellows Of Harvard College End-blocked peptides inhibiting binding capacity of gp120
JPH04211648A (ja) * 1990-07-27 1992-08-03 Nippon Kayaku Co Ltd ケト酸アミド誘導体
DE4015255A1 (de) * 1990-05-12 1991-11-14 Hoechst Ag Oxalyl-aminosaeurederivate, verfahren zu ihrer herstellung und ihrer verwendung als arzneimittel zur inhibierung der prolyl-hydroxylase
US5192773A (en) * 1990-07-02 1993-03-09 Vertex Pharmaceuticals, Inc. Immunosuppressive compounds
JPH06500561A (ja) * 1990-08-24 1994-01-20 ジ・アップジョン・カンパニー 遷移状態模擬体としてのアミノポリオール含有ペプチド
WO1992004370A1 (en) * 1990-08-29 1992-03-19 Vertex Pharmaceuticals Incorporated Modified di- and tripeptidyl immunosuppressive compounds
GB2247456A (en) * 1990-09-03 1992-03-04 Fujisawa Pharmaceutical Co Tetrahydropyrane compounds, a process for their production and a pharmaceutical composition containing the same
JPH04149166A (ja) * 1990-10-12 1992-05-22 Nippon Kayaku Co Ltd 新規ケト酸アミド誘導体
AU1677092A (en) * 1991-03-20 1992-10-21 Vertex Pharmaceuticals Incorporated Tetrahydroxyalkane derivatives as inhibitors of hiv aspartyl protease
IT1245712B (it) * 1991-04-09 1994-10-14 Boehringer Mannheim Italia Ammine eterocicliche utili terapia dell'asma e dell'infiammazione delle vie aeree
US5147877A (en) * 1991-04-18 1992-09-15 Merck & Co. Inc. Semi-synthetic immunosuppressive macrolides
EP0584217A1 (en) * 1991-05-08 1994-03-02 Vertex Pharmaceuticals Incorporated Rfkbp: a novel prolyl isomerase and rapamycin/fk506 binding protein
AU1995792A (en) * 1991-05-09 1992-12-21 Vertex Pharmaceuticals Incorporated Novel immunosuppressive compounds
MX9202466A (es) * 1991-05-24 1994-06-30 Vertex Pharma Compuestos inmunosupresores novedosos.
JPH05178824A (ja) * 1991-08-05 1993-07-20 Takeda Chem Ind Ltd アスパラギン誘導体およびその用途
AU2803692A (en) * 1991-10-11 1993-05-03 Vertex Pharmaceuticals Incorporated Isolation of an mr 52,000 fk506 binding protein and molecular cloning of a corresponding human cdna
ZA927782B (en) * 1991-10-11 1993-04-28 Ciba Geigy Novel herbicides.
WO1993013066A1 (en) * 1991-12-20 1993-07-08 Syntex (U.S.A.) Inc. Cyclic amides of 3-amino-2-hydroxy-carboxylic acids as hiv-protease inhibitors
AU4388893A (en) * 1992-05-20 1993-12-13 Vertex Pharmaceuticals Incorporated Method of detecting tissue-specific FK506 binding protein messenger RNAs and uses thereof
IT1254373B (it) * 1992-05-29 1995-09-14 Eteroprostanoidi, procedimento per la loro preparazione e loro impiegoterapeutico.
US5334719A (en) * 1992-06-17 1994-08-02 Merck Frosst Canada, Inc. Bicyclic(azaaromatic)indoles as inhibitors of leukotriene bisynthesis
IS2334B (is) * 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
NZ314207A (en) * 1992-09-28 2000-12-22 Vertex Pharma 1-(2-Oxoacetyl)-piperidine-2-carboxylic acid derivatives as multi drug resistant cancer cell sensitizers
WO1994013629A1 (en) * 1992-12-11 1994-06-23 Vertex Pharmaceuticals Incorporated Mannitol derivatives and their use as inhibitors of aspartyl protease
DE4302860A1 (de) * 1993-01-22 1994-08-04 Chemie Linz Deutschland N-Cyclische und N,N'dicyclische Harnstoffe
US5252579A (en) * 1993-02-16 1993-10-12 American Home Products Corporation Macrocyclic immunomodulators
US5319098A (en) * 1993-05-18 1994-06-07 Celgene Corporation Process for the stereoselective preparation of L-alanyl-L-proline
IT1270882B (it) * 1993-10-05 1997-05-13 Isagro Srl Oligopeptidi ad attivita' fungicida
ATE177420T1 (de) * 1993-11-04 1999-03-15 Abbott Lab Cyclobutan-derivate als inhibitoren der squalen- synthetase und der protein-farnesyltransferase
DE69512220T2 (de) * 1994-03-07 2000-03-16 Vertex Pharma Sulfonamidderivate als aspartylprotease-inhibitoren
US5744485A (en) * 1994-03-25 1998-04-28 Vertex Pharmaceuticals Incorporated Carbamates and ureas as modifiers of multi-drug resistance
US5856116A (en) * 1994-06-17 1999-01-05 Vertex Pharmaceuticals, Incorporated Crystal structure and mutants of interleukin-1 beta converting enzyme
US5716929A (en) * 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
DE69534300T2 (de) * 1994-08-18 2006-05-18 Ariad Gene Therapeutics, Inc., Cambridge Neues multimerisierendes reagenz
US5543423A (en) * 1994-11-16 1996-08-06 Vertex Pharmaceuticals, Incorporated Amino acid derivatives with improved multi-drug resistance activity
IL115685A (en) * 1994-11-16 2000-08-31 Vertex Pharma Amino acid derivatives pharmaceutical compositions containing the same and processes for the preparation thereof
US5621108A (en) * 1994-12-05 1997-04-15 Trustees Of The University Of Pennsylvania Processes and intermediates for preparing macrocycles
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
US6037370A (en) * 1995-06-08 2000-03-14 Vertex Pharmaceuticals Incorporated Methods and compositions for stimulating neurite growth

Also Published As

Publication number Publication date
LV12102B (en) 1998-10-20
AU713302B2 (en) 1999-11-25
BG62596B1 (bg) 2000-03-31
BRPI9611271A2 (pt) 2019-04-30
NZ316361A (en) 1999-08-30
WO1997016190A1 (en) 1997-05-09
EP0859614A4 (en) 2000-04-26
EP0859614A1 (en) 1998-08-26
EA001481B1 (ru) 2001-04-23
AU6857396A (en) 1997-05-22
PL326420A1 (en) 1998-09-14
BG102410A (en) 1998-12-30
KR19990067257A (ko) 1999-08-16
JPH11514643A (ja) 1999-12-14
EE9800125A (et) 1998-10-15
HUP9901752A2 (hu) 1999-10-28
MX9803356A (es) 1998-09-30
SK55998A3 (en) 1999-02-11
HUP9901752A3 (en) 2001-04-28
CZ125198A3 (cs) 1998-12-16
US5801197A (en) 1998-09-01
LV12102A (lv) 1998-08-20
CA2236328A1 (en) 1997-05-09
NO981903D0 (no) 1998-04-27
NO981903L (no) 1998-06-30

Similar Documents

Publication Publication Date Title
EA199800329A1 (ru) Ингибиторы ротамазной ферментативной активности
EA199700360A1 (ru) Ингибиторы ферментативной активности ротамазы
ATE246510T1 (de) Inhibitoren der aktivität der cyclophilin rotamase
EA199700361A1 (ru) Ингибиторы ферментативной активности ротамазы, являющиеся малыми молекулами
NZ507720A (en) Effecting neuronal activity with heterocyclic thioesters and ketones
HUP0002974A2 (hu) Szulfonamidokkal N-szubsztituált heterociklusos tioészter-származékok, eljárás előállításukra és a vegyületeket tartalmazó gyógyszerkészítmények
FI852342A0 (fi) Menetelmä desulfatohirudiinin valmistamiseksi
NO991433L (no) Heterosykliske estere og amider
ATE226193T1 (de) Substituierte zyklische amine als metalloproteaseinhibitoren
ATE170868T1 (de) Peptid-phosphinyloxymethyl-ketonen als inhibitoren von interleukin-1 beta- konvertierenden enzymen
ATE265409T1 (de) Von aminosauren und hydroxysauren substituierte benzamidinderivate und deren verwendung als antikoagulantien
DE68907366D1 (de) Verfahren zur raffinierung von stickstofftrifluoridgas.
EA199900511A1 (ru) N-связанные мочевины и карбаматы сложных гетероциклических тиоэфиров
NO992268L (no) N-bundne sulfonamider av heterocykliske tioestere
AR010744A1 (es) Inhibidores polipropilos de ciclofilina
BR0210060A (pt) Ligandos de fkbp de heterobiciclos
ES2170628B1 (es) Pequeños inhibidores de moleculas de la actividad de enzimas de rotamasa
DE69509235D1 (de) Arginin ahnliche derivate als enzym-inhibitoren
EA199900257A1 (ru) Промежуточные соединения для получения ингибиторов вич-протеазы и способы получения ингибиторов вич-протеазы

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU