DE69840586D1 - Deuterierte Cyclosporin-analoga und ihre Verwendung als immunmodulierende Agenzien - Google Patents

Deuterierte Cyclosporin-analoga und ihre Verwendung als immunmodulierende Agenzien

Info

Publication number: DE69840586D1
Authority: DE; Germany
Prior art keywords: cyclosporine; substitution; disclosed; derivatives; cyclosporine derivatives
Prior art date: 1997-10-08
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.): Expired - Fee Related

Application number

DE69840586T

Other languages

English (en)

Inventor

S Selveraj Naicker

Robert T Foster

Randall W Yatscoff

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Isotechnika Inc

Original Assignee

Isotechnika 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.)

1997-10-08

Filing date

1998-10-08

Publication date

2009-04-02

1998-10-08 Application filed by Isotechnika Inc filed Critical Isotechnika Inc

2009-04-02 Application granted granted Critical

2009-04-02 Publication of DE69840586D1 publication Critical patent/DE69840586D1/de

2018-10-09 Anticipated expiration legal-status Critical

Status Expired - Fee Related legal-status Critical Current

Links

PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical class CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 title abstract 9
239000002955 immunomodulating agent Substances 0.000 title 1
238000006467 substitution reaction Methods 0.000 abstract 4
229930105110 Cyclosporin A Natural products 0.000 abstract 3
108010036949 Cyclosporine Proteins 0.000 abstract 3
YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical group [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 abstract 2
229910052805 deuterium Inorganic materials 0.000 abstract 2
238000000034 method Methods 0.000 abstract 2
239000000126 substance Substances 0.000 abstract 2
230000001988 toxicity Effects 0.000 abstract 2
231100000419 toxicity Toxicity 0.000 abstract 2
108010036941 Cyclosporins Proteins 0.000 abstract 1
206010062016 Immunosuppression Diseases 0.000 abstract 1
125000003275 alpha amino acid group Chemical class 0.000 abstract 1
150000001413 amino acids Chemical class 0.000 abstract 1
229930182912 cyclosporin Natural products 0.000 abstract 1
230000001506 immunosuppresive effect Effects 0.000 abstract 1
230000000155 isotopic effect Effects 0.000 abstract 1
230000004060 metabolic process Effects 0.000 abstract 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/64—Cyclic peptides containing only normal peptide links
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- 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
- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/008—Peptides; Proteins
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
- C07K1/13—Labelling of peptides
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/64—Cyclic peptides containing only normal peptide links
- C07K7/645—Cyclosporins; Related peptides
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10S530/00—Chemistry: natural resins or derivatives; peptides or proteins; lignins or reaction products thereof
- Y10S530/806—Antigenic peptides or proteins
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10S530/00—Chemistry: natural resins or derivatives; peptides or proteins; lignins or reaction products thereof
- Y10S530/807—Hapten conjugated with peptide or protein

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Medicinal Chemistry (AREA)
General Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Veterinary Medicine (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
Pharmacology & Pharmacy (AREA)
Bioinformatics & Cheminformatics (AREA)
General Chemical & Material Sciences (AREA)
Engineering & Computer Science (AREA)
Public Health (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Molecular Biology (AREA)
Genetics & Genomics (AREA)
Biophysics (AREA)
Biochemistry (AREA)
Immunology (AREA)
Physical Education & Sports Medicine (AREA)
Orthopedic Medicine & Surgery (AREA)
Rheumatology (AREA)
Analytical Chemistry (AREA)
Neurology (AREA)
Neurosurgery (AREA)
Biomedical Technology (AREA)
Pain & Pain Management (AREA)
Hematology (AREA)
Diabetes (AREA)
Surgery (AREA)
Transplantation (AREA)
Urology & Nephrology (AREA)
Dermatology (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Peptides Or Proteins (AREA)

DE69840586T 1997-10-08 1998-10-08 Deuterierte Cyclosporin-analoga und ihre Verwendung als immunmodulierende Agenzien Expired - Fee Related DE69840586D1 (de)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US6136097P	1997-10-08	1997-10-08

Publications (1)

Publication Number	Publication Date
DE69840586D1 true DE69840586D1 (de)	2009-04-02

Family

ID=22035297

Family Applications (2)

Application Number	Title	Priority Date	Filing Date
DE69840586T Expired - Fee Related DE69840586D1 (de)	1997-10-08	1998-10-08	Deuterierte Cyclosporin-analoga und ihre Verwendung als immunmodulierende Agenzien
DE69832984T Expired - Lifetime DE69832984T2 (de)	1997-10-08	1998-10-08	DEUTERIERtE und undeuterierte CYCLOSPORIN-ANALOGA UND IHRE VERWENDUNG ALS IMMUNMODULIERENDE AGENtIEN

Family Applications After (1)

Application Number	Title	Priority Date	Filing Date
DE69832984T Expired - Lifetime DE69832984T2 (de)	1997-10-08	1998-10-08	DEUTERIERtE und undeuterierte CYCLOSPORIN-ANALOGA UND IHRE VERWENDUNG ALS IMMUNMODULIERENDE AGENtIEN

Country Status (15)

Country	Link
US (3)	US6613739B1 (de)
EP (1)	EP0991660B8 (de)
JP (6)	JP4261049B2 (de)
KR (1)	KR100585348B1 (de)
AT (2)	ATE314388T1 (de)
AU (1)	AU750245B2 (de)
BR (1)	BR9811716A (de)
CA (1)	CA2298572C (de)
DE (2)	DE69840586D1 (de)
DK (1)	DK0991660T3 (de)
ES (1)	ES2256959T3 (de)
HK (1)	HK1026432A1 (de)
NO (1)	NO324042B1 (de)
NZ (1)	NZ502362A (de)
WO (1)	WO1999018120A1 (de)

Families Citing this family (97)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US20030220234A1 (en)	1998-11-02	2003-11-27	Selvaraj Naicker	Deuterated cyclosporine analogs and their use as immunodulating agents
US20030119029A1 (en) *	1999-04-30	2003-06-26	Regents Of The University Of Michigan	Compositions and methods relating to novel benzodiazepine compounds and targets thereof
US7144880B2 (en) *	1999-04-30	2006-12-05	Regents Of The University Of Michigan	Compositions relating to novel compounds and targets thereof
US20050113460A1 (en) *	1999-04-30	2005-05-26	The Regents Of The University Of Michigan	Compositions and methods relating to novel compounds and targets thereof
US20040176358A1 (en) *	1999-04-30	2004-09-09	The Regents Of The University Of Michigan	Compositions and methods relating to novel compounds and targets thereof
US20060025388A1 (en)	1999-04-30	2006-02-02	Glick Gary D	Compositions and methods relating to novel compounds and targets thereof
EP1143946B1 (de) *	1999-04-30	2004-01-28	The Regents Of The University Of Michigan	Verwendung von benzodiazepinen zur behandlung von apoptose-induzierten autoimmunerkrankungen
US6784156B2 (en)	2001-03-05	2004-08-31	Enanta Pharmaceuticals, Inc.	Cyclosporins for the treatment of respiratory diseases
US6809077B2 (en)	2001-10-12	2004-10-26	Enanta Pharmaceuticals, Inc.	Cyclosporin analogs for the treatment of autoimmune diseases
US20030087813A1 (en)	2001-10-12	2003-05-08	Or Yat Sun	Cyclosporin analogs for the treatment of lung diseases
NZ531944A (en) *	2001-10-19	2006-03-31	Isotechnika Inc	Synthesis of cyclosporin analogs
EP1816138A1 (de) *	2001-10-19	2007-08-08	Isotechnika,Inc.	Cyclosporinanaloga-Gemische und ihre Verwendung als immunmodulierende Wirkstoffe
US20040110666A1 (en) *	2002-12-04	2004-06-10	Or Yat Sun	Cyclosporins for the treatment of immune disorders
DE10261807A1 (de) *	2002-12-19	2004-07-01	Turicum Drug Development Ag	Deuterierte Catecholaminderivate sowie diese Verbindungen enthaltende Arzneimittel
US7012065B2 (en)	2003-02-07	2006-03-14	Enanta Pharmaceuticals, Inc.	Cyclosporins for the treatment of immune disorders
EP1603512A2 (de)	2003-03-17	2005-12-14	Albany Molecular Research, Inc.	Neue cyclosporine
TW200505946A (en) *	2003-04-08	2005-02-16	Hoffmann La Roche	Process for preparation of cyclosporin a analog
US20040266669A1 (en) *	2003-06-20	2004-12-30	Wu Frank X. H.	Cyclosporin derivatives for the treatment of immune disorders
TW200517114A (en)	2003-10-15	2005-06-01	Combinatorx Inc	Methods and reagents for the treatment of immunoinflammatory disorders
US7705036B2 (en) *	2004-04-01	2010-04-27	Cardiome Pharma Corp.	Deuterated aminocyclohexyl ether compounds and processes for preparing same
MXPA06011420A (es) *	2004-04-01	2007-04-20	Cardiome Pharma Corp	Compuestos pegilados de modulacion de canal de iones.
US20090275099A1 (en) *	2004-04-27	2009-11-05	Regents Of The University Of Michigan	Methods and compositions for treating diseases and conditions associated with mitochondrial function
US20050272723A1 (en) *	2004-04-27	2005-12-08	The Regents Of The University Of Michigan	Methods and compositions for treating diseases and conditions associated with mitochondrial function
CA2571899A1 (en) *	2004-07-01	2006-08-03	Yale University	Targeted and high density drug loaded polymeric materials
US20060014677A1 (en) *	2004-07-19	2006-01-19	Isotechnika International Inc.	Method for maximizing efficacy and predicting and minimizing toxicity of calcineurin inhibitor compounds
CA2575280C (en) *	2004-07-29	2012-08-14	Amr Technology, Inc.	Novel processes for stereoselective synthesis of trans isatx 247
US20060052369A1 (en) *	2004-09-07	2006-03-09	The Regents Of The University Of Michigan	Compositions and methods relating to novel compounds and targets thereof
WO2006039164A2 (en)	2004-09-29	2006-04-13	Amr Technology, Inc.	Novel cyclosporin analogues and their pharmaceutical uses
JP2008514701A (ja) *	2004-09-29	2008-05-08	エーエムアールテクノロジーインコーポレイテッド	シクロスポリンアルキン類似体およびそれらの薬学的使用
US7361636B2 (en)	2004-10-06	2008-04-22	Amr Technology, Inc.	Cyclosporin alkynes and their utility as pharmaceutical agents
WO2006088525A1 (en)	2004-11-18	2006-08-24	Cardiome Pharma Corp.	Synthetic process for aminocyclohexyl ether compounds
MX2007007262A (es) *	2004-12-17	2007-10-19	Isotechnika Inc	Metabolitos de analogos de ciclosporina.
CA2593019A1 (en) *	2005-01-03	2006-07-13	The Regents Of The University Of Michigan	Compositions and methods relating to novel compounds and targets thereof
DE602006012033D1 (de) *	2005-04-06	2010-03-18	Abbott Lab	Verfahren zur messung immunsuppressiver tacrolimus-, sirolimus- und cyclosporin-a-komplexe in einer blutprobe
JP2008545757A (ja)	2005-06-01	2008-12-18	ザリージェンツオブザユニバーシティオブミシガン	溶媒和されていないベンゾジアゼピン組成物および方法
JP5159616B2 (ja) *	2005-06-15	2013-03-06	カーディオムファーマコーポレイション	アミノシクロヘキシルエーテル化合物の調製のための合成プロセス
CA2624179A1 (en) *	2005-10-06	2007-04-12	Auspex Pharmaceuticals, Inc.	Deuterated inhibitors of gastric h+, k+-atpase with enhanced therapeutic properties
US20070105844A1 (en) *	2005-10-26	2007-05-10	Regents Of The University Of Michigan	Therapeutic compositions and methods
EP2604269B1 (de)	2005-11-01	2014-09-24	The Regents Of The University Of Michigan	1,4-Benzodiazepin-2,5-Dione mit therapeutischen Eigenschaften
NZ568694A (en)	2005-11-09	2011-09-30	Zalicus Inc	Method, compositions, and kits for the treatment of medical conditions
JP5302005B2 (ja)	2005-12-01	2013-10-02	オースペックス・ファーマシューティカルズ・インコーポレイテッド	セロトニン作動性および／またはノルエピネフリン作動性の活性を有する置換フェネチルアミン
GB0604647D0 (en)	2006-03-08	2006-04-19	Shchepinov Mikhail	Stabilized food supplements and their derivatives
US7696166B2 (en) *	2006-03-28	2010-04-13	Albany Molecular Research, Inc.	Use of cyclosporin alkyne/alkene analogues for preventing or treating viral-induced disorders
US7696165B2 (en) *	2006-03-28	2010-04-13	Albany Molecular Research, Inc.	Use of cyclosporin alkyne analogues for preventing or treating viral-induced disorders
US7759338B2 (en) *	2006-04-27	2010-07-20	The Regents Of The University Of Michigan	Soluble 1,4 benzodiazepine compounds and stable salts thereof
US8155649B2 (en) *	2006-05-12	2012-04-10	Shared Spectrum Company	Method and system for classifying communication signals in a dynamic spectrum access system
CA2659549C (en)	2006-06-09	2013-07-30	The Regents Of The University Of Michigan	Compositions and methods relating to novel compounds and targets thereof
US10265407B2 (en)	2007-02-15	2019-04-23	Yale University	Modular nanodevices for smart adaptable vaccines
US20100151436A1 (en) *	2007-03-02	2010-06-17	Fong Peter M	Methods for Ex Vivo Administration of Drugs to Grafts Using Polymeric Nanoparticles
AU2008226532B2 (en) *	2007-03-09	2011-09-22	The Regents Of The University Of Michigan	Compositions and methods relating to novel compounds and targets thereof
ES2693948T3 (es)	2007-03-15	2018-12-14	Auspex Pharmaceuticals, Inc.	Fenetilamina sustituida con actividad serotoninérgica y/o norepinefrinérgica
AU2008282165A1 (en)	2007-08-01	2009-02-05	Emory University	Methods for determination of protein phosphatase activity, and uses in predicting therapeutic outcomes
AU2008298870C1 (en)	2007-09-14	2014-10-09	The Regents Of The University Of Michigan	F1F0-ATPase inhibitors and related methods
RU2010122902A (ru)	2007-11-06	2011-12-20	Дзе Риджентс оф дзе Юниверсити оф Мичиган (US)	Бензодиапениноновые соединения, применимые в лечении кожных состояний
DK2268604T3 (en)	2008-03-14	2017-03-27	Retrotope Inc	CANCER THERAPIES BY USING ISOTO-SUBSTITUTED LYSIN
MX2011000637A (es) *	2008-07-15	2011-05-02	Theracos Inc	Derivados deuretados de bencilbenceno y metodos de uso.
CN102164948A (zh) *	2008-07-30	2011-08-24	伊索技术制药公司	非免疫抑制的环孢菌素类似分子
JP5586606B2 (ja) *	2008-09-02	2014-09-10	アクチミスファーマシューティカルズインコーポレーテッド	Ｃｒｔｈ２アンタゴニストとしての同位体富化されたピリミジン−５−イル酢酸誘導体
US8252933B2 (en) *	2008-09-03	2012-08-28	Teva Pharmaceuticals Industries, Ltd.	2-oxo-1,2-dihydro-quinoline modulators of immune function
US8497307B2 (en)	2008-09-11	2013-07-30	The Regents Of The University Of Michigan	Aryl guanidine F1F0-ATPase inhibitors and related methods
NZ592993A (en) *	2008-10-22	2013-02-22	Acucela Inc	Compounds for treating ophthalmic diseases and disorders
MX2011008000A (es)	2009-01-30	2011-09-15	Enanta Pharm Inc	Analogos de ciclosporina para la prevención o tratamiento de la infeccion de hepatitis c.
US8481483B2 (en)	2009-02-19	2013-07-09	Enanta Pharmaceuticals, Inc.	Cyclosporin analogues
US8604023B2 (en)	2009-04-17	2013-12-10	The Regents Of The University Of Michigan	1,4-benzodiazepinone compounds and their use in treating cancer
US8685917B2 (en)	2009-07-09	2014-04-01	Enanta Pharmaceuticals, Inc.	Cyclosporin analogues
US8349312B2 (en)	2009-07-09	2013-01-08	Enanta Pharmaceuticals, Inc.	Proline substituted cyclosporin analogues
US8367053B2 (en)	2009-07-09	2013-02-05	Enanta Pharmaceuticals, Inc.	Cyclosporin analogues
WO2011035124A1 (en)	2009-09-18	2011-03-24	The Regents Of The University Of Michigan	Benzodiazepinone compounds and methods of treatment using same
WO2011053870A1 (en)	2009-10-30	2011-05-05	Retrotope, Inc.	Alleviating oxidative stress disorders with pufa derivatives
CN102753179A (zh)	2009-11-17	2012-10-24	密执安大学评议会	具有治疗性能的1,4-苯并二氮杂*-2,5-二酮和相关化合物
CA2780287C (en)	2009-11-17	2015-03-17	The Regents Of The University Of Michigan	1,4-benzodiazepine-2,5-diones and related compounds with therapeutic properties
US20110130711A1 (en) *	2009-11-19	2011-06-02	Follica, Inc.	Hair growth treatment
UY33226A (es) *	2010-02-19	2011-09-30	Novartis Ag	Compuestos de pirrolopirimidina deuterada como inhibidores de la cdk4/6
US8623814B2 (en)	2010-02-23	2014-01-07	Enanta Pharmaceuticals, Inc.	Antiviral agents
KR102305423B1 (ko)	2010-12-15	2021-09-27	콘트라빌 파마슈티컬스, 인코퍼레이티드	아미노산 1 및 3에서 변형된 사이클로스포린 유사체 분자
WO2012145427A1 (en)	2011-04-18	2012-10-26	The Trustees Of Columbia University In The City Of New York	Methods to treat cancer using cyclosporine and cyclosporine derivatives
WO2012148929A2 (en)	2011-04-26	2012-11-01	Retrotope, Inc.	Disorders implicating pufa oxidation
EP2701695B1 (de)	2011-04-26	2019-04-03	Retrotope, Inc.	Neurodegenerative erkrankungen und muskelerkrankungen mit polyungesättigten fettsäuren
JP6093756B2 (ja)	2011-04-26	2017-03-08	レトロトップ、インコーポレイテッドＲｅｔｒｏｔｏｐｅ，Ｉｎｃ．	損なわれたエネルギー処理障害およびミトコンドリア欠損症
KR102014524B1 (ko)	2011-04-26	2019-08-26	레트로토프 인코포레이티드	산화성 망막 질환
DE102011111991A1 (de)	2011-08-30	2013-02-28	Lead Discovery Center Gmbh	Neue Cyclosporin-Derivate
CN104053771B (zh)	2011-11-18	2016-11-09	科德克希思公司	用于制备羟基取代的氨基甲酸酯的生物催化剂
US9597385B2 (en)	2012-04-23	2017-03-21	Allertein Therapeutics, Llc	Nanoparticles for treatment of allergy
US8906853B2 (en)	2012-11-28	2014-12-09	Enanta Pharmaceuticals, Inc.	[N-Me-4-hydroxyleucine]-9-cyclosporin analogues for treatment and prevention of hepatitis C infection
JP2016516754A (ja)	2013-04-03	2016-06-09	アラーテイン・セラピューティクス・リミテッド・ライアビリティ・カンパニーＡｌｌｅｒｔｅｉｎＴｈｅｒａｐｅｕｔｉｃｓ，ＬＬＣ	新規のナノ粒子組成物
AU2014311346A1 (en)	2013-08-26	2016-03-17	Enanta Pharmaceuticals, Inc.	Cyclosporin analogues for preventing or treating hepatitis C
US10428331B2 (en)	2014-01-16	2019-10-01	Musc Foundation For Research Development	Targeted nanocarriers for the administration of immunosuppressive agents
US9669095B2 (en)	2014-11-03	2017-06-06	Enanta Pharmaceuticals, Inc.	Cyclosporin analogues for preventing or treating hepatitis C infection
US10730821B2 (en)	2015-11-23	2020-08-04	Retrotope, Inc.	Site-specific isotopic labeling of 1,4-diene systems
WO2018106928A1 (en)	2016-12-08	2018-06-14	Contravir Pharmaceuticals, Inc.	Treatment and prevention of hbv diseases by cyclosporine analogue molecules modified at amino acides 1 and 3
CN111886010A (zh) *	2018-01-12	2020-11-03	Enb治疗公司	用于治疗与etbr激活相关的癌症的氘化化合物、组合物和方法
US11584779B2 (en)	2018-10-19	2023-02-21	Teva Pharmaceuticals International Gmbh	Solid state forms of voclosporin
WO2021168311A1 (en)	2020-02-21	2021-08-26	Retrotope, Inc.	Processes for isotopic modification of polyunsaturated fatty acids and derivatives thereof
CN115298199A (zh) *	2020-03-26	2022-11-04	睿诺医疗科技（上海）有限公司	环孢菌素衍生物的制备
US12109194B2 (en)	2021-02-05	2024-10-08	Biojiva Llc	Synergistic combination therapy for treating ALS
EP4201952A1 (de)	2021-12-21	2023-06-28	Curia Spain, S.A.U.	Verfahren zur kontrollierten synthese von voclosporin
IT202300001116A1 (it) *	2023-01-25	2024-07-25	Indena Spa	Processo per la preparazione di un intermedio utile per la sintesi di voclosporina

Family Cites Families (59)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
CH614931A5 (de)	1975-11-04	1979-12-28	Sandoz Ag
US4210581A (en)	1975-11-04	1980-07-01	Sandoz Ltd.	Organic compounds
US4117118A (en)	1976-04-09	1978-09-26	Sandoz Ltd.	Organic compounds
DE2819094A1 (de)	1977-05-10	1978-11-23	Sandoz Ag	Cyclosporin-derivate, ihre verwendung und herstellung
SE448386B (sv)	1978-10-18	1987-02-16	Sandoz Ag	Nya cyklosporinderivat, forfarande for framstellning av dem samt farmaceutisk komposition innehallande dem
US4201771A (en)	1979-03-12	1980-05-06	Merck & Co., Inc.	Antibiotic A43F
US4396542A (en)	1980-02-14	1983-08-02	Sandoz Ltd.	Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production
EP0034567B1 (de)	1980-02-14	1984-11-07	Sandoz Ag	Verfahren zur Totalsynthese von Cyclosporinen und neue Cyclosporine
FR2487198A1 (fr)	1980-07-28	1982-01-29	Berri Balzac Sa	Nouvelle substance immuno-suppressive, son procede d'isolement et son application en therapeutique
US4384996A (en)	1981-01-09	1983-05-24	Sandoz Ltd.	Novel cyclosporins
CH667274A5 (de)	1984-03-23	1988-09-30	Sandoz Ag	Cyclosporine, ihre herstellung und diese enthaltende pharmazeutische zusammensetzungen.
US4727018A (en)	1984-05-18	1988-02-23	Eichner Ronald D	Immunoregulation of transplantable tissue
US5639724A (en)	1984-07-24	1997-06-17	Sandoz Ltd.	Cyclosporin galenic forms
GB8422253D0 (en)	1984-09-04	1984-10-10	Sandoz Ltd	Organic compounds
EP0194972B1 (de)	1985-03-11	1992-07-29	Sandoz Ag	Cyclosporine
US4765980A (en)	1986-04-28	1988-08-23	International Minerals & Chemical Corp.	Stabilized porcine growth hormone
US4764503A (en)	1986-11-19	1988-08-16	Sandoz Ltd.	Novel cyclosporins
NL194638C (nl)	1986-12-19	2002-10-04	Novartis Ag	Hydrosol die vaste deeltjes van een farmaceutisch actieve stof bevat en farmaceutisch preparaat dat deze hydrosol bevat.
EP0283801A3 (de) *	1987-03-27	1990-05-30	Abbott Laboratories	Fluoreszenz-Polarisations-Test für Cyclosporin A und Metaboliten und verwandte Immunogene und Antikörper
US5427960A (en)	1987-03-27	1995-06-27	Abbott Laboratories	Fluorescence polarization assay for cyclosporin A and metabolites and related immunogens and antibodies
US5239057A (en)	1987-03-27	1993-08-24	Abbott Laboratories	Fluorescence polarization assay for cyclosporin a and metabolites and related immunogens and antibodies
US4885276A (en)	1987-06-03	1989-12-05	Merck & Co., Inc.	Cyclosporin analogs with modified "C-9 amino acids"
US4798823A (en)	1987-06-03	1989-01-17	Merck & Co., Inc.	New cyclosporin analogs with modified "C-9 amino acids"
JP2577049B2 (ja)	1987-06-04	1997-01-29	三共株式会社	シクロスポリン製剤
DE3884470T2 (de) *	1987-06-17	1994-03-10	Sandoz Ag	Cyclosporine und deren Benutzung als Arzneimittel.
DE3851268T2 (de)	1987-06-19	1995-01-26	Sandoz Ag	Zyklische Peptolide.
EP0373260B1 (de)	1987-06-22	1994-03-09	Merck & Co. Inc.	Cyclosporin-Derivate, die eine modifizierte Aminosäure auf Stellung 8 tragen
GB8717300D0 (en)	1987-07-22	1987-08-26	Nat Res Dev	Cyclosporins
GB8717299D0 (en)	1987-07-22	1987-08-26	Nat Res Dev	Peptides
US5227467A (en)	1987-08-03	1993-07-13	Merck & Co., Inc.	Immunosuppressive fluorinated cyclosporin analogs
US4963362A (en)	1987-08-07	1990-10-16	Regents Of The University Of Minnesota	Freeze-dried liposome mixture containing cyclosporin
US4839342A (en)	1987-09-03	1989-06-13	University Of Georgia Research Foundation, Inc.	Method of increasing tear production by topical administration of cyclosporin
EP0391909B1 (de)	1987-09-03	1994-08-17	The University Of Georgia Research Foundation, Inc.	Cyclosporin-augenmittel
US5089390A (en)	1987-09-04	1992-02-18	Syntex (U.S.A.) Inc.	2-methyl-4-hexene- and 2-methyl-4-heptene-1,2-diol derivatives
US5236899A (en)	1987-11-16	1993-08-17	Merck & Co., Inc.	6-position cyclosporin a analogs as modifiers of cytotoxic drug resistance
US4914188A (en)	1987-11-16	1990-04-03	Merck & Co., Inc.	Novel 6-position cyclosporin analogs as non-immunosuppressive antagonists of cyclosporin binding to cyclophilin
US5013719A (en)	1988-05-13	1991-05-07	Merrell Dow Pharmaceuticals Inc.	Method of effecting immunosuppression
GB2222770B (en)	1988-09-16	1992-07-29	Sandoz Ltd	Pharmaceutical compositions containing cyclosporins
US5342625A (en)	1988-09-16	1994-08-30	Sandoz Ltd.	Pharmaceutical compositions comprising cyclosporins
JPH04502328A (ja)	1988-12-05	1992-04-23	ザ・トラステイーズ・オブ・コロンビア・ユニヴアーシテイ・イン・ザ・シテイ・オブ・ニユー・ヨーク	シクロスポリンａの新規誘導体、それに対する抗体及びその使用
US4996193A (en)	1989-03-03	1991-02-26	The Regents Of The University Of California	Combined topical and systemic method of administration of cyclosporine
US5540931A (en)	1989-03-03	1996-07-30	Charles W. Hewitt	Methods for inducing site-specific immunosuppression and compositions of site specific immunosuppressants
US5284826A (en)	1989-07-24	1994-02-08	Sandoz Ltd.	0-hydroxyethyl and acyloxyethyl derivatives of [ser]8 cyclosporins
US5214130A (en)	1990-02-27	1993-05-25	Merck & Co., Inc.	Synthesis of novel immunosuppressive cyclosporin analogs with modified amino acids at position-8
US5122511A (en)	1990-02-27	1992-06-16	Merck & Co., Inc.	Immunosuppressive cyclosporin analogs with modified amino acids at position-8
DE69116034T2 (de)	1990-08-15	1996-06-20	Abbott Lab	Immunotestreagenzien und Verfahren zur Bestimmung von Cyclosporin
FI111730B (fi)	1990-11-02	2003-09-15	Novartis Ag	Menetelmä ei-immunosuppressiivisen syklosporiinin valmistamiseksi
US5115859A (en)	1990-12-21	1992-05-26	United Technologies Corporation	Regenerable non-venting cooler for protective suit
EP0507968B1 (de)	1991-04-06	1995-09-06	Arzneimittelwerk Dresden Gmbh	Verfahren zur fermentativen Herstellung und Isolierung von Cyclosporin A sowie neue Cyclosporin- bildende Stämme
GB9204466D0 (en) *	1992-03-02	1992-04-15	Sandoz Ltd	Improvements in or relating to organic compounds
HU213553B (en)	1992-05-25	1997-07-28	Biogal Gyogyszergyar	Process for isolating of cyclosporin-a
FI92334C (fi)	1992-12-30	1994-10-25	Leiras Oy	Menetelmä syklosporiinien tuottamiseksi ja menetelmässä käytettävä uusi Tolypocladium-kanta
JPH09500103A (ja)	1993-05-04	1997-01-07	メルクエンドカンパニーインコーポレーテッド	シクロヘキサペプチジルアミノアルキルエーテル
WO1995026325A2 (en) *	1994-03-25	1995-10-05	Isotechnika Inc.	Enhancement of the efficacy of drugs by deuteration
US5639852A (en)	1994-09-01	1997-06-17	Wisconsin Alumni Research Foundation	Immunostimulatory agents
US5616595A (en)	1995-06-07	1997-04-01	Abbott Laboratories	Process for recovering water insoluble compounds from a fermentation broth
US5624902A (en)	1995-06-07	1997-04-29	Torrey Pines Institute For Molecular Studies	Peptide inhibitors of calmodulin
US5747330A (en)	1996-06-05	1998-05-05	Poli Industria Chimica	Antibiotic producing microbe
US5709797A (en)	1996-06-05	1998-01-20	Poli Industria Chimica S.P.A.	Method of isolating cyclosporins

1998
- 1998-10-08 NZ NZ502362A patent/NZ502362A/en not_active IP Right Cessation
- 1998-10-08 AT AT98947718T patent/ATE314388T1/de active
- 1998-10-08 BR BR9811716-5A patent/BR9811716A/pt not_active Application Discontinuation
- 1998-10-08 JP JP2000514928A patent/JP4261049B2/ja not_active Expired - Lifetime
- 1998-10-08 DE DE69840586T patent/DE69840586D1/de not_active Expired - Fee Related
- 1998-10-08 DK DK98947718T patent/DK0991660T3/da active
- 1998-10-08 DE DE69832984T patent/DE69832984T2/de not_active Expired - Lifetime
- 1998-10-08 KR KR1020007003743A patent/KR100585348B1/ko not_active Expired - Fee Related
- 1998-10-08 WO PCT/IB1998/001693 patent/WO1999018120A1/en active IP Right Grant
- 1998-10-08 AU AU94542/98A patent/AU750245B2/en not_active Expired
- 1998-10-08 CA CA002298572A patent/CA2298572C/en not_active Expired - Lifetime
- 1998-10-08 ES ES98947718T patent/ES2256959T3/es not_active Expired - Lifetime
- 1998-10-08 EP EP98947718A patent/EP0991660B8/de not_active Expired - Lifetime
- 1998-10-08 AT AT05024216T patent/ATE423130T1/de not_active IP Right Cessation
2000
- 2000-02-29 NO NO20001020A patent/NO324042B1/no not_active IP Right Cessation
- 2000-08-07 US US09/634,945 patent/US6613739B1/en not_active Expired - Lifetime
- 2000-08-14 US US09/639,708 patent/US6605593B1/en not_active Expired - Lifetime
- 2000-09-06 HK HK00105620A patent/HK1026432A1/xx not_active IP Right Cessation
2001
- 2001-11-07 US US09/985,997 patent/US20020132763A1/en not_active Abandoned
2003
- 2003-10-17 JP JP2003358524A patent/JP2004143168A/ja not_active Withdrawn
2005
- 2005-08-11 JP JP2005233674A patent/JP2005343904A/ja not_active Withdrawn
2007
- 2007-01-26 JP JP2007017196A patent/JP2007119489A/ja not_active Withdrawn
2008
- 2008-05-27 JP JP2008138790A patent/JP2008222725A/ja not_active Withdrawn
- 2008-05-27 JP JP2008138789A patent/JP2008222724A/ja not_active Withdrawn

Also Published As

Publication number	Publication date
EP0991660B1 (de)	2005-12-28
KR20010030978A (ko)	2001-04-16
HK1026432A1 (en)	2000-12-15
CA2298572A1 (en)	1999-04-15
KR100585348B1 (ko)	2006-06-01
JP2007119489A (ja)	2007-05-17
JP2004143168A (ja)	2004-05-20
JP2005343904A (ja)	2005-12-15
NO324042B1 (no)	2007-07-30
NO20001020D0 (no)	2000-02-29
DE69832984T2 (de)	2006-09-21
EP0991660B8 (de)	2006-04-05
ATE423130T1 (de)	2009-03-15
NZ502362A (en)	2001-05-25
ATE314388T1 (de)	2006-01-15
JP2008222724A (ja)	2008-09-25
DE69832984D1 (de)	2006-02-02
US20020132763A1 (en)	2002-09-19
BR9811716A (pt)	2000-07-18
WO1999018120A1 (en)	1999-04-15
AU9454298A (en)	1999-04-27
JP2008222725A (ja)	2008-09-25
NO20001020L (no)	2000-02-29
EP0991660A1 (de)	2000-04-12
JP4261049B2 (ja)	2009-04-30
US6613739B1 (en)	2003-09-02
DK0991660T3 (da)	2006-02-13
ES2256959T3 (es)	2006-07-16
US6605593B1 (en)	2003-08-12
AU750245B2 (en)	2002-07-11
CA2298572C (en)	2002-04-09
JP2001519355A (ja)	2001-10-23

Publication	Publication Date	Title
DE69840586D1 (de)	2009-04-02	Deuterierte Cyclosporin-analoga und ihre Verwendung als immunmodulierende Agenzien
Kruger et al.	1999	Electron capture dissociation of multiply charged peptide cations
Tomer et al.	1984	Fast-atom bombardment combined with tandem mass spectrometry for the determination of cyclic peptides
Kenny et al.	1992	Fragmentation studies of peptides: the formation of y ions
IL128829A0 (en)	2000-01-31	Improved solid-phase peptide and agent for use in such synthesis
AU9315398A (en)	1999-03-29	Chemokine peptides, variants, derivatives and analogs. their use in methods to inhibit or augment an inflammatory response
CA2235138A1 (en)	1997-05-01	Reverse-turn mimetics and methods relating thereto
HUP0002381A1 (hu)	2000-10-28	Apolipoprotein A-1 agonista hatású peptidszármazékok, ezek lipidekkel alkotott komplexei, valamint ezeket tartalmazó gyógyászati készítmények
DE69912952D1 (en)	2003-12-24	Cyclosporine
NO954342L (no)	1995-10-30	Erytropoietinanalogblandinger, samt fremgangsmåter ved fremstilling derav
DE69413085D1 (de)	1998-10-15	Immunsuppressive Aminomethylen-Peptide
JO2034B1 (en)	1999-05-15	Isotopes of the hormone peptide its uses and the chemical compounds it contains
WO1995011309A3 (en)	1995-06-08	A novel nuclear mitotic phosphoprotein: mitosin
PL297902A1 (en)	1993-09-06	Novel cyclosporines and method of obtaining them
TR199800011T1 (xx)	1998-04-21	Benzo$g] kuinolin t�revleri
NZ336793A (en)	2000-08-25	Method for stabilizing peptides by adding an organic acid and then lyophilizing the peptide mixture
PT1107981E (pt)	2005-05-31	Sintese de analogos peptidicos ciclicos de anel modificado
ATE289612T1 (de)	2005-03-15	Diagnostische verwendungen von gegen acetylcholinesterase oder deren c-terminale peptide gerichteten antikörpern
Ali et al.	2008	Solid-phase total synthesis of cyclic decapeptide phakellistatin 12
CA2255865A1 (en)	1997-11-27	Synthesis of soluble beta-sheet forming peptides
CA2511888A1 (en)	1999-04-15	Deuterated cyclosporin analogs and their use as immunomodulating agents
CA2372639A1 (en)	1999-04-15	Deuterated cyclosporine analogs and their use as immunomodulating agents
EP0438600A4 (en)	1992-07-08	Enzymes which participate in c-terminal amidation, and production and use thereof
CA2137037A1 (en)	1995-06-08	Fluorinated Diazabicycloalkane Derivatives
AU2002212623A1 (en)	2002-06-11	Compound for chelating a metal, radiopharmaceutical, manufacturing process therefor, and diagnostic kit

Legal Events

Date	Code	Title	Description
2010-03-18	8364	No opposition during term of opposition
2010-08-19	8339	Ceased/non-payment of the annual fee