OA10975A - Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides - Google Patents

Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides Download PDF

Info

Publication number: OA10975A
Authority: OA; OAPI
Prior art keywords: compound; acid; butanoyl; aspartyl; mixture
Prior art date: 1996-08-21

Application number

OA9900033A

Other languages

English (en)

Inventor

Scott I Klein

Bruce F Molino

Mark Czekaj

Charles J Gardner

Original Assignee

Rhone Poulenc Rorer 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.)

1996-08-21

Filing date

1999-02-15

Publication date

2001-11-01

1999-02-15 Application filed by Rhone Poulenc Rorer Pharma filed Critical Rhone Poulenc Rorer Pharma

2001-11-01 Publication of OA10975A publication Critical patent/OA10975A/en

Links

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229910052943 magnesium sulfate Inorganic materials 0.000 description 1
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VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
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125000001325 propanoyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 description 1
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125000003107 substituted aryl group Chemical group 0.000 description 1
KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
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HOWHQWFXSLOJEF-MGZLOUMQSA-N systemin Chemical compound NCCCC[C@H](N)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(O)=O)C(=O)OC(=O)[C@@H]1CCCN1C(=O)[C@H]1N(C(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]2N(CCC2)C(=O)[C@H]2N(CCC2)C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)CCC1 HOWHQWFXSLOJEF-MGZLOUMQSA-N 0.000 description 1
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230000001732 thrombotic effect Effects 0.000 description 1
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JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
238000011200 topical administration Methods 0.000 description 1
FGMPLJWBKKVCDB-UHFFFAOYSA-N trans-L-hydroxy-proline Natural products ON1CCCC1C(O)=O FGMPLJWBKKVCDB-UHFFFAOYSA-N 0.000 description 1
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125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 description 1
125000004953 trihalomethyl group Chemical group 0.000 description 1
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HRXKRNGNAMMEHJ-UHFFFAOYSA-K trisodium citrate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O HRXKRNGNAMMEHJ-UHFFFAOYSA-K 0.000 description 1
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OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 1
235000015112 vegetable and seed oil Nutrition 0.000 description 1
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210000003462 vein Anatomy 0.000 description 1
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UGZADUVQMDAIAO-UHFFFAOYSA-L zinc hydroxide Chemical compound [OH-].[OH-].[Zn+2] UGZADUVQMDAIAO-UHFFFAOYSA-L 0.000 description 1
229940007718 zinc hydroxide Drugs 0.000 description 1
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ORQXBVXKBGUSBA-QMMMGPOBSA-N β-cyclohexyl-alanine Chemical compound OC(=O)[C@@H](N)CC1CCCCC1 ORQXBVXKBGUSBA-QMMMGPOBSA-N 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06104—Dipeptides with the first amino acid being acidic
- C07K5/06113—Asp- or Asn-amino acid
- 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
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
- 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
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

Chemical & Material Sciences (AREA)
Health & Medical Sciences (AREA)
Organic Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Molecular Biology (AREA)
Genetics & Genomics (AREA)
Biophysics (AREA)
Biochemistry (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
Chemical Kinetics & Catalysis (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
General Chemical & Material Sciences (AREA)
Cardiology (AREA)
Heart & Thoracic Surgery (AREA)
Vascular Medicine (AREA)
Urology & Nephrology (AREA)
Diabetes (AREA)
Hematology (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Peptides Or Proteins (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

OA9900033A 1996-08-21 1999-02-15 Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides OA10975A (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US08/700,950 US5780590A (en)	1993-10-15	1996-08-21	Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides

Publications (1)

Publication Number	Publication Date
OA10975A true OA10975A (en)	2001-11-01

Family

ID=24815484

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
OA9900033A OA10975A (en)	1996-08-21	1999-02-15	Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides

Country Status (21)

Country	Link
US (1)	US5780590A (no)
EP (1)	EP0929572A4 (no)
JP (1)	JP2001501965A (no)
KR (1)	KR20000035797A (no)
CN (1)	CN1231671A (no)
AP (1)	AP904A (no)
AU (1)	AU722112B2 (no)
BG (1)	BG103197A (no)
BR (1)	BR9711205A (no)
CA (1)	CA2263732A1 (no)
EA (1)	EA001391B1 (no)
HU (1)	HUP9903961A3 (no)
IL (1)	IL128556A0 (no)
NO (1)	NO990836L (no)
NZ (1)	NZ334059A (no)
OA (1)	OA10975A (no)
PL (1)	PL331713A1 (no)
SK (1)	SK14699A3 (no)
UA (1)	UA48252C2 (no)
WO (1)	WO1998017678A1 (no)
ZA (1)	ZA977511B (no)

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US6274705B1 (en)	1996-05-02	2001-08-14	Aventis Pharmaceuticals Products Inc.	Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides
PL331772A1 (en) *	1996-08-21	1999-08-02	Rhone Poulenc Rorer Pharma	Stable non-hygroscopic crystalline form of n-[n-n-(4-piperidin-4-yl)-n-ethylglycin] compounds
WO1999019294A1 (en) *	1997-05-14	1999-04-22	Aventis Pharmaceuticals Products Inc. Legal/Patents	Process for the preparation of azacycloalkylalkanoyl pseudotetrapeptides
EA002724B1 (ru) *	1997-10-10	2002-08-29	Авентис Фармасьютикалз Продактс Инк.	Способ получения азациклоалкилалканоилпсевдотетрапептидов
WO2000040601A1 (en) *	1998-12-30	2000-07-13	Aventis Pharmaceuticals Products Inc.	Process for preparing a stable non-hygroscopic crystalline n-[n-[n- piperdin- 4-yl)butanoyl)- n.ethylglycyl]- (l)-aspartyl] -ss-cyclohexylalanine amide
US7200838B2 (en) *	2000-12-20	2007-04-03	National Instruments Corporation	System and method for automatically generating a graphical program in response to a state diagram
US7544681B2 (en)	2001-09-27	2009-06-09	Ramot At Tel Aviv University Ltd.	Conjugated psychotropic drugs and uses thereof
CA2610838A1 (en) *	2005-06-07	2006-12-14	Ramot At Tel Aviv University Ltd.	Novel salts of conjugated psychotropic drugs and processes of preparing same
WO2008010223A2 (en)	2006-07-17	2008-01-24	Ramot At Tel Aviv University Ltd.	Conjugates comprising a psychotropic drug or a gaba agonist and an organic acid and their use in treating pain and other cns disorders
US8207369B2 (en)	2008-02-11	2012-06-26	Ramot At Tel-Aviv University Ltd.	Conjugates for treating neurodegenerative diseases and disorders
EP2509603A1 (en)	2009-12-09	2012-10-17	Biolinerx Ltd.	Methods of improving cognitive functions
CA2789654A1 (en)	2010-02-24	2011-09-01	Ramot At Tel-Aviv University Ltd.	Crystalline forms of the tri-mesylate salt of perphenazine-gaba and process of producing the same
WO2012038963A1 (en)	2010-09-22	2012-03-29	Ramot At Tel-Aviv University Ltd.	An acid addition salt of a nortriptyline-gaba conjugate and a process of preparing same

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US3821188A (en) *	1972-06-14	1974-06-28	American Home Prod	Proline and pyroglutamic acid containing tripeptides
GB8600263D0 (en) *	1985-01-22	1986-02-12	Ici America Inc	Peptide derivatives
US4683291A (en) *	1985-10-28	1987-07-28	Scripps Clinic And Research Foundation	Platelet binding inhibitors
FR2608160B1 (fr) *	1986-12-15	1989-03-31	Inst Nat Sante Rech Med	Nouveaux derives peptidiques et leur application notamment en therapeutique
US4857508A (en) *	1987-12-03	1989-08-15	Monsanto Company	Novel platelet-aggregation inhibitor peptide derivatives
US4879313A (en) *	1988-07-20	1989-11-07	Mosanto Company	Novel platelet-aggregation inhibitors
US5037808A (en) *	1988-07-20	1991-08-06	Monsanto Co.	Indolyl platelet-aggregation inhibitors
US4992463A (en) *	1988-07-20	1991-02-12	Monsanto Company	Thienyl peptide mimetic compounds which are useful in inhibiting platelet aggregation
US5023233A (en) *	1989-07-28	1991-06-11	Merck & Co., Inc.	Fibrinogen receptor antagonists
CA2066047A1 (en) *	1989-09-29	1991-03-30	Scott I. Klein	Anti-thrombotic peptides and pseudopeptides
US4952562A (en) *	1989-09-29	1990-08-28	Rorer Pharmaceutical Corporation	Anti-thrombotic peptides and pseudopeptides
US5051405A (en) *	1989-10-10	1991-09-24	Rhone-Poulenc Rorer Pharmaceuticals Inc.	Anti-thrombotic peptides and pseudopeptides
US5053392A (en) *	1989-12-01	1991-10-01	Rhone-Poulenc Rorer Pharmaceuticals Inc.	Novel arginine, glycine, aspartic acid derivatives as platelet-aggregation inhibitors
US5086069A (en) *	1990-02-05	1992-02-04	Rorer Pharmaceutical Corporation	Anti-thrombotic peptide and pseudopeptide derivatives
CA2037153A1 (en) *	1990-03-09	1991-09-10	Leo Alig	Acetic acid derivatives
US5064814A (en) *	1990-04-05	1991-11-12	Rhone-Poulenc Rorer Pharmaceuticals Inc.	Anti-thrombotic peptide and pseudopeptide derivatives
GB9007751D0 (en) *	1990-04-05	1990-06-06	Ciba Geigy Ag	Novel platelet-aggregation inhibitors
IL99539A0 (en) *	1990-09-27	1992-08-18	Merck & Co Inc	Fibrinogen receptor antagonists and pharmaceutical compositions containing them
NZ239876A (en) *	1990-09-27	1993-12-23	Merck & Co Inc	Glycyl-b-alanine derivatives and pharmaceutical compositions thereof.
MX9201416A (es) *	1991-03-28	1992-10-01	Rhone Poulenc Rorer Int	Peptidos y pseudopeptidos antitromboticos.
JPH08503920A (ja) *	1991-04-11	1996-04-30	ローヌ−プーランローラーインターナショナル（ホウルディングス）インコーポレイテッド	抗血栓ペプチドおよび偽ペプチド誘導体
ATE142641T1 (de) *	1991-05-13	1996-09-15	Fujisawa Pharmaceutical Co	Neue peptid-verbindungen und verfahren zur herstellung davon
UA44258C2 (uk) *	1993-10-15	2002-02-15	Рон-Пуленк Рорер Фармасьютікалз Інк.	Антитромботичні азациклоалкілалканоілпептиди та псевдопептиди, фармацевтична композиція, що їх містить, спосіб профілактики або лікування тромбозу у ссавців (варіанти)

1996
- 1996-08-21 US US08/700,950 patent/US5780590A/en not_active Expired - Lifetime
1997
- 1997-08-15 EP EP97938424A patent/EP0929572A4/en not_active Withdrawn
- 1997-08-15 AP APAP/P/1999/001452A patent/AP904A/en active
- 1997-08-15 JP JP10519340A patent/JP2001501965A/ja not_active Ceased
- 1997-08-15 HU HU9903961A patent/HUP9903961A3/hu unknown
- 1997-08-15 UA UA99031553A patent/UA48252C2/uk unknown
- 1997-08-15 EA EA199900216A patent/EA001391B1/ru not_active IP Right Cessation
- 1997-08-15 PL PL97331713A patent/PL331713A1/xx unknown
- 1997-08-15 CN CN97198164A patent/CN1231671A/zh active Pending
- 1997-08-15 KR KR1019997001363A patent/KR20000035797A/ko not_active Ceased
- 1997-08-15 BR BR9711205A patent/BR9711205A/pt not_active Application Discontinuation
- 1997-08-15 WO PCT/US1997/014578 patent/WO1998017678A1/en not_active Ceased
- 1997-08-15 IL IL12855697A patent/IL128556A0/xx unknown
- 1997-08-15 CA CA002263732A patent/CA2263732A1/en not_active Abandoned
- 1997-08-15 SK SK146-99A patent/SK14699A3/sk unknown
- 1997-08-15 NZ NZ334059A patent/NZ334059A/xx unknown
- 1997-08-15 AU AU40749/97A patent/AU722112B2/en not_active Ceased
- 1997-08-21 ZA ZA9707511A patent/ZA977511B/xx unknown
1999
- 1999-02-15 OA OA9900033A patent/OA10975A/en unknown
- 1999-02-22 NO NO990836A patent/NO990836L/no unknown
- 1999-02-22 BG BG103197A patent/BG103197A/xx unknown

Also Published As

Publication number	Publication date
AU722112B2 (en)	2000-07-20
PL331713A1 (en)	1999-08-02
SK14699A3 (en)	2000-11-07
UA48252C2 (uk)	2002-08-15
BG103197A (bg)	2000-05-31
HUP9903961A3 (en)	2000-12-28
EA199900216A1 (ru)	1999-08-26
CN1231671A (zh)	1999-10-13
AP904A (en)	2000-11-24
EP0929572A1 (en)	1999-07-21
US5780590A (en)	1998-07-14
BR9711205A (pt)	1999-08-17
NZ334059A (en)	2000-01-28
EP0929572A4 (en)	2001-09-12
HUP9903961A2 (hu)	2000-04-28
EA001391B1 (ru)	2001-02-26
ZA977511B (en)	1998-03-03
AP9901452A0 (en)	1999-03-31
AU4074997A (en)	1998-05-15
KR20000035797A (ko)	2000-06-26
WO1998017678A1 (en)	1998-04-30
IL128556A0 (en)	2000-01-31
NO990836L (no)	1999-04-20
CA2263732A1 (en)	1998-04-30
JP2001501965A (ja)	2001-02-13
NO990836D0 (no)	1999-02-22

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