EP1347762A2 - Formulation pharmaceutique contenant des thienopyrimidines et des antithrombotiques, des inhibiteurs calciques, des prostaglandines ou des derives de prostaglandine (2) - Google Patents

Formulation pharmaceutique contenant des thienopyrimidines et des antithrombotiques, des inhibiteurs calciques, des prostaglandines ou des derives de prostaglandine (2)

Info

Publication number
EP1347762A2
EP1347762A2 EP01995677A EP01995677A EP1347762A2 EP 1347762 A2 EP1347762 A2 EP 1347762A2 EP 01995677 A EP01995677 A EP 01995677A EP 01995677 A EP01995677 A EP 01995677A EP 1347762 A2 EP1347762 A2 EP 1347762A2
Authority
EP
European Patent Office
Prior art keywords
pyrimidin
pharmaceutical formulation
atoms
formulation according
chloro
Prior art date
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.)
Withdrawn
Application number
EP01995677A
Other languages
German (de)
English (en)
Inventor
Hans-Michael Eggenweiler
Volker Eiermann
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.)
Merck Patent GmbH
Original Assignee
Merck Patent GmbH
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 DE10063221A external-priority patent/DE10063221A1/de
Priority claimed from DE2000163884 external-priority patent/DE10063884A1/de
Priority claimed from DE2000164991 external-priority patent/DE10064991A1/de
Application filed by Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of EP1347762A2 publication Critical patent/EP1347762A2/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Definitions

  • Preferred platelet aggregation inhibitors are selected from the group ditazole, cloricromene, picotamide, clopidogrel, ticlopidine, acetylsalicylic acid, dipyridamole, calcium carbassalate, epoprostenol, indobufen, lloprost, abciximab, tirofiban, aloxiprin, intrif.
  • R 4 A cycloalkyl, - [C (R 5 ) 2 ] m Ar, - [C (R 5 ) 2 ] m Het or
  • R 2 , R 2 ' , R each independently of one another H, A, CF 3 , Cl, F, COA, COOH, COOA, CONH 2 , CONHA, CONA 2 , CH 2 NH 2 , CH 2 NHCOA, CH 2 NHCOOA, OH , OA, OCF 3 , NO 2 , SO 2 A, SO2NH2, SO2NHA or SO2NA2,
  • a alkyl with 1 - 20 C atoms, in which one or two CH 2 groups by O or S atoms or by -CH CH groups and also 1-7 H atoms can be replaced by F,
  • R 1 is H, Ar, Het, cycloalkyl or A, which is replaced by OR 2 , SR 2 , N (R 2 ) 2 , Ar,
  • Example D ointment
  • a mixture of 1 kg of active ingredient of the formula I, 1 kg of an antithrombotic, 4 kg of lactose, 1, 2 kg of potato starch, 0.2 kg of talc and 0.1 kg of magnesium Sium stearate is compressed into tablets in the usual way, such that each tablet contains 10 mg of each active ingredient.
  • a solution of 100 g of an active ingredient of the formula I, 100 g of the calcium antagonist and 5 g of disodium hydrogenphosphate is adjusted to pH 6.5 in 3 l of double-distilled water with 2N hydrochloric acid, sterile filtered, filled into injection glasses, ly under sterile conditions - ophilized and sealed sterile. Each injection jar contains 5 mg of each active ingredient.
  • Example E tablets are pressed, which are then coated in a conventional manner with a coating of sucrose, potato starch, talc, tragacanth and colorant.
  • 14 g of active ingredient of the formula I and 14 g of a prostaglandin or prostaglandin derivative are dissolved in 10 I of isotonic NaCI solution and the solution is filled into commercially available spray vessels with a pump mechanism.
  • the solution can be sprayed into the mouth or nose.
  • One spray (approximately 0.1 ml) corresponds to a dose of approximately 0.14 mg of each active ingredient.

Landscapes

  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Otolaryngology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

L'invention concerne une préparation pharmaceutique contenant au moins un composé de formule (I), dans laquelle R1, R2 et X ont la signification indiquée dans la revendication 1, ou ses sels ou solvates physiologiquement acceptables, ainsi que a) au moins un antithrombotique ou b) au moins un inhibiteur calcique ou c) au moins une prostaglandine ou un dérivé de prostaglandine, pour la production d'un médicament destiné à traiter l'angine de poitrine, l'hypertension artérielle, l'hypertension pulmonaire, l'insuffisance cardiaque congestive, la broncho-pneumopathie chronique obstructive (BPCO), le coeur pulmonaire, l'insuffisance cardiaque droite, l'athérosclérose, les conditions de perméabilité réduite des vaisseaux cardiaques, les maladies vasculaires périphériques, l'accident vasculaire cérébral, la bronchite, l'asthme allergique, l'asthme chronique, la rhinite allergique, le glaucome, le syndrome du côlon irritable, les tumeurs, l'insuffisance rénale, la cirrhose du foie, ainsi que les troubles sexuels féminins.
EP01995677A 2000-12-19 2001-11-28 Formulation pharmaceutique contenant des thienopyrimidines et des antithrombotiques, des inhibiteurs calciques, des prostaglandines ou des derives de prostaglandine (2) Withdrawn EP1347762A2 (fr)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
DE10063221 2000-12-19
DE10063221A DE10063221A1 (de) 2000-12-19 2000-12-19 Pharmazeutische Formulierung enthaltend Thienopyrimidine und Antithrombotica (2)
DE10063884 2000-12-21
DE2000163884 DE10063884A1 (de) 2000-12-21 2000-12-21 Pharmazeutische Formulierung enthaltend Thienopyrimidine und Calcium-Antagonisten (2)
DE10064991 2000-12-23
DE2000164991 DE10064991A1 (de) 2000-12-23 2000-12-23 Pharmazeutische Formulierung enthaltend Thienopyrimidine und Prostaglandine oder Prostaglandinderivate (2)
PCT/EP2001/013913 WO2002049649A2 (fr) 2000-12-19 2001-11-28 Formulation pharmaceutique contenant des thienopyrimidines et des antithrombotiques, des inhibiteurs calciques, des prostaglandines ou des derives de prostaglandine (2)

Publications (1)

Publication Number Publication Date
EP1347762A2 true EP1347762A2 (fr) 2003-10-01

Family

ID=27214206

Family Applications (1)

Application Number Title Priority Date Filing Date
EP01995677A Withdrawn EP1347762A2 (fr) 2000-12-19 2001-11-28 Formulation pharmaceutique contenant des thienopyrimidines et des antithrombotiques, des inhibiteurs calciques, des prostaglandines ou des derives de prostaglandine (2)

Country Status (16)

Country Link
US (1) US20040058940A1 (fr)
EP (1) EP1347762A2 (fr)
JP (1) JP2004516268A (fr)
KR (1) KR20030059350A (fr)
CN (1) CN1481243A (fr)
AR (1) AR035675A1 (fr)
AU (1) AU2002226362A1 (fr)
BR (1) BR0116247A (fr)
CA (1) CA2431147A1 (fr)
CZ (1) CZ20031722A3 (fr)
HU (1) HUP0401368A2 (fr)
MX (1) MXPA03005441A (fr)
NO (1) NO20032771L (fr)
PL (1) PL361812A1 (fr)
SK (1) SK8032003A3 (fr)
WO (1) WO2002049649A2 (fr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050107394A1 (en) * 2001-12-17 2005-05-19 Ardeschir Ghofrani Novel use of selective pde5 inhibitors
AU2007272956B2 (en) * 2006-07-11 2013-05-02 Janssen Pharmaceutica, N.V. Benzofuro-and benzothienopyryimidine modulators of the histamine H4 receptor
US20200009105A1 (en) * 2017-02-28 2020-01-09 Vanderbilt University Prostacyclin, prostacyclin analogs, and methods of treating or preventing rejection of solid organ transplants

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2353285A1 (fr) * 1975-09-17 1977-12-30 Doms Laboratoires Medicament vasodilatateur coronarien perfectionne
JPS5459266A (en) * 1977-10-14 1979-05-12 Ono Pharmaceut Co Ltd Prostaglandin i2 analogs and their preparation
FR2568774B2 (fr) * 1984-05-30 1989-05-19 Choay Sa Medicaments favorisant les proprietes d'ecoulement du sang et leur utilisation en therapeutique
FR2672601B1 (fr) * 1991-02-08 1994-10-14 Synthelabo Derives de benzo-1,5-thiazepine, leur preparation et leur application en therapeutique.
US6143746A (en) * 1994-01-21 2000-11-07 Icos Corporation Tetracyclic cyclic GMP-specific phosphodiesterase inhibitors, process of preparation and use
EP1027054A4 (fr) * 1997-10-28 2002-11-04 Vivus Inc Apport local d'inhibiteurs de phosphodiesterases, dans le traitement du dysfonctionnement erectile
US6156753A (en) * 1997-10-28 2000-12-05 Vivus, Inc. Local administration of type III phosphodiesterase inhibitors for the treatment of erectile dysfunction
DE19819023A1 (de) * 1998-04-29 1999-11-04 Merck Patent Gmbh Thienopyrimidine
DE19943815A1 (de) * 1999-09-14 2001-03-15 Merck Patent Gmbh Verwendung von Thienopyrimidinen

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO0249649A2 *

Also Published As

Publication number Publication date
HUP0401368A2 (hu) 2004-10-28
PL361812A1 (en) 2004-10-04
JP2004516268A (ja) 2004-06-03
CA2431147A1 (fr) 2002-06-27
AU2002226362A1 (en) 2002-07-01
WO2002049649A3 (fr) 2002-11-21
WO2002049649A2 (fr) 2002-06-27
CZ20031722A3 (cs) 2003-09-17
SK8032003A3 (en) 2003-11-04
AR035675A1 (es) 2004-06-23
BR0116247A (pt) 2003-11-04
KR20030059350A (ko) 2003-07-07
MXPA03005441A (es) 2003-09-10
CN1481243A (zh) 2004-03-10
NO20032771D0 (no) 2003-06-18
NO20032771L (no) 2003-06-18
US20040058940A1 (en) 2004-03-25

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