RU97102581A - ORTHO-SUBSTITUTED BENZOILGUANIDINES, METHOD FOR PRODUCING, USE AS MEDICINES OR DIAGNOSTIC MEDICINES, AND ALSO THE DRUG ON THEIR BASIS - Google Patents

ORTHO-SUBSTITUTED BENZOILGUANIDINES, METHOD FOR PRODUCING, USE AS MEDICINES OR DIAGNOSTIC MEDICINES, AND ALSO THE DRUG ON THEIR BASIS

Info

Publication number
RU97102581A
RU97102581A RU97102581/04A RU97102581A RU97102581A RU 97102581 A RU97102581 A RU 97102581A RU 97102581/04 A RU97102581/04 A RU 97102581/04A RU 97102581 A RU97102581 A RU 97102581A RU 97102581 A RU97102581 A RU 97102581A
Authority
RU
Russia
Prior art keywords
compound
chloro
manufacture
hydrochloride
medicinal product
Prior art date
Application number
RU97102581/04A
Other languages
Russian (ru)
Other versions
RU2218329C2 (en
Inventor
Альбус Удо
Брендель Йоахим
Клееманн Хайнц-Вернер
Йохен Ланг Ханс
Шольц Вольфганг
Шварк Ян-Роберт
Вайхерт Андреас
Original Assignee
Хехст АГ
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 DE19606509A external-priority patent/DE19606509A1/en
Application filed by Хехст АГ filed Critical Хехст АГ
Publication of RU97102581A publication Critical patent/RU97102581A/en
Application granted granted Critical
Publication of RU2218329C2 publication Critical patent/RU2218329C2/en

Links

Claims (15)

1. Орто-замещенные бензоилгуанидины формулы I
Figure 00000001

где
R(2) и R(3) - независимо друг от друга - водород, Cl, Br, I, (C1-C8)-алкил, (C3-C8)-циклоалкил или -OR(5),
R(5) - (C1-C8)-алкил или -CdH2d-(C3-C8)-циклоалкил,
d - 0, 1 или 2,
причем одним из двух заместителей R(2) и R(3) всегда является водород, однако оба заместителя R(2) и R(3) одновременно не являются водородами, а также их фармацевтически приемлемые соли.1. Ortho-substituted benzoylguanidines of the formula I
Figure 00000001

Where
R (2) and R (3) are independently hydrogen, Cl, Br, I, (C 1 -C 8 ) -alkyl, (C 3 -C 8 ) -cycloalkyl or -OR (5),
R (5) - (C 1 -C 8 ) -alkyl or -C d H 2d - (C 3 -C 8 ) -cycloalkyl,
d - 0, 1 or 2,
moreover, one of the two substituents R (2) and R (3) is always hydrogen, however, both of the substituents R (2) and R (3) are simultaneously not hydrogens, as well as their pharmaceutically acceptable salts. 2. Соединения формулы I по п. 1, в которых R(2) и R(3) - независимо друг от друга - водород, Cl, Br, I, (C1-C8)-алкил, (C3-C8)-циклоалкил или -OR(5), R(5) - C1-C8-алкил,
а также их фармацевтически приемлемые соли.2. The compounds of formula I according to claim 1, in which R (2) and R (3) are independently from each other hydrogen, Cl, Br, I, (C 1 -C 8 ) -alkyl, (C 3 -C 8 ) -cycloalkyl or -OR (5), R (5) - C 1 -C 8 -alkyl,
and their pharmaceutically acceptable salts. 3. Соединение формулы I по п. 1, выбранное из группы, состоящей из гидрохлорида 2-хлор-4-метокси-5-трифторметилбензоилгуанидина, гидрохлорида 2-хлор-3-метокси-5-трифторметилбензоилгуанидина, гидрохлорида 2-хлор-3-иод-5-трифторметилбензоилгуанидина, гидрохлорида 2-хлор-3-метил-5-трифторметилбензоилгуанидина, гидрохлорида 2-хлор-3-н-пропил-5-трифторметилбензоилгуанидина, гидрохлорида 2-хлор-3-изопропил-5-трифторметилбензоилгуанидина, гидрохлорида 2-хлор-3-трет-бутил-5-трифторметилбензоилгуанидина, гидрохлорида 2-хлор-3-циклопентил-5-трифторметилбензоилгуанидина, гидрохлорида 2-хлор-4-метил-5-трифторметилбензоилгуанидина, гидрохлорида 2-хлор-4-н-пропилн-5-трифторметилбензоилгуанидина, гидрохлорида 2-хлор-4-изопропил-5-трифторметилбензоилгуанидина, гидрохлорида 2-хлор-4-трет-бутил-5-трифторметилбензоилгуанидина, гидрохлорида 2-хлор-4-циклопентил-5-трифторметилбензоилгуанидина. 3. The compound of formula I according to claim 1, selected from the group consisting of 2-chloro-4-methoxy-5-trifluoromethylbenzoylguanidine hydrochloride, 2-chloro-3-methoxy-5-trifluoromethylbenzoylguanidine hydrochloride, 2-chloro-3-iodine hydrochloride -5-trifluoromethylbenzoylguanidine, 2-chloro-3-methyl-5-trifluoromethylbenzoylguanidine hydrochloride, 2-chloro-3-n-propyl-5-trifluoromethylbenzoylguanidine hydrochloride, 2-chloro-3-isopropyl-5-trifluoromethylbenzo-chloro-2-hydrochloride -3-tert-butyl-5-trifluoromethylbenzoylguanidine, 2-chloro-3-cyclopentyl-5-trifluoromethylbenzene hydrochloride ilguanidine, 2-chloro-4-methyl-5-trifluoromethylbenzoylguanidine hydrochloride, 2-chloro-4-n-propyl-5-trifluoromethylbenzoylguanidine hydrochloride, 2-chloro-4-isopropyl-5-trifluoromethylbenzoylguanidine hydrochloride, 4-hydrochloride tert-butyl-5-trifluoromethylbenzoylguanidine, 2-chloro-4-cyclopentyl-5-trifluoromethylbenzoylguanidine hydrochloride. 4. Способ получения соединения формулы I по п. 1, отличающийся тем, что соединение формулы II:
Figure 00000002

в котором заместители R(2) и R(3) обладают указанной выше структурой, а L - отщепляемая группа, способная к легкому нуклеофильному замещению, подвергают взаимодействию с гуанидином.4. A method of obtaining a compound of formula I according to claim 1, characterized in that the compound of formula II:
Figure 00000002

in which the substituents R (2) and R (3) have the above structure, and L is a cleavable group capable of easy nucleophilic substitution, is reacted with guanidine. 5. Соединение I по п. 1 для изготовления лекарственного препарата, предназначенного для лечения или профилактики заболеваний, вызванных ишемическими состояниями. 5. Compound I according to claim 1 for the manufacture of a medicinal product intended for the treatment or prevention of diseases caused by ischemic conditions. 6. Соединение I по п. 1 для изготовления лекарственного препарата, предназначенного для лечения и профилактики инфаркта сердца. 6. Compound I according to claim 1 for the manufacture of a medicinal product intended for the treatment and prevention of heart attack. 7. Соединение I по п. 1 для изготовления лекарственного препарата, предназначенного для лечения и профилактики стенокардии. 7. Compound I according to claim 1 for the manufacture of a medicinal product intended for the treatment and prevention of angina pectoris. 8. Соединение I по п. 1 для изготовления лекарственного препарата, предназначенного для лечения или профилактики ишемических состояний сердца. 8. Compound I according to claim 1 for the manufacture of a medicinal product intended for the treatment or prevention of ischemic conditions of the heart. 9. Соединение I по п. 1 для изготовления лекарственного препарата, предназначенного для лечения или профилактики ишемических состояний периферической и центральной нервных систем и инсульта. 9. Compound I according to claim 1 for the manufacture of a medicinal product intended for the treatment or prevention of ischemic conditions of the peripheral and central nervous systems and stroke. 10. Соединение I по п. 1 для изготовления лекарственного препарата, предназначенного для лечения или профилактики ишемических состояний периферических органов и конечностей. 10. Compound I according to claim 1 for the manufacture of a medicinal product intended for the treatment or prevention of ischemic conditions of peripheral organs and limbs. 11. Соединение I по п. 1 для изготовления лекарственного препарата, предназначенного для лечения шоковых состояний. 11. Compound I according to claim 1 for the manufacture of a medicinal product intended for the treatment of shock conditions. 12. Соединение I по п. 1 для изготовления лекарственного препарата, предназначенного для использования при проведении хирургических операций и при трансплантации органов. 12. Compound I according to claim 1 for the manufacture of a medicinal product intended for use in surgical operations and organ transplantation. 13. Соединение I по п. 1 для изготовления лекарственного препарата, предназначенного для консервирования и хранения трансплантантов, используемых в хирургических операциях. 13. Compound I according to claim 1 for the manufacture of a medicinal product intended for the preservation and storage of transplants used in surgical operations. 14. Соединение I по п. 1 для изготовления лекарственного препарата, предназначенного для лечения заболеваний, первичной или вторичной причиной которых является пролиферация клеток, и, таким образом, применение соединения I для изготовления антиатеросклеротических медикаментов, средства против поздних осложнений диабета, раковых заболеваний, фибротических заболеваний: фиброза легких, печени или почки, гиперплазии простаты. 14. Compound I according to claim 1 for the manufacture of a medicinal product intended for the treatment of diseases, the primary or secondary cause of which is cell proliferation, and, thus, the use of compound I for the manufacture of anti-atherosclerotic drugs, an agent against late complications of diabetes, cancer, fibrotic diseases: fibrosis of the lungs, liver or kidney, prostatic hyperplasia. 15. Лекарственный препарат, отличающийся активным содержанием соединения формулы I по пп. 1 - 3. 15. A drug, characterized by the active content of the compounds of formula I according to paragraphs. 13.
RU97102581/04A 1996-02-22 1997-02-21 Ortho-substituted benzoylguanidines, method for preparing, using as medicinal or diagnostic agents and medicinal preparation based on thereof also RU2218329C2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19606509.7 1996-02-22
DE19606509A DE19606509A1 (en) 1996-02-22 1996-02-22 Ortho-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic agent, and medicament containing them

Publications (2)

Publication Number Publication Date
RU97102581A true RU97102581A (en) 1999-02-27
RU2218329C2 RU2218329C2 (en) 2003-12-10

Family

ID=7786043

Family Applications (1)

Application Number Title Priority Date Filing Date
RU97102581/04A RU2218329C2 (en) 1996-02-22 1997-02-21 Ortho-substituted benzoylguanidines, method for preparing, using as medicinal or diagnostic agents and medicinal preparation based on thereof also

Country Status (30)

Country Link
US (1) US5856574A (en)
EP (1) EP0791577B1 (en)
JP (1) JP3974677B2 (en)
KR (1) KR100476796B1 (en)
CN (1) CN1060764C (en)
AR (1) AR005933A1 (en)
AT (1) ATE186296T1 (en)
AU (1) AU723096B2 (en)
BR (1) BR9701046A (en)
CA (1) CA2198176A1 (en)
CZ (1) CZ287843B6 (en)
DE (2) DE19606509A1 (en)
DK (1) DK0791577T3 (en)
ES (1) ES2140922T3 (en)
GR (1) GR3032293T3 (en)
HR (1) HRP970101B1 (en)
HU (1) HUP9700502A3 (en)
ID (1) ID16042A (en)
IL (1) IL120259A (en)
MX (1) MX9701323A (en)
MY (1) MY117642A (en)
NO (1) NO307046B1 (en)
NZ (1) NZ314268A (en)
PL (1) PL185752B1 (en)
RU (1) RU2218329C2 (en)
SI (1) SI0791577T1 (en)
SK (1) SK281753B6 (en)
TR (1) TR199700144A2 (en)
TW (1) TW404937B (en)
ZA (1) ZA971514B (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19713427A1 (en) * 1997-04-01 1998-10-08 Hoechst Ag Ortho-substituted benzoylguanidines, processes for their preparation, their use as medicaments or diagnostic agents and medicaments containing them
CN111099959B (en) * 2019-12-30 2022-09-02 西安瑞联新材料股份有限公司 Industrial production method of 1, 4-dibromo-2, 5-diiodobenzene

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK0612723T3 (en) * 1993-02-20 1998-03-30 Hoechst Ag Substituted benzoylguanidines, method of preparation, their use as a drug, as an inhibitor of cellular Na + / H + exchange or as a diagnostic, and as a drug containing it
DE4328869A1 (en) * 1993-08-27 1995-03-02 Hoechst Ag Ortho-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic agent, and medicament containing them
DE19517848A1 (en) * 1995-05-16 1996-11-21 Merck Patent Gmbh Fluorine-containing benzoylguanidines
US5596407A (en) * 1995-06-07 1997-01-21 Varian Associates, Inc Optical detector for echelle spectrometer

Similar Documents

Publication Publication Date Title
RU95101843A (en) 4-amino-1-piperidylbenzoyl guanidines
KR950022159A (en) Substituted 1-oxo-1,2-dihydroisoquinolinoylguanidine and 1,1-dioxo-2H-1,2-benzothiazinoylguanidine, their preparation, use as a medicament or diagnostic agent And medicaments comprising them
JPH069545A (en) O-substituted benzoylguanidine, its production, its use as medicine or diagnostic agent, and medicine containing it
HU223537B1 (en) Perfluoroalkyl-substituted benzoyl-guanidine, process for producing them, use of them as medicament or diagnosticum, and pharmaceutical composition containing them
RU96121572A (en) SULPHONIMIDAMIDES, METHOD FOR PRODUCING THEM, PHARMACEUTICAL COMPOSITION, METHOD FOR PRODUCING IT, METHOD FOR TREATMENT
KR960041152A (en) Fluorophenyl-substituted alkenylcarboxylic acid guanidides, their preparation, their use as medicaments or diagnostic agents and medicaments containing them
JP3875731B2 (en) 3,5-substituted aminobenzoylguanidines, their preparation, their use as medicaments or diagnostics and medicaments containing them
CA2152137A1 (en) Phenyl-substituted alkenylcarboguanidides carrying perfluoroalkyl groups, a process for their preparation, their use as a medicament or diagnostic agent, and also a medicament containing them
RU2227751C2 (en) Pharmaceutical combined preparation consisting of inhibitor of sodium-hydrogen exchange and medicinal agents for treatment of cardiovascular diseases
RU2003134629A (en) CEPHEMA COMPOUNDS
RU96109699A (en) GUANIDIDES OF ALKENILKARBONIC ACIDS, METHOD OF THEIR RECEIVING, CONTAINING THEIR MEDICATION OR DIAGNOSTIC TOOL
KR970015568A (en) Substituted Benzoylguanidine, Method of Making the Same, Use thereof as a medicament or a diagnostic agent, and a pharmaceutical comprising the same
KR970006281A (en) Substituted cinnamic acid guanidide, a process for its preparation, its use as a drug or diagnostic agent and medicaments containing it
RU97109003A (en) SUBSTITUTED 2-NAPTOYLGUANIDINES, METHOD FOR PRODUCING THEM AND MEDICINE ON THEIR BASIS
KR950032129A (en) Substituted bicyclic heteroaroylguanidines, methods for their preparation, their use as medicaments or diagnostic agents and medicaments containing the same
RU95115511A (en) BENZOILGUANIDINES, METHOD FOR THEIR PRODUCTION, THEIR USE AS A MEDICAL OR DIAGNOSTIC MEDICINE CONTAINING THEIR MEDICINAL AND INTERMEDIATE CONNECTIONS FOR THEIR RECEIVING
KR960029320A (en) Basic substituted benzoylguanidines, their preparation, their use as medicaments or diagnostic agents and medicaments containing them
CA2176796A1 (en) Substituted benzyloxycarbonylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing them
RU97102581A (en) ORTHO-SUBSTITUTED BENZOILGUANIDINES, METHOD FOR PRODUCING, USE AS MEDICINES OR DIAGNOSTIC MEDICINES, AND ALSO THE DRUG ON THEIR BASIS
RU97109913A (en) ORTHO-SUBSTITUTED BENZOILGUANIDINES, METHOD FOR PRODUCING THEM, THEIR APPLICATION AS A MEDICINE OR DIAGNOSTIC MEDICINES AND CONTAINING THEIR MEDICINE
RU2218329C2 (en) Ortho-substituted benzoylguanidines, method for preparing, using as medicinal or diagnostic agents and medicinal preparation based on thereof also
JPH0812643A (en) O-amino-substituted benzoylguanidine and its production
RU2001104454A (en) IMIDAZOLE DERIVATIVES WITH BIPHENYL SULPHONYL SUBSTITUTION, METHOD FOR PRODUCING THEM, USE AS A MEDICINAL PRODUCT OR A DIAGNOSTIC, AND ALSO CONTAINING THEIR MEDICINAL
RU2227796C2 (en) Ortho-substituted benzoylguanidines, method for their preparing and medicinal agent based on thereof
RU95115408A (en) SUBSTITUTED BENZOILGUANIDINES, METHOD FOR PRODUCING THERE, CONTAINING THEIR MEDICINAL PRODUCT, METHOD OR MEANS FOR ITS PRODUCTION, METHOD OF TREATMENT