RU95113107A - new pyrrolocarbazoles - Google Patents

new pyrrolocarbazoles


Publication number
RU95113107A RU95113107/04A RU95113107A RU95113107A RU 95113107 A RU95113107 A RU 95113107A RU 95113107/04 A RU95113107/04 A RU 95113107/04A RU 95113107 A RU95113107 A RU 95113107A RU 95113107 A RU95113107 A RU 95113107A
Prior art keywords
pharmaceutically acceptable
Prior art date
Application number
Other languages
Russian (ru)
Other versions
RU2162089C2 (en
Аллен Брока Крис
Original Assignee
Ф.Хоффманн-Ля Рош 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.)
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Priority to US28604394A priority Critical
Priority to US286043 priority
Priority to US286.043 priority
Application filed by Ф.Хоффманн-Ля Рош Аг filed Critical Ф.Хоффманн-Ля Рош Аг
Publication of RU95113107A publication Critical patent/RU95113107A/en
Application granted granted Critical
Publication of RU2162089C2 publication Critical patent/RU2162089C2/en


Claims (10)

1. Соединение, отвечающее формуле I 1. A compound of formula I
Figure 00000001

где R 1 обозначает водородный атом или низший алкил; wherein R 1 is hydrogen or lower alkyl;
R 2 обозначает гетероарил; R 2 represents heteroaryl;
R 3 и R 4 независимо друг от друга обозначают водородные атомы или низшие алкилы, R 3 and R 4 independently are hydrogen or lower alkyl,
или его фармацевтически приемлемая соль. or a pharmaceutically acceptable salt thereof.
2. Соединение по п. 1, где R 1 обозначает водородный атом. 2. A compound according to Claim. 1, where R 1 is hydrogen.
3. Соединение по п. 2, где R 2 обозначает 3-тиофенил. 3. A compound according to claim. 2, where R 2 is 3-thiophenyl.
4. Соединение по п. 3, где R 3 обозначает водородный атом и R 4 обозначает низший алкил. 4. A compound according to claim. 3, where R 3 represents a hydrogen atom and R 4 is lower alkyl.
5. Соединение по п. 4, где R 3 обозначает водородный атом и R 4 обозначает метил, а именно 1,3-диоксо-6-(3-метиламинопропил)-1,2,3,6-тетрагидро-4- (тиофен-3-ил)-пирроло [3,4-с]карбазол. 5. A compound according to claim. 4, where R 3 represents a hydrogen atom and R 4 is methyl, namely 1,3-dioxo-6- (3-methylaminopropyl) -1,2,3,6-tetrahydro-4- (thiophen -3-yl) pyrrolo [3,4-c] carbazole.
6. Фармацевтическая композиция, содержащая соединение или соль по п. 1, и фармацевтически приемлемый эксципиент. 6. A pharmaceutical composition comprising a compound or salt thereof according to Claim. 1, and a pharmaceutically acceptable excipient.
7. Способ получения соединений формулы I, определенных в п. 1, и их фармацевтически приемлемых солей, при осуществлении которого предусмотрена реакция соединения формулы V или Vа 7. A process for preparing compounds of formula I, as defined in claim. 1, and pharmaceutically acceptable salts thereof, which comprises the reaction of a compound of formula V or Va
Figure 00000002

Figure 00000003

где значения R 1 -R 4 определены в п. 1, а Y обозначает аминозащитную группу, wherein the values of R 1 -R 4 are as defined in claim. 1, and Y is an amino protective group,
с малеимидом с последующими, если необходимо, удалением защитной группы Y, и, если желательно, конверсией соединения формулы I в фармацевтически приемлемую соль. with maleimide, followed, if necessary, removing the protecting group Y, and, if desired, converting a compound of formula I into a pharmaceutically acceptable salt thereof.
8. Соединения по любому из пп. 8. Compounds according to any one of claims. 1-5, полученные способом по п. 7, или его очевидному химическому эквиваленту. 1-5, obtained by the process of claim. 7 or an obvious chemical equivalent.
9. Применение соединения или его соли по п. 1 при приготовлении фармацевтической композиции для лечения злокачественных заболеваний, в частности мелкоклеточной легочной карциномы, карциномы толстой кишки и новообразований почек и предстательной железы. 9. Use of a compound or salt thereof according to Claim. 1 for preparing a pharmaceutical composition for the treatment of malignant diseases, particularly small cell lung carcinoma, colon carcinoma and renal and prostate tumors.
10. Новые соединения, композиции, способ и применение, описанные выше. 10. The novel compounds, composition and method of use described above.
RU95113107A 1994-08-04 1995-08-03 New pyrrolocarbazoles RU2162089C2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
US28604394A true 1994-08-04 1994-08-04
US286043 1994-08-04
US286.043 1994-08-04

Publications (2)

Publication Number Publication Date
RU95113107A true RU95113107A (en) 1997-07-20
RU2162089C2 RU2162089C2 (en) 2001-01-20



Family Applications (1)

Application Number Title Priority Date Filing Date
RU95113107A RU2162089C2 (en) 1994-08-04 1995-08-03 New pyrrolocarbazoles

Country Status (29)

Country Link
US (1) US5721267A (en)
EP (1) EP0695755B1 (en)
JP (1) JP2672290B2 (en)
CN (1) CN1051551C (en)
AT (1) AT172463T (en)
AU (1) AU692563B2 (en)
BR (1) BR9503536A (en)
CA (1) CA2155148A1 (en)
CO (1) CO4410329A1 (en)
CZ (1) CZ288583B6 (en)
DE (2) DE69505470D1 (en)
DK (1) DK0695755T3 (en)
ES (1) ES2123873T3 (en)
FI (1) FI111258B (en)
HK (1) HK1012341A1 (en)
HU (1) HU225567B1 (en)
IL (1) IL114785A (en)
MA (1) MA23639A1 (en)
MY (1) MY117092A (en)
NO (1) NO304833B1 (en)
NZ (1) NZ272687A (en)
PE (1) PE34996A1 (en)
PL (1) PL180801B1 (en)
RU (1) RU2162089C2 (en)
SA (1) SA403B1 (en)
TR (1) TR199500954A1 (en)
TW (1) TW403652B (en)
UY (1) UY24010A1 (en)
ZA (1) ZA9506327B (en)

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Publication number Priority date Publication date Assignee Title
US6020298A (en) * 1997-03-05 2000-02-01 Ausimont S.P.A. Solvent cleaning agents including additives of the formula Rf -CFX-L containing perfluoroalkylenic units
IT1283203B1 (en) * 1996-03-07 1998-04-16 Ausimont Spa Extinguishing compositions flame
DE19744257B4 (en) * 1997-10-07 2004-04-15 Zentaris Gmbh Beta-Carboline and their use for the treatment of malignant and other diseases based on pathological cell proliferations
US7122679B2 (en) 2000-05-09 2006-10-17 Cephalon, Inc. Multicyclic compounds and the use thereof
US20050070591A1 (en) * 2001-12-18 2005-03-31 Fumihiko Kanai Indole derivative
US7094798B1 (en) 2002-04-26 2006-08-22 Pfizer Inc Inhibitors of checkpoint kinases (Wee1 and Chk1)
CA2483496A1 (en) * 2002-04-26 2003-11-06 Warner-Lambert Company Llc Inhibitors of checkpoint kinases (wee1 and chk1)
JP2012051804A (en) * 2008-12-26 2012-03-15 Kyoto Univ Eg5 INHIBITOR
PT2975024T (en) * 2009-06-10 2018-05-14 Chugai Pharmaceutical Co Ltd Tetracyclic compounds
US9714229B2 (en) 2014-04-25 2017-07-25 Chugai Seiyaku Kabushiki Kaisha Crystal of tetracyclic compound
SG11201607623XA (en) 2014-04-25 2016-11-29 Chugai Pharmaceutical Co Ltd Preparation containing tetracyclic compound at high dose
TW201613906A (en) 2014-08-08 2016-04-16 Chugai Pharmaceutical Co Ltd Amorphous body of tetracyclic compound

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GB8611762D0 (en) * 1986-05-14 1986-06-25 Wellcome Found Polycyclic biocidal compounds
US4785085A (en) * 1986-11-21 1988-11-15 Bristol-Myers Company Rebeccamycin analogs
NZ227850A (en) * 1988-02-10 1991-11-26 Hoffmann La Roche Indole substituted pyrrole derivatives; preparatory process and medicaments for use against inflammatory immunological, bronchopulmonary or vascular disorders
DE3833008A1 (en) * 1988-09-29 1990-04-05 Goedecke Ag Pyrrolocarbozol derivatives, processes for their preparation and their use as medicines
MC2096A1 (en) * 1989-02-23 1991-02-15 Hoffmann La Roche pyrroles substituted
US5166204A (en) * 1989-11-01 1992-11-24 Toyama Chemical Co., Ltd. Isoindole derivatives and salts thereof and antitumor agent comprising the same
DE4005969A1 (en) * 1990-02-26 1991-08-29 Boehringer Mannheim Gmbh New tri-substituted pyrroles, methods for their manufacture and which contain these compounds drug,
DE4217964A1 (en) * 1992-05-30 1993-12-02 Goedecke Ag Indolocarbazole imides and their use
AU678435B2 (en) * 1993-05-10 1997-05-29 F. Hoffmann-La Roche Ag Substituted pyrroles
US5516771A (en) * 1993-05-28 1996-05-14 Cephalon, Inc. Use of indolocarbazole derivatives to treat a pathological condition of the prostate

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