AR012244A1 - COMPOUNDS DERIVED FROM 9-OXIME ERYTHOMYCIN, PHARMACEUTICAL COMPOSITION CONTAINING THEM, PROCEDURE FOR THE TREATMENT OF A PROTOZOA BACTERIAL INFECTION, PROCEDURE FOR ITS PREPARATION. - Google Patents
COMPOUNDS DERIVED FROM 9-OXIME ERYTHOMYCIN, PHARMACEUTICAL COMPOSITION CONTAINING THEM, PROCEDURE FOR THE TREATMENT OF A PROTOZOA BACTERIAL INFECTION, PROCEDURE FOR ITS PREPARATION.Info
- Publication number
- AR012244A1 AR012244A1 ARP980102703A ARP980102703A AR012244A1 AR 012244 A1 AR012244 A1 AR 012244A1 AR P980102703 A ARP980102703 A AR P980102703A AR P980102703 A ARP980102703 A AR P980102703A AR 012244 A1 AR012244 A1 AR 012244A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- procedure
- formula
- preparation
- integer
- Prior art date
Links
Classifications
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
- C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
Abstract
Se describen los compuestos de formula I y a las sales Farmacéuticamente aceptables de los mismos, en la que R1, R2, R6 y X son lo definido en lapresente. También se describen composiciones farmacéuticas que contienen los compuestos de formulaI en el tratamiento de las infecciones bacterianas yprotozoarias y a procedimientos para la preparacion de dichos compuestos de formula I, donde en la que en dicho anillo de formula XVI, r y p son cada unode ellos independientemente un numero enntero de 1 a 3, q es 0 o 1 y X1 es -CH2- , O, S, -C(S)-, -SO2-, -CH=CH-, -CH(OH)CH(OH)-, o -NH-; y donde las partes(CH2), y (CH2)p de dicho anillo de formula XVI están opcionalmente sustituidas con 1 a 4 sustituyentes y el átomo de nitrogeno cuandoX1es -NH-estáopcionalmente sustituido con 1 sustituyente, estando dichos sustituyentes opcionales independientemente seleccionados entre el grupo constituido por-C(O)O(alquilo C1-C10), alcoxi C1-C10, alcanoílo C1-C10, halogeno, nitro, ciian o, heterociclilo de 5-10 elementos, alquilo C1-C10, -NR7R8, arilo C6-C10,-s(O)n (alquilo C1-C10) donde n es un numero entero de o a 2, y -SO2NR7R8; R1 es H o alquilo C1-C10, donde de 1 a 3 carbonos de dicho alquilo estánopcionalmente remplazadosporun heteroátomo seleccionado entre O, S y N, estando dicho alquilo opcionalmente sustituido con 1 a 3 sustituyentesseleccionados independientemente entre el grupo conastituido por -C(O)O(alquilo C1-C10), alcoxi C1-C10, alcanoílo C1-C10, aloggeno , nitro, ciano, heterociclilode 5-10 elementos, alquilo C1-C10, -NR7R8, arilo C6-C10, -S(O)n(alquilo C1-C10) donde n es un numero entero de 0 a 2 y -SO2NR7R8; R2 es (i) H, R4, -C(O)R4,-C(O)OR4 o -(CR7R8)mR3 cuando X es -NR7-, o (ii) H, R4, o -(CR7R8)mR3 cuando X es -CR7R8-, donde para ambos (i) y (ii) m es un numero entero de 0a 6 y tantoThe compounds of formula I and the Pharmaceutically acceptable salts thereof are described, wherein R1, R2, R6 and X are as defined herein. Also described are pharmaceutical compositions containing the compounds of formula I in the treatment of bacterial and protozoal infections and to processes for the preparation of said compounds of formula I, wherein in said formula XVI ring, r and p are each independently a number integer from 1 to 3, q is 0 or 1 and X1 is -CH2-, O, S, -C (S) -, -SO2-, -CH = CH-, -CH (OH) CH (OH) -, or -NH-; and where the (CH2), and (CH2) p parts of said formula XVI ring are optionally substituted with 1 to 4 substituents and the nitrogen atom when X1 is -NH-is optionally substituted with 1 substituent, said optional substituents being independently selected from the group consisting of -C (O) O (C1-C10 alkyl), C1-C10 alkoxy, C1-C10 alkanoyl, halogen, nitro, cyan or, 5-10 membered heterocyclyl, C1-C10 alkyl, -NR7R8, C6 aryl -C10, -s (O) n (C1-C10 alkyl) where n is an integer from oa to 2, and -SO2NR7R8; R1 is H or C1-C10 alkyl, where from 1 to 3 carbons of said alkyl are optionally replaced by a heteroatom selected from O, S and N, said alkyl being optionally substituted with 1 to 3 substituents independently selected from the group consisting of -C (O) O (C1-C10 alkyl), C1-C10 alkoxy, C1-C10 alkanoyl, allogeneic, nitro, cyano, 5-10-membered heterocyclyl, C1-C10 alkyl, -NR7R8, C6-C10 aryl, -S (O) n ( C1-C10 alkyl) where n is an integer from 0 to 2 and -SO2NR7R8; R2 is (i) H, R4, -C (O) R4, -C (O) OR4 or - (CR7R8) mR3 when X is -NR7-, or (ii) H, R4, or - (CR7R8) mR3 when X is -CR7R8-, where for both (i) and (ii) m is an integer from 0 to 6 and both
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4934997P | 1997-06-11 | 1997-06-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR012244A1 true AR012244A1 (en) | 2000-09-27 |
Family
ID=21959341
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP980102703A AR012244A1 (en) | 1997-06-11 | 1998-06-09 | COMPOUNDS DERIVED FROM 9-OXIME ERYTHOMYCIN, PHARMACEUTICAL COMPOSITION CONTAINING THEM, PROCEDURE FOR THE TREATMENT OF A PROTOZOA BACTERIAL INFECTION, PROCEDURE FOR ITS PREPARATION. |
Country Status (31)
| Country | Link |
|---|---|
| EP (1) | EP0988308A1 (en) |
| JP (1) | JP2000513026A (en) |
| KR (1) | KR20010013660A (en) |
| CN (1) | CN1259135A (en) |
| AP (1) | AP9801253A0 (en) |
| AR (1) | AR012244A1 (en) |
| AU (1) | AU7226798A (en) |
| BG (1) | BG103947A (en) |
| BR (1) | BR9810021A (en) |
| CA (1) | CA2293335A1 (en) |
| CO (1) | CO4940506A1 (en) |
| CZ (1) | CZ9904388A3 (en) |
| EA (1) | EA199901016A1 (en) |
| GT (1) | GT199800074A (en) |
| HN (1) | HN1998000073A (en) |
| HR (1) | HRP980316A2 (en) |
| HU (1) | HUP0002252A3 (en) |
| ID (1) | ID24529A (en) |
| IL (1) | IL132767A0 (en) |
| IS (1) | IS5251A (en) |
| MA (1) | MA26505A1 (en) |
| NO (1) | NO996108L (en) |
| OA (1) | OA11225A (en) |
| PA (1) | PA8451801A1 (en) |
| PE (1) | PE79899A1 (en) |
| PL (1) | PL337606A1 (en) |
| TN (1) | TNSN98083A1 (en) |
| TR (1) | TR199902995T2 (en) |
| TW (1) | TW448174B (en) |
| WO (1) | WO1998056800A1 (en) |
| ZA (1) | ZA985018B (en) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HN1998000159A (en) * | 1997-10-29 | 1999-02-09 | Monsanto Co | DERIVATIVES OF 9- AMINO - 3 CETO ERITROMICINA |
| WO2000017218A1 (en) | 1998-09-22 | 2000-03-30 | Pfizer Products Inc. | Carbamate and carbazate ketolide antibiotics |
| FR2786188B1 (en) * | 1998-11-24 | 2002-10-31 | Hoechst Marion Roussel Inc | NOVEL ERYTHROMYCIN DERIVATIVES, THEIR PREPARATION PROCESS AND THEIR APPLICATION AS MEDICAMENTS |
| US6258785B1 (en) | 1998-12-02 | 2001-07-10 | Pfizer Inc. | Crystalline 9-E-(O-methyl)oxime of 11, 12-dideoxy-3-de(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribohexopyranosyloxy)-6-O-methyl-12,11-(iminocarbonyl-(2-(3-(4-(3-pyridinyl)1H-imadazol-1-yl)propyl)hydrazono))-3-oxoerythromycin |
| EP1298138B1 (en) * | 1998-12-10 | 2006-11-02 | Pfizer Products Inc. | Carbamate and Carbazate Ketolide Antibiotics |
| US6284732B1 (en) * | 1998-12-18 | 2001-09-04 | Bio-Rad Laboratories, Inc. | Peptides and peptide analogues designed from HFE protein and their uses in the treatment of iron overload diseases |
| WO2000063225A2 (en) * | 1999-04-16 | 2000-10-26 | Kosan Biosciences, Inc. | Macrolide antiinfective agents |
| OA11945A (en) | 1999-05-24 | 2006-04-13 | Pfizer Prod Inc | 13-Methyl erythromycin derivatives. |
| PT1181300E (en) * | 1999-06-07 | 2004-02-27 | Abbott Lab | DERIVATIVES 6-O-CARBAMATE OF CETOLID |
| ID27331A (en) * | 1999-09-29 | 2001-03-29 | Pfizer Prod Inc | MAKING ANTIBIOTIC-ANTIBIOTIC KETOLIDA CARBAMATE |
| EP1114826A3 (en) * | 1999-12-29 | 2001-10-31 | Pfizer Products Inc. | Novel antibacterial and prokinetic macrolides |
| EP1439186A3 (en) * | 1999-12-29 | 2004-11-03 | Pfizer Products Inc. | Intermediates for novel antibacterial and prokinetic macrolides |
| US6946446B2 (en) | 2000-02-24 | 2005-09-20 | Abbott Laboratories | Anti-infective agents useful against multidrug-resistant strains of bacteria |
| US6403776B1 (en) | 2000-07-05 | 2002-06-11 | Pfizer Inc. | Synthesis of carbamate ketolide antibiotics |
| WO2003090761A1 (en) * | 2002-04-25 | 2003-11-06 | Abbott Laboratories | 9-oxime macrolide antibacterials |
| TW200420573A (en) | 2002-09-26 | 2004-10-16 | Rib X Pharmaceuticals Inc | Bifunctional heterocyclic compounds and methods of making and using same |
| US7601695B2 (en) * | 2003-03-10 | 2009-10-13 | Optimer Pharmaceuticals, Inc. | Antibacterial agents |
| CN102816194A (en) | 2004-02-27 | 2012-12-12 | 瑞伯-X医药品有限公司 | Macrocyclic compounds and methods of making and using the same |
| WO2009055557A1 (en) | 2007-10-25 | 2009-04-30 | Cempra Pharmaceuticals, Inc. | Process for the preparation of macrolide antibacterial agents |
| EP3031460A1 (en) | 2008-10-24 | 2016-06-15 | Cempra Pharmaceuticals Inc. | Biodefenses using triazole-containing macrolides |
| US9937194B1 (en) | 2009-06-12 | 2018-04-10 | Cempra Pharmaceuticals, Inc. | Compounds and methods for treating inflammatory diseases |
| EP2475253B1 (en) | 2009-09-10 | 2016-10-26 | Cempra Pharmaceuticals, Inc. | Methods for treating malaria, tuberculosis and mac diseases |
| CN102146085B (en) * | 2010-02-09 | 2014-03-26 | 北京理工大学 | 9-oxime-ether ketolide derivative, and preparation method and medical composite thereof |
| DK2550286T3 (en) | 2010-03-22 | 2016-02-29 | Cempra Pharmaceuticals Inc | CRYSTALLINE FORMS OF A MACROLID AND APPLICATIONS THEREOF |
| US9051346B2 (en) | 2010-05-20 | 2015-06-09 | Cempra Pharmaceuticals, Inc. | Process for preparing triazole-containing ketolide antibiotics |
| KR20180110181A (en) | 2010-09-10 | 2018-10-08 | 셈프라 파마슈티컬스, 인크. | Hydrogen bond forming fluoro ketolides for treating diseases |
| MX2014011537A (en) | 2012-03-27 | 2015-02-10 | Cempra Pharmaceuticals Inc | Parenteral formulations for administering macrolide antibiotics. |
| RU2015138796A (en) | 2013-03-14 | 2017-04-19 | Семпра Фармасьютикалс, Инк. | METHODS AND COMPOSITIONS FOR TREATMENT OF RESPIRATORY DISEASES |
| EP2968384A4 (en) | 2013-03-15 | 2017-02-15 | Cempra Pharmaceuticals, Inc. | Convergent processes for preparing macrolide antibacterial agents |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL114589A (en) * | 1990-11-21 | 1999-12-22 | Roussel Uclaf | Intermediates for the preparation of erythromycin derivatives |
| US5527780A (en) * | 1992-11-05 | 1996-06-18 | Roussel Uclaf | Erythromycin derivatives |
| FR2718450B1 (en) * | 1994-04-08 | 1997-01-10 | Roussel Uclaf | New erythromycin derivatives, their preparation process and their use as drugs. |
-
1998
- 1998-05-15 IL IL13276798A patent/IL132767A0/en unknown
- 1998-05-15 BR BR9810021-1A patent/BR9810021A/en not_active IP Right Cessation
- 1998-05-15 WO PCT/IB1998/000741 patent/WO1998056800A1/en not_active Application Discontinuation
- 1998-05-15 CA CA002293335A patent/CA2293335A1/en not_active Abandoned
- 1998-05-15 HU HU0002252A patent/HUP0002252A3/en unknown
- 1998-05-15 EA EA199901016A patent/EA199901016A1/en unknown
- 1998-05-15 KR KR1019997011672A patent/KR20010013660A/en not_active Application Discontinuation
- 1998-05-15 PL PL98337606A patent/PL337606A1/en unknown
- 1998-05-15 CN CN98805848A patent/CN1259135A/en active Pending
- 1998-05-15 EP EP98919394A patent/EP0988308A1/en not_active Withdrawn
- 1998-05-15 JP JP11501928A patent/JP2000513026A/en active Pending
- 1998-05-15 AU AU72267/98A patent/AU7226798A/en not_active Abandoned
- 1998-05-15 CZ CZ19994388A patent/CZ9904388A3/en unknown
- 1998-05-15 ID IDW991570A patent/ID24529A/en unknown
- 1998-05-15 TR TR1999/02995T patent/TR199902995T2/en unknown
- 1998-05-19 HN HN1998000073A patent/HN1998000073A/en unknown
- 1998-05-21 PA PA19988451801A patent/PA8451801A1/en unknown
- 1998-06-04 AP APAP/P/1998/001253A patent/AP9801253A0/en unknown
- 1998-06-05 GT GT199800074A patent/GT199800074A/en unknown
- 1998-06-08 PE PE1998000470A patent/PE79899A1/en not_active Application Discontinuation
- 1998-06-08 TW TW087109086A patent/TW448174B/en active
- 1998-06-09 AR ARP980102703A patent/AR012244A1/en unknown
- 1998-06-10 TN TNTNSN98083A patent/TNSN98083A1/en unknown
- 1998-06-10 MA MA25105A patent/MA26505A1/en unknown
- 1998-06-10 ZA ZA9805018A patent/ZA985018B/en unknown
- 1998-06-11 HR HR60/049,349A patent/HRP980316A2/en not_active Application Discontinuation
- 1998-06-11 CO CO98033538A patent/CO4940506A1/en unknown
-
1999
- 1999-11-16 IS IS5251A patent/IS5251A/en unknown
- 1999-12-03 BG BG103947A patent/BG103947A/en unknown
- 1999-12-03 OA OA9900269A patent/OA11225A/en unknown
- 1999-12-10 NO NO996108A patent/NO996108L/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| PL337606A1 (en) | 2000-08-28 |
| EP0988308A1 (en) | 2000-03-29 |
| KR20010013660A (en) | 2001-02-26 |
| TW448174B (en) | 2001-08-01 |
| TR199902995T2 (en) | 2000-02-21 |
| NO996108L (en) | 2000-02-10 |
| NO996108D0 (en) | 1999-12-10 |
| TNSN98083A1 (en) | 2005-03-15 |
| EA199901016A1 (en) | 2000-06-26 |
| IL132767A0 (en) | 2001-03-19 |
| CZ9904388A3 (en) | 2002-10-16 |
| HUP0002252A3 (en) | 2002-01-28 |
| PE79899A1 (en) | 1999-08-25 |
| CA2293335A1 (en) | 1998-12-17 |
| BR9810021A (en) | 2000-09-19 |
| HN1998000073A (en) | 1999-01-08 |
| PA8451801A1 (en) | 2000-05-24 |
| IS5251A (en) | 1999-11-16 |
| BG103947A (en) | 2000-07-31 |
| HUP0002252A2 (en) | 2000-12-28 |
| JP2000513026A (en) | 2000-10-03 |
| GT199800074A (en) | 1999-11-27 |
| ID24529A (en) | 2000-07-20 |
| CN1259135A (en) | 2000-07-05 |
| ZA985018B (en) | 1999-12-10 |
| AU7226798A (en) | 1998-12-30 |
| MA26505A1 (en) | 2004-12-20 |
| WO1998056800A1 (en) | 1998-12-17 |
| OA11225A (en) | 2003-07-17 |
| HRP980316A2 (en) | 1999-04-30 |
| CO4940506A1 (en) | 2000-07-24 |
| AP9801253A0 (en) | 1999-12-04 |
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