EP0353678A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
FR-901154 and FR-901155 substances, a process for their production
Assignee: Astellas Pharma Inc
•
Filing: 1989-07-29
•
Granted: —
•
Expires: 2009-07-29
Abstract
Abstract The invention relates to novel compounds, FR-901154 and FR-901155 substances which have pharmacological activities such as immunosuppressive activity, antimicrobial activity, and the like, to a process for their production, to a pharmaceutical composition containing the same and to a use thereof as a medicament.
Inventors
- 👤 Masakuni Okuhara
- 👤 Toshio Goto
- 👤 Hiroshi Hatanaka
- 👤 Seiichi 72-7 Aza-Icchobata Yuasa
- 👤 Isami Nakatani
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-02 00:23
CPC Classifications
C; C12; C12P; C12P19/00; C12P19/44; C12P19/445; A; A61; A61P; A61P31/00; A61P31/10; A61P37/00; A61P37/02; A61P37/06; C07; C07H; C07H19/00; C07H19/01
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
407 words
A compound selected from FR-901154 substance and FR-901155 substance, wherein 1) FR-901154 Substance having the following physical and chemical properties; (1) Form and Color: white powder (2) Mass Spectrum: FAB-MS: m/z 812 (M+Na) (3) Molecular Formula: C₄₃H₆₇NO₁₂ (4) Elemental Analysis for C₄₃H₆₇NO₁₂.H₂O: C H N Found : 63.80 %, 8.81 %, 1.79 % Calcd.: 63.92 % 8.61 % 1.73 % (5) Color Reaction: Positive: cerium sulfate reaction, sulfuric acid reaction, Ehrlich reaction, Dragendorff reaction and iodine vapor reaction Negative: ferric chloride reaction, ninhydrin reaction and Molish reaction (6) Solubility: Soluble : methanol, ethanol, acetone, ethyl acetate, chloroform, diethyl ether, benzene and acetonitrile Sparingly Soluble: n-hexane and petroleum ether Insoluble: water (7) Melting Point: 96 - 97 °C (8) Specific Rotation: [α] 23 D : -65° (c = 1.7, CHCl₃) (9) Ultraviolet Absorption Spectrum: end absorption (10) Infrared Absorption Spectrum: 3570, 3500, 2920, 2860, 2820, 1740, 1710, 1700, 1640, 1460, 1450, 1380, 1340, 1280, 1210, 1190, 1170, 1140, 1100, 1090, 1050, 1010, 1000, 990, 960, 920 cm⁻¹ (11) ¹³C Nuclear Magnetic Resonance Spectrum: (12) ¹H Nuclear Magnetic Resonance Spectrum: the chart of which being shown in Figure 1, (13) Thin Layer Chromatography: Stationary Phase Developing Solvent Rf Values silica gel plate ethyl acetate 0.22 (14) Property of the Substance: neutral substance and 2)FR-901155 Substance having the following physical and chemical properties; (1) Form and Color: white powder (2) Mass Spectrum: FAB-MS: m/z 810 (M+Na) (3) Molecular Formula: C₄₃H₆₅NO₁₂ (4) Elemental Analysis for C₄₃H₆₅NO₁₂: C H N Found : 65.27 % 8.88 % 1.63 % Calcd.: 65.54 % 8.31 % 1.78 % (5) Color Reaction: Positive: cerium sulfate reaction, sulfuric acid reaction, Ehrlich reaction, Dragendorff reaction and iodine vapor reaction Negative: ferric chloride reaction, ninhydrin reaction and Molish reaction (6) Solubility: Soluble : methanol, ethanol, acetone, ethyl acetate, chloroform, diethyl ether, benzene and acetonitrile Sparingly Soluble: n-hexane and petroleum ether Insoluble: water (7) Melting Point: 76 - 81 °C (8) Specific Rotation: [α] 23 D : -53° (c = 1.8, CHCl₃) (9) Ultraviolet Absorption Spectrum: end absorption (10) Infrared Absorption Spectrum: 3500, 2920, 2870, 2820, 1740, 1710, 1640, 1460, 1450, 1380, 1340, 1320, 1280, 1230, 1190, 1170, 1140, 1100, 1040, 1000, 990, 960, 910 cm⁻¹ (11) ¹³C Nuclear Magnetic Resonance Spectrum: (12) ¹H Nuclear Magnetic Resonance Spectrum: the chart of which being shown in Figure 2, (13) Thin Layer Chromatography: Stationary Phase Developing Solvent Rf Value silica gel plate ethyl acetate 0.64 (14) Property of the Substance: neutral substance.
Claim 2
Dependent Claim
407 words
A compound selected from FR-901154 substance and FR-901155 substance, wherein 1) FR-901154 Substance having the following physical and chemical properties; (1) Form and Color: white powder (2) Mass Spectrum: FAB-MS: m/z 812 (M+Na) (3) Molecular Formula: C₄₃H₆₇NO₁₂ (4) Elemental Analysis for C₄₃H₆₇NO₁₂.H₂O: C H N Found : 63.80 %, 8.81 %, 1.79 % Calcd.: 63.92 % 8.61 % 1.73 % (5) Color Reaction: Positive: cerium sulfate reaction, sulfuric acid reaction, Ehrlich reaction, Dragendorff reaction and iodine vapor reaction Negative: ferric chloride reaction, ninhydrin reaction and Molish reaction (6) Solubility: Soluble : methanol, ethanol, acetone, ethyl acetate, chloroform, diethyl ether, benzene and acetonitrile Sparingly Soluble: n-hexane and petroleum ether Insoluble: water (7) Melting Point: 96 - 97 °C (8) Specific Rotation: [α] 23 D : -65° (c = 1.7, CHCl₃) (9) Ultraviolet Absorption Spectrum: end absorption (10) Infrared Absorption Spectrum: 3570, 3500, 2920, 2860, 2820, 1740, 1710, 1700, 1640, 1460, 1450, 1380, 1340, 1280, 1210, 1190, 1170, 1140, 1100, 1090, 1050, 1010, 1000, 990, 960, 920 cm⁻¹ (11) ¹³C Nuclear Magnetic Resonance Spectrum: (12) ¹H Nuclear Magnetic Resonance Spectrum: the chart of which being shown in Figure 1, (13) Thin Layer Chromatography: Stationary Phase Developing Solvent Rf Values silica gel plate ethyl acetate 0.22 (14) Property of the Substance: neutral substance and 2)FR-901155 Substance having the following physical and chemical properties; (1) Form and Color: white powder (2) Mass Spectrum: FAB-MS: m/z 810 (M+Na) (3) Molecular Formula: C₄₃H₆₅NO₁₂ (4) Elemental Analysis for C₄₃H₆₅NO₁₂: C H N Found : 65.27 % 8.88 % 1.63 % Calcd.: 65.54 % 8.31 % 1.78 % (5) Color Reaction: Positive: cerium sulfate reaction, sulfuric acid reaction, Ehrlich reaction, Dragendorff reaction and iodine vapor reaction Negative: ferric chloride reaction, ninhydrin reaction and Molish reaction (6) Solubility: Soluble : methanol, ethanol, acetone, ethyl acetate, chloroform, diethyl ether, benzene and acetonitrile Sparingly Soluble: n-hexane and petroleum ether Insoluble: water (7) Melting Point: 76 - 81 °C (8) Specific Rotation: [α] 23 D : -53° (c = 1.8, CHCl₃) (9) Ultraviolet Absorption Spectrum: end absorption (10) Infrared Absorption Spectrum: 3500, 2920, 2870, 2820, 1740, 1710, 1640, 1460, 1450, 1380, 1340, 1320, 1280, 1230, 1190, 1170, 1140, 1100, 1040, 1000, 990, 960, 910 cm⁻¹ (11) ¹³C Nuclear Magnetic Resonance Spectrum: (12) ¹H Nuclear Magnetic Resonance Spectrum: the chart of which being shown in Figure 2, (13) Thin Layer Chromatography: Stationary Phase Developing Solvent Rf Value silica gel plate ethyl acetate 0.64 (14) Property of the Substance: neutral substance.
Claim 3
Dependent Claim
41 words
A process for production of a compound selected from FR-901154 substance and FR-901155 substance which comprises culturing a FR-901154 substance- and/or FR-901155 substance-producing strain belonging to the genus Streptomyces in a nutrient medium and recovering the FR-901154 substance and/or FR-901155 substance.
Claim 4
Dependent Claim
41 words
A process for production of a compound selected from FR-901154 substance and FR-901155 substance which comprises culturing a FR-901154 substance- and/or FR-901155 substance-producing strain belonging to the genus Streptomyces in a nutrient medium and recovering the FR-901154 substance and/or FR-901155 substance.
Claim 5
Dependent Claim
16 words
A pharmaceutical composition containing a compound selected from FR-901154 substance and FR-901155 substance as an ingredient.
Claim 6
Dependent Claim
16 words
A pharmaceutical composition containing a compound selected from FR-901154 substance and FR-901155 substance as an ingredient.
Claim 7
Dependent Claim
15 words
A use of a compound selected from FR-901154 substance and FR-901155 substance as a medicament.
Claim 8
Dependent Claim
15 words
A use of a compound selected from FR-901154 substance and FR-901155 substance as a medicament.
Claim 9
Independent Claim
35 words
A method for treating or preventing rejection by transplantation, graft-versus-host diseases by medulla ossium, autoimmune diseases and infectious diseases which comprises administering a compound selected from FR-901154 substance and FR-901155 substance to human or animal.
Claim 10
Independent Claim
35 words
A method for treating or preventing rejection by transplantation, graft-versus-host diseases by medulla ossium, autoimmune diseases and infectious diseases which comprises administering a compound selected from FR-901154 substance and FR-901155 substance to human or animal.
Claim 11
Dependent Claim
27 words
A process for production of FR-901156 substance which comprises culturing a FR-901156 substance-producing strain belonging to the genus Streptomyces in a nutrient medium and recovering the same.
Claim 12
Dependent Claim
27 words
A process for production of FR-901156 substance which comprises culturing a FR-901156 substance-producing strain belonging to the genus Streptomyces in a nutrient medium and recovering the same.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
Maintenance schedule is calculated for granted US utility patents.