Therapeutic Agent for Hematopoietic Tumor

1 . A therapeutic and/or prophylactic agent for a hematopoietic tumor, which comprises a thiadiazoline derivative represented by the general formula (I):

{wherein, n represents an integer of 1 to 3,

R 1 represents a hydrogen atom,

R 2 represents lower alkyl, or

R 1 and R 2 are combined together to represent alkylene,

R 3 represents lower alkyl,

R 4 represents a hydrogen atom,

NHSO 2 R 6 (wherein R 6 represents lower alkyl which may be substituted with one or two substituents selected from the group consisting of hydroxy, lower alkoxy, amino, hydroxyamino, (lower alkyl)amino, di-(lower alkyl)amino, N-hydroxy(lower alkyl)amino, amino-substituted (lower alkyl)thio, (lower alkyl)amino-substituted (lower alkyl)thio and di-(lower alkyl)amino-substituted (lower alkyl)thio, or lower alkenyl),

NHR 7 [wherein R 7 represents lower alkyl which may be substituted with one or two substituents selected from the group consisting of hydroxy, lower alkoxy, amino, (lower alkyl)amino and di-(lower alkyl)amino, COR 8 (wherein R 8 represents lower alkyl which may be substituted with one or two substituents selected from the group consisting of hydroxy, lower alkoxy, amino, (lower alkyl)amino, di-(lower alkyl)amino, carboxy, phenyl, hydroxyphenyl, imidazolyl, guanidyl, methylthio and (lower alkoxy)carbonylamino, a nitrogen-containing aliphatic heterocyclic group which may be substituted with (lower alkoxy)carbonyl or oxo, or lower alkoxy), or a hydrogen atom], or

CONHR 9 (wherein R 9 represents lower alkyl which may be substituted with one or two substituents selected from the group consisting of hydroxy, lower alkoxy, amino, (lower alkyl)amino and di-(lower alkyl)amino), and

R 5 represents aryl which may be substituted with one to three substituents selected from the group consisting of halogen, hydroxy, lower alkoxy, nitro, amino, cyano and carboxy}, or a pharmaceutically acceptable salt thereof.

2 . The therapeutic and/or prophylactic agent according to claim 1 , wherein the thiadiazoline derivative is a thiadiazoline derivative represented by the following formula (II):

(wherein R 1 , R 2 , R 3 , R 4 , R 5 , and n have the same meanings as those mentioned above), which shows a negative value as a specific rotation at 20° for sodium D line (wavelength: 589.3 nm) when the thiadiazoline derivative or the pharmaceutically acceptable salt thereof is dissolved in methanol.

3 . The therapeutic and/or prophylactic agent according to claim 1 , wherein R 5 is phenyl.

4 . The therapeutic and/or prophylactic agent according to claim 1 , wherein R 3 is methyl, ethyl, isopropyl, or tert-butyl.

5 . The therapeutic and/or prophylactic agent according to claim 1 , wherein R 1 is a hydrogen atom.

6 . The therapeutic and/or prophylactic agent according to claim 1 , wherein R 2 is methyl, or tert-butyl.

7 . The therapeutic and/or prophylactic agent according to claim 1 , wherein R 1 and R 2 are combined together to form trimethylene, or tetramethylene.

8 . The therapeutic and/or prophylactic agent according to claim 1 , wherein R 4 is NHSO 2 R 6 (wherein R 6 has the same meaning as that mentioned above).

9 . The therapeutic and/or prophylactic agent according to claim 1 , wherein R 4 is CONHR 9 (wherein R 9 has the same meaning as that mentioned above).

10 . The therapeutic and/or prophylactic agent according to claim 1 , wherein n is 1 or 2.

11 . The therapeutic and/or prophylactic agent according to claim 2 , wherein the thiadiazoline derivative is a thiadiazoline derivative represented by any one of the following formulas (a) to (q).

12 . The therapeutic and/or prophylactic agent according to claim 1 , wherein the hematopoietic tumor is a tumor selected from the group consisting of leukemia, lymphoma, multiple myeloma, plasmocytoma, myelodysplastic syndrome, and chronic myeloproliferative disorder.

13 . The therapeutic and/or prophylactic agent according to claim 1 , wherein the hematopoietic tumor is a tumor selected from the group consisting of acute myeloid leukemia, acute lymphoblastic leukemia, chronic myeloid leukemia, chronic lymphoblastic leukemia, plasma cell leukemia, Hodgkin's lymphoma, non-Hodgkin's lymphoma, adult T-cell leukemia/lymphoma, multiple myeloma, plasmocytoma, myelodysplastic syndrome, and chronic myeloproliferative disorder.

14 . A method for therapeutic and/or prophylactic treatment of a hematopoietic tumor, which comprises administering an effective amount of the thiadiazoline derivative or the pharmaceutically acceptable salt thereof described in claim 1 .

15 . The method according to claim 14 , wherein the hematopoietic tumor is a tumor selected from the group consisting of leukemia, lymphoma, multiple myeloma, plasmocytoma, myelodysplastic syndrome, and chronic myeloproliferative disorder.

16 . The method according to claim 14 , wherein the hematopoietic tumor is a tumor selected from the group consisting of acute myeloid leukemia, acute lymphoblastic leukemia, chronic myeloid leukemia, chronic lymphoblastic leukemia, plasma cell leukemia, Hodgkin's lymphoma, non-Hodgkin's lymphoma, adult T-cell leukemia/lymphoma, multiple myeloma, plasmocytoma, myelodysplastic syndrome, and chronic myeloproliferative disorder.

17 . Use of the thiadiazoline derivative or the pharmaceutically acceptable salt thereof described in claim 1 for the manufacture of a therapeutic and/or prophylactic agent for a hematopoietic tumor.

18 . The use according to claim 17 , wherein the hematopoietic tumor is a tumor selected from the group consisting of leukemia, lymphoma, multiple myeloma, plasmocytoma, myelodysplastic syndrome, and chronic myeloproliferative disorder.

19 . The use according to claim 17 , wherein the hematopoietic tumor is a tumor selected from the group consisting of acute myeloid leukemia, acute lymphoblastic leukemia, chronic myeloid leukemia, chronic lymphoblastic leukemia, plasma cell leukemia, Hodgkin's lymphoma, non-Hodgkin's lymphoma, adult T-cell leukemia/lymphoma, multiple myeloma, plasmocytoma, myelodysplastic syndrome, and chronic myeloproliferative disorder.