Pyrimidyl cyclopentanes as akt/protein kinase inhibitors

IPC classes for russian patent Pyrimidyl cyclopentanes as akt/protein kinase inhibitors (RU 2486181):

C07D409/14 - containing three or more hetero rings

C07D403/14 - containing three or more hetero rings

C07D401/12 - linked by a chain containing hetero atoms as chain links

A61K35 - Medicinal preparations containing material or reaction products thereof with undetermined constitution

A61K31/5377 -

A61K31/517 -

Another patents in same IPC classes:

Pyrimidyl cyclopentanes as akt-protein kinase inhibitors / 2486178

Present invention refers to new compounds of formula I, enantiomers and pharmaceutically acceptable salts thereof which have selective inhibitory action on AKT protein kinase, in particular protein kinase B. In formula I: A represents R¹ and R^1a are independently specified in H, Me, Et. vinyl, CF₃, CHF₂ or CH₂F:R₂ represents H, OH, OMe or F; R^2a represents H, Me or F; R³ represents H. Me. Et or CF₃; G represents phenyl optionally substituted by one to four groups R^c, or 5-6-member heteroaryl containing one heteroatom specified in sulphur optionally substituted by halogen; R⁵ and R⁶ independently represent H, OCH₃, C₃-C₆-cycloalkyl independently substituted by F, OH, C₁-C₃alkyl or O(C₁-C₃alkyl), 4-6-member heterocyclyl containing one heteroatom specified in nitrogen optionally substituted by F, OH, C₁-C₃alkyl, cyclopropylmethyl or -C(=O)(C₁-C₃alkyl), or C₁-C₆-alkyl optionally substituted by one or more groups independently specified in OH, oxo O(C₁-C₆-alkyl), CN, F, NH₂. NH(C₁-C₆-alkyl), O(C₁-C₆-alkyl)₂. cyclopropyl. phenyl, imidazolyl, piperidinyl, pyrrolidinyl, morpholinyl, tetrahydrofuranyl, oxetanil or tetrahydropyranyl. The other radical values are specified in the patent claim.

Carboxamide compounds and use thereof as calpain inhibitors / 2485114

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3,8-diaminotetrahydroquinoline derivative / 2482117

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Cyclopenta(d)pyrimidines as protein kinase akt inhibitors / 2481336

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Hydroxylated and methoxylated cyclopenta[b]pyrimidines as protein kinase inhibitors / 2478632

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Substituted n-phenylbipyrrolidine carboxamides and therapeutic use thereof / 2477719

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Polycyclic indazole-derivatives and their application as erk inhibitors for cancer treatment / 2475484

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Amino compounds and medical application thereof / 2470929

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Pyrimidyl cyclopentanes as akt-protein kinase inhibitors / 2486178

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Invention relates to a method of producing substituted pyrimidin-5-yl carboxylic acids of formula I and can be used in organic chemistry. The method is realised by reacting N-substituted guanidines and hetarylamidines with ethoxymethylene derivatives of 1,3-ketoesters according to a scheme given below (where the substitutes are as defined in the claim).

Method of producing benzimidazoles / 2482118

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Crystalline modifications of 3-(1h-indol-3-yl)-4-(4-methylpiperazin-1-yl)quinazolin-4-yl)pyrrol-2,5-dione / 2481341

Present invention refers to novel crystalline forms of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrol-2,5-dione acetate salt, their use for the treating the diseases mediated by T-lymphocytes or PKC, to a pharmaceutical compositions thereof, and a method for preparing them. The presented crystalline forms have: a strong diffraction peak at the angle of 2θ making 21.5° for the A form, or a strong diffraction peak at the angle of 2θ making 9.7° for the B form. The mentioned crystalline forms can be prepared by dissolving 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrol-2,5-dione in 2-propanol at higher temperature, and then cooling after salt formation for preparing the A form, or dissolving 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrol-2,5-dione in ethyl acetate at higher temperature and then cooling after salt formation for preparing the B form.

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Phenylpyrazol derivatives / 2480456

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Method of producing n, n'-bis(β-piperazinoethyl)-2-aryl(alkyl)imidazolidines / 2479583

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Heteroaryl pyrrolidinyl and piperidinyl ketone derivatives / 2479575

Invention relates to a compound of formula I or use thereof to prepare a medicine for treating depression, anxiety or both: or pharmaceutically acceptable salts thereof, where m is 0-3; n is 0-2; Ar is: optionally substituted indolyl; optionally substituted indazolyl; azaindolyl; 2,3-dihydro-indolyl; 1,3-dihydro-indol-2-one-yl; optionally substituted benzothiophenyl; benzothiazolyl; benzisothiazolyl; optionally substituted quinolinyl; 1,2,3,4-tetrahydroquinolinyl; quinolin-2-one-yl; optionally substituted naphthalenyl; optionally substituted pyridinyl; optionally substituted thiophenyl or optionally substituted phenyl; R¹ is: C_1-6alkyl; hetero-C_1-6alkyl; halo-C_1-6alkyl; halo-C_2-6alkenyl; C_3-7cycloalkyl; C_3-7cycloalkyl-C_1-6alkyl; C_1-6alkyl-C_3-6cycloalkyl-C_1-6alkyl; C_1-6alkoxy; C_1-6alkylsulphonyl; phenyl; tetrahydropyranyl-C_1-6alkyl; phenyl-C_1-3alkyl, where the phenyl part is optionally substituted; heteroaryl-C_1-3alkyl; R² is: hydrogen or C_1-6alkyl; and each R^a and R^b is independently: hydrogen; C_1-6alkyl; C_1-6alkoxy; halo; hydroxy or oxo; or R^a and R^b together form C_1-2alkylene; under the condition that, when m is 1, n is 2, and Ar is an optionally substituted phenyl, then R¹ is not methyl or ethyl, and where optionally substituted denotes 1-3 substitutes selected from alkyl, cycloalkyl, alkoxy, halo, haloalkyl, haloalkoxy, cyano, amino, acylamino, monoalkylamino, dialkylamino, hydroxyalkyl, alkoxyalkyl, pyrazolyl, -(CH₂)_q-S(O)_rR^f; -(CH₂)_q-C(=O)-NR^gR^h; -(CH₂)_q-N(R^f)-C(=O)-Rⁱ or -(CH₂)_q-C(=O)-Rⁱ; where q is 0, r is 0 or 2, each R^f, R^g and R^h is independently hydrogen or alkyl, and each Rⁱ is independently alkyl, and where "heteroaryl" denotes a monocyclic radical having 5-6 ring atoms, including 1-2 ring heteroatoms selected from N or S, wherein the rest of the ring atoms are C atoms, "heteroalkyl" denotes an alkyl radical, including a branched C₄-C₇-alkyl, where one hydrogen atom is substituted by substitutes selected from a group consisting of -OR^a, -NR^bH, based on the assumption that the bonding of heteroalkyl radical occurs through a carbon atom, where R^a is hydrogen or C_1-6alkyl, R^b is C_1-6alkyl. Pharmaceutical compositions based on said compound are also disclosed.

1, 2, 4-triazine-3, 5-dione derivatives for treating disorders reacting on dopamine d<sub>3</sub> receptor modulation

1, 2, 4-triazine-3, 5-dione derivatives for treating disorders reacting on dopamine d₃ receptor modulation / 2478633

There are described new 1,2,4-triazine-3,5-dione derivatives of general formula (I) wherein A is a saturated hydrocarbon chain with chain length 4 to 6 atoms; R¹ and R² are optionally hydrogen or C₁-C₃-alkyl; R³ is branched C₄-C₆-alkyl or C₃-C₆-cycloalkyl; R⁴ - C₁-C₆-alkyl, C₃-C₆-cycloalkyl or fluorinated C₁-C₃-alkyl, their physiologically acceptable salts and N-oxides, and a pharmaceutical composition containing them.

Hydroxylated and methoxylated cyclopenta[b]pyrimidines as protein kinase inhibitors / 2478632

Pyrimidyl cyclopentanes as akt-protein kinase inhibitors / 2486178

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula I, enantiomers and pharmaceutically acceptable salts thereof having the properties of AKT/protein kinase inhibitors. In formula 1 G represents phenyl, naphthalene, 5-member heteroaryl with 1 sulphur atom in a ring or 9-member bicyclic heteroaryl specified in indolyl wherein phenyl, naphthalene, 5-member heteroaryl is optionally substituted by one of three R^a groups; R¹ and R^1a are independently specified in H, Me, Et, -CH₂OH, CF₃, CHF₂ or CH₂F; R² represents H, -OH, -OMe or F; R^2a representsH, Me or F; R³ represents H, Me, Et; R⁴ represents H, 6-member heterocyclyl containing an oxygen atom as a heteroatom, cyclopropyl methyl or C₁-C₄ alkyl is optionally substituted F,-OH or -O(C₁-C₃ alkyl); R⁵ and R^5a are independently specified in H and C₁-C₄ alkyl, or R⁵ and R^5a together with an atom whereto attached form a carbonyl group or 5-6-member cycloalkyl; each R^a independently represents halogen, C₁-C₆-alkyl, C₃-C₆-cycloalkyl,-O-(C₁-C₆-alkyl), CF₃, CN, phenyl, pyrazole, CH₂F, CHF₂, -OCH₂F, -OCHF₂, -OH, -SO₂(C₁-C₆-alkyl), C(O)NH₂; and j represents 1 or 2; and provided j represents 2, j-ring carbon atom, opposite NR⁴, may be substituted by heteroatom O.

EFFECT: compounds may be used for treating hyperproliferative diseases, such as cancer.

35 cl, 9 dwg, 4 tbl, 141 ex

The text descriptions are given in facsimile form.

1. The compound of the formula

and enantiomers and pharmaceutically-acceptable salts, where:
G represents a phenyl, naphthalene, 5-membered heteroaryl 1 sulfur atom in the ring or 9-membered bicyclic heteroaryl selected from indolyl, in which the phenyl, naphthalene, 5-membered heteroaryl is optionally substituted with one to three R^agroups;
R¹and R^1aare independently selected from H, Me, Et, -CH₂HE,CF ₃, CHF₂or CH₂F;
R²represents H, -OH, -OMe or F;
R^2arepresents H, Me or F;
R³represents H, Me, Et;
R⁴represents H, 6-membered heterocycle containing an oxygen atom as a heteroatom, cyclopropylmethyl or₁-C₄alkyl, optionally substituted by F,
-HE or-O(C₁-C₃by alkyl);
R⁵and R^5aare independently selected from H and C₁-C₄the alkyl, or R⁵and R^5atogether with the atom to which they are attached, form a carbonyl group or a 5-6-membered cycloalkyl;
each R^arepresents independently halogen, C₁-C₆-alkyl, C₃-C₆-cycloalkyl, -O-(C₁-C₆-alkyl), CF₃, CN, phenyl, pyrazole, CH₂F, CHF₂, -OCH₂F, -OCHF₂-IT, -SO₂(C₁-C₆-alkyl), C(O)NH₂;
j represents 1 or 2; and when j is 2, j is a ring carbon atom, opposite NR⁴may be substituted by a heteroatom O.

2. The compound according to claim 1, in which:
G represents a phenyl, optionally substituted with one to three R^agroups, or 5-membered heteroaryl, 1 sulfur atom in the ring, optionally substituted with halogen;
R¹and R^1aare independently selected from H, Me, Et, -CH₂HE, CF₃, CHF₂and the and CH ₂F;
R²represents H, -OH, -OMe or F;
R^2arepresents H, Me or F;
R³represents H, Me, Et;
R⁴represents H, 6-membered heterocycle containing an oxygen atom as a heteroatom, cyclopropylmethyl or₁-C₄alkyl, optionally substituted by F,
-HE or-O(C₁-C₃by alkyl);
R⁵and R^5aare independently selected from H and C₁-C₄the alkyl, or R⁵and R^5atogether with the atom to which they are attached, form a 5-6-membered cycloalkyl;
each R^arepresents independently halogen, C₁-C₆-alkyl, C₃-C₆-cycloalkyl, -O-(C₁-C₆-alkyl), CF₃, CN, CH₂F, CHF₂, -OCH₂F, -OCHF₂-IT, -SO₂(C₁-C₆-alkyl), C(O)NH₂;
j represents 1 or 2; and when j is 2, j is a ring carbon atom, opposite NR⁴may be substituted by a heteroatom O.

3. The compound according to claim 2, in which R²selected from H, -OH, -OMe or F;
R^2aselected from H, Me or F;
R⁴represents H, 6-membered heterocycle containing an oxygen atom as a heteroatom, cyclopropylmethyl or C₁-C₄alkyl, optionally substituted
-HE or-O(C₁-C₃by alkyl);
R⁵and R^5aare independently chosen is C N and C ₁-C₄of alkyl; and
j represents 1 or 2.

4. The compound according to claim 1, in which R³represents N.

5. The compound according to claim 4, in which R⁵represents N.

6. The compound according to claim 5, in which R^5arepresents N.

7. The compound according to claim 4, in which R⁵represents methyl.

8. The connection according to claim 7, in which R^5arepresents methyl.

9. The compound according to claim 4, in which R⁵represents ethyl.

10. The connection according to claim 9, in which R^5arepresents ethyl.

11. The compound according to claim 4, in which R⁵and R^5atogether with the atom to which they are attached, form a 5-6-membered cycloalkyl having the structure

in which k represents 1 or 2, G, R⁴and j have values such as defined according to claim 1 and the wavy line is where the structure is attached to the desired piperazine of formula I.

12. The compound according to claim 4, in which R¹represents methyl.

13. The connection section 12, in which R¹represents methyl optionally in the (R) configuration.

14. The connection 13, in which R^1arepresents N.

15. Connection 4, in which R^1arepresents N.

16. The connection indicated in paragraph 15, in which R²is a F.

17. The connection indicated in paragraph 15, in which R²represents the t a HE.

18. The compound according to claim 4, in which G represents 4-chlorophenyl, 4-bromophenyl, 4-cyclopropylmethyl, 4-triptoreline, 4-cyanophenyl, 4-benzamide, 4-(methylsulphonyl)phenyl, 2-fluoro-4-triptoreline, 3-fluoro-4-chlorophenyl, 3-fluoro-4-triptoreline, 3-fluoro-4-cyanophenyl, 4-chloro-2,5-differenl, 4-chloro-2-forfinal, 4-bromo-2-forfinal, 4-bromo-3-forfinal, 3-chlorophenyl, 2-fluoro-4-were, 2,4-dichlorophenyl, 3,4-dichlorophenyl, 4-forfinal, 4-fluoro-3-triptoreline, 3-bromophenyl, 3-triptoreline, 3-forfinal, 2-fluoro-4-methoxyphenyl, 4-(1H-pyrazole-4-yl)phenyl, biphenyl-4-yl, 4-tert-butylphenyl, 2,3-debtor-4-(trifluoromethyl)phenyl, 2-fluoro-3-(trifluoromethyl)phenyl, 2-fluoro-5-(trifluoromethyl)phenyl.

19. The compound according to claim 4, in which R⁴choose from among methyl, ethyl, isopropyl, isobutyl, CH₂-CH₂-OH, CH₂CH₂CH₂OH, CH₂C(CH₃)₂HE and CH₂CH₂OCH₃.

20. The compound according to claim 4, in which R⁴is cyclopropylmethyl.

21. The compound according to claim 4, in which R⁴represents N.

22. The compound according to claim 4, in which j represents 1.

23. The compound according to claim 4, in which j represents 2.

24. The compound according to claim 1, having the structure

25. The connection point 24, having the structure

26. The connection point 24, having the structure

27. The connection point 24, having the structure

28. The connection point 24, having the structure

29. The connection point 24, having the structure

30. The connection point 24, having the structure

31. The connection point 24, having the structure

32. The connection point 24, having the structure

33. The connection point 24, having the structure

34. The connection point 24, having the structure

35. Pharmaceutical composition having the properties of the inhibitor ACT-protein kinases containing an effective amount of a compound according to claim 1 together with a pharmaceutically acceptable carrier or excipient.