30 results about "Pyrrolopyridazine" patented technology

Compounds, pharmaceutical compositions and methods that are useful in the treatment or prevention of metabolic and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the activity of proteins involved in lipid metabolism and cell proliferation.

Pyrrolopyridazine derivatives having the general formula. In the above formula, R1 represents a C2-C6alkenyl-group, a halogeno-C2-C6-alkenyl group, a C6-C10 aryl-C2-C6-alkenyl group, a C2-C6 alkynyl group, a C3-C7 cycloalkyl group, a C3-C7 cycloalkyl-C1-C6-alkyl group, a C5-C7 cycloalkenyl-C1-C6-alkyl group or a halogeno-C1-C6-alkyl group; R2 and R3 are the same or different and each represents a hydrogen atom, a C1-C6 alkyl group or a C6-C10 aryl group; R4 represents a hydrogen atom or a C1-C6 alkyl group; R5 represents a C6-C10 aryl group or a 5-10 membered heteroaryl group comtaining heteroatom(s) selected from nitrogen, oxygen and sulfur;

The invention discloses pyrrolopyridazine compounds used for treating or preventing HIV (human immunodeficiency virus) infection or other virus infections. The compounds can be used for as inhibitors for inhibiting HIV replication and can be used with other treatment drugs (particularly other antiviral drugs). Specifically, the invention discloses compounds for inhibiting HIV replication, a drug containing the compounds and a method for treating retrovirus infection through the compounds, for example, HIV infection. More specifically, the invention discloses an integrase allosteric inhibitor.

Disclosed are compounds of Formula (I), and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.

A pyrrolopyridazine compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. (In the formula, R<1> is C2-6 alkenyl, C2-6 halogenoalkenyl, optionally substituted C3-7 cycloalkyl, or optionally substituted C1-6 alkyl substituted by C3-7 cycloalkyl; R<2> is C1-6 alkyl; R<3> is hydroxymethyl, C2-6 aliphatic acyloxymethyl, optionally substituted (C6-10 aryl)carbonyloxymethyl, (C1-6 alkoxy)carbonyloxymethyl, formyl, carboxy, (C1-6 alkoxy)carbonyl, or optionally substituted (C6-10 aryl)oxycarbonyl; R<4> is optionally substituted C6-10 aryl; and A is imino, oxygen, or sulfur.) The pyrrolopyridazine compound is highly effective in inhibiting the secretion of gastric hydrochloric acid, protecting the gastric mucosa, and the like. It is useful as a medicine, especially a preventive / remedy for ulcerative diseases.

The present invention discloses a pyrrolopyridazinone compound represented by the formula (1):useful, for example, as an anti-inflammatory agent or an inhibitor of respiratory tract contraction.

The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.

The present invention discloses a pyrrolopyridazinone compound represented by the formula (1):wherein R1 represents C1-C2 alkyl group or halogeno C1-C2 alkyl group,R2 repersents C3-C5 cycloalkyl group, (C3-C5 cycloalkyl)C1-C2 alkyl group or C1-C3 alkyl group,R3 represents hydrogen atom, or methylene group or cis-vinylene group for forming substituted oxygen-containing hetero ring in combination with group —O—R2,R4 represents hydrogen atom, halogen atom, C1-C8 alkyl group, C2-C6 alkenyl group, C2-C6 alkynyl group, hydroxy C3-C6 alkenyl group, hydroxy C3-C6 alkynyl group, C1-C6 alkyl group substituted by substituent(s) selected from Substituent group (a), C3-C6 cycloalkyl group which may be substituted by substituent(s) selected from Substituent group (b), “C1-C3 alkyl group which is substituted by C3-C6 cycloalkyl group which may be substituted by substituent(s) selected from Substituent group (b), and which may be substituted by a hydroxy group”, an aromatic ring group or heteroaromatic ring group each of which may be substituted by a substituent(s) selected from Substituent group (c) or “C1-C2 alkyl group which is substituted by aromatic ring group or heteroaromatic ring group each of which may be substituted by group(s) selected from Substituent group (c), and which may be substituted by a hydroxy group”,Substituent group (a) represents a halogen atom, hydroxy group, cyano group, carboxy group, C1-C5 alkoxy group, halogeno C1-C4 alkoxy group, C3-C6 cycloalkoxy group, (C3-C6 cycloalkyl)C1-C2 alkoxy group, C1-C4 alkoxycarbonyl group, C2-C4 alkanoyl group, C2-C4 alkanoyloxy group or C1-C4 alkyl-substituted amino group,Substituent group (b) represents a hydroxy group or a halogen atom,Substituent group (c) represents a halogen atom, a hydroxy group, a cyano group, a nitro group, a carboxy group, C1-C5 alkoxy group, C1-C4 alkoxycarbonyl group, C2-C4 alkanoyloxy group, C1-C4 alkyl-substituted amino group or a C1-C4 alkyl group which may be substituted by a substituent(s) selected from the group consisting of (a halogen atom, a hydroxy group and a carboxy group),or a pharmaceutically acceptable salt thereof.

A solid dispersion, a method for preparing same, and a solid preparation including the solid dispersion. The solid dispersion contains (R)-4-amino-1-(1-(but-2-ynylacyl)pyrrolidin-3-yl)-3-(4-(2,6-difluorophenoxy)phenyl)-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazine-7-one or a pharmaceutically acceptable salt thereof, and a carrier material. The carrier material is selected from hydroxypropyl methylcellulose acetate succinate and hydroxypropyl methylcellulose phthalate.

The invention provides a pharmaceutically acceptable salt and a crystal form of a pyrrolo[2,3-d]pyridazin-7-one derivative and a preparation method of the pharmaceutically acceptable salt and the crystal form. The invention specifically provides a BTK kinase inhibitor, namely (R)-4-amino-1-(1-(butyl-2-acetylenyl)pyrrolidin-3-yl)-3-(4-(2,6-difluorophenoxy)phenyl)-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazin-7-one salt, and a crystal form and a preparation method thereof. The preparation method comprises the steps of salt formation, dissolving, crystallizing and the like, and prepares the stable crystal form.

A compound of formula (I) wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.

Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.

The invention discloses a pyrimido-pyrrolopyridazine derivative as well as an intermediate, a preparation method, a pharmaceutical composition and application thereof. The preparation method of the pyrimido-pyrrolopyridazine derivative of a formula I shown in the description comprises the following step: in a solvent, under the action of additives, performing a reaction shown in the description onthe compound of a formula IV shown in the description. By adopting the preparation method disclosed by the invention, defects such as multi-step synthesis and low separation yields in a traditional method can be overcome, and various novel heterocyclic compounds with important biological activity can be rapidly synthesized. The pyrimido-pyrrolopyridazine derivative disclosed by the invention hasgood activity of inhibiting production of NO by macrophage RAW264.7.

The present invention relates to ortho substituted phenylpyrazolo- and pyrrolo-pyridazine derivatives having dual pharmacological activity towards both the α2δ subunit, in particular the α2δ-1 subunit, of the voltage-gated calcium channel and the μ-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

Disclosed are compounds of Formula (I), and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.

The present invention relates to compounds of formula (I), or their isotopic forms, stereoisomers, tautomers or pharmaceutically acceptable salt (s) thereof as muscarinic M1 receptor positive allosteric modulators (M1 PAMs). The present invention describes the preparation, pharmaceutical composition and the use of such compounds.

Solid dispersion and a preparation method therefor. In a specific embodiment, the solid dispersion contains an active ingredient (R)-4-amino-1-(1-(but-2-ynyl)pyrrolidin-3-yl))-3-(4-(2,6-difluorophenoxy)phenyl)-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazin-7-one or a salt thereof, and a carrier material, and the pH value is adjusted; employing a method that adds an appropriate amount of acid effectively inhibits an emulsification phenomenon in a reverse solvent process, thereby obtaining solid dispersion having a moderate particle size and uniform content.

A solid dispersion, a method for preparing same, and a solid preparation comprising the solid dispersion. The solid dispersion contains (R)-4-amino-1-(1-(but-2-ynylacyl)pyrrolidin-3-yl)-3-(4-(2,6-difluorophenoxy)phenyl)-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazine-7-one or a pharmaceutically acceptable salt thereof, and a carrier material. The carrier material is selected from hydroxypropyl methylcellulose acetate succinate and hydroxypropyl methylcellulose phthalate.

The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.

A compound of formula (I) wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.

A solid dispersion, a preparation method thereof, and a solid formulation comprising the solid dispersion. The solid dispersion contains (R)-4-amino-1-(1-(but-2-ynoyl)pyrrolidin-3-yl)-3-(4-(2,6-difluorophenoxy )phenyl)-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazin-7-one or a pharmaceutically acceptable salt thereof and a carrier material selected from hypromellose acetate Sucuccinate, Hypromellose Phthalate.

Pyrrolopyridazine derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof, in formula (I) R1 is C2-C6 alkenyl, halogenated C2-C6 alkenyl, optionally substituted C3 -C7 cycloalkyl or optionally substituted C3-C7 cycloalkyl -C1-C6 alkyl; R2 is C1-C6 alkyl; R3 is hydroxymethyl, C2-C6 aliphatic acyloxymethyl, optionally substituted C6-C10 arylcarbonyloxymethyl, C1-C6 alkoxycarbonyloxymethyl, formyl, carboxyl, C1-C6 alkoxycarbonyl or optionally substituted C6-C10 aryloxycarbonyl; R4 is optionally substituted C6-C10 aryl; A is imino, oxygen or sulfur. The pyrrolopyridazine derivative has excellent gastric acid secretion inhibitory effects, gastric mucosa protective effects, etc., and can be effectively used as a drug, especially as a preventive drug and a therapeutic drug for ulcer diseases. ∴

A solid dispersion, a method for preparing same, and a solid preparation including the solid dispersion. The solid dispersion contains (R)-4-amino-1-(1-(but-2-ynylacyl)pyrrolidin-3-yl)-3-(4-(2,6-difluorophenoxy)phenyl)-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazine-7-one or a pharmaceutically acceptable salt thereof, and a carrier material. The carrier material is selected from hydroxypropyl methylcellulose acetate succinate and hydroxypropyl methylcellulose phthalate.

The present invention relates to compounds of formula (I), or their isotopic forms, stereoisomers, tautomers or pharmaceutically acceptable salt (s) thereof as muscarinic M1 receptor positive allosteric modulators (M1 PAMs). The present invention describes the preparation, pharmaceutical composition and the use of such compounds. (I)

Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.