46 results about "Nk3 receptor" patented technology

The present invention relates to a method of treating schizophrenia which comprises administering a therapeutically effective amount of a compound of formula I wherein R1, R2, and R3 are as defined in the specification or to pharmaceutically active acid-addition salts thereof.

The present invention provides a method for the treatment of schizophrenia which comprises administering a compound of formula wherein the substituents are as described herein or a pharmaceutically active acid-addition salt thereof. In particular, the invention provides methods for treating both positive and negative symptoms of schizophrenia through dual inhibition of NK1 and NK3 receptors. The invention also provides novel compounds with formula I and methods for preparing compounds of the invention.

The invention relates to a compound of general formulawhereinAr, R1, R2, R3, R4, n, o, p, s, X andare as defined herein or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

The present invention relates to compounds of formula Iwherein R1, R2, R3, R′, Ar, m, n, and o are as defined herein. The invention also relates to pharmaceutical compositions containing compounds of formula I and methods for the manufacture of such compounds and compositions. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

The present invention relates to cyclopropyl derivatives of formula (I) and salt thereof. These compounds are NK3 receptor antagonists and may therefore be useful for treatment of diseases where the NK3 receptor is implicated, e.g. psychotic disorders.

The invention relates to a compound of formula IwhereinAr1,Ar2,R1,R2, R3, R4, n, o, p, and q are as defined herein and to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

The present invention relates to compounds of formula Iwherein R1, R2, R3, R′, Ar, m, n, and o are as defined herein. The invention also relates to pharmaceutical compositions containing compounds of formula I and methods for the manufacture of such compounds and compositions. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

The present invention relates to cyclopropyl derivatives of formula (I) and salt thereof. These compounds are NK3 receptor antagonists and may therefore be useful for treatment of diseases where the NK3 receptor is implicated, e.g. psychotic disorders.

The present invention relates to a compounds of formula Iwherein A, Ar, R, R2, R3, R4, p, and o are as defined in the specification and claims or to a pharmaceutically active salt thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, bipolar disorders, anxiety and attention deficit hyperactivity disorder (ADHD).

The invention relates to pyrrolidine derivatives of formulawhereinR1,R2,R3,n, and o are defined in the specification and to pharmaceutically active acid-addition salts thereof. Compounds of formula I have a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1 / NK3 receptor antagonists), useful in the treatment of schizophrenia.

Disclosed are compounds of formula (I) or pharmaceutically acceptable non-toxic salts or pharmaceutically acceptable solvates thereof wherein: (II) represents (a), (b), (c) or (d) and W, X, Y, A, B, C, D, E are variables as described herein. These compounds are highly selective agonists or antagonists at NK3 receptors or prodrugs thereof. The novel tachykinin NK-3 receptor antagonists contained in this invention have potential utility in the treatment of a broad array of disorders and diseases of the central nervous system (CNS) and periphery in mammals in which activation of NK-3 receptors is of importance.

The present invention relates to a compound of formula Iwherein R1, R2, R3, Ar, and n are as defined herein or to a pharmaceutically active acid addition salt. Compounds of formula I show a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1 / NK3 receptor antagonists), useful in the treatment of schizophrenia.

The present application relates to compounds of formulawherein the definitions are as described herein. The present compounds are high potential NK-3 receptor antagonists that are useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

The present invention relates to a compounds of formula Iwherein R1, R2, Ar1, Ar2, R′, R″, m, n, and o are defined in the specification or to a pharmaceutically active salt, racemic mixture, enantiomer, optical isomer or to tautomeric form thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

The present invention relates to a compound of formula IwhereinR1, R2, R3, and n are as defined herein or to a pharmaceutically acceptable acid addition salt thereof. These compounds are NK3 receptor antagonists, useful for the treatment of such disorders as depression, pain, bipolar disorders, psychosis, Parkinson's disease, schizophrenia, anxiety, and attention deficit hyperactivity disorder (ADHD).

The invention relates to a compound of general formulawhereinAr, R1, R2, R3, R4, n, o, p, s, X andare as defined herein or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

The invention belongs to the technical field of tumor treatment, and particularly relates to a synthetic peptide NK3R-A2 based on an NK3 receptor. The synthetic peptide NK3R-A2 based on the NK3 receptor has the tumor angiogenesis resisting effect. The molecular weight of the synthetic peptide is 1536.70 Da, and the specific sequence of the synthetic peptide is CNGRCGGDFF(MeF)GLM-NH2. The synthetic peptide is prepared through an Fmoc solid-phase polypeptide synthesis method and can be used for preparing anti-tumor preparations. Through in-vitro cell viability experiments, cell scratch experiments and cell migration experiments, the angiogenesis resisting effect of the synthetic peptide is verified; meanwhile, through further chicken chorioallantoic membrane carrier experiments and euangiotic mice S180 transplantation tumor model experiments on the synthetic peptide, it is verified that the synthetic peptide is obvious in tumor inhibiting effect, has the tumor angiogenesis resisting effect and has no obvious toxic or side effect; the synthetic peptide has good medical application prospects and also provides a targeting sequence with great potential for tumor treatment.